lapatinib profile

ID Source	ID
PubMed CID	208908
CHEMBL ID	554
CHEBI ID	49603
SCHEMBL ID	8100
MeSH ID	M0473129

Synonym
AC-1314
gw572016
lapatinib ,
cid_208908
n-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)quinazolin-4-amine
chembl554 ,
bdbm5445
n-{3-chloro-4-[(3-fluoro-benzyl)oxy]phenyl}-6-[5-({2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
HY-50898
c29h26clfn4o4s
AB01273965-01
AB01273965-03
gw-572016
NCHEMBIO866-COMP20
n-(3-chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-((2-methylsulfonylethylamino)methyl)-2-furyl)quinazolin-4-amine
n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
FMM ,
DB01259
n-(3-chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine
1XKK
gsk 572016
NCGC00167507-01
lapatinib [inn]
4-quinazolinamine, n-(3-chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-
gw 282974x
gw 572016
CHEBI:49603 ,
n-[3-chloro-4-(3-fluorobenzyloxy)phenyl]-6-[5-({[2-(methanesulfonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-amine
231277-92-2
HMS2089H10
gw-572016x
gsk-572016
AKOS005145766
D08108
lapatinib (inn)
FT-0659650
nsc-745750
tykerb (tn) (glaxo smith kline)
n-(3-chloro-4-{[(3-fluorophenyl)methyl]oxy}phenyl)-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine
lapatinib free base
nsc745750
KINOME_3685
KINOME_3684
n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
A25184
gw-2016;n-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine;4-[[3-chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline
NCGC00167507-02
NCGC00167507-03
cas-231277-92-2
dtxsid7046675 ,
dtxcid5026675
tox21_112505
0vua21238f ,
lapatinib [inn:ban]
unii-0vua21238f
hsdb 8209
913989-15-8
BRD-K19687926-001-01-7
BCP9000837
BCP9000838
HMS3244N10
HMS3244N14
HMS3244N06
BCPP000189
BCPP000188
lapatinib base
n-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine
lapatinib [who-dd]
lapatinib [vandf]
lapatinib [ema epar]
lapatinib [mi]
gtpl5692
AM20090641
4-quinazolinamine, n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-
SCHEMBL8100
tox21_112505_1
NCGC00167507-04
AB01273965-02
n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methane sulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
BCFGMOOMADDAQU-UHFFFAOYSA-N
n-{3-chloro-4[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methane sulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
n-[3-chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
Q-101353
n-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine
AB01273965_05
AB01273965_04
mfcd09264194
1210608-87-9
EX-A402
gsk572016
n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-amine
SR-05000001472-1
n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl] quinazolin-4-amine
NCGC00167507-09
n3-chloro-4-(3-fluorophenyl)methoxyphenyl-6-5-(2-methylsulfonylethylamino)methyl-2-furylquinazolin-4-amine
SW199101-5
231277-92-2 (free base)
Q420323
lapatinib (free base)
1092929-10-6
AS-14065
BCP01874
BRD-K19687926-379-02-5
SB16918
n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
HMS3744K11
CCG-270133
nsc-800780
nsc800780
lapatinib (gw572016)
lapatinib, free base
lapatinib base- bio-x
BC164610
EN300-117254
L0360

Excerpt	Reference	Relevance
"Lapatinib is a dual tyrosine kinase inhibitor targeting EGFR and Her2, and berberine (BBR) is a plant-based alkaloid suggested to inhibit several cancer signaling pathways."	( Pharmacotranscriptomic profiling of resistant triple-negative breast cancer cells treated with lapatinib and berberine shows upregulation of PI3K/Akt signaling under cytotoxic stress. Chen, Y; Hin Cho, C; Imani, S; Jabbarzadeh Kaboli, P; Jomhori, M; Li, M; Luo, S; Shen, J; Wu, X; Wu, Z; Xiang, S; Xiao, Z; Zhao, Y, 2022)	1.66
"Lapatinib is a dual tyrosine kinase inhibitor that inhibits both EGFR and HER2."	( Lapatinib as first-line treatment for muscle-invasive urothelial carcinoma in dogs. Iio, A; Kaji, K; Maeda, S; Momoi, Y; Motegi, T; Nakazawa, M; Sakai, K; Yonezawa, T, 2022)	2.89
"Lapatinib is a highly selective reversible inhibitor of the tyrosine kinase domains of HER2 and EGFR, approved for the treatment of advanced stage HER2-overexpressing breast cancers. "	( AMPK activation attenuates HER3 upregulation and Neuregulin-Mediated rescue of cell proliferation in HER2-Overexpressing breast cancer cell lines exposed to lapatinib. Buccinnà, B; Piccinini, M; Ramondetti, C, 2022)	2.36
"Lapatinib is an anticancer used for treatment of the patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug capecitabine or with letrozole for the treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer. "	( Lapatinib: A comprehensive profile. Abdelgalil, AA; Alkahtani, HM, 2023)	3.8
"Lapatinib is an oral small-molecule tyrosine kinase inhibitor indicated for advanced or metastatic HER2-positive breast cancer. "	( Dose-sparing effect of lapatinib co-administered with a high-fat enteral nutrition emulsion: preclinical pharmacokinetic study. Ding, H; Fang, L; Kong, S; Song, Y; Tong, Y; Xu, G; Yang, D; Zhu, J, 2023)	2.66
"Lapatinib is a dual tyrosine kinase inhibitor associated with rare but potentially severe idiosyncratic hepatotoxicity. "	( Interindividual Variation in CYP3A Activity Influences Lapatinib Bioactivation. Abouda, AA; Bissada, JE; Crouch, RD; Jackson, KD; Truong, V; Wines, KJ, 2019)	2.2
"Lapatinib is a targeted tyrosine kinase inhibitor therapeutic drug also used to treat NPC, but high doses are often required to achieve a result."	( Lapatinib sensitivity in nasopharyngeal carcinoma is modulated by SIRT2-mediated FOXO3 deacetylation. Aimjongjun, S; Alasiri, G; Janvilisri, T; Jiramongkol, Y; Lam, EW; Mahmud, Z; Yagüe, E; Yao, S, 2019)	2.68
"Lapatinib is a small molecule tyrosine kinase inhibitor used to treat breast cancer, often in combination with chemotherapy. "	( The GLP-2 analogue elsiglutide reduces diarrhoea caused by the tyrosine kinase inhibitor lapatinib in rats. Bateman, E; Bowen, JM; Keefe, DM; Mayo, BJ; Pietra, C; Secombe, KR; Thorpe, D; Wignall, AD, 2020)	2.22
"Lapatinib (LAP) is an anticancer drug, which is metabolized to the N- and O-dealkylated products (N-LAP and O-LAP, respectively). "	( Characterization of Locally Excited and Charge-Transfer States of the Anticancer Drug Lapatinib by Ultrafast Spectroscopy and Computational Studies. Andreu, I; Consuelo Cuquerella, M; González-Bello, C; Lence, E; Miranda, MA; Navarrete-Miguel, M; Roca-Sanjuán, D; Vayá, I, 2020)	2.22
"Lapatinib is a candidate drug for treatment of trastuzumab-resistant, human epidermal growth factor receptor 2 (HER2)-positive gastric cancer (GC). "	( FOXO1 Suppression is a Determinant of Acquired Lapatinib-Resistance in HER2-Positive Gastric Cancer Cells Through MET Upregulation. Chang, MS; Choi, Y; Jang, BG; Kim, MA; Kim, Y; Ko, YS; Lee, BL; Lee, JS; Park, J; Park, JW; Pyo, JS, 2018)	2.18
"Lapatinib is a tyrosine kinase inhibitor that targets the human epidermal growth factor receptor 2 (HER2) and the epidermal growth factor receptor (EGFR/HER1), and there are concerns about its cardiac toxicity. "	( Cardiac toxicities of lapatinib in patients with breast cancer and other HER2-positive cancers: a meta-analysis. Chang, MJ; Choi, HD, 2017)	2.21
"Lapatinib (LPT) is an orally administered drug for the treatment of metastatic breast cancer. "	( CD44 targeting hyaluronic acid coated lapatinib nanocrystals foster the efficacy against triple-negative breast cancer. Agrawal, S; Ahmad, H; Arya, A; Chadchan, SB; Dwivedi, AK; Dwivedi, M; Jha, RK; Kaushik, S; Mitra, K; Sikandar, R, 2018)	2.19
"Lapatinib is a small molecule epidermal growth factor receptor tyrosine kinase inhibitor that can inhibit epidermal growth factor receptor and human epidermal growth factor receptor 2, though its effect on pyruvate kinase type M2 remains elusive."	( Lapatinib Inhibits Breast Cancer Cell Proliferation by Influencing PKM2 Expression. Dong, D; Guan, M; Liu, X; Niu, R; Shao, J; Tong, Y; Wang, M; Zhang, F; Zhou, Y, 2018)	2.64
"Lapatinib is a tyrosine kinase inhibitor (TKI), approved for the treatment of human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer."	( A pharmacokinetic study on lapatinib in type 2 diabetic rats. Grabowski, T; Grześkowiak, E; Karbownik, A; Klupczynska, A; Kokot, ZJ; Moch, M; Plewa, S; Sobańska, K; Szałek, E; Wolc, A, 2018)	1.5
"Lapatinib is a dual tyrosin kinase inhibitor of EGFR and HER2."	( Design and development of PEGylated liposomal formulation of HER2 blocker Lapatinib for enhanced anticancer activity and diminished cardiotoxicity. Asif, M; Bhadauria, S; Chourasia, MK; Khanna, A; Shrivastava, R; Singh, PK; Trivedi, S, 2018)	1.43
"Lapatinib is a small-molecule dual HER2/epidermal growth factor receptor inhibitor that has demonstrated intracranial activity against HER2+ breast cancer brain metastases."	( Stereotactic radiosurgery with concurrent lapatinib is associated with improved local control for HER2-positive breast cancer brain metastases. Ahluwalia, MS; Angelov, L; Barnett, GH; Chao, ST; Juloori, A; Kotecha, R; Miller, JA; Mohammadi, AM; Murphy, ES; Parsai, S; Peereboom, DM; Suh, JH; Vogelbaum, MA, 2019)	1.5
"Lapatinib (LP) is an FDA-approved dual EGFR/HER2 inhibitor for HER2-amplified breast cancer."	( (-)-Oleocanthal Combined with Lapatinib Treatment Synergized against HER-2 Positive Breast Cancer In Vitro and In Vivo. Akl, MR; Ayoub, NM; Ebrahim, HY; El Sayed, KA; Goda, AA; Hananeh, WM; Liu, YY; Meyer, SA; Mohyeldin, MM; Nagumalli, SK; Siddique, AB, 2019)	1.52
"Lapatinib is a potent EGFR and human epidermal growth factor receptor 2 (HER2) inhibitor that inhibits cell proliferation and induces apoptosis in various human cancer cells."	( Lapatinib Inhibits Amphiregulin-induced BeWo Choriocarcinoma Cell Proliferation by Reducing ERK1/2 and AKT Signaling Pathways. Brum, IS; Cheng, JC; Cordero, E; Leung, PCK; Pires, LV; Pizzolato, LS; Yi, Y, 2019)	2.68
"Lapatinib is a dual inhibitor of the EGF receptor and EGF receptor 2 approved by the US FDA to treat advanced breast cancer."	( Incorporation of lapatinib into lipoprotein-like nanoparticles with enhanced water solubility and anti-tumor effect in breast cancer. Cao, S; Chen, C; Gao, H; Jiang, X; Pan, S; Pang, Z; Xi, Z; Yang, Z; Zhang, Q, 2013)	1.45
"Lapatinib is an oral small-molecule tyrosine kinase inhibitor of both epidermal growth factor receptor and human epidermal growth factor receptor 2 (HER2). "	( Randomized trial of lapatinib versus placebo added to paclitaxel in the treatment of human epidermal growth factor receptor 2-overexpressing metastatic breast cancer. Arpornwirat, W; Chen, G; DeSilvio, ML; Gomez, H; Guan, Z; Jiang, Z; Leung, WL; Lorvidhaya, V; Makhson, A; Newstat, B; Oliva, C; Russo, MW; Shen, Z; Tong, Z; Wang, L; Xu, B; Yang, J, 2013)	2.16
"Lapatinib is a dual tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) and human EGFR-2 (HER2) tyrosine kinase domains. "	( Lapatinib inhibits the growth of esophageal squamous cell carcinoma and synergistically interacts with 5-fluorouracil in patient-derived xenograft models. Bachman, KE; Fei, M; Greshock, J; Hou, W; Liu, L; Liu, P; Moon, H; Qin, X; Wang, H; Ye, BC; Zang, CY; Zhang, P; Zhu, X, 2013)	3.28
"Lapatinib is an oral dual tyrosine kinase inhibitor (TKI) that targets both EGFR and HER2 to inhibit the proliferation of breast cancer cells."	( Autophagy stimulates apoptosis in HER2-overexpressing breast cancers treated by lapatinib. Chen, S; Feng, D; Han, T; Jiang, R; Liu, X; Ma, Y; Qiao, H; Wei, Y; Wu, L; Zhang, J; Zhang, S; Zhang, Y; Zhu, X, 2013)	1.34
"Lapatinib-resistance is a major problem for HER2-positive breast cancer treatment. "	( RON confers lapatinib resistance in HER2-positive breast cancer cells. Lou, L; Quan, H; Wang, L; Wang, Q; Xie, C; Zhao, J, 2013)	2.21
"Lapatinib is a dual EGFR and ErbB-2 tyrosine kinase inhibitor that has significantly improved the clinical outcome of ErbB-2-overexpressing breast cancer patients. "	( Src and CXCR4 are involved in the invasiveness of breast cancer cells with acquired resistance to lapatinib. Bode, AM; D'Alessio, A; De Luca, A; Gallo, M; Maiello, MR; Normanno, N, 2014)	2.06
"Lapatinib is a dual EGFR and HER2 inhibitor that is used to treat HER2-overexpressing cancers. "	( Incorporation of lapatinib into core-shell nanoparticles improves both the solubility and anti-glioma effects of the drug. Cao, S; Chen, C; Chen, J; Gao, H; Jiang, X; Wang, Y; Wei, Y, 2014)	2.18
"Lapatinib is a tyrosine kinase inhibitor targeting EGFR1 and HER2: it binds the intracellular domain of these receptors and blocks their downstream signaling pathways."	( 18FDG-PET for early prediction of complete response to lapatinib and capecitabine in HER2-positive metastatic breast cancer: a case report. Barbato, C; Carrillo, G; Cartenì, G; Minelli, S; Mocerino, C; Riccardi, F; Trunfio, M; Vitale, MG, )	1.1
"Lapatinib is a dual tyrosine kinase inhibitor (TKI), blocking HER1 and HER2 tyrosine kinase activity by binding to the ATP-binding site of the receptor's intracellular domain."	( Lapatinib. Nolting, M; Schneider-Merck, T; Trepel, M, 2014)	2.57
"Lapatinib is a dual inhibitor of EGFR and human epidermal growth factor receptor 2 (HER2), and used to treat advanced breast cancer. "	( Lapatinib-incorporated lipoprotein-like nanoparticles: preparation and a proposed breast cancer-targeting mechanism. Gao, HL; He, Q; Ruan, SB; Zhang, L; Zhang, QY; Zhang, S, 2014)	3.29
"Lapatinib is a poor brain penetrant."	( Are capecitabine and the active metabolite 5-Fu CNS penetrable to treat breast cancer brain metastasis? Bai, Y; Cheng, Z; Li, S; Lv, J; Xie, L; Yan, Y; Zhang, J; Zhang, L; Zhang, X; Zhong, W, 2015)	1.14
"Lapatinib (Tykerb) is a small-molecule and dual inhibitor of human epidermal growth factor receptor1 and 2 (EGFR and HER2, respectively) which are both high-risk predictors of BMBC."	( Heparanase mediates a novel mechanism in lapatinib-resistant brain metastatic breast cancer. Marchetti, D; Ngo, JA; Wetzel, MD; Zhang, L, 2015)	1.4
"Lapatinib is a dual tyrosine kinase inhibitor that targets epidermal growth factor receptor and HER2. "	( Phase I Study of Lapatinib and Pemetrexed in the Second-Line Treatment of Advanced or Metastatic Non-Small-Cell Lung Cancer With Assessment of Circulating Cell Free Thymidylate Synthase RNA as a Potential Biomarker. Kaneko, T; Lau, MR; Lunec, J; Margetts, J; Novello, S; Nutt, J; Plummer, R; Ramlau, R; Reck, M; Scagliotti, GV; Thomas, M, 2015)	2.2
"Lapatinib is a possible option for HER2-positive metastatic breast cancer patients with brain metastasis."	( Effective Treatment of Solitary Pituitary Metastasis with Panhypopituitarism in HER2-Positive Breast Cancer by Lapatinib. Kim, EH; Kim, H; Lee, S; Park, Y; Suh, CO, 2016)	1.37
"Lapatinib based therapy is an effective treatment for women with advanced/metastatic HER2(+)BC after prior exposure to trastuzumab. "	( Lapatinib-based therapy for women with advanced/metastatic HER2 positive breast cancer. Al-Foheidi, M; Al-Rehaily, S; Darwish, T; Karim, SM; Mahrous, M; Mansour, M; Mokhtar, M; Rizvi, A; Zekri, J, 2015)	3.3
"Lapatinib (LPT) is a dual tyrosine kinase inhibitor with a significant potential to inhibit p-glycoproteins which form one of the main groups of proteins responsible for efflux pump mediated MDR."	( Liposomal formulation for co-delivery of paclitaxel and lapatinib, preparation, characterization and optimization. Dorkoosh, FA; Kelishadi, PD; Ravar, F; Saadat, E, 2016)	1.4
"Lapatinib is a potent HER1 and HER2 inhibitor. "	( Results from a Phase I Study of Lapatinib with Gemcitabine and Cisplatin in Advanced or Metastatic Bladder Cancer: EORTC Trial 30061. Agerbaek, M; Cerbone, L; Collette, S; Daugaard, G; Marreaud, S; Sengeløv, L; Sternberg, CN; Van Herpen, C; Zhang, J, 2016)	2.16
"Lapatinib is a tyrosine kinase inhibitor that binds to both EGFR and HER-2."	( Phase II study of lapatinib and capecitabine in second-line treatment for metastatic pancreatic cancer. Gabrielson, A; He, AR; Hwang, JJ; Ley, L; Marshall, JL; Pishvaian, MJ; Weiner, LM; Wu, Z; Zhuang, T, 2015)	1.47
"Lapatinib is a commonly used drug that interrupts signaling from the epidermal growth factor receptors, EGFR and HER2/neu. "	( Combination of lapatinib with isothiocyanates overcomes drug resistance and inhibits migration of HER2 positive breast cancer cells. Herman-Antosiewicz, A; Kaczyńska, A, 2017)	2.25
"Lapatinib is an inhibitor of human epidermal growth factor receptor 2 (HER2), which is overexpressed in 20-25% of breast cancers. "	( Interleukin-6 expression contributes to lapatinib resistance through maintenance of stemness property in HER2-positive breast cancer cells. Chen, TM; Chen, YJ; Chien, PH; Huang, WC; Hung, CM; Lin, YM; Pan, HL; Wei, CT, 2016)	2.14
"Lapatinib is an orally bioavailable dual inhibitor of the intracellular domain of both the HER2 protein and the epidermal growth factor receptor. "	( [A Case of Interstitial Pneumonitis Induced by Lapatinib plus Letrozole]. Yamamoto, C; Yamamoto, D; Yamamoto, M, 2016)	2.13
"Lapatinib is an oral receptor tyrosine kinase inhibitor that targets HER2 and the EGFR."	( Drug Insight: intracellular inhibitors of HER2--clinical development of lapatinib in breast cancer. Cameron, DA; Stein, S, 2008)	1.3
"Lapatinib is a selective competitive inhibitor of both the HER2 and EGFR tyrosine kinases."	( Activity of lapatinib is independent of EGFR expression level in HER2-overexpressing breast cancer cells. Bartholomeusz, C; Bornmann, WG; Esteva, FJ; Hortobagyi, GN; Pal, A; Ueno, NT; Yamasaki, F; Zhang, D, 2008)	1.45
"Lapatinib is a small-molecule tyrosine kinase inhibitor that dually targets human epidermal growth factor receptors 1 and 2 (HER2). "	( Lapatinib: a dual tyrosine kinase inhibitor for metastatic breast cancer. Paul, B; Thompson, J; Trovato, JA, 2008)	3.23
"Lapatinib is a dual inhibitor of the epidermal growth factor receptor and HER2 tyrosine kinase."	( The growth inhibitory effect of lapatinib, a dual inhibitor of EGFR and HER2 tyrosine kinase, in gastric cancer cell lines. Bang, YJ; Hur, HS; Im, SA; Kang, S; Kim, HP; Kim, JH; Kim, JW; Kim, TY; Lee, DS; Oh, DY; Yoon, YK, 2008)	1.35
"Lapatinib is a dual inhibitor of the EGFR and HER2 tyrosine kinases. "	( Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Goodin, S; Medina, PJ, 2008)	3.23
"Lapatinib is an oral dual tyrosine kinase inhibitor against members of the human epidermal growth factor receptor (HER) family (HER1 or epidermal growth factor receptor [EGFR], and HER2)."	( Lapatinib and ixabepilone for the treatment of metastatic breast cancer. Halterman, PA, 2008)	2.51
"Lapatinib is an orally active, reversible, small-molecule tyrosine kinase inhibitor that potently inhibits both HER1 and HER2 tyrosine kinase activity."	( Jumping higher: is it still possible? The ALTTO trial challenge. de Azambuja, E; Dinh, P; Piccart-Gebhart, M; Snoj, N; Tomasello, G, 2008)	1.07
"Lapatinib is a tyrosine kinase inhibitor approved for use in combination with capecitabine to treat advanced or metastatic breast cancers overexpressing human epidermal receptor 2 (ErbB2). "	( An unexpected synergist role of P-glycoprotein and breast cancer resistance protein on the central nervous system penetration of the tyrosine kinase inhibitor lapatinib (N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}meth Castellino, S; Chism, JP; Demby, VE; John-Williams, LS; Olson, KL; Otto, V; Polli, JW; Woodard, SM; Yeager, RL, 2009)	1.99
"Lapatinib is a human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor (TKI) that has clinical activity in HER2-amplified breast cancer. "	( Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity. Arribas, J; Baselga, J; Guzman, M; Jimenez, J; Landolfi, S; Parra, JL; Pedersen, K; Ramon y Cajal, S; Scaltriti, M; Smith, DJ; Verma, C, 2009)	3.24
"Lapatinib monotherapy is a potentially effective treatment for relapsed or refractory HER2+ inflammatory breast cancer."	( Lapatinib monotherapy in patients with HER2-overexpressing relapsed or refractory inflammatory breast cancer: final results and survival of the expanded HER2+ cohort in EGF103009, a phase II study. Awada, A; Bachelot, T; Blackwell, K; DeSilvio, M; Johnston, S; Kaufman, B; Salazar, V; Spector, N; Trudeau, M; Westlund, R; Zaks, T, 2009)	3.24
"Lapatinib is a small molecule inhibitor that is active at the ATP binding site of the tyrosine kinase involved in HER signaling."	( Lapatinib as a chemotherapeutic drug. Obajimi, O, 2009)	2.52
"Lapatinib is a dual tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR) and HER-2."	( The dual EGFR/HER-2 tyrosine kinase inhibitor lapatinib sensitizes colon and gastric cancer cells to the irinotecan active metabolite SN-38. Fazzone, W; LaBonte, MJ; Ladner, RD; Lenz, HJ; Louie, SG; Manegold, PC; Wilson, PM, 2009)	1.33
"Lapatinib is a small molecule reversible tyrosine kinase inhibitor of EGFR and ErbB2 that shows in vitro and in vivo activity against a range of EGFR and ErbB2-dependent adult cancer cell lines and that has clinical efficacy against ErbB2-overexpressing breast cancer."	( Initial testing (stage 1) of lapatinib by the pediatric preclinical testing program. Carol, H; Gorlick, R; Houghton, PJ; Keir, ST; Kolb, EA; Lock, R; Maris, JM; Morton, CL; Phelps, D; Reynolds, CP; Schaiquevich, P; Smith, MA; Stewart, C; Wu, J, 2009)	2.09
"Lapatinib is a dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) with activity in HER2-amplified metastatic breast cancer (MBC). "	( Estrogen receptor, progesterone receptor, human epidermal growth factor receptor 2 (HER2), and epidermal growth factor receptor expression and benefit from lapatinib in a randomized trial of paclitaxel with lapatinib or placebo as first-line treatment in Arbushites, M; Dering, J; Di Leo, A; Finn, RS; Koehler, M; Oliva, C; Press, MF; Williams, LS, 2009)	1.99
"Lapatinib is a more potent inhibitor of MRP7 than erlotinib."	( Lapatinib and erlotinib are potent reversal agents for MRP7 (ABCC10)-mediated multidrug resistance. Chen, X; Chen, ZS; Fu, LW; Hopper-Borge, E; Kuang, YH; Lee, JW; Shen, T; Sodani, K; Tiwari, AK, 2010)	2.52
"Lapatinib is an inhibitor of epidermal growth factor receptor and HER2/NEU both implicated in hepatocarcinogenesis."	( A multi-institutional phase II study of the efficacy and tolerability of lapatinib in patients with advanced hepatocellular carcinomas. Balint, C; Bekaii-Saab, T; Campbell, A; Chen, H; Culler, K; Dai, Z; Dancey, J; Eng, C; Grever, M; Heerema, N; Lee, RM; Markowitz, J; O'Neil, B; Papp, A; Prescott, N; Sadee, W; Villalona-Calero, M; Wei, L; Zalupski, M, 2009)	1.31
"Lapatinib is a dual inhibitor of HER2 and epidermal growth factor receptor kinases."	( Prognostic and predictive value of HER2 extracellular domain in metastatic breast cancer treated with lapatinib and paclitaxel in a randomized phase III study. Arbushites, M; Di Leo, A; Finn, RS; Gagnon, R; Koehler, M; Press, MF, 2009)	1.29
"Lapatinib is an oral, small-molecule, dual kinase inhibitor that targets both HER2 and the EGF receptor. "	( Lapatinib in metastatic breast cancer. Berton-Rigaud, D; Bourbouloux, E; Campone, M; Frenel, JS; Sadot-Lebouvier, S; Zanetti, A, 2009)	3.24
"Lapatinib is an oral, small-molecule dual inhibitor of human EGF receptor 1 (EGFR/erbB1) and 2 (HER2/erbB2). "	( Lapatinib plus letrozole for postmenopausal patients with advanced HER2(+)/HR(+) breast cancer. Guarneri, V, 2009)	3.24
"Lapatinib is a small molecule inhibitor of both HER2 and the epidermal growth factor receptor (EGFR). "	( In vitro and in vivo evidence that a combination of lapatinib plus S-1 is a promising treatment for pancreatic cancer. Amano, R; Hirakawa, K; Kawajiri, H; Komoto, M; Nakata, B; Nishii, T; Shinto, O; Yamada, N; Yashiro, M, 2010)	2.05
"Lapatinib is an oral small-molecule tyrosine kinase inhibitor directed against EGFR and HER2."	( Molecular predictors of response to trastuzumab and lapatinib in breast cancer. Esteva, FJ; Hortobagyi, GN; Hung, MC; Yu, D, 2010)	1.33
"Lapatinib (GW572016) is a selective and potent dual tyrosine kinase inhibitor of the epidermal growth factor 1 (EGFR) and 2 (HER2), approved in the treatment of HER2 positive breast cancer. "	( A multicenter phase II clinical trial of lapatinib (GW572016) in hormonally untreated advanced prostate cancer. Chin, JL; Dancey, JE; Gregg, R; Hedley, D; Hotte, SJ; Hudes, GR; Moore, MJ; Pham, NA; Sridhar, SS; Trachtenberg, J; Tran-Thanh, D; Tsao, MS; Wang, L, 2010)	2.07
"Lapatinib is a dual tyrosine kinase inhibitor selective for inhibition of epidermal growth factor receptor (EGFR1/ErbB1) and HER2/ErbB2."	( [Lapatinib treatment-option in trastuzumab-resistant breast cancer]. Pikó, B, 2009)	1.98
"Lapatinib is a novel dual tyrosine kinase inhibitor, blocking HER1 and HER2 tyrosine kinase activity by binding to the ATP-binding site of the receptor's intracellular domain."	( Lapatinib. Schneider-Merck, T; Trepel, M, 2010)	2.52
"Lapatinib is an oral, small-molecule, reversible inhibitor of both epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor-2 (HER2) tyrosine kinases. "	( Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer. Kolesar, JM; Tevaarwerk, AJ, 2009)	3.24
"Lapatinib (GW572016) is a small molecule that is administrated orally and functions as a reversible inhibitor of both EGFR and HER-2 tyrosine kinases."	( Antitumor effects of lapatinib (GW572016), a dual inhibitor of EGFR and HER-2, in combination with cisplatin or paclitaxel on head and neck squamous cell carcinoma. Fujita, K; Ishiguro, Y; Kimura, M; Kondo, N; Matsuda, H; Sakakibara, A; Takahashi, H; Toth, G; Tsukuda, M, 2010)	1.4
"Lapatinib is a novel tyrosine kinase inhibitor for treatment of breast cancer with human epidermal growth factor receptor 2 (HER2) amplification."	( Survival benefits from lapatinib therapy in women with HER2-overexpressing breast cancer: a systematic review. Chow, LW; Ong, EY; Tse, LA; Yip, AY, 2010)	1.39
"Lapatinib is an oral dual tyrosine kinase inhibitor targeting epidermal growth factor receptor and HER2. "	( Lapatinib side-effect management. Frankel, C; Palmieri, FM, 2010)	3.25
"Lapatinib is an orally active, low molecular weight, reversible inhibitor of the intracellular tyrosine kinase domains of both human epidermal growth factor receptor (HER) type 1 (HER1) and type 2 (HER2). "	( Lapatinib: in postmenopausal women with hormone receptor-positive, HER2-positive metastatic breast cancer. Curran, MP, 2010)	3.25
"Lapatinib is an oral dual erbB 1/2 tyrosine kinase inhibitor that inhibits human EGF receptor 2 (HER2) and blocks the EGF receptor. "	( Lapatinib and breast cancer: current indications and outlook for the future. Kaklamani, V; Moreira, C, 2010)	3.25
"Lapatinib is a specific HER1 and 2 targeted tyrosine kinase inhibitor now widely used in combination with chemotherapy in the clinical setting. "	( A synergistic interaction between lapatinib and chemotherapy agents in a panel of cell lines is due to the inhibition of the efflux pump BCRP. Ghazaly, E; Joel, S; Kitromilidou, C; McGrowder, EH; Perry, J; Powles, T, 2010)	2.08
"Lapatinib is a small-molecule tyrosine kinase inhibitor that blocks phosphorylation of the epidermal growth factor receptor and HER2 in breast cancer cells, resulting in apoptosis."	( Fatty acid synthase phosphorylation: a novel therapeutic target in HER2-overexpressing breast cancer cells. Baek, JM; Boulbes, D; Esteva, FJ; Gomez-Cabello, D; Hawke, DH; Hortobagyi, GN; Hung, MC; Jin, Q; Lee, MH; Wang, YN; Yeung, SC; Yuan, LX, 2010)	1.08
"Lapatinib is an oral tyrosine kinase inhibitor which has both HER-1 and -2 activities and has been licensed for use in recurrent breast cancer that overexpresses HER-2."	( Lapatinib for breast cancer: a review of the current literature. Gelmon, KA; MacFarlane, RJ, 2011)	2.53
"Lapatinib is a dual tyrosine kinase inhibitor of the EGFR and HER2 tyrosine kinase domains. "	( Lapatinib inhibits receptor phosphorylation and cell growth and enhances antibody-dependent cellular cytotoxicity of EGFR- and HER2-overexpressing esophageal cancer cell lines. Choudhury, A; Fujii, H; Inoue, M; Izawa, S; Kawaguchi, Y; Kiessling, R; Kono, K; Kono, T; Maruyama, T; Mimura, K; Mizukami, Y; Shiba, S; Watanabe, M, 2011)	3.25
"Lapatinib is an oral inhibitor of EGFR and HER-2."	( A phase II study of lapatinib, a dual EGFR and HER-2 tyrosine kinase inhibitor, in patients with castration-resistant prostate cancer. Armstrong, AJ; Crane, JM; George, DJ; Godley, PA; Grigson, G; Kim, WY; Moore, DT; Morris, K; Pruthi, RS; Rathmell, WK; Wallen, EM; Watkins, CP; Whang, YE, 2013)	1.43
"Lapatinib (GW572016) is a dual tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2/ErbB2), which are reported as overexpressed in 15%-45% of gastric cancers, making them potential targets."	( Southwest Oncology Group study S0413: a phase II trial of lapatinib (GW572016) as first-line therapy in patients with advanced or metastatic gastric cancer. Blanke, CD; Danenberg, KD; Fenoglio-Preiser, CM; Goldman, B; Iqbal, S; Lenz, HJ; Shibata, SI; Zhang, W, 2011)	2.06
"Lapatinib is an EGFR/HER2 kinase inhibitor suppressing signaling through the RAS/RAF/MEK (MAP/ERK kinase)/MAPK (mitogen-activated protein kinase) and PI3K (phosphoinositide 3-kinase)/AKT pathways."	( The dual EGFR/HER2 inhibitor lapatinib synergistically enhances the antitumor activity of the histone deacetylase inhibitor panobinostat in colorectal cancer models. El-Khoueiry, A; Fazzone, W; LaBonte, MJ; Ladner, RD; Lenz, HJ; Louie, SG; Russell, J; Wilson, PM, 2011)	1.38
"Lapatinib is an inhibitor of the tyrosine kinases of human epidermal growth factor receptor type 2 (HER2) and epidermal growth factor receptor type 1, with clinical activity in HER2-positive metastatic breast cancer. "	( Lapatinib-induced hepatitis: a case report. Kalofonos, H; Koutras, A; Labropoulou-Karatza, C; Makatsoris, T; Onyenadum, A; Peroukides, S; Tsamandas, A, 2011)	3.25
"Lapatinib is an orally administered small-molecule, reversible inhibitor of both EGFR and HER2 tyrosine kinase, and its activities include subsequent inhibition of its down- stream MAPK-ERK1/2, and the AKT signaling pathway."	( [Tykerb for breast cancer]. Okamura, T; Saito, Y; Suzuki, Y; Tokuda, Y, 2011)	1.09
"Lapatinib is a small molecule dual RTK inhibitor that targets epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2)."	( Lapatinib, a preventive/therapeutic agent against mammary cancer, suppresses RTK-mediated signaling through multiple signaling pathways. Bode, AM; Carper, A; Cho, YY; Ericson, ME; Grubbs, CJ; Langfald, A; Li, J; Lubet, RA, 2011)	2.53
"Lapatinib is a dual inhibitor of epidermal growth factor receptor (EGFR) and human EGFR-2 (HER-2) tyrosine kinases. "	( Effects of lapatinib monotherapy: results of a randomised phase II study in therapy-naive patients with locally advanced squamous cell carcinoma of the head and neck. Biswas-Baldwin, N; Bourhis, J; Carracedo, C; Compton, N; Cupissol, D; De Raucourt, D; Del Campo, JM; Downie, L; El-Hariry, I; Harrington, KJ; Hitt, R; Lokanatha, D; Maroudias, N; Midwinter, D; Nutting, CM; Sebastian, P; Temam, S, 2011)	2.2
"Lapatinib ditosylate is an orally available, small molecule targeting the tyrosine activity of the HER2 receptor."	( Lapatinib ditosylate: expanding therapeutic options for receptor tyrosine-protein kinase erbB-2-positive breast cancer. Awada, A; Bozovic-Spasojevic, I; Saliba, W, 2011)	2.53
"Lapatinib is an oral, small-molecule, dual tyrosine kinase inhibitor of epidermal growth factor receptors (EGFR, or ErbB/Her) in solid tumors. "	( Lapatinib induces autophagy, apoptosis and megakaryocytic differentiation in chronic myelogenous leukemia K562 cells. Chen, YC; Chen, YJ; Huang, HL; Huang, YC; Pan, Hy; Shih, SP; Yang, KC, 2011)	3.25
"Lapatinib is a clinically important component of the treatment for HER2-positive metastatic breast cancer and has an acceptable safety profile. "	( Lapatinib-induced liver injury characterized by class II HLA and Gilbert's syndrome genotypes. Dollery, CT; Hunt, CM; Parham, LR; Spraggs, CF, 2012)	3.26
"Lapatinib is a dual inhibitor of epidermal growth factor receptor (EGFR) and HER2/neu, both implicated in cholangiocarcinogenesis."	( HER2/neu may not be an interesting target in biliary cancers: results of an early phase II study with lapatinib. Bekaii-Saab, T; O'Neil, B; Peck, J; Villalona Calero, M; Wei, L; Zalupski, M, 2012)	1.32
"Lapatinib is a potent reversible and selective inhibitor of the tyrosine kinase domains of epidermal growth factor receptor and human epidermal growth factor receptor (HER)-2 that exerts its action by competitive binding to the intracellular ATP-binding site of the receptor. "	( Lapatinib for advanced or metastatic breast cancer. Beijnen, JH; Guchelaar, HJ; Opdam, FL; Schellens, JH, 2012)	3.26
"Lapatinib is a tyrosine kinase inhibitor targeting epidermal growth factor receptors 1 (EGFR/HER1) and 2 (HER2) used in the treatment of patients with HER2-positive breast cancer. "	( High lapatinib plasma levels in breast cancer patients: risk or benefit? Bouchalova, K; Cizkova, M; Cwiertka, K; Friedecky, D; Hajduch, M; Janostakova, A; Melichar, B; Polynkova, A; Radova, L; Trojanec, R; Zezulova, M; Zlevorova, M, )	2.09
"Lapatinib is a dual tyrosine kinase inhibitor (TKI) that has a considerable efficacy in ErbB2-positive metastatic breast cancer (MBC). "	( Evaluation of cardiac safety of lapatinib therapy for ErbB2-positive metastatic breast cancer: a single center experience. Altundag, K; Dogan, E; Ozer, N; Ozisik, Y; Petekkaya, I; Yorgun, H, 2012)	2.11
"As lapatinib is a strong inhibitor of several ATP-dependent ABC-type efflux transporters, this likely occurred because lapatinib blocked doxorubicin efflux, thereby increasing intracellular doxorubicin concentrations and, thus, increasing myocyte damage."	( The dual-targeted HER1/HER2 tyrosine kinase inhibitor lapatinib strongly potentiates the cardiac myocyte-damaging effects of doxorubicin. Hasinoff, BB; Patel, D; Wu, X, 2013)	1.15
"Lapatinib is a clinically potent kinase inhibitor for breast cancer patients because of its outstanding selectivity for epidermal growth factor receptor (EGFR) and EGFR2 (also known as HER2). "	( Temporal profiling of lapatinib-suppressed phosphorylation signals in EGFR/HER2 pathways. Imami, K; Imamura, H; Ishihama, Y; Sugiyama, N; Taniguchi, M; Toi, M; Tomita, M; Ueno, T; Wakabayashi, M, 2012)	2.14
"Lapatinib is an effective anti-HER2 therapy in advanced breast cancer and docetaxel is one of the most active agents in breast cancer. "	( An European Organisation for Research and Treatment of Cancer phase I study of lapatinib and docetaxel as neoadjuvant treatment for human epidermal growth factor receptor 2 (HER2) positive locally-advanced/inflammatory or large operable breast cancer. Bartlett, J; Bogaerts, J; Bonnefoi, H; Cameron, D; Debled, M; Fiche, M; Fournier, M; Koch, KM; Marreaud, S; Nobahar, M; Pierga, JY; Zaman, K; Zimmer, A, 2013)	2.06
"Lapatinib is a dual tyrosine kinase inhibitor targeting EGFR and HER2."	( Lapatinib acts on gastric cancer through both antiproliferative function and augmentation of trastuzumab-mediated antibody-dependent cellular cytotoxicity. Fujii, H; Inoue, A; Inoue, M; Izawa, S; Kawaguchi, Y; Kono, K; Maruyama, T; Mimura, K; Shiba, S; Shiraishi, K; Watanabe, M, 2013)	2.55
"Lapatinib is an oral 4-anilinoquinazoline derivative that dually inhibits epidermal growth factor receptor and human epidermal growth factor receptor 2 (HER2). "	( Physiologically based pharmacokinetic model of lapatinib developed in mice and scaled to humans. Gustafson, DL; Hudachek, SF, 2013)	2.09
"Lapatinib is a dual tyrosine kinase inhibitor selective for inhibition of epidermal growth factor receptor and human epidermal growth factor receptor-2 autophosphorylation, leading to suppression of proliferation pathways of solid tumors."	( Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Dolder, CR; Nelson, MH, 2006)	2.5
"Lapatinib (GW572016) is a selective inhibitor of both epidermal growth factor receptor (EGFR) and HER-2 tyrosine kinases. "	( Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Berger, M; Finn, R; Gilmer, TM; Keith, BR; Konecny, GE; Mullin, RJ; Pegram, MD; Podratz, KC; Rahmeh, M; Rusnak, DW; Slamon, DJ; Spehar, G; Untch, M; Venkatesan, N; Yang, G, 2006)	2.05
"Lapatinib is an oral dual tyrosine kinase inhibitor that targets epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor-2 (HER2), both frequently overexpressed in human cancer. "	( Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Johnston, SR; Leary, A, 2006)	3.22
"Lapatinib is an oral receptor tyrosine kinase inhibitor, targeting both the ErbB-1 and ErbB-2 receptors. "	( Lapatinib: current status and future directions in breast cancer. Goss, PE; Moy, B, )	3.02
"Lapatinib (GW 572016) is an oral inhibitor of the tyrosine kinase activity of epidermal growth factor receptor (EGFR) and human EGFR-2 (HER2), which are both frequently altered in human malignant tumors. "	( Lapatinib: a dual inhibitor of EGFR and HER2 tyrosine kinase activity. Aglietta, M; Montemurro, F; Valabrega, G, 2007)	3.23
"Lapatinib is an oral, small molecule, reversible dual inhibitor of ErbB1 (epidermal growth factor receptor) and ErbB2 (HER2) tyrosine kinases."	( Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy. Griffiths, TR; Kriajevska, M; McHugh, LA; Mellon, JK, 2007)	1.31
"Lapatinib is a tyrosine kinase inhibitor, blocking tryosine kinase domains of both epidermal growth factor receptor and HER-2."	( HER-2-positive breast cancer: hope beyond trastuzumab. Bartsch, R; Steger, GG; Wenzel, C; Zielinski, CC, 2007)	1.06
"Lapatinib (GW572016) is a small-molecule dual inhibitor of epidermal growth factor receptor (ErbB1) and ErbB2 receptor kinase activities currently in phase III clinical trials. "	( Delineation of molecular mechanisms of sensitivity to lapatinib in breast cancer cell lines using global gene expression profiles. Alligood, K; Bertiaux, M; Gagnon, R; Gilmer, TM; Hegde, PS; Rusnak, D; Strum, J, 2007)	2.03
"Lapatinib is an oral dual tyrosine kinase inhibitor selective for inhibition of epidermal growth factor receptor (EGFR/ErbB1) and HER2/ErbB2."	( Lapatinib in breast cancer. Bilancia, D; Dinota, A; Germano, D; Manzione, L; Romano, R; Rosati, G, 2007)	2.5
"Lapatinib is an oral receptor tyrosine kinase inhibitor, inhibiting both the ErbB-1 and ErbB-2 receptors. "	( Lapatinib-associated toxicity and practical management recommendations. Goss, PE; Moy, B, 2007)	3.23
"Lapatinib is a dual (ErbB-1 and ErB-2) receptor tyrosine kinase inhibitor (TKI) that was recently approved by the FDA for the treatment of advanced breast cancer. "	( Lapatinib: a tyrosine kinase inhibitor with a clinical role in breast cancer. Chan, S; Dhadda, AS; Mukherjee, A; Shehata, M, 2007)	3.23
"Lapatinib is a small molecule, dual tyrosine kinase inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor type 2 (HER2). "	( A phase III randomized comparison of lapatinib plus capecitabine versus capecitabine alone in women with advanced breast cancer that has progressed on trastuzumab: updated efficacy and biomarker analyses. Cameron, D; Campone, M; Casey, M; Chan, A; Chan, S; Crown, J; Davidson, N; Geyer, CE; Gorbounova, V; Jagiello-Gruszfeld, A; Kaufman, B; Lindquist, D; Newstat, B; Oliva, C; Paoletti, P; Pienkowski, T; Press, M; Raats, JI; Romieu, CG; Roychowdhury, D; Rubin, S; Skarlos, D; Stein, S; Viens, P, 2008)	2.06
"Lapatinib is a substrate for the efflux transporters P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP)."	( The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Castellino, S; Harmon, KA; Humphreys, JE; John-Williams, LS; Koch, KM; O'Mara, MJ; Olson, KL; Polli, JW; Serabjit-Singh, CJ, 2008)	1.26
"Lapatinib is an oral dual tyrosine kinase inhibitor targeting EGFR1 and EGFR2 (HER2). "	( Lapatinib: a sword with two edges. Kopper, L, 2008)	3.23
"Lapatinib is an orally reversible inhibitor of epidermal growth factor receptor (EGFR)/human epidermal growth factor receptor 2 (HER-2) tyrosine kinases with demonstrated activity in patients with HER-2-positive breast cancer. "	( Lapatinib versus hormone therapy in patients with advanced renal cell carcinoma: a randomized phase III clinical trial. Audhuy, B; El-Hariry, I; Gardner, JP; Gore, M; Harper, P; Hawkins, R; Machiels, JP; Pétavy, F; Ravaud, A; Rolland, F; Schöffski, P; von der Maase, H; Zantl, N, 2008)	3.23

Excerpt	Reference	Relevance
"Some lapatinib derivatives have been previously synthesized by modification at the methylsulfonylethylaminomethylfuryl group and biologically evaluated, demonstrating that the 2i compound shows potent inhibitory activity against EGFR/HER2-overexpressing cancer cells."	( Dissecting the molecular recognition of dual lapatinib derivatives for EGFR/HER2. Bello, M; Guadarrama-García, C; Rodriguez-Fonseca, RA, 2020)	1.27
"Lapatinib (LAP) has been approved by the FDA in combination with other anticancer agents for the treatment of HER2-positive breast cancer."	( Lapatinib enhances paclitaxel toxicity in MCF-7, T47D, and MDA-MB-321 breast cancer cells. Nycz, J; Wilczok, A; Zajdel, A, 2021)	2.79
"Lapatinib has been widely used as a HER2-targeted therapy, however, a number of patients develop lapatinib resistance and still suffer from poor prognosis."	( Phosphoproteomic analysis reveals PAK2 as a therapeutic target for lapatinib resistance in HER2-positive breast cancer cells. Chang, Y; Han, KC; Lee, JE; Park, KH, 2018)	1.44
"Lapatinib has clinical efficacy in the treatment of trastuzumab-refractory HER2-positive breast cancer. "	( Development of acquired resistance to lapatinib may sensitise HER2-positive breast cancer cells to apoptosis induction by obatoclax and TRAIL. Browne, BC; Conlon, NT; Crown, J; Espina, V; Eustace, AJ; Gallagher, C; Gallagher, WM; Ginther, C; Holmes, FA; Liotta, LA; Madden, SF; McDermott, MSJ; O'Brien, NA; O'Donovan, N; O'Driscoll, L; O'Leary, P; O'Shaughnessy, J; Rani, S; Slamon, D; Walsh, N; Watson, WR; Zagozdzon, R, 2018)	2.19
"Lapatinib has antiproliferative effects in a subgroup of HER2(-) nonamplified tumors characterized by high HER3 expression. "	( Antiproliferative Effect of Lapatinib in HER2-Positive and HER2-Negative/HER3-High Breast Cancer: Results of the Presurgical Randomized MAPLE Trial (CRUK E/06/039). A'Hern, R; Bliss, JM; Bundred, N; Coombes, G; Detre, S; Dowsett, M; Evans, A; Harper-Wynne, C; Haynes, BP; Hills, M; Johnston, SR; Leary, A; Sahoo, R; Smith, I, 2015)	2.15
"Lapatinib has been used in combination with capecitabine or paclitaxel to treat patients with progressive HER2-overexpressing metastatic breast cancer (MBC). "	( Lapatinib promotes the incidence of hepatotoxicity by increasing chemotherapeutic agent accumulation in hepatocytes. Chen, Z; Dai, C; Fu, L; Huang, Z; Ma, S; To, K; Wang, F; Wu, X; Zhao, H, 2015)	3.3
"Lapatinib has proven efficacy as monotherapy and in combination with capecitabine in patients with metastatic breast cancer (MBC) overexpressing HER2 and/or EGFR. "	( Phase I and pharmacological trial of lapatinib in combination with gemcitabine in patients with advanced breast cancer. Beijnen, JH; Boss, DS; Grob, M; Huitema, AD; Keessen, M; Rehorst, H; Rosing, H; Schellens, JH; Smit, WM; Tibben, MM; van der Noll, R; Wymenga, AN, 2015)	2.13
"Lapatinib has demonstrated efficacy in combination with capecitabine in patients with previously treated HER2-positive metastatic breast cancer. "	( Lapatinib: a dual tyrosine kinase inhibitor for metastatic breast cancer. Paul, B; Thompson, J; Trovato, JA, 2008)	3.23
"Lapatinib has been reported to have antitumor activity in Phase II trials when used as first-line therapy for MBC, in patients with inflammatory breast cancer, and in patients with central nervous system metastases."	( Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Goodin, S; Medina, PJ, 2008)	2.51
"Lapatinib has little activity against the xenografts of the PPTP's in vivo panel, and its in vitro activity occurs at concentrations above those associated with specific EGFR/ErbB2 inhibition. "	( Initial testing (stage 1) of lapatinib by the pediatric preclinical testing program. Carol, H; Gorlick, R; Houghton, PJ; Keir, ST; Kolb, EA; Lock, R; Maris, JM; Morton, CL; Phelps, D; Reynolds, CP; Schaiquevich, P; Smith, MA; Stewart, C; Wu, J, 2009)	2.09
"Lapatinib has recently been approved, in combination with capecitabine, for the treatment of HER2-positive metastatic breast cancer patients failing trastuzumab therapy."	( Lapatinib plus letrozole for postmenopausal patients with advanced HER2(+)/HR(+) breast cancer. Guarneri, V, 2009)	2.52
"Lapatinib has provided an alternative for the treatment of advanced HER-2 overexpressing breast cancer and is currently being assessed in early disease."	( Lapatinib for breast cancer: a review of the current literature. Gelmon, KA; MacFarlane, RJ, 2011)	3.25
"Lapatinib has already been approved by the US Food and Drug Administration for treatment of selected cases of breast cancer."	( A phase I study of capecitabine, oxaliplatin, and lapatinib in metastatic or advanced solid tumors. Alberti, D; Bowen, CJ; Dar, MM; Dennie, TW; Fleming, RA; Holen, KD; Loconte, N; Mulkerin, D; Oliver, K, 2011)	1.34
"Lapatinib has minimal activity in recurrent ovarian cancer. "	( A phase II evaluation of lapatinib in the treatment of persistent or recurrent epithelial ovarian or primary peritoneal carcinoma: a gynecologic oncology group study. Armstrong, DK; Carolla, RL; Fischer, EG; Garcia, AA; Godwin, AK; Lankes, HA; Leslie, KK; Liepman, MK; Mannel, RS; Sill, MW; Spirtos, NM, 2012)	2.13
"Lapatinib has shown clinical activity in solid tumors, with the most notable in advanced or metastatic breast cancer, including tumors refractory to trastuzumab."	( Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Dolder, CR; Nelson, MH, 2006)	2.5
"Lapatinib has novel, dual tyrosine kinase inhibitory properties selective for factors overexpressed in some solid tumors. "	( Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Dolder, CR; Nelson, MH, 2006)	3.22
"Lapatinib has been shown to have activity in ErbB-2-overexpressing breast cancer in several phase II and III clinical trials."	( Lapatinib-associated toxicity and practical management recommendations. Goss, PE; Moy, B, 2007)	2.5
"Lapatinib has demonstrated benefit in combination with capecitabine in patients with HER2-positive locally advanced and metastatic breast cancer that has progressed after prior treatment with an anthracycline, a taxane, and trastuzumab."	( The emerging role of lapatinib in HER2-positive breast cancer. Geyer, CE; Greenberg, L; Ulhoa-Cintra, A, 2008)	1.39

Excerpt	Reference	Relevance
"Lapatinib and BBR activate Akt through upregulation of alternative signaling, which lead to chemoresistance in TNBC cell."	( Pharmacotranscriptomic profiling of resistant triple-negative breast cancer cells treated with lapatinib and berberine shows upregulation of PI3K/Akt signaling under cytotoxic stress. Chen, Y; Hin Cho, C; Imani, S; Jabbarzadeh Kaboli, P; Jomhori, M; Li, M; Luo, S; Shen, J; Wu, X; Wu, Z; Xiang, S; Xiao, Z; Zhao, Y, 2022)	1.66
"Lapatinib may not enhance the anti-tumor effects of gemcitabine for pancreatic cancer."	( In vitro effects of lapatinib with gemcitabine for pancreatic cancer cells. Amano, R; Hirakawa, K; Hirata, K; Kimura, K; Komoto, M; Murata, A; Nakata, B, 2013)	2.16
"Lapatinib did not enhance the risk of radiation or anthracycline-induced cardiac toxicity in mice up to 40 weeks after treatment, but mitochondrial damage was more severe after doxorubicin combined with lapatinib."	( Radiation- and anthracycline-induced cardiac toxicity and the influence of ErbB2 blocking agents. Hoving, S; Russell, NS; Seemann, I; Song, JY; Stewart, FA; te Poele, JA, 2013)	1.11
"Lapatinib was shown to increase the accumulation of doxorubicin in ABCB1-overexpressing hepatocellular cancer cells and normal liver tissues without altering the protein level of ABCB1."	( Lapatinib promotes the incidence of hepatotoxicity by increasing chemotherapeutic agent accumulation in hepatocytes. Chen, Z; Dai, C; Fu, L; Huang, Z; Ma, S; To, K; Wang, F; Wu, X; Zhao, H, 2015)	2.58
"Lapatinib failed to inhibit AKT phosphorylation in PIK3CA mutant cells, likely because of hyperactivation of the phosphatidylinositol 3-kinase (PI3K) signaling pathway by the mutation."	( Roles of BIM induction and survivin downregulation in lapatinib-induced apoptosis in breast cancer cells with HER2 amplification. Fumita, S; Nakagawa, K; Nishio, K; Okamoto, I; Okamoto, W; Tanizaki, J, 2011)	1.34
"Lapatinib may also enable reduced-dose chemotherapy, a potential toxicity-sparing strategy."	( Combined treatment of bladder cancer cell lines with lapatinib and varying chemotherapy regimens--evidence of schedule-dependent synergy. Griffiths, TR; Kriajevska, M; McHugh, LA; Mellon, JK, 2007)	1.31

Excerpt	Reference	Relevance
"Lapatinib treatment of a panel of HER2+ breast cancer cell lines increased HER3 expression in the lapatinib-resistant cell line MDA-MB 453 but not the lapatinib-resistant cell-line HCC-1569. "	( HER3 PET Imaging Identifies Dynamic Changes in HER3 in Response to HER2 Inhibition with Lapatinib. Austin, E; Kalomeris, T; Larimer, B; Mahmood, U; Nesti, S; Sinevici, N; Wehrenberg-Klee, E, 2021)	2.29
"With lapatinib treatment, lapatinib-resistant breast cancer cells demonstrated sustained lipogenesis compared with the sensitive cells."	( Evaluating HER2 amplification status and acquired drug resistance in breast cancer cells using Raman spectroscopy. Arteaga, CL; Bi, X; Guo, M; Mahadevan-Jansen, A; Rexer, B, 2014)	0.86
"In lapatinib-treated patients, there was a significant difference in ALT case incidence between HLA carriers and noncarriers. "	( Prospective validation of HLA-DRB1*07:01 allele carriage as a predictive risk factor for lapatinib-induced liver injury. Cardon, LR; Cox, CJ; Curran, J; Ejlertsen, B; Finkelstein, DM; Goss, PE; McDonnell, SK; Parham, LR; Rappold, E; Schaid, DJ; Spraggs, CF, 2014)	1.25
"Lapatinib treatment of "sensitive" Her2(+) cells induces apoptotic cell death and enhances transcript and protein levels of Bim, a pro-apoptotic Bcl2 family member. "	( PTK6 inhibition promotes apoptosis of Lapatinib-resistant Her2(+) breast cancer cells by inducing Bim. Halstead-Nussloch, G; Irie, HY; Ito, K; Katsyv, I; Olcott, W; Park, SH, 2015)	2.13
"Lapatinib-treated Asian participants and those less than 60 years had significant improvement in progression-free survival (PFS), particularly among those whose cancers had 5.01-10.0 and >10.0-fold amplification of HER2 In conclusion, HER2 is commonly amplified in UGI adenocarcinomas with amplification highly correlated to overexpression, and HER2 amplification levels correlated with PFS."	( HER2 Status in Advanced or Metastatic Gastric, Esophageal, or Gastroesophageal Adenocarcinoma for Entry to the TRIO-013/LOGiC Trial of Lapatinib. Afenjar, K; Bang, YJ; Buyse, M; Chung, HC; Ellis, CE; Estrada, MC; Gagnon, RC; Grob, TJ; Hecht, JR; Jeziorski, K; Liang, Z; Ma, Y; Park, JO; Press, MF; Qin, SK; Robinson, DM; Sauter, G; Scherer, SJ; Slamon, DJ; Villalobos, I; Wu, S; Xu, J, 2017)	1.38
"Lapatinib treatment also produced a significant suppression of intrahepatic cholangiocarcinoma growth when administered early to rats, but was without effect in inhibiting liver tumor growth in rats with more advanced tumors."	( Preclinical assessment of simultaneous targeting of epidermal growth factor receptor (ErbB1) and ErbB2 as a strategy for cholangiocarcinoma therapy. Almenara, JA; Campbell, DJ; Dewitt, JL; Oyesanya, RA; Sirica, AE; Zhang, Z, 2010)	1.08
"Lapatinib treatment significantly augments the concentration of the inactive (unphosphorylated) form of HER2 protein at the tumor cell membrane and promotes an exacerbated HER2 ECD shedding to the extracellular milieu of HER2-overexpressing cancer cells."	( Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth. Cufí, S; Del Barco, S; Martin-Castillo, B; Menendez, JA; Oliveras-Ferraros, C; Vazquez-Martin, A, 2011)	2.53
"Oral lapatinib treatment caused tumor shrinkage and serum PRL suppression both in HER2CA transfectant-inoculated Wistar-Furth rats and in estrogen-induced Fischer344 rat prolactinomas."	( HER2/ErbB2 receptor signaling in rat and human prolactinoma cells: strategy for targeted prolactinoma therapy. Bannykh, S; Cooper, O; Fukuoka, H; Melmed, S; Mizutani, J; Ren, SG; Tong, Y, 2011)	0.82
"Lapatinib treatment of BT474 or SKBR3 cells resulted in nuclear translocation and activation of FOXO3a, followed by a reduction in VEGF expression."	( FOXO3a represses VEGF expression through FOXM1-dependent and -independent mechanisms in breast cancer. Brosens, JJ; Chan, KY; Chen, J; Cheung, YN; Feltes, A; Gomes, AR; Ho, KK; Karadedou, CT; Khoo, US; Lam, EW; Petkovic, M; Tsang, JW; Wong, SY; Zwolinska, AK, 2012)	1.1
"Lapatinib treatment alone only slightly induced myocyte damage."	( The dual-targeted HER1/HER2 tyrosine kinase inhibitor lapatinib strongly potentiates the cardiac myocyte-damaging effects of doxorubicin. Hasinoff, BB; Patel, D; Wu, X, 2013)	1.36
"The lapatinib-treated cells showed a dose-dependent inhibition of cell proliferation and induction of apoptosis at the same concentrations that blocked ErbB1/ErbB2 phosphorylation."	( Dual ErbB1 and ErbB2 receptor tyrosine kinase inhibition exerts synergistic effect with conventional chemotherapy in pancreatic cancer. Drebin, JA; Pippin, JA; Singla, S, 2012)	0.86
"Lapatinib treatment caused a 50% inhibition in tumor growth, an effect correlated with a blockade of both ErbB1 and ErbB2 phosphorylation levels, and of downstream signaling pathways (Akt, ERKs and Stat3)."	( ErbBs inhibition by lapatinib blocks tumor growth in an orthotopic model of human testicular germ cell tumor. Casanovas, O; Castillo-Ávila, W; Condom, E; Garcia Del Muro, X; Germà, JR; Graupera, M; Hernández-Losa, J; Juliachs, M; Pandiella, A; Piulats, JM; Teixidó, C; Vidal, A; Villanueva, A; Viñals, F, 2013)	1.43
"Rats treated with lapatinib and elsiglutide had less severe diarrhoea than rats treated with lapatinib alone. "	( The GLP-2 analogue elsiglutide reduces diarrhoea caused by the tyrosine kinase inhibitor lapatinib in rats. Bateman, E; Bowen, JM; Keefe, DM; Mayo, BJ; Pietra, C; Secombe, KR; Thorpe, D; Wignall, AD, 2020)	1.11
"Treatment with lapatinib reduced BeWo cell proliferation by inducing apoptosis. "	( Lapatinib Inhibits Amphiregulin-induced BeWo Choriocarcinoma Cell Proliferation by Reducing ERK1/2 and AKT Signaling Pathways. Brum, IS; Cheng, JC; Cordero, E; Leung, PCK; Pires, LV; Pizzolato, LS; Yi, Y, 2019)	2.31
"Treatment with lapatinib plus capecitabine for HER2-positive metastatic breast cancer (MBC) with primary or acquired resistance to trastuzumab was analyzed retrospectively."	( Ki-67 index as a prognostic factor of subsequent lapatinib-based therapy in HER2-positive metastatic breast cancer with resistance to trastuzumab. Bian, L; Du, G; Guo, YF; Jiang, ZF; Li, W; Song, ST; Wang, T; Wu, SK; Zhang, HQ; Zhang, SH, 2014)	1
"Upon treatment with lapatinib, 93% of these "mini-foci" were reversed."	( Impact of ERBB2 mutations on in vitro sensitivity of bladder cancer to lapatinib. Clozel, T; de Martino, M; Elemento, O; Klatte, T; Krzywinski, M; Rieken, M; Rouprêt, M; Shariat, SF; Xylinas, E; Zhuang, D, 2014)	0.95
"Pretreatment of lapatinib increased the radiosensitivity of SKBR3 (sensitizer enhancement ratio [SER]: 1.21 at a surviving fraction of 0.5) and BT474 (SER: 1.26 at a surviving fraction of 0.5) cells and hindered the repair of DNA damage, as suggested by the prolongation of radiation-induced γH2AX foci and the down-regulation of phosphorylated DNA-dependent protein kinase, catalytic subunit (p-DNAPKcs)."	( Radiosensitizing effect of lapatinib in human epidermal growth factor receptor 2-positive breast cancer cells. Cho, BJ; Choi, EJ; Kim, DH; Kim, IA; Park, JM; Yu, T, 2016)	1.07
"Cotreatment with lapatinib and SN-38 also resulted in enhanced cell cycle arrest and the induction of apoptosis with subsequent cellular pharmacokinetic analysis demonstrating that lapatinib promoted the increased intracellular accumulation and retention of SN-38 when compared to SN-38 treatment alone."	( The dual EGFR/HER-2 tyrosine kinase inhibitor lapatinib sensitizes colon and gastric cancer cells to the irinotecan active metabolite SN-38. Fazzone, W; LaBonte, MJ; Ladner, RD; Lenz, HJ; Louie, SG; Manegold, PC; Wilson, PM, 2009)	0.94
"Treatment of lapatinib-resistant SUM185 cells with CI-1040 restored radiosensitization with 45% fewer surviving colonies when combined with radiation."	( Mechanism of lapatinib-mediated radiosensitization of breast cancer cells is primarily by inhibition of the Raf>MEK>ERK mitogen-activated protein kinase cascade and radiosensitization of lapatinib-resistant cells restored by direct inhibition of MEK. Camp, JT; Kimple, RJ; Sambade, MJ; Sartor, CI; Shields, JM, 2009)	1.08
"Treatment with lapatinib beginning 5 days after MNU was highly effective in preventing cancer development."	( Lapatinib, a preventive/therapeutic agent against mammary cancer, suppresses RTK-mediated signaling through multiple signaling pathways. Bode, AM; Carper, A; Cho, YY; Ericson, ME; Grubbs, CJ; Langfald, A; Li, J; Lubet, RA, 2011)	2.15
"The treatment with lapatinib plus capecitabine was well tolerated, with grade 3-4 toxicity reported in few patients, and no treatment-related deaths were noted."	( Lapatinib-based therapy in heavily pretreated HER2-positive metastatic breast cancer: a single institution experience. Carli, P; Crivellari, D; Lombardi, D; Militello, L; Miolo, G; Russo, AE; Sorio, R; Spazzapan, S; Talamini, R; Torrisi, E; Veronesi, A, )	1.89

Excerpt	Reference	Relevance
" The most frequently reported drug-related adverse events were diarrhea (42%) and rash (31%)."	( Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. Blackwell, KL; Burris, HA; Dees, EC; Dowlati, A; Ellis, MJ; Harris, JL; Hurwitz, HI; Jones, SF; Koch, KM; Mangum, S; Marcom, PK; O'Neil, B; Overmoyer, B; Smith, DA; Spector, NL; Stead, A, 2005)	0.57
" We analyzed cardiac events defined as symptomatic (grade 3 or 4 left ventricular systolic dysfunction according to the National Cancer Institute Common Terminology Criteria for Adverse Events) or asymptomatic (LVEF decreases > or = 20% relative to baseline and below the institution's lower limit of normal; no symptoms)."	( Cardiac safety of lapatinib: pooled analysis of 3689 patients enrolled in clinical trials. Byrne, J; Ewer, MS; Koehler, M; Perez, EA; Preston, AJ; Rappold, E, 2008)	0.68
" Collectively, our data demonstrate that Obatoclax mediated inhibition of MCL-1 rapidly enhances Lapatinib toxicity in tumor cells via a toxic form of autophagy and via AIF release from the mitochondrion."	( Inhibition of MCL-1 enhances lapatinib toxicity and overcomes lapatinib resistance via BAK-dependent autophagy. Dent, P; Grant, S; Martin, AP; Mitchell, C; Nephew, KP; Rahmani, M, 2009)	0.86
" The most frequent adverse event was diarrhoea."	( Lapatinib monotherapy in patients with relapsed, advanced, or metastatic breast cancer: efficacy, safety, and biomarker results from Japanese patients phase II studies. Allen, KE; Aogi, K; Arai, T; Ellis, CE; Fujiwara, Y; Gagnon, RC; Ito, Y; Iwata, H; Katsura, K; Nakamura, S; Rai, Y; Sasaki, Y; Taguchi, T; Takashima, S; Toi, M; Tokuda, Y; Wakamatsu, T; Watanabe, J, 2009)	1.8
" Common adverse events included diarrhea, rash, alopecia, and nausea (> 50% of patients in both cohorts)."	( Phase II study to evaluate the efficacy and safety of neoadjuvant lapatinib plus paclitaxel in patients with inflammatory breast cancer. Boussen, H; Cristofanilli, M; DeSilvio, M; Salazar, V; Spector, N; Zaks, T, 2010)	0.6
" Tolerable dose, need for supportive treatments, and early signals for toxic effect were evaluated in a planned safety analysis of 270 patients."	( Integrating bevacizumab, everolimus, and lapatinib into current neoadjuvant chemotherapy regimen for primary breast cancer. Safety results of the GeparQuinto trial. Blohmer, JU; Costa, SD; Eidtmann, H; Fasching, PA; Fehm, T; Gerber, B; Hanusch, C; Hilfrich, J; Kreienberg, R; Loibl, S; Nekljudova, V; Solbach, C; Strumberg, D; Untch, M; von Minckwitz, G, 2011)	0.64
" Adverse events such as congestive heart failure and life threatening diarrhoea are sometimes observed because of off-target drug effects."	( Prevention and management of major side effects of targeted agents in breast cancer. Awada, A; Azim, HA; Metzger Filho, O; Saini, KS, 2012)	0.38
"Hepatobiliary adverse events (AEs) have been observed in a small proportion of patients with metastatic breast cancer (MBC) treated with lapatinib."	( HLA-DQA1*02:01 is a major risk factor for lapatinib-induced hepatotoxicity in women with advanced breast cancer. Bing, N; Briley, LP; Budde, LR; Cardon, LR; Cox, CJ; King, KS; Mooser, VE; Preston, AJ; Spraggs, CF; Stein, SH; Whittaker, JC, 2011)	0.84
" Although agents such as gefitinib, erlotinib, cetuximab, lapatinib, and panitumumab have less systemic side-effects than traditional cytotoxic chemotherapy, dermatologic adverse events from EGFRIs are significantly more common."	( Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors. Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA, 2011)	0.61
"This review provides a symptom-based treatment approach to the common dermatologic adverse effects seen with the epidermal growth factor receptor antagonists: papulopustular rash, xerosis, pruritus as well as hair, nail, and mucosal changes."	( Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors. Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA, 2011)	0.37
"Although the field continues to evolve, this review presents the most up-to-date information on managing dermatologic adverse effects of EGFRIs."	( Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors. Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA, 2011)	0.37
" According to our findings, lapatinib was safe and well tolerated and has a low incidence of cardiac side effects."	( Evaluation of cardiac safety of lapatinib therapy for ErbB2-positive metastatic breast cancer: a single center experience. Altundag, K; Dogan, E; Ozer, N; Ozisik, Y; Petekkaya, I; Yorgun, H, 2012)	0.96
"Objectives were to assess maximum tolerated dose, dose-limiting toxicity (DLT) and to recommend a safe dose of LAP when administered with 4 cycles of TPF followed by CRT."	( EORTC 24051: unexpected side effects in a phase I study of TPF induction chemotherapy followed by chemoradiation with lapatinib, a dual EGFR/ErbB2 inhibitor, in patients with locally advanced resectable larynx and hypopharynx squamous cell carcinoma. Andry, G; Awada, A; Bogaerts, J; El-Hariry, I; Fortpied, C; Lacombe, D; Lalami, Y; Langendijk, JA; Liberatoscioli, C; Specenier, PM; Vermorken, JB, 2012)	0.59
" Despite their selective molecular targeting and demonstrated clinical benefit, TKIs produce a range of serious adverse events, including drug-induced liver injury, that require careful patient management to maintain treatment benefit without harm."	( Genetic characterization to improve interpretation and clinical management of hepatotoxicity caused by tyrosine kinase inhibitors. Hunt, CM; Spraggs, CF; Xu, CF, 2013)	0.39
"Although dual HER2 blockade shows promising results in patients with HER2-positive breast cancer it is unclear whether this treatment strategy increases the risk for cardiac adverse events."	( Cardiac toxicity in breast cancer patients treated with dual HER2 blockade. Lind, P; Nearchou, A; Polyzos, NP; Valachis, A, 2013)	0.39
" The majority of drug-related adverse events were mild to moderate (grade 1 or 2); the most common adverse events reported were palmar-plantar erythrodysesthesia syndrome (76 %), diarrhea (67 %) and stomatitis (41 %)."	( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study. Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015)	0.62
"The most frequent adverse events (AEs) for all cohorts were diarrhea (89%), rash (79%), fatigue (73%), alopecia (63%), nausea (63%), and vomiting (40%)."	( An open-label safety study of lapatinib plus trastuzumab plus paclitaxel in first-line HER2-positive metastatic breast cancer. Brewster, AM; Esteva, FJ; Florance, AM; Franco, SX; Hagan, MK; Perez, A; Somer, RA; Stein, S; Turner, S; Williams, W, 2013)	0.68
" In a cell-based model, sunitinib reduced CDK5 phosphorylation (pCDK5), calpain-dependent p35/p25 conversion and protected neuronal cells from the toxic effects of gp120."	( Neuroprotective effects of the anti-cancer drug sunitinib in models of HIV neurotoxicity suggests potential for the treatment of neurodegenerative disorders. Crews, LA; Gonzales, T; Kouznetsova, VL; Masliah, E; Overk, CR; Patrick, C; Paulino, A; Price, D; Rockenstein, E; Stocking, E; Tsigelny, IF; Wrasidlo, W, 2014)	0.4
" Outcomes included pathologic complete response (pCR), overall survival (OS), progression-free survival (PFS), and adverse events."	( Effect and safety of dual anti-human epidermal growth factor receptor 2 therapy compared to monotherapy in patients with human epidermal growth factor receptor 2-positive breast cancer: a systematic review. He, J; Li, YS; Wei, X; Yu, FF; Zhang, TY; Zhang, X; Zhang, XJ, 2014)	0.4
" Dual anti-HER2 therapy was associated with more frequent adverse events than monotherapy, but no statistical differences were observed in cardiac toxicity."	( Effect and safety of dual anti-human epidermal growth factor receptor 2 therapy compared to monotherapy in patients with human epidermal growth factor receptor 2-positive breast cancer: a systematic review. He, J; Li, YS; Wei, X; Yu, FF; Zhang, TY; Zhang, X; Zhang, XJ, 2014)	0.4
" The most common drug-related adverse events were diarrhea (88%) and palmar-plantar erythrodysesthesia syndrome (48%)."	( Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer. Baselga, J; Cortés, J; Garcia-Saenz, JA; Germa, C; Harb, W; Kiger, C; Kim, SB; Martin, M; Moroose, R; Pluard, T; Saura, C; Wang, K; Xu, B, 2014)	0.4
" The most common adverse events (AEs) related to the study treatment were alopecia, diarrhea and decreased hemoglobin."	( Safety, pharmacokinetics and efficacy findings in an open-label, single-arm study of weekly paclitaxel plus lapatinib as first-line therapy for Japanese women with HER2-positive metastatic breast cancer. Aogi, K; Armour, A; Inoue, K; Iwata, H; Kuroi, K; Masuda, N; Nakayama, T; Nishimura, Y; Rai, Y; Sasaki, Y; Shimizu, S, 2015)	0.63
" The objective of this study was to estimate the costs of managing treatment-related grade ≥ 3 adverse events (AEs) that occurred in ≥ 2% of patients and grade 2 AEs that occurred in ≥ 5% of patients taking T-DM1 compared with patients taking CAP + LAP based on the EMILIA trial, from the perspective of Canadian public payers."	( Safety Profile and Costs of Related Adverse Events of Trastuzumab Emtansine for the Treatment of HER2-Positive Locally Advanced or Metastatic Breast Cancer Compared to Capecitabine Plus Lapatinib from the Perspective of the Canadian Health-Care System. Moser, A; Piwko, C; Pollex, E; Prady, C; Yunger, S, 2015)	0.61
" The majority of reported adverse events (AE) were grade 1 and 2 in severity with diarrhea being the most commonly observed AE CONCLUSION: In this heavily pretreated patient population, combination of vinorelbine plus lapatinib showed encouraging activity and was characterized by an acceptable safety profile."	( Phase II study on the efficacy and safety of Lapatinib administered beyond disease progression and combined with vinorelbine in HER-2/neu- positive advanced breast cancer: results of the CECOG LaVie trial. Bartsch, R; Brodowicz, T; Knittelfelder, R; Kuhar, CG; Lang, I; Melichar, B; Petruzelka, L; Singer, CF; Thallinger, C; Zielinski, C, 2016)	0.88
" This includes less toxic drugs, more selective towards tumor cells, causing less damage to the patient."	( Phosphatidylinositol 3-Kinase/AKT Pathway Inhibition by Doxazosin Promotes Glioblastoma Cells Death, Upregulation of p53 and Triggers Low Neurotoxicity. Battastini, AM; Coelho, BP; de Quadros, AH; Gaelzer, MM; Gonçalves, CA; Guerra, MC; Guma, FC; Hoppe, JB; Salbego, CG; Setton-Avruj, P; Terra, SR; Usach, V, 2016)	0.43
" Our study suggests that the combination of two anti-HER2 agents does not significantly increase the risk for adverse compared with anti-HER2 monotherapy in patients with adequate cardiac function prior to start of therapy."	( Applications of cardiotoxicity in breast cancer: a meta-analysis. Davoodzadeh, H; Ebadi, A; Rahmani, H; Shahriary, A; Sheikhi, MA, 2017)	0.46
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."	( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016)	0.43
" More frequent grade 3 or 4 adverse events, including diarrhoea, rash or erythema, neutropenia and hepatic adverse events, were found in the combination group than in the trastuzumab or lapatinib group."	( Efficacy and safety of lapatinib and trastuzumab for HER2-positive breast cancer: a systematic review and meta-analysis of randomised controlled trials. Gao, L; Gao, X; Li, N; Liu, PJ; Tie, XJ; Xu, ZQ; Zhang, Y, 2017)	0.96
"Adverse side effects of cancer agents are of great concern in the context of childhood tumors where they can reduce the quality of life in young patients and cause life-long adverse effects."	( Lapatinib potentiates cytotoxicity of YM155 in neuroblastoma via inhibition of the ABCB1 efflux transporter. Brunak, S; Halasz, M; Huber, KVM; Kolch, W; Papamarkou, T; Radic-Sarikas, B; Superti-Furga, G; Tsafou, KP; Winter, GE, 2017)	1.9
" We aimed to determine whether or not pulse high-dose lapatinib was a safe and tolerable regimen in addition to standard therapy."	( Report of safety of pulse dosing of lapatinib with temozolomide and radiation therapy for newly-diagnosed glioblastoma in a pilot phase II study. Cloughesy, TF; Faiq, N; Green, R; Green, S; Hu, J; Lai, A; Mellinghoff, I; Nghiemphu, PL; Yu, A, 2017)	0.98
" Reportedly, lapatinib has induced cardiovascular adverse events including QT-interval prolongation and heart failure."	( Precise safety pharmacology studies of lapatinib for onco-cardiology assessed using in vivo canine models. Ando, K; Cao, X; Wada, T, 2020)	1.2
" Twenty-two adverse events were observed in 19 (36."	( First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects. Cao, Y; Gong, LY; Guo, CX; Hua, Y; Huang, J; Kuang, Y; Pei, Q; Wang, MN; Yang, GP, 2020)	0.56
" Toxicity was evaluated via a selected subset of adverse events of interest (AEI)."	( Tolerability and toxicity of trastuzumab or trastuzumab + lapatinib in older patients: a sub-analysis of the ALTTO trial (BIG 2-06; NCCTG (Alliance) N063D). Agbor-Tarh, D; Dal Lago, L; de Azambuja, E; Dueck, AC; Gelber, RD; Hilbers, F; Jackisch, C; Jatoi, A; Korde, LA; Moreno-Aspitia, A; Piccart, M; Pondé, N; Sotiriou, C; Werner, O, 2021)	0.87
" Adverse events of interest were likewise more common in the trastuzumab + lapatinib arm with higher AEI rates (63."	( Tolerability and toxicity of trastuzumab or trastuzumab + lapatinib in older patients: a sub-analysis of the ALTTO trial (BIG 2-06; NCCTG (Alliance) N063D). Agbor-Tarh, D; Dal Lago, L; de Azambuja, E; Dueck, AC; Gelber, RD; Hilbers, F; Jackisch, C; Jatoi, A; Korde, LA; Moreno-Aspitia, A; Piccart, M; Pondé, N; Sotiriou, C; Werner, O, 2021)	1.1
"Trastuzumab plus lapatinib was significantly more toxic among older patients and had worse treatment completion."	( Tolerability and toxicity of trastuzumab or trastuzumab + lapatinib in older patients: a sub-analysis of the ALTTO trial (BIG 2-06; NCCTG (Alliance) N063D). Agbor-Tarh, D; Dal Lago, L; de Azambuja, E; Dueck, AC; Gelber, RD; Hilbers, F; Jackisch, C; Jatoi, A; Korde, LA; Moreno-Aspitia, A; Piccart, M; Pondé, N; Sotiriou, C; Werner, O, 2021)	1.21
" Additionally, neutropenia, diarrhoea and fatigue were the most common adverse events caused by these drugs, followed by pain, nausea, decreased appetite, anaemia and vomiting."	( Efficacy and safety of targeted drugs in advanced or metastatic gastric and gastroesophageal junction cancer: A network meta-analysis. Ge, L; Gong, H; Hou, L; Jin, X; Leng, G; Li, C; Li, T; Liu, Y; Ma, L; Niu, S; Su, Y; Zhang, H; Zhang, L; Zhao, L, 2022)	0.72
" The data analytical platform Molecular Health Effect was utilized to map population ADR data from the US Food and Drug Administration (FDA) Adverse Event Reporting System to chemical and biological databases (such as UniProt and Reactome), for hypothesis generation regarding the underlying molecular mechanisms causing cardiotoxicity."	( A case study of a patient-centered reverse translational systems-based approach to understand adverse event profiles in drug development. Jackson, DB; Kim, S; Lahu, G; Lesko, LJ; Soldatos, TG; Trame, MN; Vakilynejad, M, 2022)	0.72
" Pre-treatment PRO associations with overall survival (OS), progression-free survival (PFS), and grade ≥3 adverse events were evaluated via Cox proportional hazards regression."	( Patient-reported outcomes predict survival and adverse events following anticancer treatment initiation in advanced HER2-positive breast cancer. Abuhelwa, AY; Badaoui, S; Danell, NO; Haseloff, M; Hopkins, AM; McKinnon, RA; Modi, ND; Perry, RNA; Rathod, A; Shahnam, A; Sorich, MJ; Swain, SM; Welslau, M, 2022)	0.72
"PROs were identified as independent prognostic factors for OS, PFS, and grade ≥3 adverse events in patients with human epidermal growth factor receptor 2 (HER2)-positive advanced BC initiating contemporary treatment options."	( Patient-reported outcomes predict survival and adverse events following anticancer treatment initiation in advanced HER2-positive breast cancer. Abuhelwa, AY; Badaoui, S; Danell, NO; Haseloff, M; Hopkins, AM; McKinnon, RA; Modi, ND; Perry, RNA; Rathod, A; Shahnam, A; Sorich, MJ; Swain, SM; Welslau, M, 2022)	0.72
"Human epidermal growth factor receptor 2 (HER2)-targeted therapies improve survival for patients with HER2-positive breast cancer but carry risks of hematologic, cardiopulmonary, gastro-hepatobiliary, and other adverse events (AEs)."	( Incidence of adverse events with therapies targeting HER2-positive metastatic breast cancer: a literature review. Cortes, J; Dang, C; Gilsenan, A; Hackshaw, MD; Layton, JB; Lee, C; Perez, EA; Singh, J; Wang, K, 2022)	0.72
" Mechanistically, downregulated expression of the DNA repair protein HMGB1 played a critical role in these toxic reaction processes."	( Decreased HMGB1 expression contributed to cutaneous toxicity caused by lapatinib. Ai, L; He, Q; Jiang, L; Luo, P; Xu, Z; Yan, H; Yang, B; Yang, X; Zeng, Y, 2022)	0.95
" Adverse events occurred in 92."	( Efficacy and safety of pyrotinib-containing regimen in the patients with HER2-positive metastatic breast cancer: A multicenter real-world study. Chi, Y; Du, Y; Li, H; Man, X; Shan, C; Shang, M; Tan, Q; Wang, J; Yi, W; Yin, S, 2023)	0.91

Excerpt	Reference	Relevance
" Pharmacokinetic samples were obtained on days 1 and 20."	( Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. Blackwell, KL; Burris, HA; Dees, EC; Dowlati, A; Ellis, MJ; Harris, JL; Hurwitz, HI; Jones, SF; Koch, KM; Mangum, S; Marcom, PK; O'Neil, B; Overmoyer, B; Smith, DA; Spector, NL; Stead, A, 2005)	0.57
" Part 1 was designed to determine the OTR and part 2 was the pharmacokinetic part of the study."	( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors. Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007)	0.58
" Additional patients were treated at the OTR dose level to further evaluate safety and for pharmacokinetic analyses."	( Phase I and pharmacokinetic study of lapatinib in combination with capecitabine in patients with advanced solid malignancies. Arya, N; Chu, QS; Curtright, J; de Bono, J; Fleming, RA; Ho, PT; Koch, KM; Pandite, L; Rowinsky, EK; Schwartz, G; Smith, DA; Versola, MJ, 2007)	0.61
"Lapatinib and capecitabine administered on a 3-week schedule were well tolerated, and no pharmacokinetic interaction was observed."	( Phase I and pharmacokinetic study of lapatinib in combination with capecitabine in patients with advanced solid malignancies. Arya, N; Chu, QS; Curtright, J; de Bono, J; Fleming, RA; Ho, PT; Koch, KM; Pandite, L; Rowinsky, EK; Schwartz, G; Smith, DA; Versola, MJ, 2007)	2.06
" Co-administration of lapatinib increased the area under the plasma concentration-time curve of SN-38, the active metabolite of irinotecan, by an average of 41%; no other pharmacokinetic interactions were observed."	( A phase I and pharmacokinetic study of lapatinib in combination with infusional 5-fluorouracil, leucovorin and irinotecan. Flaherty, KT; Fleming, RA; Kerr, DJ; Koch, KM; Middleton, MR; Midgley, RS; O'Dwyer, PJ; Pratap, SE; Smith, DA; Stevenson, JP; Versola, M; Ward, C, 2007)	0.92
" No pharmacokinetic interaction was observed."	( Phase I and pharmacokinetic study of lapatinib and docetaxel in patients with advanced cancer. Arya, N; Burris, HA; Fleming, RA; Gadgeel, S; Jones, SF; Koch, KM; Loftiss, J; LoRusso, PM; Pandite, L; Weber, BL, 2008)	0.62
" Additional patients were enrolled at the OTR dose level to further evaluate safety and for pharmacokinetic analyses."	( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer. Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008)	0.62
"Thirty-nine patients were enrolled in the study: 12 in the dose-escalation group, 7 in the OTR safety group, and 20 in the pharmacokinetic group."	( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer. Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008)	0.62
"Clinically relevant doses of lapatinib in combination with letrozole were well tolerated and did not result in a pharmacokinetic interaction, and clinical antitumor activity was observed."	( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer. Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008)	0.91
" The pharmacokinetic profile of lapatinib in Japanese patients was comparable to that of western subjects."	( Phase I dose-escalation and pharmacokinetic trial of lapatinib (GW572016), a selective oral dual inhibitor of ErbB-1 and -2 tyrosine kinases, in Japanese patients with solid tumors. Fukuoka, M; Kanezaki, M; Kawada, K; Kurata, T; Minami, H; Minamide, Y; Mukai, H; Mukaiyama, A; Nakagawa, K; Nogami, T; Sasaki, Y; Uejima, H, 2009)	0.89
" Post marketing study commitments have been made upon (accelerated) approval such as additional pharmacokinetic studies in patients with renal- or hepatic impairment, in children, additional interactions studies and studies on the relative or absolute bioavailability."	( Clinical pharmacokinetics of tyrosine kinase inhibitors. Gelderblom, H; Guchelaar, HJ; van Erp, NP, 2009)	0.35
" Clinical assessments of safety and antitumor activity were recorded and blood was sampled for pharmacokinetic assessments."	( A phase I and pharmacokinetic study of oral lapatinib administered once or twice daily in patients with solid malignancies. Arya, N; Burris, HA; Fleming, RA; Jones, SF; Koch, KM; Pandite, L; Smith, DA; Spector, N; Taylor, CW; Versola, MJ; Wilding, G, 2009)	0.61
" For pharmacokinetic analysis, 7 time point samples were collected on D1 of cycle 1 for lapatinib and vinorelbine assays."	( Pharmacokinetic evaluation of the vinorelbine-lapatinib combination in the treatment of breast cancer patients. Berille, J; Bonneterre, J; Brain, E; Dieras, V; Isambert, N; Lokiec, F; Rezai, K; Roche, H; Urien, S, 2011)	0.85
" The population pharmacokinetic parameters were CL = 27."	( Pharmacokinetic evaluation of the vinorelbine-lapatinib combination in the treatment of breast cancer patients. Berille, J; Bonneterre, J; Brain, E; Dieras, V; Isambert, N; Lokiec, F; Rezai, K; Roche, H; Urien, S, 2011)	0.63
"The pharmacokinetic modeling of vinorelbine and lapatinib was consistent with the results previously reported."	( Pharmacokinetic evaluation of the vinorelbine-lapatinib combination in the treatment of breast cancer patients. Berille, J; Bonneterre, J; Brain, E; Dieras, V; Isambert, N; Lokiec, F; Rezai, K; Roche, H; Urien, S, 2011)	0.88
" During the escalation phase, pazopanib and lapatinib doses were escalated in serial patient cohorts, and a limited blood sampling scheme was applied for pharmacokinetic evaluation."	( Phase I and pharmacokinetic study of pazopanib and lapatinib combination therapy in patients with advanced solid tumors. Arumugham, T; de Jonge, MJ; Hamberg, P; Hodge, J; Hurwitz, HI; Pandite, LN; Savage, S; Suttle, AB; Verweij, J, 2013)	0.9
" Using this data, we subsequently developed a physiologically based pharmacokinetic (PBPK) model of lapatinib in mice that accurately predicted the tissue concentrations after doses of 30, 60 and 90 mg/kg."	( Physiologically based pharmacokinetic model of lapatinib developed in mice and scaled to humans. Gustafson, DL; Hudachek, SF, 2013)	0.86
"In total, 25 patients were included, of whom 12 were evaluable for the pharmacokinetic analysis."	( Effects of low-fat and high-fat meals on steady-state pharmacokinetics of lapatinib in patients with advanced solid tumours. Arya, N; Botbyl, J; Cartee, L; Chu, QS; Devriese, LA; Koch, KM; Ma, WW; Matthys, GM; Mergui-Roelvink, M; Orford, KW; Robidoux, A; Schellens, JH; Stephenson, JJ, 2014)	0.63
" This study examined whether oral administration of MS-275 to the rats with lapatinib led to any pharmacokinetic interactions."	( Pharmacokinetic interaction of entinostat and lapatinib following single and co-oral administration in rats. Chen, M; Hu, L; Yang, X; Zhang, Q, 2014)	0.89
"This phase I study assessed the pharmacokinetic (PK), tolerability, safety and preliminary clinical activity of tamoxifen (T) and lapatinib (L) in patients with metastatic breast cancer (MBC)."	( A phase I pharmacokinetics study of lapatinib and tamoxifen in metastatic breast cancer (EORTC 10053 Lapatam study). Awada, A; Bogaerts, J; Brain, E; Cardoso, F; Fumoleau, P; Hayward, L; Koch, KM; Lokiec, F; Marréaud, S; Rezai, K; Werutsky, G, 2014)	0.88
" This study examines pharmacokinetic interactions in simultaneous oral administration of SAHA and lapatinib to rats."	( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats. Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015)	0.9
"Statistically significant pharmacokinetic differences appeared for lapatinib levels between the lapatinib and the coadministration group."	( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats. Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015)	0.91
"The resulting data indicate that, when administered together, lapatinib does not influence the pharmacokinetic profile of SAHA in rats, while, in contrast, SAHA influences the pharmacokinetic profile of lapatinib."	( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats. Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015)	0.92
" The systemic exposure to maximum plasma concentration and area under the plasma concentration curve (AUC) for lapatinib, as well as the AUC of paclitaxel, were increased when combined."	( Safety, pharmacokinetics and efficacy findings in an open-label, single-arm study of weekly paclitaxel plus lapatinib as first-line therapy for Japanese women with HER2-positive metastatic breast cancer. Aogi, K; Armour, A; Inoue, K; Iwata, H; Kuroi, K; Masuda, N; Nakayama, T; Nishimura, Y; Rai, Y; Sasaki, Y; Shimizu, S, 2015)	0.84
" Since green tea polyphenols (GTP) are known to be inhibitors of receptor tyrosine kinases, GTE could likely potentiate the anticancer effect of TKIs, but with a possibility of pharmacokinetic (PK) interaction with co-administered TKIs."	( UPLC-ESI-MS/MS study of the effect of green tea extract on the oral bioavailability of erlotinib and lapatinib in rats: Potential risk of pharmacokinetic interaction. Abahussain, AO; Alzoman, NZ; Maher, HM; Shehata, SM, 2017)	0.67
"Diabetes mellitus (DM) is a complex metabolic disorder which affects the function of numerous tissues and alters the pharmacokinetic parameters of many drugs."	( A pharmacokinetic study on lapatinib in type 2 diabetic rats. Grabowski, T; Grześkowiak, E; Karbownik, A; Klupczynska, A; Kokot, ZJ; Moch, M; Plewa, S; Sobańska, K; Szałek, E; Wolc, A, 2018)	0.78
" The most potent derivatives were further studied for their cellular uptake levels and in vivo pharmacokinetic properties."	( Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy. Dimitrakis, S; Doukatas, A; Gavriil, ES; Karampelas, T; Marakos, P; Mikros, E; Myrianthopoulos, V; Pouli, N; Tamvakopoulos, C, 2019)	0.51
"5 h, with a mean elimination half-life between 13."	( First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects. Cao, Y; Gong, LY; Guo, CX; Hua, Y; Huang, J; Kuang, Y; Pei, Q; Wang, MN; Yang, GP, 2020)	0.56
"This study evaluated the central nervous system (CNS) pharmacokinetics and target engagement of lapatinib, neratinib, and tucatinib in patients with cancer, using a physiologically based pharmacokinetic (PBPK) modeling approach."	( Mechanistic Modeling of Central Nervous System Pharmacokinetics and Target Engagement of HER2 Tyrosine Kinase Inhibitors to Inform Treatment of Breast Cancer Brain Metastases. Alley, SC; Bao, X; Jiang, J; Kumar, V; Lee, AJ; Li, J; Peterson, S, 2022)	0.94
" The proposed LC-MS/MS method was applied to pharmacokinetic studies of lapatinib, with or without TPF-T, in rabbit and rat plasma."	( Dose-sparing effect of lapatinib co-administered with a high-fat enteral nutrition emulsion: preclinical pharmacokinetic study. Ding, H; Fang, L; Kong, S; Song, Y; Tong, Y; Xu, G; Yang, D; Zhu, J, 2023)	1.45

Excerpt	Reference	Relevance
"This phase I study was designed to determine the optimally tolerated regimen (OTR), safety, and clinical activity of lapatinib in combination with FOLFOX4 [oxaliplatin/leucovorin/5-fluorouracil (5-FU)] in patients with solid tumors."	( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors. Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007)	0.79
" No dose-limiting toxicities were observed and the OTR was established at 1,500 mg/d lapatinib in combination with the standard FOLFOX4 regimen."	( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors. Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007)	0.8
"Lapatinib can be safely administered in combination with the standard FOLFOX4 regimen."	( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors. Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007)	2.02
"This study determined the optimally tolerated regimen (OTR) of oral lapatinib administered in combination with infusional 5-fluorouracil (5-FU), leucovorin and irinotecan (FOLFIRI) and assessed the safety, tolerability and pharmacokinetics of the combination."	( A phase I and pharmacokinetic study of lapatinib in combination with infusional 5-fluorouracil, leucovorin and irinotecan. Flaherty, KT; Fleming, RA; Kerr, DJ; Koch, KM; Middleton, MR; Midgley, RS; O'Dwyer, PJ; Pratap, SE; Smith, DA; Stevenson, JP; Versola, M; Ward, C, 2007)	0.84
"Lapatinib [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, GW572016, Tykerb] is a tyrosine kinase inhibitor approved for use in combination with capecitabine to treat advanced or metastatic breast cancers overexpressing HER2 (ErbB2)."	( The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Castellino, S; Harmon, KA; Humphreys, JE; John-Williams, LS; Koch, KM; O'Mara, MJ; Olson, KL; Polli, JW; Serabjit-Singh, CJ, 2008)	1.98
"Cohorts of three patients with ErbB2-positive advanced breast cancer were treated with escalating doses of lapatinib (750 to 1,500 mg) administered once daily (continuous) in combination with trastuzumab (4 mg/kg loading dose then 2 mg/kg weekly) to determine the OTR."	( Phase I dose escalation and pharmacokinetic study of lapatinib in combination with trastuzumab in patients with advanced ErbB2-positive breast cancer. Arya, N; Burris, HA; Fleming, RA; Ho, PT; Jones, SF; Koch, KM; Lebowitz, PF; Loftiss, J; Overmoyer, B; Pandite, L; Paul, E; Peacock, NW; Pegram, MD; Silverman, P; Storniolo, AM, 2008)	0.81
" In conclusion, honokiol, either alone or in combination with other therapeutics, could serve as a new, promising approach for breast cancer treatment."	( Anti-tumor effect of honokiol alone and in combination with other anti-cancer agents in breast cancer. Elstner, E; Emde, A; Eucker, J; Kühnl, A; Liu, H; Planas-Silva, MD; Possinger, K; Rosche, M; Schulz, CO; Zang, C, 2008)	0.35
"The main objectives of this phase I and pharmacokinetic, open-label study were to determine the optimally tolerated regimen (OTR), safety, pharmacokinetics, and clinical activity of lapatinib in combination with letrozole in patients with advanced solid malignancies."	( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer. Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008)	0.81
"Clinically relevant doses of lapatinib in combination with letrozole were well tolerated and did not result in a pharmacokinetic interaction, and clinical antitumor activity was observed."	( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer. Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008)	0.91
"To determine the maximum tolerated dose (MTD), spectrum of toxicities, clinical activity, and pharmacokinetics of carboplatin given in combination with lapatinib in women with a first recurrence of platinum sensitive epithelial ovarian carcinoma."	( A phase I study of lapatinib in combination with carboplatin in women with platinum sensitive recurrent ovarian carcinoma. Alvarez, RD; Barnes, MN; Estes, JM; Kimball, KJ; Kirby, TO; Koch, KM; Matei, DE; Numnum, TM; Zamboni, WC, 2008)	0.87
" Cohorts of 3-6 patients were to receive up to 6 cycles of intravenous carboplatin AUC of 6 every 21 days in combination with escalating dosages of oral lapatinib (starting at a dose of 750 mg daily)."	( A phase I study of lapatinib in combination with carboplatin in women with platinum sensitive recurrent ovarian carcinoma. Alvarez, RD; Barnes, MN; Estes, JM; Kimball, KJ; Kirby, TO; Koch, KM; Matei, DE; Numnum, TM; Zamboni, WC, 2008)	0.87
" Food and Drug Administration approved lapatinib (Tykerb tablets; GlaxoSmithKline, Philadelphia), an oral, small molecule, dual tyrosine kinase inhibitor of ErbB-2 and ErbB-1, for use in combination with capecitabine for the treatment of patients with human epidermal growth factor receptor (HER)-2-overexpressing metastatic breast cancer who had received prior therapy including an anthracycline, a taxane, and trastuzumab."	( FDA drug approval summary: lapatinib in combination with capecitabine for previously treated metastatic breast cancer that overexpresses HER-2. Cohen, MH; Ibrahim, A; Johnson, J; Justice, R; Ko, CW; Pazdur, R; Ryan, Q; Sridhara, R, 2008)	0.91
" The tolerability and efficacy of IPI-504 combined with either trastuzumab or lapatinib were also investigated in HER2(+) tumor xenograft models."	( Antitumor efficacy of IPI-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib. Chang, Y; Chesebrough, J; Coats, S; Coffman, KT; Fazenbaker, CA; Gooya, J; Jackson, D; Jallal, B; Leow, CC; Weng, D, 2009)	0.77
" EGF104900 compared the activity of lapatinib alone or in combination with trastuzumab in patients with ErbB2-positive, trastuzumab-refractory metastatic breast cancer (MBC)."	( Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer. Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Casey, M; Ellis, C; Koehler, M; O'Shaughnessy, J; Rugo, H; Sledge, G; Storniolo, AM; Vukelja, S, 2010)	0.96
"Patients with ErbB2-positive MBC who experienced progression on prior trastuzumab-containing regimens were randomly assigned to receive either lapatinib alone or in combination with trastuzumab."	( Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer. Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Casey, M; Ellis, C; Koehler, M; O'Shaughnessy, J; Rugo, H; Sledge, G; Storniolo, AM; Vukelja, S, 2010)	0.89
"Despite disease progression on prior trastuzumab-based therapy, lapatinib in combination with trastuzumab significantly improved PFS and CBR versus lapatinib alone, thus offering a chemotherapy-free option with an acceptable safety profile to patients with ErbB2-positive MBC."	( Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer. Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Casey, M; Ellis, C; Koehler, M; O'Shaughnessy, J; Rugo, H; Sledge, G; Storniolo, AM; Vukelja, S, 2010)	0.92
" These results suggest that: i) lapatinib has antitumor effects in vitro and in vivo; ii) lapatinib may be more effective in combination with cisplatin or paclitaxel; and iii) lapatinib might provide useful clinical benefits to HNSCC patients."	( Antitumor effects of lapatinib (GW572016), a dual inhibitor of EGFR and HER-2, in combination with cisplatin or paclitaxel on head and neck squamous cell carcinoma. Fujita, K; Ishiguro, Y; Kimura, M; Kondo, N; Matsuda, H; Sakakibara, A; Takahashi, H; Toth, G; Tsukuda, M, 2010)	0.96
"Our data suggest that lapatinib combined with fractionated radiotherapy may be useful against EGFR+ and HER2+ breast cancers and that inhibition of downstream signaling to ERK1/2 and AKT correlates with sensitization in EGFR+ and HER2+ cells, respectively."	( Lapatinib in combination with radiation diminishes tumor regrowth in HER2+ and basal-like/EGFR+ breast tumor xenografts. Camp, JT; Kimple, RJ; Livasy, CA; Peters, E; Sambade, MJ; Sartor, CI; Shields, JM, 2010)	2.12
"Lapatinib, an orally active tyrosine kinase inhibitor of epidermal growth factor receptor ErbB1 (EGFR) and ErbB2 (HER2), has activity as monotherapy and in combination with chemotherapy in HER2-overexpressing metastatic breast cancer (MBC)."	( A single-arm phase II trial of first-line paclitaxel in combination with lapatinib in HER2-overexpressing metastatic breast cancer. Abbey, R; DeSilvio, M; Dobrovolskaya, N; Jagiello-Gruszfeld, A; Manikhas, A; Pienkowski, T; Ridderheim, M; Tjulandin, S, 2010)	2.03
"This phase II single-arm trial assessed the safety and efficacy of first-line lapatinib in combination with paclitaxel in previously untreated patients with HER2-overexpressing MBC."	( A single-arm phase II trial of first-line paclitaxel in combination with lapatinib in HER2-overexpressing metastatic breast cancer. Abbey, R; DeSilvio, M; Dobrovolskaya, N; Jagiello-Gruszfeld, A; Manikhas, A; Pienkowski, T; Ridderheim, M; Tjulandin, S, 2010)	0.82
"Chemotherapy in combination with small-molecule epidermal growth factor receptor inhibitors has yielded inconsistent results."	( Phase I study of continuous and intermittent schedules of lapatinib in combination with vinorelbine in solid tumors. Chew, HK; Christensen, S; Davies, AM; Gandour-Edwards, R; Gitlitz, B; Linden, H; Mack, PC; Solis, LJ; Somlo, G; Yang, X, 2012)	0.62
" Optimal effects are obtained when these compounds are used in combination with chemotherapy, as shown in preclinical models and more recently in clinical trials."	( Docetaxel combined with targeted therapies in metastatic breast cancer. Cortes, J; Roché, H, 2012)	0.38
" The conventional schedule of capecitabine limits full dosing in combination with other agents due to toxicity."	( Phase II trial of a novel capecitabine dosing schedule in combination with lapatinib for the treatment of patients with HER2-positive metastatic breast cancer. Chen, C; D'Andrea, G; Drullinsky, P; Feigin, K; Gajria, D; Gonzalez, J; Hudis, CA; Lake, D; Norton, L; Patil, S; Theodoulou, M; Traina, TA, 2012)	0.61
"To review the clinical effectiveness and cost-effectiveness evidence base for lapatinib (LAP) in combination with an aromatase inhibitor (AI) and trastuzumab (TRA) in combination with an AI for the first-line treatment of patients who have hormone receptor-positive (HR+)/human epidermal growth factor 2-positive (HER2+) mBC."	( Lapatinib and trastuzumab in combination with an aromatase inhibitor for the first-line treatment of metastatic hormone receptor-positive breast cancer which over-expresses human epidermal growth factor 2 (HER2): a systematic review and economic analysis. Armstrong, A; Bagust, A; Blundell, M; Boland, A; Davis, H; Dickson, R; Dundar, Y; Fleeman, N; Moonan, M; Oyee, J; Thorp, N, 2011)	2.04
"Three trials were included in the systematic review [the patient populations of the efficacy and safety of lapatinib combined with letrozole (EGF30008) trial, the efficacy and safety of trastuzumab combined with anastrozole (TAnDEM) trial and the efficacy and safety of letrozole combined with trastuzumab (eLEcTRA) trial]."	( Lapatinib and trastuzumab in combination with an aromatase inhibitor for the first-line treatment of metastatic hormone receptor-positive breast cancer which over-expresses human epidermal growth factor 2 (HER2): a systematic review and economic analysis. Armstrong, A; Bagust, A; Blundell, M; Boland, A; Davis, H; Dickson, R; Dundar, Y; Fleeman, N; Moonan, M; Oyee, J; Thorp, N, 2011)	2.03
" Unless long-term outcome data show different results, lapatinib should not be used outside of clinical trials as single anti-HER2-treatment in combination with neoadjuvant chemotherapy."	( Lapatinib versus trastuzumab in combination with neoadjuvant anthracycline-taxane-based chemotherapy (GeparQuinto, GBG 44): a randomised phase 3 trial. Bischoff, J; Blohmer, JU; Eidtmann, H; Fasching, PA; Gerber, B; Hanusch, C; Hilfrich, J; Huober, J; Jackisch, C; Kaufmann, M; Kreienberg, R; Kühn, T; Loibl, S; Nekljudova, V; Rezai, M; Strumberg, D; Tesch, H; Untch, M; von Minckwitz, G, 2012)	2.07
"Patients with HER2-positive MBC whose disease progressed during prior trastuzumab-based therapies were randomly assigned to receive lapatinib monotherapy or lapatinib in combination with trastuzumab."	( Overall survival benefit with lapatinib in combination with trastuzumab for patients with human epidermal growth factor receptor 2-positive metastatic breast cancer: final results from the EGF104900 Study. Aktan, G; Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Ellis, C; Florance, A; O'Shaughnessy, J; Rugo, HS; Sledge, G; Storniolo, AM; Vukelja, S, 2012)	0.87
" We evaluated the antitumor effect of a c-Src/Abl kinase inhibitor, saracatinib (AZD0530), alone or combined with chemotherapeutic agents in gastric cancer cell lines and a NCI-N87 xenograft model."	( Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer. Bang, YJ; Elvin, P; Han, SW; Im, SA; Kim, HP; Kim, TY; Min, A; Nam, HJ; Oh, DY; Song, SH; Yoon, YK, 2013)	0.39
" Lapatinib combined with CRT was well-tolerated."	( Randomised Phase II study of oral lapatinib combined with chemoradiotherapy in patients with advanced squamous cell carcinoma of the head and neck: rationale for future randomised trials in human papilloma virus-negative disease. Berrier, A; Biswas-Baldwin, N; Compton, N; de Mendoza, FH; El-Hariry, I; Fayette, J; Franklin, N; Harrington, K; Housset, M; Kumar, R; Lau, M; Legenne, P; Mehanna, H; Remenar, E; Robinson, M, 2013)	1.58
"Lapatinib combined with CRT is well-tolerated with numeric increases in CRR at 6 months post-CRT and median PFS in p16-negative disease."	( Randomised Phase II study of oral lapatinib combined with chemoradiotherapy in patients with advanced squamous cell carcinoma of the head and neck: rationale for future randomised trials in human papilloma virus-negative disease. Berrier, A; Biswas-Baldwin, N; Compton, N; de Mendoza, FH; El-Hariry, I; Fayette, J; Franklin, N; Harrington, K; Housset, M; Kumar, R; Lau, M; Legenne, P; Mehanna, H; Remenar, E; Robinson, M, 2013)	2.11
"The results from a phase III trial conducted outside of Japan demonstrated a significant improvement in time to progression (TTP) when lapatinib was combined with capecitabine compared with capecitabine alone in patients with HER2-positive advanced or metastatic breast cancer."	( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study. Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015)	0.82
"Lapatinib in combination with capecitabine was well tolerated in the 51 patients enrolled in this study."	( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study. Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015)	2.06
"Lapatinib in combination with capecitabine in Japanese HER2-positive breast cancer patients was well tolerated."	( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study. Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015)	2.06
"This phase IB, open-label, dose-escalation study evaluated the safety, tolerability, and optimally tolerated regimen (OTR) of lapatinib in combination with docetaxel and trastuzumab in patients with previously untreated stage IV metastatic breast cancer (MBC) tumors overexpressing human epidermal growth factor receptor 2 (HER2)."	( Optimally tolerated dose of lapatinib in combination with docetaxel plus trastuzumab in first-line treatment of HER2-positive metastatic breast cancer. Burris, HA; Crown, J; DeSilvio, M; Diéras, V; Espie, M; Kennedy, MJ; Koch, KM; Kothari, D; Lau, MR; Marty, M; Tresca, P, 2013)	0.89
"The aim of this explorative phase II study was to evaluate the activity and safety of lapatinib in combination with intravenous vinorelbine in women with HER2 positive metastatic or recurrent breast cancer."	( Phase II study of lapatinib in combination with vinorelbine in patients with HER2 positive recurrent or metastatic breast cancer: a multicentric Turkish Oncology Group (TOG) trial. Basaran, G; Benekli, M; Cetin, B; Eralp, Y; Isikdogan, A; Karaca, H; Kucukoner, M; Onur, H; Ozkan, M; Saip, P; Sen, F; Un, O, 2013)	0.95
" In a PIK3CA-mutant HER2+ xenograft, PI3K inhibition with BKM120 in combination with lapatinib and trastuzumab was required to achieve tumor regression."	( Direct inhibition of PI3K in combination with dual HER2 inhibitors is required for optimal antitumor activity in HER2+ breast cancer cells. Arteaga, CL; Chanthaphaychith, S; Dahlman, K; Rexer, BN, 2014)	0.63
"A phase 1 study of pazopanib alone or in combination with lapatinib was conducted to assess the safety, tolerability, and pharmacokinetics of these oral tyrosine kinase inhibitors in Japanese patients with solid tumors."	( Phase 1 study of pazopanib alone or combined with lapatinib in Japanese patients with solid tumors. Ando, Y; Araki, K; Inada-Inoue, M; Ishida, H; Kawada, K; Mitsuma, A; Mizuno, K; Nagamatsu, K; Nagashima, F; Sasaki, Y; Sawaki, M; Sunakawa, Y; Takekura, A; Yamashita, K; Yokoyama, T, 2014)	0.9
"We assessed the maximum tolerated regimen (MTR) and dose-limiting toxicities of pazopanib and lapatinib in combination with weekly paclitaxel, and the effect of pazopanib and lapatinib on paclitaxel pharmacokinetics."	( Phase I study of weekly paclitaxel in combination with pazopanib and lapatinib in advanced solid malignancies. Bendell, J; Burris, HA; Dowlati, A; Infante, JR; Jones, SF; Kane, MP; Levinson, KT; Stein, MN; Suttle, AB; Tan, AR, 2014)	0.86
"Pazopanib 400 mg per day and lapatinib 1000 mg per day can be combined with paclitaxel 80 mg m(-2) in 28-day cycles."	( Phase I study of weekly paclitaxel in combination with pazopanib and lapatinib in advanced solid malignancies. Bendell, J; Burris, HA; Dowlati, A; Infante, JR; Jones, SF; Kane, MP; Levinson, KT; Stein, MN; Suttle, AB; Tan, AR, 2014)	0.93
"Neratinib in combination with capecitabine had a manageable toxicity profile and showed promising antitumor activity in patients with HER2-positive metastatic breast cancer pretreated with trastuzumab and lapatinib."	( Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer. Baselga, J; Cortés, J; Garcia-Saenz, JA; Germa, C; Harb, W; Kiger, C; Kim, SB; Martin, M; Moroose, R; Pluard, T; Saura, C; Wang, K; Xu, B, 2014)	0.59
" FW-04-806, a novel Hsp90 N-terminal inhibitor that disassociates the Hsp90/Cdc37/client complex and degrades Hsp90 clients, was studied alone or in combination with the EGFR/HER2 tyrosine kinase inhibitor lapatinib in HER2+ breast cancer cells."	( Novel Hsp90 inhibitor FW-04-806 displays potent antitumor effects in HER2-positive breast cancer cells as a single agent or in combination with lapatinib. Cao, PR; Huang, W; Kong, YL; Wu, QD; Xu, JH; Ye, M; Zhang, M; Zheng, W, 2015)	0.81
" We explored multiple intermittent dose levels of pazopanib combined with continuous daily dosing of lapatinib in patients with solid tumors."	( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors. Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015)	0.85
"Every other day dosing of pazopanib combined with daily lapatinib was tolerated at the established MTD, but no complete or partial tumor responses were observed at these dose levels."	( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors. Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015)	0.88
"Lapatinib has proven efficacy as monotherapy and in combination with capecitabine in patients with metastatic breast cancer (MBC) overexpressing HER2 and/or EGFR."	( Phase I and pharmacological trial of lapatinib in combination with gemcitabine in patients with advanced breast cancer. Beijnen, JH; Boss, DS; Grob, M; Huitema, AD; Keessen, M; Rehorst, H; Rosing, H; Schellens, JH; Smit, WM; Tibben, MM; van der Noll, R; Wymenga, AN, 2015)	2.13
" The secondary target that can afford the highest potential for clinical translation is the one with the highest synergy against tumor cells in combination with HER2-inhibition, allowing the widest therapeutic index for clinical translation."	( Chemical probing of HER2-amplified cancer cells identifies TORC2 as a particularly effective secondary target for combination with lapatinib. Amin, DN; Gulizia, N; Moasser, MM; Ruiz-Saenz, A, 2015)	0.62
" In this context, alternatives to the lapatinib (L) and capecitabine (C) regimen, evaluating L combined with other cytotoxic drugs, are warranted."	( A Phase II Randomized Study of Lapatinib Combined With Capecitabine, Vinorelbine, or Gemcitabine in Patients With HER2-Positive Metastatic Breast Cancer With Progression After a Taxane (Latin American Cooperative Oncology Group 0801 Study). Barrios, CH; Bines, J; Blajman, C; Capó, A; Fanelli, M; Fein, L; Gómez, HL; Ismael, G; Lerzo, G; Mano, M; Martínez-Mesa, J; Neciosup, S; Nerón, Y; Pinczowski, H; Sampaio, C; Santi, PX; Tosello, C; Varela, MS; Werutsky, G; Zarba, JJ, 2016)	0.99
"In the present phase II, multicenter study, patients with HER2(+) MBC with progression after taxane were randomized between L, 1250 mg, combined with C, 2000 mg/m(2) on days 1 to 14 (LC), vinorelbine (V), 25 mg/m(2) on days 1 and 8 (LV), or gemcitabine (G), 1000 mg/m(2) on days 1 and 8 (LG), every 21 days."	( A Phase II Randomized Study of Lapatinib Combined With Capecitabine, Vinorelbine, or Gemcitabine in Patients With HER2-Positive Metastatic Breast Cancer With Progression After a Taxane (Latin American Cooperative Oncology Group 0801 Study). Barrios, CH; Bines, J; Blajman, C; Capó, A; Fanelli, M; Fein, L; Gómez, HL; Ismael, G; Lerzo, G; Mano, M; Martínez-Mesa, J; Neciosup, S; Nerón, Y; Pinczowski, H; Sampaio, C; Santi, PX; Tosello, C; Varela, MS; Werutsky, G; Zarba, JJ, 2016)	0.72
" The aims of this study are to investigate the inhibitory effects of TKIs on UDP-glucuronosyltransferase (UGT) activities, and to quantitatively evaluate their potential to cause drug-drug interactions (DDIs)."	( Drug-Drug Interaction Potentials of Tyrosine Kinase Inhibitors via Inhibition of UDP-Glucuronosyltransferases. Jeong, H; Liu, Y; Zhang, N, 2015)	0.42
" The present study was set out to evaluate the efficacy and safety of vinorelbine when combined with lapatinib, an anti-HER2 tyrosine-kinase inhibitor, as late-line regimen administered beyond previous disease progression on prior lapatinib in patients with HER-2/neu- positive MBC."	( Phase II study on the efficacy and safety of Lapatinib administered beyond disease progression and combined with vinorelbine in HER-2/neu- positive advanced breast cancer: results of the CECOG LaVie trial. Bartsch, R; Brodowicz, T; Knittelfelder, R; Kuhar, CG; Lang, I; Melichar, B; Petruzelka, L; Singer, CF; Thallinger, C; Zielinski, C, 2016)	0.91
"MK-2206 combined with lapatinib can be tolerated with both drugs above biologically active single-agent doses."	( Phase I Study of an AKT Inhibitor (MK-2206) Combined with Lapatinib in Adult Solid Tumors Followed by Dose Expansion in Advanced HER2+ Breast Cancer. Bell, MC; Burkard, ME; Eickhoff, J; Flynn, C; Kolesar, JM; Liu, G; Rampurwala, M; Tevaarwerk, AJ; Wisinski, KB, 2016)	0.99
" Thirteen different TKIs were combined with or without SZU-101 and studied to determine their effects on immunocytes."	( Immunomodulatory and Antitumor Effects of a Novel TLR7 Agonist Combined with Lapatinib. Diao, Y; Gao, N; Jiang, W; Jin, G; Jin, Z; Li, W; Liu, Y; Wang, X; Wang, Z; Zhong, J, 2016)	0.66
"HLA-DRB1*07:01 allele carriage was characterised as a risk biomarker for lapatinib-induced liver injury in a large global study evaluating lapatinib, alone and in combination with trastuzumab and taxanes, as adjuvant therapy for advanced breast cancer (adjuvant lapatinib and/or trastuzumab treatment optimisation)."	( Characterisation of the HLA-DRB1*07:01 biomarker for lapatinib-induced liver toxicity during treatment of early-stage breast cancer patients with lapatinib in combination with trastuzumab and/or taxanes. Ahmed, S; Andersson, M; Armour, A; Aziz, Z; Briley, LP; Byrne, J; Crescenzo, R; Demetriou, G; Fraser, DJ; Gralow, J; Harris, L; Jackson, N; Jiang, Z; Mehta, A; Parham, LR; Perez, E; Piccart, M; Spraggs, CF; Toi, M; Warren, L; Williams, LS; Zujewski, JA, 2018)	0.96
"PIKHER2 phase IB study aimed primarily to determine a maximum tolerated dose (MTD) and propose a recommended phase II dose (RP2D) for buparlisib in combination with lapatinib in HER2-positive, trastuzumab-resistant, advanced breast cancer."	( PIKHER2: A phase IB study evaluating buparlisib in combination with lapatinib in trastuzumab-resistant HER2-positive advanced breast cancer. Autret, A; Bertucci, F; Boher, JM; Camerlo, J; Campone, M; Charafe-Jauffret, E; Extra, JM; Gonçalves, A; Guerin, M; Hervieu, A; Isambert, N; Lokiec, F; Pakradouni, J; Provansal, M; Rezai, K; Sabatier, R; Viens, P, 2017)	0.89
" There was no significant evidence for drug-drug PK interaction."	( PIKHER2: A phase IB study evaluating buparlisib in combination with lapatinib in trastuzumab-resistant HER2-positive advanced breast cancer. Autret, A; Bertucci, F; Boher, JM; Camerlo, J; Campone, M; Charafe-Jauffret, E; Extra, JM; Gonçalves, A; Guerin, M; Hervieu, A; Isambert, N; Lokiec, F; Pakradouni, J; Provansal, M; Rezai, K; Sabatier, R; Viens, P, 2017)	0.69
" The present study was to evaluate the antitumor effects of lapatinib, a dual tyrosine inhibitor of both epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), combined with paclitaxel on the esophageal squamous cancer."	( Lapatinib in combination with paclitaxel plays synergistic antitumor effects on esophageal squamous cancer. Dou, QH; Guo, XF; Li, SS; Liu, D; Zhu, XF, 2018)	2.17
" We assessed the efficacy and tolerability of pyrotinib versus lapatinib, both in combination with capecitabine, in women with human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer in an open-label, multicenter, randomized phase II study."	( Pyrotinib or Lapatinib Combined With Capecitabine in HER2-Positive Metastatic Breast Cancer With Prior Taxanes, Anthracyclines, and/or Trastuzumab: A Randomized, Phase II Study. Feng, J; Hu, X; Jiang, Z; Li, H; Li, W; Liu, Y; Ma, F; Ouyang, Q; Tong, Z; Wang, S; Xu, B; Yu, S; Zhu, X; Zou, J, 2019)	1.12
" To evaluate whether miRNAs can sensitize HER2 + cells to treatment, we performed a high-throughput screen of 1626 miRNA mimics and inhibitors in combination with trastuzumab and lapatinib in HER2 + breast cancer cells."	( MicroRNA in combination with HER2-targeting drugs reduces breast cancer cell viability in vitro. Aure, MR; Haugen, MH; Hongisto, V; Kristensen, VN; Leivonen, SK; Mælandsmo, GM; Normann, LS; Sahlberg, KK, 2021)	0.81
" Moreover, when it used in combination with liposomal doxorubicin, it extended the time to end from 22."	( Development of a stable and high loaded liposomal formulation of lapatinib with enhanced therapeutic effects for breast cancer in combination with Caelyx®: In vitro and in vivo evaluations. Badiee, A; Jafari, MR; Karimi, M; Mansouri, A; Mehrabian, A; Nikpoor, AR; Sadri, K; Shokooh Saremi, S, 2021)	0.86
" Collectively, these results indicated that the lysosome‑targeted drug combination induces multiple organelle dysfunction and exerts a marked cytotoxic effect in PDAC cells."	( Lysosome‑targeted drug combination induces multiple organelle dysfunctions and non‑canonical death in pancreatic cancer cells. Hiramoto, M; Hirota, A; Kazama, H; Miyazaki, M; Miyazawa, K; Ogawa, M; Ota, K; Suzuki, S; Takano, N, 2022)	0.72

Excerpt	Reference	Relevance
"This study was conducted to characterize the effect of food on the relative bioavailability of lapatinib."	( Effects of food on the relative bioavailability of lapatinib in cancer patients. Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009)	0.82
" Increased bioavailability in the fed state did not significantly decrease relative variability."	( Effects of food on the relative bioavailability of lapatinib in cancer patients. Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009)	0.6
"These large increases in lapatinib bioavailability and absolute variability support the recommendation for dosing in the fasted state to achieve consistent therapeutic exposure."	( Effects of food on the relative bioavailability of lapatinib in cancer patients. Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009)	0.91
" They are characterized by a moderate rate of absorption after oral administration with peak plasma concentrations at several hours post-dose."	( Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on 4-anilinoquinazolines. Di Gion, P; Doroshyenko, O; Fuhr, U; Scheffler, M; Wolf, J, 2011)	0.37
" Our compound optimization that has led to synthesis of several potent 4-anilinoquinazolines, including NEU617, 23a, a highly potent, orally bioavailable inhibitor of trypanosome replication."	( Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis. Behera, R; Edwards, P; Guyett, PJ; Karver, CE; Mensa-Wilmot, K; Patel, G; Pollastri, MP; Roncal, NE; Sullenberger, C, 2013)	0.61
"To improve the solubility, bioavailability and anti-tumor effect of lapatinib, lapatinib-incorporated lipid nanoparticles (LTNPs) were prepared and characterized."	( In vivo behavior and safety of lapatinib-incorporated lipid nanoparticles. Cao, S; Chen, C; Chen, J; Gao, H; Jiang, X; Xi, Z; Zhang, Q, 2014)	0.92
" Unfortunately, the low oral bioavailability of lapatinib and drug efflux by blood-brain barrier have resulted in low drug delivery efficiency into the brain and limited therapeutic effects for patients with brain metastasis in clinical trials."	( Lapatinib-loaded human serum albumin nanoparticles for the prevention and treatment of triple-negative breast cancer metastasis to the brain. Jiang, T; Jiang, X; Pang, X; Pang, Z; Wan, X; Xu, W; Zhang, Q; Zhang, Z; Zhao, J; Zheng, X, 2016)	2.13
" Additionally, there was no statistical difference in tlag or tmax , suggesting no difference in the absorption rate between treatments."	( Bioequivalence study with lapatinib powder for oral suspension and the original tablet formulation in cancer patients. Arya, N; Cartee, L; Curran, D; D'Amelio, AM; Ferron-Brady, G; Hollyfield, H; Koch, KM; Lemmon, C; Piepszak, A; Swaby, RF, )	0.43
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."	( Highly predictive and interpretable models for PAMPA permeability. Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017)	0.46
"Lapatinib is an orally bioavailable dual inhibitor of the intracellular domain of both the HER2 protein and the epidermal growth factor receptor."	( [A Case of Interstitial Pneumonitis Induced by Lapatinib plus Letrozole]. Yamamoto, C; Yamamoto, D; Yamamoto, M, 2016)	2.13
" The results revealed that a significant reduction in the oral bioavailability was recorded with both ERL and LAP following the ingestion of GTE particularly for short-term administration."	( UPLC-ESI-MS/MS study of the effect of green tea extract on the oral bioavailability of erlotinib and lapatinib in rats: Potential risk of pharmacokinetic interaction. Abahussain, AO; Alzoman, NZ; Maher, HM; Shehata, SM, 2017)	0.67
" Oral area under the plasma concentration-time curve (AUC) and bioavailability of well known BCRP (sulfasalazine and rosuvastatin), P-glycoprotein (fexofenadine, aliskiren, and talinolol), and CYP3A (midazolam) substrates were investigated in the presence and absence of inhibitors."	( Curcumin as an In Vivo Selective Intestinal Breast Cancer Resistance Protein Inhibitor in Cynomolgus Monkeys. Abe, K; Ando, O; Imaoka, T; Karibe, T, 2018)	0.48
" This study provided the insight of introducing theoretical models to guide SD formulation/process development and illustrating the potential of bioavailability enhancement for LB-DT."	( Preparation of lapatinib ditosylate solid dispersions using solvent rotary evaporation and hot melt extrusion for solubility and dissolution enhancement. Hageman, MJ; Hu, XY; Lou, H, 2018)	0.83
" Nevertheless, most SMAs are currently administered orally due to their poor solubility, resulting in a low bioavailability and unavoidable side effects."	( Cysteine-based redox-responsive nanoparticles for small-molecule agent delivery. Dai, C; He, S; Hu, H; Lou, Q; Wang, L; Wu, J; You, X; Zhang, J; Zhao, M, 2019)	0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
"We assessed the pharmacokinetics and safety of a single oral administration of selatinib to healthy Chinese subjects and evaluated the potential bioavailability advantage of selatinib relative to lapatinib."	( First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects. Cao, Y; Gong, LY; Guo, CX; Hua, Y; Huang, J; Kuang, Y; Pei, Q; Wang, MN; Yang, GP, 2020)	0.75
"Stimulus-responsive nanosystem is a powerful method to improve the bioavailability and reduce the side effects of anticancer agents."	( Lapatinib-loaded acidity-triggered charge switchable polycarbonate-doxorubicin conjugate micelles for synergistic breast cancer chemotherapy. Fan, Y; Guo, Z; Hu, J; Liang, E; Ma, M; Sui, J; Sun, Y; Wang, J; Yang, L, 2020)	2
"The bioavailability of lapatinib is affected by food, even following the 1 hour fast recommended by the package insert."	( Overnight fasting before lapatinib administration to breast cancer patients leads to reduced toxicity compared with nighttime dosing: a retrospective cohort study from a randomized clinical trial. Bando, H; Homma, M; Ishiguro, H; Kuroi, K; Masuda, N; Morita, S; Ohgami, M; Shimizu, S; Takano, T; Toi, M; Toriguchi, N; Tsuda, M; Yamamoto, N; Yanagita, Y, 2020)	1.17
" Additionally, an ∼85% correlation was obtained between PAMPA pH 5 permeability and in vivo oral bioavailability in mice and rats."	( Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability. Itkin, M; Kabir, M; Mathé, EA; Nguyễn, ÐT; Padilha, EC; Shah, P; Shinn, P; Siramshetty, V; Wang, AQ; Williams, J; Xu, X; Yu, KR; Zhao, T, 2022)	0.72
" Multiple-target inhibitors of efflux transporter can be overcome the resistance and improve the oral bioavailability of chemotherapy drugs."	( Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel. Cai, Z; Ghaleb, H; Huang, W; Jiang, Y; Liu, Y; Qian, H; Qiu, Q; Shi, W; Yin, Z; Zhang, P; Zhou, J; Zou, F, 2022)	0.72
" Nevertheless, the drug is poorly absorbed post oral administration and possess low aqueous solubility."	( Glycol chitosan stabilized nanomedicine of lapatinib and doxorubicin for the management of metastatic breast tumor. Aggarwal, A; Jaganathan, M; Kaur, N; Munawara, R; Shanavas, A; Sharma, P, 2023)	1.17

Excerpt	Relevance	Reference
"This study (EGF10004) assessed the safety/tolerability, pharmacokinetics, and clinical activity of daily oral dosing with lapatinib (GW572016) in patients with ErbB1-expressing and/or ErbB2-overexpressing advanced-stage refractory solid tumors."	( Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. Blackwell, KL; Burris, HA; Dees, EC; Dowlati, A; Ellis, MJ; Harris, JL; Hurwitz, HI; Jones, SF; Koch, KM; Mangum, S; Marcom, PK; O'Neil, B; Overmoyer, B; Smith, DA; Spector, NL; Stead, A, 2005)	0.77
" Both effects depend on the dosage of the drug, which shows saturation kinetics."	( relocating job wise? A mathematical model separates quantitatively the cytostatic and cytotoxic effects of a HER2 tyrosine kinase inhibitor. Arteaga, CL; Hinow, P; Wang, SE; Webb, GF, 2007)	0.34
" In contrast, systemic exposure of lapatinib after oral dosing was unchanged when efflux by Pgp and BCRP was absent from the gastrointestinal tract."	( The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions. Castellino, S; Harmon, KA; Humphreys, JE; John-Williams, LS; Koch, KM; O'Mara, MJ; Olson, KL; Polli, JW; Serabjit-Singh, CJ, 2008)	0.82
" There were no significant differences in clinical activity or the AE profile between the dosing schedules."	( Efficacy and safety of lapatinib as first-line therapy for ErbB2-amplified locally advanced or metastatic breast cancer. Ang, PC; Arbushites, MC; Aziz, Z; Berger, MS; Casey, MA; Chavez, MA; Chow, LW; Doval, DC; Franco, SX; Gomez, HL; Nag, S; Ng, C; Sledge, GW; Stein, SH, 2008)	0.66
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug and food interactions, dosage and administration, and role in therapy of lapatinib in metastatic breast cancer are reviewed."	( Lapatinib: a dual tyrosine kinase inhibitor for metastatic breast cancer. Paul, B; Thompson, J; Trovato, JA, 2008)	1.99
" The approved dosing of lapatinib is 1,250 mg PO QD given continuously in combination with capecitabine 2,000 mg/m(2) daily administered in 2 divided doses on days 1 to 14 of a 21-day cycle."	( Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Goodin, S; Medina, PJ, 2008)	2.1
"Lapatinib was dosed at 1,500 mg/day orally continuously."	( A phase II study of lapatinib in patients with advanced biliary tree and hepatocellular cancer. Belani, CP; Dancey, J; Gandara, DR; Gandour-Edwards, R; Iqbal, S; Kindler, HL; Lenz, HJ; Longmate, J; Lurje, G; Mack, PC; Ramanathan, RK; Singh, DA; Tanaka, M; Yen, Y, 2009)	2.12
"These large increases in lapatinib bioavailability and absolute variability support the recommendation for dosing in the fasted state to achieve consistent therapeutic exposure."	( Effects of food on the relative bioavailability of lapatinib in cancer patients. Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009)	0.91
" Twice-daily dosing was implemented to further explore tolerability, and was limited by diarrhea to 500 mg twice daily."	( A phase I and pharmacokinetic study of oral lapatinib administered once or twice daily in patients with solid malignancies. Arya, N; Burris, HA; Fleming, RA; Jones, SF; Koch, KM; Pandite, L; Smith, DA; Spector, N; Taylor, CW; Versola, MJ; Wilding, G, 2009)	0.61
" Dose-response curves were generated to determine sensitivity to lapatinib, erlotinib, and trastuzumab."	( Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Anghel, A; Ayala, R; Desai, AJ; Fejzo, MS; Finn, RS; Hecht, JR; Luo, T; Safran, B; Slamon, DJ; Wainberg, ZA, 2010)	2.04
" Adverse events were similar across dosing regimens."	( Randomized phase II multicenter trial of two schedules of lapatinib as first- or second-line monotherapy in patients with advanced or metastatic non-small cell lung cancer. Aisner, J; Allen, KE; Blumenschein, GR; Damjanov, N; Dowlati, A; Garst, J; Hassani, H; Leopold, L; Rigas, JR; Ross, HJ; Shepherd, FA; Smylie, M; Zaks, TZ, 2010)	0.6
" The synergy with docetaxel depended on the treatment sequence; a schedule of MK-2206 dosed before docetaxel was not effective."	( MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo. Hatch, H; Hirai, H; Kotani, H; Majumder, PK; Miyama, K; Nakatsuru, Y; Pan, BS; Sootome, H; Taguchi, S; Tsujioka, K; Ueno, Y, 2010)	0.36
" Lapatinib dosage was related linearly to area under the [concentration-time] curve from start time to 12 hours later (AUC(0-12)) and dose-normalized maximum serum concentration and AUC values for patients in stratum II were both significantly higher (P = ."	( Phase I trial of lapatinib in children with refractory CNS malignancies: a Pediatric Brain Tumor Consortium study. Blaney, SM; Boyett, JM; Fouladi, M; Gajjar, A; Gilbertson, RJ; Kun, LE; Onar-Thomas, A; Packer, RJ; Schaiquevich, P; Stewart, CF, 2010)	1.61
" Dose modification including dose reduction and dosing schedule modification may be utilized to manage toxicities, but this must be based on careful hematologic, neurologic, and liver function monitoring."	( Optimizing ixabepilone treatment schedules in patients with advanced or metastatic breast cancer. Egerton, N, 2010)	0.36
" L + T for short duration (14 and 42 days), intermittent administration (14 days on/off), and reduced dosing (half dose) was also investigated."	( Reduced dose and intermittent treatment with lapatinib and trastuzumab for potent blockade of the HER pathway in HER2/neu-overexpressing breast tumor xenografts. Arpino, G; Gutierrez, C; Hilsenbeck, SG; Huang, C; Massarweh, S; Migliaccio, I; Osborne, CK; Rimawi, MF; Schiff, R; Soliz, R; Wang, YC; Ward, R; Wiechmann, LS; Wu, MF, 2011)	0.63
" The recommended dosage is not dependent on body weight either."	( Lapatinib in breast cancer - the predictive significance of HER1 (EGFR), HER2, PTEN and PIK3CA genes and lapatinib plasma level assessment. Bouchalova, K; Cizkova, M; Cwiertka, K; Friedecky, D; Hajduch, M; Trojanec, R, 2010)	1.8
" Taken together, this non-clinical study shows that lapatinib and capecitabine modulate each other's molecular determinants of response and that concomitant dosing seems to be the optimal way to combine these drugs."	( Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants. Chefrour, M; Ciccolini, J; Denden, A; Fischel, JL; Formento, P; Giacometti, S; Iliadis, A; Milano, G; Renée, N, 2012)	0.92
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."	( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011)	0.37
"Our group applied mathematical modeling to capecitabine dosing and predicted 7 days of treatment followed by 7 days of rest (7-7) would improve efficacy and minimize toxicity."	( Phase II trial of a novel capecitabine dosing schedule in combination with lapatinib for the treatment of patients with HER2-positive metastatic breast cancer. Chen, C; D'Andrea, G; Drullinsky, P; Feigin, K; Gajria, D; Gonzalez, J; Hudis, CA; Lake, D; Norton, L; Patil, S; Theodoulou, M; Traina, TA, 2012)	0.61
" Adequate monitoring and early intervention are recommended to prevent debilitating toxicity and suboptimal dosing of EGFRI."	( The risk of nail changes with epidermal growth factor receptor inhibitors: a systematic review of the literature and meta-analysis. Garden, BC; Lacouture, ME; Wu, S, 2012)	0.38
" The lack of direct comparison PFS and treatment dosage modification data were the main limitations."	( Budget impact analysis of the use of oral and intravenous anti-cancer drugs for the treatment of HER2-positive metastatic breast cancer. Benjamin, L; Buthion, V; Farah, B; Iskedjian, M; Rioufol, C; Vidal-Trécan, G, 2013)	0.39
" Similar dose-response lapatinib experiments were conducted with varying concentrations of 5-FU or GEM and isobolograms were constructed to evaluate therapeutic synergy."	( Dual ErbB1 and ErbB2 receptor tyrosine kinase inhibition exerts synergistic effect with conventional chemotherapy in pancreatic cancer. Drebin, JA; Pippin, JA; Singla, S, 2012)	0.69
" Multiple dosing levels were studied, combining pazopanib up to 800 mg/day with lapatinib up to 1,500 mg/day."	( Phase I and pharmacokinetic study of pazopanib and lapatinib combination therapy in patients with advanced solid tumors. Arumugham, T; de Jonge, MJ; Hamberg, P; Hodge, J; Hurwitz, HI; Pandite, LN; Savage, S; Suttle, AB; Verweij, J, 2013)	0.87
" This allows the usage of p110α-specific PI3K inhibitors and thus may spare patients the toxicities of pan-PI3K inhibition to allow maximal dosage and efficacy."	( Enhanced PI3K p110α signaling confers acquired lapatinib resistance that can be effectively reversed by a p110α-selective PI3K inhibitor. Brady, SW; Seok, D; Wang, H; Yu, D; Zhang, J, 2014)	0.66
" donovani in the BALB/c mouse model of infection; dosing on days 7-11 with a 50 mg/kg oral dose of sunitinib, lapatinib or sorafenib reduced liver amastigote burdens by 41%, 36% and 30%, respectively, compared with untreated control mice."	( Activity of anti-cancer protein kinase inhibitors against Leishmania spp. Croft, SL; Sanderson, L; Yardley, V, 2014)	0.61
" Lapatinib dose was escalated to 7,000 mg per day in twice-daily dosing with no DLTs; however, plasma lapatinib concentrations plateaued in this dose range."	( Phase I dose-escalation study of 5-day intermittent oral lapatinib therapy in patients with human epidermal growth factor receptor 2-overexpressing breast cancer. Auerback, G; Chien, AJ; Goga, A; Khanafshar, E; Koch, KM; Melisko, ME; Moasser, MM; Munster, PN; Ordovas, K; Park, JW; Rugo, HS, 2014)	1.56
"Lapatinib exposure can be safely and significantly increased through intermittent dosing but reaches a ceiling that currently impedes clinical translation of the treatment hypothesis."	( Phase I dose-escalation study of 5-day intermittent oral lapatinib therapy in patients with human epidermal growth factor receptor 2-overexpressing breast cancer. Auerback, G; Chien, AJ; Goga, A; Khanafshar, E; Koch, KM; Melisko, ME; Moasser, MM; Munster, PN; Ordovas, K; Park, JW; Rugo, HS, 2014)	2.09
"To review the pharmacology, pharmacokinetics, efficacy, adverse effects, drug-drug interactions, dosage and administration, and formulary considerations for ado-trastuzumab emtansine."	( Ado-trastuzumab emtansine: a HER2-positive targeted antibody-drug conjugate. Auten, JJ; Cicci, TA; Corrigan, PA; Lowe, DK, 2014)	0.4
" Our results suggest that the use of a hybrid system may allow a decrease in the dosage regimen without the loss of therapeutic effect."	( Novel nanosystem to enhance the antitumor activity of lapatinib in breast cancer treatment: Therapeutic efficacy evaluation. Huo, ZJ; Liu, K; Liu, P; Pang, B; Wang, SJ; Wang, ZQ; Zuo, WS, 2015)	0.67
" Clinically, continuous dosing of pazopanib/lapatinib combination was associated with a higher response rate than with lapatinib monotherapy, with poor tolerance."	( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors. Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015)	0.89
"The present study used a phase 1, modified 3 + 3, dose-escalation design to evaluate the safety and tolerability of the combination of orally received pazopanib once every other day with continuous daily dosing of lapatinib for 28 days."	( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors. Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015)	0.82
"Every other day dosing of pazopanib combined with daily lapatinib was tolerated at the established MTD, but no complete or partial tumor responses were observed at these dose levels."	( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors. Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015)	0.88
" Dose-response studies, biochemical and cytometric assessment of the effect of OOS on cell cycle and apoptosis, and drug combination analyses were performed on BT474 and SKBR3 cells, 2 HER2-overexpressing breast cancer cell lines."	( Effect of Oncoxin Oral Solution in HER2-Overexpressing Breast Cancer. González, V; Hernández-García, S; Pandiella, A; Sanz, E, 2015)	0.42
" It was dosed daily with gemcitabine (1,000 mg/m2 on days 1, 8 and 15) and cisplatin (70 mg/m2 on day 2) every 28 days."	( Results from a Phase I Study of Lapatinib with Gemcitabine and Cisplatin in Advanced or Metastatic Bladder Cancer: EORTC Trial 30061. Agerbaek, M; Cerbone, L; Collette, S; Daugaard, G; Marreaud, S; Sengeløv, L; Sternberg, CN; Van Herpen, C; Zhang, J, 2016)	0.72
" Optimal dosing is currently determined using concentrations of tyrosine kinase inhibitors in plasma as a surrogate for tumor concentrations."	( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor. Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015)	1.86
"Mice bearing BT474 HER2+ human breast cancer xenografts were dosed once or twice daily (BID) with lapatinib."	( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor. Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015)	2.08
" Tumor concentrations exceeded the in vitro IC90 (~ 900 nM or 500 ng/mL) for inhibition of HER2 phosphorylation throughout the 12-hour dosing interval."	( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor. Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015)	1.86
"Plasma lapatinib concentrations underestimated tumor drug levels, suggesting that optimal dosing should be focused on the site of action to avoid to inappropriate dose escalation."	( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor. Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015)	2.31
"Plasma lapatinib concentrations underestimated tumor drug levels, suggesting that optimal dosing should be focused on the site of action to avoid to inappropriate dose escalation."	( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor. Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015)	2.31
"The dose escalation cohort enrolled adults with advanced solid tumors, who received MK-2206 dosed 30 to 60 mg every other day and lapatinib 1,000 to 1,500 mg daily continuously, escalated using a 3+3 design."	( Phase I Study of an AKT Inhibitor (MK-2206) Combined with Lapatinib in Adult Solid Tumors Followed by Dose Expansion in Advanced HER2+ Breast Cancer. Bell, MC; Burkard, ME; Eickhoff, J; Flynn, C; Kolesar, JM; Liu, G; Rampurwala, M; Tevaarwerk, AJ; Wisinski, KB, 2016)	0.88
" This study was an open-label, randomized, adaptive design, two-period crossover bioequivalence study of the powder for suspension relative to the commercial tablet at steady state following once daily dosing for 7 days in patients with advanced cancer."	( Bioequivalence study with lapatinib powder for oral suspension and the original tablet formulation in cancer patients. Arya, N; Cartee, L; Curran, D; D'Amelio, AM; Ferron-Brady, G; Hollyfield, H; Koch, KM; Lemmon, C; Piepszak, A; Swaby, RF, )	0.43
"The stability of extemporaneously prepared erlotinib, lapatinib, and imatinib oral liquid dosage forms using two commercially available vehicles when stored at 4 and 25 °C was evaluated."	( Stability of extemporaneous erlotinib, lapatinib, and imatinib oral suspensions. Griffith, N; Kolli, S; Li, Q; Liu, Z; Poi, MJ; Wetz, K, 2016)	0.95
" Synergistic drug combinations can lessen potential toxic side effects through lower dosing and simultaneously help to overcome drug resistance."	( Lapatinib potentiates cytotoxicity of YM155 in neuroblastoma via inhibition of the ABCB1 efflux transporter. Brunak, S; Halasz, M; Huber, KVM; Kolch, W; Papamarkou, T; Radic-Sarikas, B; Superti-Furga, G; Tsafou, KP; Winter, GE, 2017)	1.9
" Here, we developed a computational approach to model the in vitro cellular dynamics of the EGFR-mutant cell line SF268 in response to different lapatinib concentrations and dosing schedules."	( Mathematical modeling identifies optimum lapatinib dosing schedules for the treatment of glioblastoma patients. Haeno, H; Michor, F; Stein, S; Vivanco, I; Zhao, R, 2018)	0.95
" weekly dosing with EGFR inhibitors (gefitinib and lapatinib) and an AKT inhibitor (MK2206) were compared in two rodent breast cancer models."	( Daily or weekly dosing with EGFR inhibitors, gefitinib and lapatinib, and AKt inhibitor MK2206 in mammary cancer models. Bode, A; Grubbs, CJ; Juliana, MM; Lubet, RA; Moeinpour, F; Steele, VE, 2018)	0.98
" Deterministic, probabilistic sensitivity analyses and a scenario analysis examined parameter uncertainty and accounted for drug wastage in dosage and cost calculations."	( A cost-effectiveness analysis of trastuzumab-containing treatment sequences for HER-2 positive metastatic breast cancer patients in Taiwan. Ali, AA; Alqhtani, H; Balkrishnan, R; de Lima Lopes, G; Diaby, V; Ko, Y; Palacio, S; van Boemmel-Wegmann, S; Wang, CY, 2020)	0.56
"Lapatinib and trametinib could be combined in an intermittent dosing schedule in patients with manageable toxicity."	( Phase I study of lapatinib plus trametinib in patients with KRAS-mutant colorectal, non-small cell lung, and pancreatic cancer. Beijnen, JH; Bernards, R; Huijberts, SCFA; Huitema, ADR; Marchetti, S; Monkhorst, K; Opdam, FL; Pulleman, S; Rosing, H; Schellens, JHM; Steeghs, N; Thijssen, B; van Brummelen, EMJ; van Geel, RMJM, 2020)	2.34
" The in vivo research revealed that there were overwhelming advantages in using HPP-Dox/Lap to inhibit tumor growth, progression, and lung metastasis even at a low dosage (1 mg kg-1), and it decreased postoperative recurrence and pulmonary metastatic nodules."	( Acid-labile polysaccharide prodrug via lapatinib-sensitizing effect substantially prevented metastasis and postoperative recurrence of triple-negative breast cancer. Fan, Y; Guo, Z; Liang, J; Ma, M; Sui, J; Sun, Y; Xu, Z; Yang, Y; Zhang, X; Zhao, M, 2020)	0.83
" Other studies on this drug substance include drug stability, pharmaceutical applications, mechanism of action, pharmacodynamics, and a dosing information are also reviewed."	( Lapatinib: A comprehensive profile. Abdelgalil, AA; Alkahtani, HM, 2023)	2.35
" Exploratory twice daily dosing improved PFS for neratinib but not lapatinib."	( Dissecting sources of variability in patient response to targeted therapy: anti-HER2 therapies as a case study. Cao, Y; Qi, T, 2023)	1.15

Role	Description
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
tyrosine kinase inhibitor	Any protein kinase inhibitor that interferes with the action of tyrosine kinase.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
organofluorine compound	An organofluorine compound is a compound containing at least one carbon-fluorine bond.
organochlorine compound	An organochlorine compound is a compound containing at least one carbon-chlorine bond.
quinazolines	Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
furans	Compounds containing at least one furan ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathway	Proteins	Compounds
Disease	1278	231
Diseases of signal transduction by growth factor receptors and second messengers	262	31
Signaling by ERBB2 in Cancer	16	10
Drug resistance in ERBB2 KD mutants	4	6
Resistance of ERBB2 KD mutants to lapatinib	3	1
Integrated breast cancer pathway	98	18

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
hypoxia-inducible factor 1 alpha subunit	Homo sapiens (human)	Potency	21.4552	3.1890	29.8841	59.4836	AID1224846; AID1224894
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	33.7136	0.0060	38.0041	19,952.5996	AID1159521; AID1159523
SMAD family member 2	Homo sapiens (human)	Potency	9.0029	0.1737	34.3047	61.8120	AID1346859; AID1346924
PPM1D protein	Homo sapiens (human)	Potency	32.9993	0.0052	9.4661	32.9993	AID1347411
SMAD family member 3	Homo sapiens (human)	Potency	9.0029	0.1737	34.3047	61.8120	AID1346859; AID1346924
GLI family zinc finger 3	Homo sapiens (human)	Potency	5.0194	0.0007	14.5928	83.7951	AID1259369; AID1259392
AR protein	Homo sapiens (human)	Potency	14.2341	0.0002	21.2231	8,912.5098	AID1259243; AID1259247; AID743053
caspase 7, apoptosis-related cysteine protease	Homo sapiens (human)	Potency	33.4915	0.0133	26.9810	70.7614	AID1346978
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	12.1416	0.0006	57.9133	22,387.1992	AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	3.0499	0.0010	22.6508	76.6163	AID1224838; AID1224893
progesterone receptor	Homo sapiens (human)	Potency	10.4155	0.0004	17.9460	75.1148	AID1346784; AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	1.5487	0.0123	7.9835	43.2770	AID1645841
EWS/FLI fusion protein	Homo sapiens (human)	Potency	6.0312	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	25.8614	0.0030	41.6115	22,387.1992	AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	17.3810	0.0008	17.5051	59.3239	AID1159527; AID1159531
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	8.2320	0.0015	30.6073	15,848.9004	AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptor	Homo sapiens (human)	Potency	25.1547	0.3758	27.4851	61.6524	AID743217; AID743220
pregnane X nuclear receptor	Homo sapiens (human)	Potency	23.0404	0.0054	28.0263	1,258.9301	AID1346982; AID1346985
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	29.9252	0.0002	29.3054	16,493.5996	AID1259244; AID1259248; AID743075
G	Vesicular stomatitis virus	Potency	1.3803	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	3.4671	0.0010	8.3798	61.1304	AID1645840
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	26.7776	0.0010	24.5048	61.6448	AID743212; AID743215
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	14.6017	0.0010	19.4141	70.9645	AID743094; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	30.1607	0.0237	23.2282	63.5986	AID743222; AID743223
caspase-3	Homo sapiens (human)	Potency	33.4915	0.0133	26.9810	70.7614	AID1346978
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a	Homo sapiens (human)	Potency	26.8325	19.7391	45.9784	64.9432	AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)	Homo sapiens (human)	Potency	21.3138	0.0578	21.1097	61.2679	AID1159526
heat shock protein beta-1	Homo sapiens (human)	Potency	25.1547	0.0420	27.3789	61.6448	AID743210; AID743228
tyrosine-protein kinase Yes	Homo sapiens (human)	Potency	4.3432	0.0000	5.0182	79.2586	AID686947
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	5.0856	0.0006	27.2152	1,122.0200	AID743202; AID743219
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	3.2197	0.0056	12.3677	36.1254	AID624032
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	29.8493	0.0015	57.7890	15,848.9004	AID1259244
Interferon beta	Homo sapiens (human)	Potency	23.0500	0.0033	9.1582	39.8107	AID1347407; AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	1.3803	0.0123	8.9648	39.8107	AID1645842
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	29.8493	0.0015	51.7393	15,848.9004	AID1259244
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	0.7079	0.0096	10.5250	35.4813	AID1479145
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	1.3803	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	1.3803	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Epidermal growth factor receptor	Homo sapiens (human)	Ki	0.0030	0.0030	0.0030	0.0030	AID977610
Histone deacetylase 3	Homo sapiens (human)	IC50 (µMol)	55.0000	0.0004	0.6196	10.0000	AID546545; AID546549
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	7.3750	0.1100	7.1903	10.0000	AID1443980; AID1443989; AID1449628; AID1674183
Tyrosine-protein kinase ABL1	Homo sapiens (human)	IC50 (µMol)	23.0000	0.0001	0.7128	10.0000	AID546555
Epidermal growth factor receptor	Homo sapiens (human)	IC50 (µMol)	6.5561	0.0000	0.5369	10.0000	AID1168535; AID1201367; AID1201370; AID1244850; AID1256452; AID1268284; AID1315424; AID1330935; AID1341757; AID1341758; AID1353459; AID1378273; AID1402963; AID1407099; AID1407100; AID1407101; AID1424361; AID1439619; AID1463973; AID1532891; AID1532893; AID1535425; AID1545475; AID1589887; AID1595620; AID1664188; AID1664192; AID1664193; AID1667574; AID1667575; AID1676511; AID1676512; AID1676513; AID1676514; AID1676515; AID1724046; AID1738031; AID1738032; AID1738033; AID1751473; AID1795774; AID1798859; AID1799771; AID1809346; AID1882632; AID1894161; AID1904122; AID1915705; AID263980; AID270617; AID345876; AID441963; AID441965; AID461251; AID463638; AID474116; AID517323; AID546551; AID546565; AID634136; AID636384; AID638067; AID642760; AID662804; AID664631; AID664632; AID69892
Epidermal growth factor receptor	Homo sapiens (human)	Ki	0.0030	0.0000	0.2953	3.5000	AID1525532
Receptor tyrosine-protein kinase erbB-2	Homo sapiens (human)	IC50 (µMol)	0.0537	0.0001	0.5453	10.0000	AID1062007; AID1168534; AID1256453; AID1268283; AID1306575; AID1315425; AID1330925; AID1330936; AID1424362; AID1532892; AID1545519; AID1664189; AID1667576; AID1676531; AID1718898; AID1795774; AID1798859; AID1799771; AID1882631; AID1894160; AID1915714; AID263981; AID270616; AID404519; AID441964; AID461252; AID463639; AID474117; AID517324; AID546552; AID634138; AID636385; AID638068; AID664633; AID68106
Insulin receptor	Homo sapiens (human)	IC50 (µMol)	17.0000	0.0017	0.8479	10.0000	AID546554
Insulin-like growth factor 1 receptor	Homo sapiens (human)	IC50 (µMol)	20.0000	0.0003	0.4308	8.0000	AID474115; AID517322
Platelet-derived growth factor receptor beta	Homo sapiens (human)	IC50 (µMol)	104.2500	0.0006	0.8007	8.5000	AID1168536; AID546553
Mast/stem cell growth factor receptor Kit	Homo sapiens (human)	IC50 (µMol)	200.0000	0.0007	0.4708	10.0000	AID1168538
Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)	IC50 (µMol)	251.1890	0.1200	4.0480	10.0000	AID1207374
Platelet-derived growth factor receptor alpha	Homo sapiens (human)	IC50 (µMol)	20.0000	0.0001	0.4912	10.0000	AID1366911
Cytochrome P450 3A5	Homo sapiens (human)	Ki	37.6000	0.0220	2.6040	7.6000	AID1215636
G1/S-specific cyclin-E1	Homo sapiens (human)	IC50 (µMol)	20.0000	0.0010	1.0404	10.0000	AID1366912
Cyclin-dependent kinase 2	Homo sapiens (human)	IC50 (µMol)	15.5000	0.0004	1.0444	10.0000	AID1366912; AID546556
Vascular endothelial growth factor receptor 2	Homo sapiens (human)	IC50 (µMol)	105.0000	0.0000	0.4830	8.8000	AID1168537; AID636160
D(1A) dopamine receptor	Sus scrofa (pig)	IC50 (µMol)	0.0600	0.0010	0.1203	0.3000	AID634138
Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)	IC50 (µMol)	251.1890	0.1200	4.0480	10.0000	AID1207374
Serine/threonine-protein kinase PLK1	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0001	0.7734	9.0000	AID546558
Histone deacetylase 4	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0006	1.0526	10.0000	AID546545
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	33,543.9857	0.0009	1.9014	10.0000	AID1207468; AID1207498; AID1207528
Histone deacetylase 1	Homo sapiens (human)	IC50 (µMol)	55.0000	0.0001	0.5543	9.9000	AID546545; AID546547
Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)	IC50 (µMol)	8,922.0802	0.0003	2.2545	9.6000	AID1207284; AID1207562
Sodium channel protein type 5 subunit alpha	Homo sapiens (human)	IC50 (µMol)	3,162.2800	0.0003	3.6484	9.2000	AID1207314
Receptor tyrosine-protein kinase erbB-4	Homo sapiens (human)	IC50 (µMol)	0.2586	0.0001	0.1736	2.5900	AID1664190; AID1772926; AID1798859; AID1799771; AID664634
Histone deacetylase 7	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0007	1.0260	9.9000	AID546545
Histone deacetylase 2	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0001	0.7221	9.9700	AID546545
Polyamine deacetylase HDAC10	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0005	0.7245	9.9000	AID546545
Histone deacetylase 11	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0003	0.9298	9.9000	AID546545
Histone deacetylase 8	Homo sapiens (human)	IC50 (µMol)	55.0000	0.0007	0.9947	9.9000	AID546545; AID546550
Alpha-1A adrenergic receptor	Sus scrofa (pig)	IC50 (µMol)	0.0600	0.0600	0.1800	0.3000	AID634138
Histone deacetylase 6	Homo sapiens (human)	IC50 (µMol)	55.0000	0.0000	0.5376	9.9000	AID546545; AID546548
Histone deacetylase 9	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0005	0.9413	9.9000	AID546545
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	IC50 (µMol)	3.2000	0.0040	1.9666	10.0000	AID1873221
Histone deacetylase 5	Homo sapiens (human)	IC50 (µMol)	100.0000	0.0007	0.9610	10.0000	AID546545
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Leukotriene C4 synthase	Cavia porcellus (domestic guinea pig)	Kd	10.0000	0.9300	2.5478	5.7000	AID625128
Bone morphogenetic protein receptor type-1B	Homo sapiens (human)	Kd	20.0000	0.0009	1.1413	3.7000	AID1424922; AID624825
Membrane-associated progesterone receptor component 1	Homo sapiens (human)	Kd	30.0000	0.2040	0.2040	0.2040	AID1425109
Cell division cycle 7-related protein kinase	Homo sapiens (human)	Kd	30.0000	0.5110	0.5110	0.5110	AID1424936
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)	Kd	10.0000	0.0033	1.5175	7.6000	AID624974
Serine/threonine-protein kinase PLK4	Homo sapiens (human)	Kd	16.6667	0.0008	1.5144	9.0000	AID1425121; AID436044; AID625076
Serine/threonine-protein kinase 25	Homo sapiens (human)	Kd	10.0000	0.0120	2.5734	9.2000	AID435329; AID625059
ATP-dependent RNA helicase DDX3X	Homo sapiens (human)	Kd	30.0000	0.4350	0.4350	0.4350	AID1424975
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)	Kd	0.6700	0.0005	1.0152	5.2000	AID624877
Pyridoxal kinase	Homo sapiens (human)	Kd	30.0000	0.2860	5.0765	16.4040	AID1425106
Citron Rho-interacting kinase	Homo sapiens (human)	Kd	16.6667	0.0330	3.0646	48.8760	AID1424954; AID435523; AID625065
Serine/threonine-protein kinase RIO3	Homo sapiens (human)	Kd	10.0000	0.0077	1.4099	9.7000	AID435191; AID624926
Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)	Kd	4.4000	0.0270	1.4471	5.3000	AID624722
Serine/threonine-protein kinase Chk1	Homo sapiens (human)	Kd	16.6667	0.0028	1.4744	8.7000	AID1424953; AID435396; AID624831
Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)	Kd	10.0000	0.0120	1.5827	6.3000	AID624836
Peripheral plasma membrane protein CASK	Homo sapiens (human)	Kd	10.0000	0.0190	0.9330	2.8000	AID624749
Aurora kinase A	Homo sapiens (human)	Kd	16.6667	0.0001	0.7342	9.3000	AID1424917; AID435518; AID624919
Cyclin-G-associated kinase	Homo sapiens (human)	Kd	16.6667	0.0003	0.9086	28.6510	AID1425009; AID435821; AID625012
Serine/threonine-protein kinase DCLK1	Homo sapiens (human)	Kd	10.0000	0.0049	1.8360	8.1000	AID435284; AID624966
Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)	Kd	10.0000	0.0058	1.5058	5.9000	AID624832
Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)	Kd	10.0000	0.0031	0.6128	4.1000	AID435678; AID625022
Ephrin type-B receptor 6	Homo sapiens (human)	Kd	20.0000	0.0000	1.0768	9.0000	AID1424995; AID624957
Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)	Kd	30.0000	0.0260	1.3140	2.6020	AID1424896
Mitogen-activated protein kinase 13	Homo sapiens (human)	Kd	10.0000	0.0001	1.4667	6.6000	AID624892
3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0017	1.3432	3.5000	AID435189; AID624876
Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)	Kd	10.0000	0.0160	0.9316	5.3000	AID624965
Death-associated protein kinase 3	Homo sapiens (human)	Kd	10.0000	0.0010	1.8241	9.9000	AID435155; AID435398; AID624834
Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)	Kd	10.0000	0.0015	1.6660	8.5000	AID624724
Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)	Kd	12.4000	0.0020	1.6212	11.4330	AID1425155; AID435935; AID624925
Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)	Kd	30.0000	0.0940	1.3910	3.5070	AID1424926
NUAK family SNF1-like kinase 1	Homo sapiens (human)	Kd	10.0000	0.0037	0.5214	5.9000	AID435150; AID625088
Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)	Kd	30.0000	0.0170	0.3610	0.7050	AID1425097
Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)	Kd	10.0000	0.0180	2.4890	6.7000	AID624751
Tyrosine-protein kinase JAK2	Homo sapiens (human)	Kd	10.0000	0.0000	0.8851	7.0000	AID435658; AID624973
Eukaryotic translation initiation factor 5B	Homo sapiens (human)	Kd	30.0000	0.2320	0.2320	0.2320	AID1424986
Rho-associated protein kinase 2	Homo sapiens (human)	Kd	20.0000	0.0002	2.7105	56.0660	AID1425158; AID624969
Serine/threonine-protein kinase ULK1	Homo sapiens (human)	Kd	20.0000	0.0008	1.8410	23.2730	AID1425208; AID624916
Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)	Kd	20.0000	0.0057	2.0095	12.2010	AID1424997; AID624835
Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)	Kd	14.0000	0.0170	1.9737	29.9570	AID1425162; AID435831; AID436051; AID624736; AID624967
U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)	Kd	30.0000	1.3820	1.3820	1.3820	AID1425174
Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)	Kd	14.0000	0.0120	1.6396	7.2000	AID1425161; AID435325; AID435441; AID624806; AID624927
Serine/threonine-protein kinase 16	Homo sapiens (human)	Kd	16.6667	0.0017	1.2483	9.9690	AID1425179; AID435692; AID624775
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)	Kd	7.5000	0.0032	1.0024	7.5000	AID624958
Serine/threonine-protein kinase PAK 3	Homo sapiens (human)	Kd	10.0000	0.0005	1.4483	5.7000	AID435823; AID624873
Cyclin-dependent kinase-like 5	Homo sapiens (human)	Kd	23.3333	0.0017	1.4788	7.3000	AID1424951; AID624905
Serine/threonine-protein kinase 17B	Homo sapiens (human)	Kd	10.0000	0.0048	2.1982	9.4000	AID435401; AID624942
Serine/threonine-protein kinase 10	Homo sapiens (human)	Kd	10.3500	0.0000	2.9234	57.4530	AID1425177; AID256604; AID435677; AID625030
Serine/threonine-protein kinase D3	Homo sapiens (human)	Kd	16.6667	0.0089	2.2738	23.3410	AID1425137; AID435554; AID625024
Cyclin-dependent kinase 14	Homo sapiens (human)	Kd	10.0000	0.0160	0.9920	3.6000	AID435689; AID625070
Structural maintenance of chromosomes protein 2	Homo sapiens (human)	Kd	30.0000	0.2090	0.6575	1.1060	AID1425173
Mitogen-activated protein kinase kinase kinase 6	Homo sapiens (human)	Kd	10.0000	0.1700	1.5781	8.0000	AID624962
Serine/threonine-protein kinase OSR1	Homo sapiens (human)	Kd	10.0000	0.0480	2.3498	8.0000	AID624977
Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)	Kd	16.6667	0.0082	2.3645	62.7720	AID1425054; AID435910; AID624756
Serine/threonine-protein kinase LATS1	Homo sapiens (human)	Kd	16.6667	0.0140	1.8393	10.7330	AID1425033; AID435529; AID624963
Serine/threonine-protein kinase PAK 4	Homo sapiens (human)	Kd	16.6667	0.0027	2.5694	30.3710	AID1425100; AID435929; AID624811
Serine/threonine-protein kinase Chk2	Homo sapiens (human)	Kd	10.0000	0.0071	1.2729	7.7000	AID624803
Tyrosine-protein kinase ABL1	Homo sapiens (human)	Kd	10.8696	0.0000	1.0411	13.4530	AID1424890; AID435146; AID435514; AID435515; AID435644; AID435775; AID435776; AID435897; AID624978; AID624979; AID624980; AID624981; AID624982; AID624983; AID624984; AID624985; AID624986; AID624987; AID624988; AID624989; AID624990; AID624991; AID624992
Epidermal growth factor receptor	Homo sapiens (human)	Kd	0.4228	0.0001	1.3514	20.8270	AID1424983; AID1595618; AID1664200; AID256664; AID435156; AID435157; AID435402; AID435525; AID435652; AID435653; AID435791; AID435792; AID435906; AID435907; AID624996; AID624997; AID624998; AID624999; AID625000; AID625001; AID625002; AID625003; AID625004; AID625005; AID625006; AID625007
RAF proto-oncogene serine/threonine-protein kinase	Homo sapiens (human)	Kd	10.0000	0.0066	1.1467	4.4000	AID435556; AID624897
Receptor tyrosine-protein kinase erbB-2	Homo sapiens (human)	Kd	0.0083	0.0008	1.2931	5.1000	AID256662; AID435796; AID624804
High affinity nerve growth factor receptor	Homo sapiens (human)	Kd	16.6667	0.0020	1.3484	9.2000	AID1425094; AID435201; AID624808
Guanine nucleotide-binding protein G(i) subunit alpha-2	Homo sapiens (human)	Kd	30.0000	0.1840	0.1840	0.1840	AID1425011
ADP/ATP translocase 2	Homo sapiens (human)	Kd	30.0000	0.4510	0.4510	0.4510	AID1425169
Protein kinase C beta type	Homo sapiens (human)	Kd	30.0000	0.0013	2.7081	26.3240	AID1425130
Insulin receptor	Homo sapiens (human)	Kd	16.6667	0.0017	1.0823	7.9060	AID1425026; AID435408; AID624784
Tyrosine-protein kinase Lck	Homo sapiens (human)	Kd	16.6667	0.0002	1.1174	24.2210	AID1425034; AID435676; AID625013
Tyrosine-protein kinase Fyn	Homo sapiens (human)	Kd	16.6667	0.0008	1.4238	8.4000	AID1425008; AID435800; AID624727
Cyclin-dependent kinase 1	Homo sapiens (human)	Kd	30.0000	0.2880	1.4952	3.0490	AID1424937
Glycogen phosphorylase, liver form	Homo sapiens (human)	Kd	30.0000	2.1210	2.1210	2.1210	AID1425146
Tyrosine-protein kinase Fes/Fps	Homo sapiens (human)	Kd	16.6667	0.0048	1.0986	7.4000	AID1425003; AID435161; AID624852
Macrophage colony-stimulating factor 1 receptor	Homo sapiens (human)	Kd	10.0000	0.0006	0.6993	8.1000	AID435280; AID624995
Adenine phosphoribosyltransferase	Homo sapiens (human)	Kd	30.0000	0.0290	0.0290	0.0290	AID1424914
Tyrosine-protein kinase Yes	Homo sapiens (human)	Kd	20.0000	0.0003	1.3708	17.1520	AID1425212; AID435328; AID625018
Tyrosine-protein kinase Lyn	Homo sapiens (human)	Kd	20.0000	0.0006	1.0485	5.7000	AID1425037; AID435804; AID624862
Proto-oncogene tyrosine-protein kinase receptor Ret	Homo sapiens (human)	Kd	12.8571	0.0007	0.8642	27.5420	AID1425154; AID435323; AID435434; AID625121; AID625122; AID625123; AID625124
Insulin-like growth factor 1 receptor	Homo sapiens (human)	Kd	16.6667	0.0010	1.9211	19.2170	AID1425022; AID435164; AID624800
ATP-dependent translocase ABCB1	Homo sapiens (human)	EC50 (µMol)	2.7900	0.0160	0.6786	3.1000	AID1904123
Signal recognition particle receptor subunit alpha	Homo sapiens (human)	Kd	30.0000	0.0080	0.0080	0.0080	AID1425176
Cytochrome c1, heme protein, mitochondrial	Homo sapiens (human)	Kd	30.0000	0.2020	0.2020	0.2020	AID1424969
Hepatocyte growth factor receptor	Homo sapiens (human)	Kd	14.0000	0.0002	1.6297	8.5000	AID1425076; AID435312; AID624794; AID624795; AID624796
Tyrosine-protein kinase HCK	Homo sapiens (human)	Kd	16.6667	0.0003	2.0343	15.9930	AID1425017; AID435311; AID624857
Proto-oncogene tyrosine-protein kinase ROS	Homo sapiens (human)	Kd	10.0000	0.0005	1.1741	5.8000	AID435192; AID624899
Platelet-derived growth factor receptor beta	Homo sapiens (human)	Kd	16.6667	0.0001	1.0050	11.1070	AID1425104; AID435926; AID624875
Tyrosine-protein kinase Fgr	Homo sapiens (human)	Kd	16.6667	0.0005	1.0721	7.8000	AID1425005; AID435798; AID625011
Wee1-like protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0039	2.1874	9.4000	AID624746
Uncharacterized serine/threonine-protein kinase SBK3	Homo sapiens (human)	Kd	10.0000	0.0250	1.4739	5.8000	AID624747
Serine/threonine-protein kinase A-Raf	Homo sapiens (human)	Kd	30.0000	0.0470	9.6832	33.6550	AID1424915
Mast/stem cell growth factor receptor Kit	Homo sapiens (human)	Kd	10.0000	0.0002	0.8159	9.8000	AID435167; AID435410; AID435411; AID435675; AID435802; AID599957; AID599959; AID624786; AID624787; AID624788; AID624789; AID624790; AID624791; AID624792; AID624793
Glycogen phosphorylase, brain form	Homo sapiens (human)	Kd	30.0000	3.5690	3.5690	3.5690	AID1425145
Breakpoint cluster region protein	Homo sapiens (human)	Kd	30.0000	0.0030	1.2196	17.3640	AID1424919
Serine/threonine-protein kinase pim-1	Homo sapiens (human)	Kd	16.6667	0.0010	1.1393	19.3160	AID1425111; AID435931; AID624878
Fibroblast growth factor receptor 1	Homo sapiens (human)	Kd	16.6667	0.0003	1.5581	6.2000	AID1425004; AID435526; AID625132
DNA topoisomerase 2-alpha	Homo sapiens (human)	Kd	30.0000	0.0640	0.2750	0.4860	AID1425202
Myosin light chain kinase, smooth muscle	Gallus gallus (chicken)	Kd	10.0000	0.0020	0.3203	1.7000	AID435413
Cyclin-dependent kinase 4	Homo sapiens (human)	Kd	16.6667	0.0033	1.6050	8.6000	AID1424946; AID624780; AID624781
ADP/ATP translocase 3	Homo sapiens (human)	Kd	30.0000	0.0060	0.2505	0.4950	AID1425170
Proto-oncogene tyrosine-protein kinase Src	Homo sapiens (human)	Kd	16.6667	0.0002	1.5077	9.6000	AID1425175; AID435195; AID625016
cAMP-dependent protein kinase type II-alpha regulatory subunit	Homo sapiens (human)	Kd	30.0000	0.0520	1.7535	3.4550	AID1425128
Insulin receptor-related protein	Homo sapiens (human)	Kd	10.0000	0.0062	1.3814	4.6000	AID435430; AID625075
Serine/threonine-protein kinase B-raf	Homo sapiens (human)	Kd	14.0000	0.0002	1.6258	26.0180	AID1424924; AID435901; AID435902; AID624946; AID624947
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Homo sapiens (human)	Kd	16.6667	0.0001	2.0569	9.5000	AID1425110; AID435930; AID624797
Ribosyldihydronicotinamide dehydrogenase [quinone]	Homo sapiens (human)	Kd	30.0000	0.0040	6.7556	88.9030	AID1425093
Platelet-derived growth factor receptor alpha	Homo sapiens (human)	Kd	10.0000	0.0004	0.7090	8.8000	AID435827; AID625034
Tyrosine-protein kinase Fer	Homo sapiens (human)	Kd	16.6667	0.0014	1.3604	8.8000	AID1425002; AID435160; AID625010
Protein kinase C alpha type	Homo sapiens (human)	Kd	30.0000	0.0003	1.7922	21.3520	AID1425129
cAMP-dependent protein kinase catalytic subunit alpha	Homo sapiens (human)	Kd	16.6667	0.0039	2.9479	23.2450	AID1425123; AID435932; AID624881
Vascular endothelial growth factor receptor 1	Homo sapiens (human)	Kd	10.0000	0.0007	0.9585	9.9000	AID435429; AID624853
General transcription and DNA repair factor IIH helicase subunit XPD	Homo sapiens (human)	Kd	30.0000	0.0020	1.6906	12.0220	AID1424996
Interferon-induced, double-stranded RNA-activated protein kinase	Homo sapiens (human)	Kd	10.0000	0.1200	2.3238	7.4000	AID435555; AID624896
Casein kinase II subunit alpha'	Homo sapiens (human)	Kd	16.6667	0.0010	2.5309	28.8720	AID1424968; AID435789; AID624849
Ras-related protein Rab-6A	Homo sapiens (human)	Kd	30.0000	0.0330	0.0330	0.0330	AID1425150
Serine/threonine-protein kinase MAK	Homo sapiens (human)	Kd	10.0000	0.0280	1.3461	2.6000	AID625025
Cyclin-dependent kinase 11B	Homo sapiens (human)	Kd	10.0000	0.0084	0.8679	2.1000	AID435395; AID624708
Ephrin type-A receptor 1	Homo sapiens (human)	Kd	16.6667	0.0041	1.8000	9.8000	AID1424987; AID435793; AID625008
Fibroblast growth factor receptor 2	Homo sapiens (human)	Kd	10.0000	0.0310	1.1579	5.5000	AID435290; AID625131
Receptor tyrosine-protein kinase erbB-3	Homo sapiens (human)	Kd	5.5000	0.0008	2.2545	9.2000	AID624851
Multifunctional protein ADE2	Homo sapiens (human)	Kd	30.0000	5.4810	5.4810	5.4810	AID1425098
Fibroblast growth factor receptor 4	Homo sapiens (human)	Kd	10.0000	0.1100	2.6773	7.2000	AID435656; AID625130
Fibroblast growth factor receptor 3	Homo sapiens (human)	Kd	10.0000	0.0230	1.2652	6.9000	AID435291; AID435527; AID624782; AID624783
cAMP-dependent protein kinase catalytic subunit gamma	Homo sapiens (human)	Kd	30.0000	0.0020	8.5577	49.2780	AID1425125
cAMP-dependent protein kinase catalytic subunit beta	Homo sapiens (human)	Kd	16.6667	0.0130	0.7408	4.1000	AID1425124; AID435182; AID624882
Ferrochelatase, mitochondrial	Homo sapiens (human)	Kd	30.0000	0.2430	6.4343	67.9140	AID1425001
Ribosomal protein S6 kinase beta-1	Homo sapiens (human)	Kd	20.0000	0.0013	1.1805	4.8000	AID1425164; AID624906
Tyrosine-protein kinase JAK1	Homo sapiens (human)	Kd	15.0000	0.0016	1.2166	7.8000	AID1425030; AID435165; AID624858; AID624859
Protein kinase C eta type	Homo sapiens (human)	Kd	10.0000	0.0004	0.2881	1.8000	AID436034; AID625049
Cyclin-dependent kinase 2	Homo sapiens (human)	Kd	16.6667	0.0070	1.5179	10.4870	AID1424944; AID435785; AID624844
Beta-adrenergic receptor kinase 1	Homo sapiens (human)	Kd	30.0000	0.1700	5.5791	22.4940	AID1424908
Probable ATP-dependent RNA helicase DDX6	Homo sapiens (human)	Kd	30.0000	4.1030	4.1030	4.1030	AID1424977
Activin receptor type-2A	Homo sapiens (human)	Kd	10.0000	0.0100	2.0789	8.9000	AID436004; AID624838
Mitogen-activated protein kinase 3	Homo sapiens (human)	Kd	16.6667	0.4300	5.2743	9.8000	AID1425061; AID436016; AID624885
MAP/microtubule affinity-regulating kinase 3	Homo sapiens (human)	Kd	16.6667	0.0030	3.9689	58.2400	AID1425069; AID435659; AID624863
Deoxycytidine kinase	Homo sapiens (human)	Kd	30.0000	0.0120	1.0875	2.1630	AID1424970
Mitogen-activated protein kinase 1	Homo sapiens (human)	Kd	20.0000	0.0001	2.7441	7.3000	AID1425056; AID435654; AID624713
Ephrin type-A receptor 2	Homo sapiens (human)	Kd	16.6667	0.0009	1.0752	8.1980	AID1424988; AID435908; AID624951
Ephrin type-A receptor 3	Homo sapiens (human)	Kd	10.0000	0.0001	2.1521	8.6000	AID435794; AID625009
Ephrin type-A receptor 8	Homo sapiens (human)	Kd	10.0000	0.0002	1.2875	7.7000	AID435287; AID625120
Ephrin type-B receptor 2	Homo sapiens (human)	Kd	16.6667	0.0004	3.1536	53.1980	AID1424992; AID435288; AID625105
Leukocyte tyrosine kinase receptor	Homo sapiens (human)	Kd	10.0000	0.0010	2.0631	7.5000	AID435168; AID624743
Non-receptor tyrosine-protein kinase TYK2	Homo sapiens (human)	Kd	15.0000	0.0009	1.5575	8.7000	AID1425207; AID435444; AID624912; AID624913
UMP-CMP kinase	Homo sapiens (human)	Kd	30.0000	0.0030	0.0045	0.0060	AID1424959
Phosphatidylethanolamine-binding protein 1	Homo sapiens (human)	Kd	30.0000	0.0030	0.0030	0.0030	AID1425107
Wee1-like protein kinase	Homo sapiens (human)	Kd	16.6667	0.0014	3.5389	65.1580	AID1425210; AID435204; AID624914
Heme oxygenase 2	Homo sapiens (human)	Kd	30.0000	0.1190	0.1190	0.1190	AID1425018
Tyrosine-protein kinase receptor UFO	Homo sapiens (human)	Kd	10.0000	0.0001	1.2891	6.3000	AID436007; AID624840
Mitogen-activated protein kinase 4	Homo sapiens (human)	Kd	10.0000	1.1000	3.0556	5.4000	AID436017; AID624886
DnaJ homolog subfamily A member 1	Homo sapiens (human)	Kd	30.0000	0.9620	0.9620	0.9620	AID1424980
RAC-alpha serine/threonine-protein kinase	Homo sapiens (human)	Kd	16.6667	0.0006	1.0621	4.4000	AID1424910; AID435899; AID624994
RAC-beta serine/threonine-protein kinase	Homo sapiens (human)	Kd	16.6667	0.0021	1.6196	8.7000	AID1424911; AID435517; AID624839
G protein-coupled receptor kinase 4	Homo sapiens (human)	Kd	10.0000	0.0120	1.6852	7.3000	AID624739
Dual specificity protein kinase TTK	Homo sapiens (human)	Kd	16.6667	0.0065	1.6269	8.5000	AID1425205; AID435203; AID624910
DNA replication licensing factor MCM4	Homo sapiens (human)	Kd	30.0000	0.6290	0.6290	0.6290	AID1425072
Prostaglandin G/H synthase 2	Homo sapiens (human)	Kd	10.0000	0.0090	1.8725	8.4000	AID625141
Myosin-10	Homo sapiens (human)	Kd	30.0000	0.2290	0.4935	0.7580	AID1425079
Tyrosine-protein kinase receptor Tie-1	Homo sapiens (human)	Kd	10.0000	0.0003	1.0645	5.7000	AID435198; AID625017
Vascular endothelial growth factor receptor 3	Homo sapiens (human)	Kd	10.0000	0.0015	0.9450	7.2000	AID436018; AID624854
Vascular endothelial growth factor receptor 2	Homo sapiens (human)	Kd	10.0000	0.0002	0.8063	5.7000	AID435327; AID624860
Dual specificity mitogen-activated protein kinase kinase 2	Homo sapiens (human)	Kd	16.6667	0.0039	1.6429	9.6000	AID1425039; AID435169; AID625137
Receptor-type tyrosine-protein kinase FLT3	Homo sapiens (human)	Kd	11.5385	0.0002	0.9559	9.9000	AID1425006; AID435162; AID435310; AID435406; AID435407; AID435799; AID624934; AID624935; AID624936; AID624937; AID624938; AID624939; AID624940
Bone morphogenetic protein receptor type-1A	Homo sapiens (human)	Kd	16.6667	0.0600	1.5010	7.0000	AID1424921; AID435276; AID624945
Activin receptor type-1B	Homo sapiens (human)	Kd	16.6667	0.0040	1.5110	15.2580	AID1424901; AID435898; AID624943
TGF-beta receptor type-1	Homo sapiens (human)	Kd	20.0000	0.0050	2.2785	9.6000	AID1425196; AID435938; AID624961
Serine/threonine-protein kinase receptor R3	Homo sapiens (human)	Kd	10.0000	0.0029	1.9936	9.5000	AID435645; AID624778
TGF-beta receptor type-2	Homo sapiens (human)	Kd	16.6667	0.0800	1.8351	6.9000	AID1425197; AID435693; AID624909
Electron transfer flavoprotein subunit beta	Homo sapiens (human)	Kd	30.0000	0.0120	0.0120	0.0120	AID1424999
Tyrosine-protein kinase CSK	Homo sapiens (human)	Kd	16.6667	0.0010	3.4578	39.5530	AID1424960; AID435904; AID624948
Glycine--tRNA ligase	Homo sapiens (human)	Kd	30.0000	0.0400	0.0400	0.0400	AID1425010
Protein kinase C iota type	Homo sapiens (human)	Kd	20.0000	0.0260	9.3316	51.0180	AID1425133; AID624883
Exosome RNA helicase MTR4	Homo sapiens (human)	Kd	30.0000	2.6070	2.6070	2.6070	AID1425168
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Homo sapiens (human)	Kd	10.0000	0.0006	0.8462	7.4000	AID435552; AID436033; AID625036; AID625037; AID625038; AID625039; AID625040; AID625041; AID625042; AID625043; AID625044; AID625045
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	Homo sapiens (human)	Kd	10.0000	0.0017	0.8316	6.7000	AID625046
Serine/threonine-protein kinase mTOR	Homo sapiens (human)	Kd	10.0000	0.0001	0.5993	9.2000	AID624972
Megakaryocyte-associated tyrosine-protein kinase	Homo sapiens (human)	Kd	10.0000	0.2600	3.0700	7.7000	AID624864
Tyrosine-protein kinase Tec	Homo sapiens (human)	Kd	16.6667	0.0010	1.0095	8.7000	AID1425193; AID435197; AID624908
Tyrosine-protein kinase TXK	Homo sapiens (human)	Kd	10.0000	0.0006	1.9196	6.0000	AID435443; AID624911
Tyrosine-protein kinase ABL2	Homo sapiens (human)	Kd	16.6667	0.0002	1.1249	14.9240	AID1424891; AID435777; AID624993
Tyrosine-protein kinase FRK	Homo sapiens (human)	Kd	16.6667	0.0003	1.2424	10.8370	AID1425007; AID436019; AID624855
G protein-coupled receptor kinase 6	Homo sapiens (human)	Kd	30.0000	1.1890	1.4020	1.6150	AID1425012
Tyrosine-protein kinase ZAP-70	Homo sapiens (human)	Kd	10.0000	0.0160	1.6844	4.2000	AID435445; AID624744
Tyrosine-protein kinase SYK	Homo sapiens (human)	Kd	16.6667	0.0070	2.0052	9.2260	AID1425188; AID435442; AID624907
26S proteasome regulatory subunit 6B	Homo sapiens (human)	Kd	30.0000	0.0050	0.0050	0.0050	AID1425141
Mitogen-activated protein kinase 8	Homo sapiens (human)	Kd	16.6667	0.0110	2.0965	26.0590	AID1425063; AID435166; AID624889
Mitogen-activated protein kinase 9	Homo sapiens (human)	Kd	16.6667	0.0020	1.4596	8.1000	AID1425064; AID435409; AID624717
Dual specificity mitogen-activated protein kinase kinase 4	Homo sapiens (human)	Kd	10.0000	0.0038	1.6264	9.9000	AID435822; AID624902
Dual specificity mitogen-activated protein kinase kinase 3	Homo sapiens (human)	Kd	16.6667	0.0050	2.0462	6.6000	AID1425040; AID436022; AID624894
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha	Homo sapiens (human)	Kd	30.0000	0.2080	3.6125	7.0170	AID1425113
Casein kinase I isoform alpha	Homo sapiens (human)	Kd	20.0000	0.0010	2.5756	19.3520	AID1424961; AID624846
Casein kinase I isoform delta	Homo sapiens (human)	Kd	16.6667	0.0150	2.2270	18.3960	AID1424962; AID435524; AID624716
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Homo sapiens (human)	Kd	10.0000	0.0026	1.4602	8.4000	AID624879
MAP kinase-activated protein kinase 2	Homo sapiens (human)	Kd	16.6667	0.0003	2.0274	14.7420	AID1425065; AID435180; AID624703
Cyclin-dependent kinase 8	Homo sapiens (human)	Kd	10.0000	0.0014	1.2908	8.0000	AID435903; AID624829
Elongation factor Tu, mitochondrial	Homo sapiens (human)	Kd	30.0000	0.4640	0.4640	0.4640	AID1425206
Choline-phosphate cytidylyltransferase A	Homo sapiens (human)	Kd	30.0000	0.0410	0.0410	0.0410	AID1425103
Cysteine--tRNA ligase, cytoplasmic	Homo sapiens (human)	Kd	30.0000	0.0120	0.3320	0.6520	AID1424932
Casein kinase I isoform epsilon	Homo sapiens (human)	Kd	16.6667	0.0130	1.4086	12.4090	AID1424963; AID435650; AID624847
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial	Homo sapiens (human)	Kd	30.0000	1.6890	1.6890	1.6890	AID1424894
Dual specificity protein kinase CLK1	Homo sapiens (human)	Kd	16.6667	0.0020	1.8791	29.8810	AID1424955; AID435786; AID624764
Dual specificity protein kinase CLK2	Homo sapiens (human)	Kd	16.6667	0.0070	1.1384	6.5000	AID1424956; AID435787; AID624932
Dual specificity protein kinase CLK3	Homo sapiens (human)	Kd	16.6667	0.0100	2.4499	9.0000	AID1424957; AID436011; AID624931
Glycogen synthase kinase-3 alpha	Homo sapiens (human)	Kd	16.6667	0.0060	2.4754	22.5430	AID1425013; AID435801; AID625114
Glycogen synthase kinase-3 beta	Homo sapiens (human)	Kd	16.6667	0.0070	1.0057	6.1680	AID1425014; AID435163; AID624856
Cyclin-dependent kinase 7	Homo sapiens (human)	Kd	16.6667	0.0025	1.6783	7.7000	AID1424949; AID435278; AID624845
Cyclin-dependent kinase 9	Homo sapiens (human)	Kd	16.6667	0.0010	1.6166	9.9010	AID1424950; AID435279; AID624830
Ras-related protein Rab-27A	Homo sapiens (human)	Kd	30.0000	4.4930	4.4930	4.4930	AID1425149
Tyrosine-protein kinase Blk	Homo sapiens (human)	Kd	10.0000	0.0002	0.8228	7.9000	AID435646; AID624841
Interleukin-1 receptor-associated kinase 1	Homo sapiens (human)	Kd	20.0000	0.0061	1.5252	8.5000	AID1425027; AID624837
Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)	Kd	16.6667	0.0170	2.8896	37.6050	AID1425160; AID435558; AID624960
Cytoplasmic tyrosine-protein kinase BMX	Homo sapiens (human)	Kd	10.0000	0.0014	1.5489	7.4000	AID435781; AID624842
cAMP-dependent protein kinase catalytic subunit PRKX	Homo sapiens (human)	Kd	10.0000	0.0072	1.3066	5.8000	AID436047; AID624976
Serine/threonine-protein kinase Nek2	Homo sapiens (human)	Kd	16.6667	0.1100	1.5649	6.5000	AID1425086; AID435665; AID624869
Serine/threonine-protein kinase Nek3	Homo sapiens (human)	Kd	20.0000	0.1700	5.9368	38.0880	AID1425087; AID624870
Serine/threonine-protein kinase Nek4	Homo sapiens (human)	Kd	10.0000	0.4600	1.5320	2.7000	AID624904
Tyrosine-protein kinase JAK3	Homo sapiens (human)	Kd	10.0000	0.0002	1.0688	8.7000	AID435674; AID624785
Dual specificity mitogen-activated protein kinase kinase 6	Homo sapiens (human)	Kd	16.6667	0.0034	2.3943	6.5000	AID1425043; AID435911; AID624895
Serine/threonine-protein kinase PLK1	Homo sapiens (human)	Kd	20.0000	0.0001	0.5711	5.0000	AID1425120; AID435934; AID624975
Death-associated protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0014	1.2542	4.7000	AID435283; AID624971
LIM domain kinase 1	Homo sapiens (human)	Kd	20.0000	0.0260	1.7840	21.0890	AID1425035; AID435803; AID624861
LIM domain kinase 2	Homo sapiens (human)	Kd	16.6667	0.0570	4.9717	52.0560	AID1425036; AID435294; AID625021
Mitogen-activated protein kinase 12	Homo sapiens (human)	Kd	10.0000	0.0001	2.2138	9.9000	AID435438; AID624766
Mitogen-activated protein kinase 10	Homo sapiens (human)	Kd	16.6667	0.0010	1.6354	5.9000	AID1425057; AID435293; AID624891
Tyrosine--tRNA ligase, cytoplasmic	Homo sapiens (human)	Kd	30.0000	3.3160	3.3160	3.3160	AID1425211
5'-AMP-activated protein kinase subunit gamma-1	Homo sapiens (human)	Kd	30.0000	0.0060	1.4681	10.2120	AID1425126
5'-AMP-activated protein kinase catalytic subunit alpha-2	Homo sapiens (human)	Kd	10.0000	0.0120	0.7798	5.0000	AID435149; AID625047
Ephrin type-B receptor 3	Homo sapiens (human)	Kd	16.6667	0.0069	2.1713	6.4100	AID1424993; AID435159; AID624955
Ephrin type-A receptor 5	Homo sapiens (human)	Kd	16.6667	0.0002	1.2100	5.9000	AID1424990; AID435158; AID624737
Ephrin type-B receptor 4	Homo sapiens (human)	Kd	16.6667	0.0003	2.1678	26.3990	AID1424994; AID435404; AID624956
Ephrin type-B receptor 1	Homo sapiens (human)	Kd	10.0000	0.0004	1.7216	7.3000	AID435403; AID624954
Ephrin type-A receptor 4	Homo sapiens (human)	Kd	16.6667	0.0012	3.1525	43.9420	AID1424989; AID435795; AID624952
Adenylate kinase 2, mitochondrial	Homo sapiens (human)	Kd	30.0000	1.0360	1.0360	1.0360	AID1424909
Adenosine kinase	Homo sapiens (human)	Kd	30.0000	0.0130	1.8368	3.4930	AID1424907
Hormonally up-regulated neu tumor-associated kinase	Homo sapiens (human)	Kd	10.0000	0.0037	2.5139	9.8000	AID625084
Serine/threonine-protein kinase SIK1	Homo sapiens (human)	Kd	10.0000	0.0022	1.1530	3.2000	AID435560; AID624733
Receptor-interacting serine/threonine-protein kinase 4	Homo sapiens (human)	Kd	10.0000	0.0130	1.5506	9.8000	AID624763
Ras-related protein Rab-10	Homo sapiens (human)	Kd	30.0000	1.3480	1.3480	1.3480	AID1425148
Cell division control protein 2 homolog	Plasmodium falciparum 3D7	Kd	10.0000	0.8000	3.2333	5.6000	AID624760
Actin-related protein 3	Homo sapiens (human)	Kd	30.0000	0.0360	2.7735	5.5110	AID1424899
Actin-related protein 2	Homo sapiens (human)	Kd	30.0000	0.0040	0.0040	0.0040	AID1424898
Calcium-dependent protein kinase 1	Plasmodium falciparum 3D7	Kd	10.0000	0.0003	0.8538	3.3000	AID624759
GTP-binding nuclear protein Ran	Homo sapiens (human)	Kd	30.0000	0.7590	0.7590	0.7590	AID1425153
Tubulin alpha-1A chain	Rattus norvegicus (Norway rat)	Kd	0.0540	0.0210	0.8982	4.9000	AID435797
Casein kinase II subunit alpha	Homo sapiens (human)	Kd	10.0000	0.0006	1.7635	7.5000	AID436012; AID624848
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta	Homo sapiens (human)	Kd	10.0000	0.0170	0.8655	7.8000	AID435828; AID624915
SRSF protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0150	0.2803	1.1000	AID435196; AID624768
Casein kinase I isoform gamma-2	Homo sapiens (human)	Kd	10.0000	0.0460	1.4506	6.6000	AID435282; AID624833
Mitogen-activated protein kinase kinase kinase 9	Homo sapiens (human)	Kd	10.0000	0.0035	2.2093	9.9000	AID435297; AID624706
Serine/threonine-protein kinase PknB	Mycobacterium tuberculosis H37Rv	Kd	10.0000	0.0032	1.2724	5.5000	AID624753
Cyclin-dependent kinase 3	Homo sapiens (human)	Kd	16.6667	0.0080	3.0602	63.6140	AID1424945; AID435277; AID624828
Cyclin-dependent kinase-like 1	Homo sapiens (human)	Kd	10.0000	0.0130	0.7332	2.1000	AID624941
Cyclin-dependent kinase 6	Homo sapiens (human)	Kd	30.0000	0.0320	1.2007	3.3560	AID1424948
Cyclin-dependent-like kinase 5	Homo sapiens (human)	Kd	16.6667	0.0430	1.3757	8.3000	AID1424947; AID436010; AID624970
Cyclin-dependent kinase 16	Homo sapiens (human)	Kd	16.6667	0.0011	1.5855	10.0000	AID1424941; AID435925; AID625033
Cyclin-dependent kinase 17	Homo sapiens (human)	Kd	16.6667	0.0010	0.8233	5.6000	AID1424942; AID435688; AID624776
ATP-dependent 6-phosphofructokinase, platelet type	Homo sapiens (human)	Kd	30.0000	0.9830	0.9830	0.9830	AID1425108
Protein kinase C epsilon type	Homo sapiens (human)	Kd	10.0000	0.0002	0.5849	8.1000	AID435320; AID625014
Dual specificity mitogen-activated protein kinase kinase 1	Homo sapiens (human)	Kd	16.6667	0.0002	1.1386	8.7730	AID1425038; AID435808; AID624893
Angiopoietin-1 receptor	Homo sapiens (human)	Kd	10.0000	0.0031	1.3464	6.7000	AID435939; AID624799
Mitogen-activated protein kinase kinase kinase 10	Homo sapiens (human)	Kd	10.0000	0.0038	2.1074	6.9000	AID435432; AID624867
DNA topoisomerase 2-beta	Homo sapiens (human)	Kd	30.0000	0.1480	1.2270	2.5970	AID1425203
Protein kinase C theta type	Homo sapiens (human)	Kd	16.6667	0.0007	1.6140	7.2000	AID1425134; AID435321; AID625051
Activin receptor type-1	Homo sapiens (human)	Kd	16.6667	0.0040	1.4853	16.1210	AID1424900; AID435274; AID624819
Macrophage-stimulating protein receptor	Homo sapiens (human)	Kd	20.0000	0.0030	2.0718	8.4000	AID1425078; AID624868
Focal adhesion kinase 1	Homo sapiens (human)	Kd	20.0000	0.0005	1.2255	13.0390	AID1425142; AID435184; AID624729
Protein kinase C delta type	Homo sapiens (human)	Kd	16.6667	0.0002	1.1261	9.2060	AID1425131; AID435553; AID625048
Tyrosine-protein kinase BTK	Homo sapiens (human)	Kd	16.6667	0.0006	1.5299	10.1530	AID1424925; AID436008; AID624779
Tyrosine-protein kinase receptor TYRO3	Homo sapiens (human)	Kd	10.0000	0.0020	2.2066	9.3000	AID435326; AID625057
Cyclin-dependent kinase 18	Homo sapiens (human)	Kd	16.6667	0.0140	1.4941	8.4000	AID1424943; AID435826; AID624874
Activated CDC42 kinase 1	Homo sapiens (human)	Kd	16.6667	0.0020	1.7138	9.6000	AID1425201; AID435694; AID624807
Epithelial discoidin domain-containing receptor 1	Homo sapiens (human)	Kd	20.0000	0.0002	1.6314	71.4840	AID1424972; AID435400; AID624850
Tyrosine-protein kinase ITK/TSK	Homo sapiens (human)	Kd	10.0000	0.0130	0.8600	5.6000	AID435292; AID625020
Myotonin-protein kinase	Homo sapiens (human)	Kd	10.0000	0.0035	2.0528	7.0000	AID435285; AID624950
Mitogen-activated protein kinase kinase kinase kinase 2	Homo sapiens (human)	Kd	20.0000	0.0031	1.4681	14.0430	AID1425052; AID624959
Mitogen-activated protein kinase kinase kinase 12	Homo sapiens (human)	Kd	10.0000	0.0220	1.0554	6.3000	AID624762
Tyrosine-protein kinase Mer	Homo sapiens (human)	Kd	10.0000	0.0003	1.7055	6.8000	AID436023; AID624767
Serine/threonine-protein kinase 4	Homo sapiens (human)	Kd	16.6667	0.0002	1.7120	25.9020	AID1425185; AID435433; AID625055
5'-AMP-activated protein kinase catalytic subunit alpha-1	Homo sapiens (human)	Kd	16.6667	0.0037	1.8913	15.3890	AID1425122; AID435148; AID624773
Serine/threonine-protein kinase PAK 1	Homo sapiens (human)	Kd	10.0000	0.0006	1.6206	4.4000	AID435318; AID624871
Dual specificity mitogen-activated protein kinase kinase 5	Homo sapiens (human)	Kd	15.5500	0.0002	2.6590	65.6770	AID1425042; AID624721
Mitogen-activated protein kinase 7	Homo sapiens (human)	Kd	16.6667	0.0420	2.0073	9.9000	AID1425062; AID435655; AID624888
Serine/threonine-protein kinase PAK 2	Homo sapiens (human)	Kd	16.6667	0.0031	2.3045	6.0000	AID1425099; AID435439; AID624872
Serine/threonine-protein kinase 3	Homo sapiens (human)	Kd	16.6667	0.0002	1.8602	17.5260	AID1425182; AID435662; AID625054
Mitogen-activated protein kinase kinase kinase 1	Homo sapiens (human)	Kd	20.0000	0.0970	2.5995	12.4730	AID1425044; AID625026
cGMP-dependent protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0031	0.8310	3.6000	AID435322; AID625053
Integrin-linked protein kinase	Homo sapiens (human)	Kd	30.0000	0.0200	0.4603	1.3290	AID1425024
Rho-associated protein kinase 1	Homo sapiens (human)	Kd	20.0000	0.0003	1.7555	13.4620	AID1425157; AID625015
Non-receptor tyrosine-protein kinase TNK1	Homo sapiens (human)	Kd	16.6667	0.0018	1.0064	11.2690	AID1425200; AID435833; AID624930
Serine/threonine-protein kinase PRP4 homolog	Homo sapiens (human)	Kd	10.0000	0.0084	1.1899	7.6000	AID624750
Receptor-interacting serine/threonine-protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0200	1.1487	5.4000	AID435557; AID624924
Calcium/calmodulin-dependent protein kinase type II subunit beta	Homo sapiens (human)	Kd	10.0000	0.0013	1.7221	6.8000	AID435394; AID624827
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Homo sapiens (human)	Kd	16.6667	0.0005	1.0209	7.8000	AID1424929; AID435784; AID624731
Calcium/calmodulin-dependent protein kinase type II subunit delta	Homo sapiens (human)	Kd	16.6667	0.0003	1.5044	20.3010	AID1424928; AID435647; AID624770
Dual specificity tyrosine-phosphorylation-regulated kinase 1A	Homo sapiens (human)	Kd	20.0000	0.0001	2.1016	40.2910	AID1424981; AID624712
Activin receptor type-2B	Homo sapiens (human)	Kd	16.6667	0.0076	2.7328	9.9000	AID1424902; AID435147; AID624820
Bone morphogenetic protein receptor type-2	Homo sapiens (human)	Kd	16.6667	0.0190	2.5917	14.3770	AID1424923; AID435780; AID624826
Protein-tyrosine kinase 6	Homo sapiens (human)	Kd	16.6667	0.0043	1.7430	9.0000	AID1425144; AID436049; AID625029
cGMP-dependent protein kinase 1	Homo sapiens (human)	Kd	16.6667	0.0016	0.7072	3.8000	AID1425138; AID435546; AID625052
Cyclin-dependent kinase 13	Homo sapiens (human)	Kd	20.0000	0.0009	1.2571	4.5180	AID1424940; AID624761
Calcium/calmodulin-dependent protein kinase type 1	Homo sapiens (human)	Kd	10.0000	0.0270	2.2925	7.0000	AID436009; AID624922
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Homo sapiens (human)	Kd	16.6667	0.0051	1.1093	8.3000	AID1425023; AID435657; AID625074
Protein-tyrosine kinase 2-beta	Homo sapiens (human)	Kd	16.6667	0.0011	1.9450	30.4140	AID1425143; AID436048; AID624732
Maternal embryonic leucine zipper kinase	Homo sapiens (human)	Kd	16.6667	0.0049	2.2835	29.9330	AID1425074; AID435660; AID625087
Structural maintenance of chromosomes protein 1A	Homo sapiens (human)	Kd	30.0000	0.3650	0.3650	0.3650	AID1425172
Chromodomain-helicase-DNA-binding protein 4	Homo sapiens (human)	Kd	30.0000	0.0030	0.0030	0.0030	AID1424952
Peroxisomal acyl-coenzyme A oxidase 1	Homo sapiens (human)	Kd	30.0000	0.0140	0.1425	0.2710	AID1424895
Cyclin-dependent kinase 10	Homo sapiens (human)	Kd	30.0000	0.0090	0.0090	0.0090	AID1424938
Serine/threonine-protein kinase D1	Homo sapiens (human)	Kd	10.0000	0.0140	1.4116	8.4000	AID436045; AID624884
Serine/threonine-protein kinase 38	Homo sapiens (human)	Kd	10.0000	0.0560	1.5651	9.4000	AID625067
Receptor tyrosine-protein kinase erbB-4	Homo sapiens (human)	Kd	0.0540	0.0009	1.2548	7.0000	AID1664203; AID624815
Ribosomal protein S6 kinase alpha-2	Homo sapiens (human)	Kd	10.0000	0.0089	2.0421	9.6000	AID435830; AID436050; AID624805; AID625127
Ephrin type-A receptor 7	Homo sapiens (human)	Kd	16.6667	0.0025	1.4445	6.5000	AID1424991; AID435286; AID624953
Delta(24)-sterol reductase	Homo sapiens (human)	Kd	30.0000	0.4320	0.4320	0.4320	AID1424978
Ribosomal protein S6 kinase alpha-1	Homo sapiens (human)	Kd	14.0000	0.0280	2.5286	22.7260	AID1425159; AID435690; AID435829; AID624900; AID624901
Dual specificity testis-specific protein kinase 1	Homo sapiens (human)	Kd	16.6667	0.0330	1.7568	5.6000	AID1425194; AID435937; AID625056
Myosin light chain kinase, smooth muscle	Homo sapiens (human)	Kd	20.0000	0.0030	1.2088	7.9000	AID1425081; AID435664; AID624709
Mitogen-activated protein kinase 11	Homo sapiens (human)	Kd	16.6667	0.0001	0.4610	3.7430	AID1425058; AID435551; AID624890
Serine/threonine-protein kinase STK11	Homo sapiens (human)	Kd	16.6667	0.0030	0.9949	5.9000	AID1425178; AID435909; AID624798
Rhodopsin kinase GRK1	Homo sapiens (human)	Kd	10.0000	0.0010	0.6864	2.2000	AID624898
NT-3 growth factor receptor	Homo sapiens (human)	Kd	10.0000	0.0034	1.2020	8.6000	AID435202; AID624765
Serine/threonine-protein kinase N1	Homo sapiens (human)	Kd	16.6667	0.0013	3.1729	49.8130	AID1425117; AID435319; AID624745
Serine/threonine-protein kinase N2	Homo sapiens (human)	Kd	16.6667	0.0018	1.7527	9.9000	AID1425118; AID435933; AID625050
Mitogen-activated protein kinase 14	Homo sapiens (human)	Kd	16.6667	0.0000	0.5036	8.5000	AID1425059; AID435181; AID624714
Calcium/calmodulin-dependent protein kinase type IV	Homo sapiens (human)	Kd	20.0000	0.0300	1.9215	5.4600	AID1424930; AID435152; AID624843
Mitogen-activated protein kinase kinase kinase 11	Homo sapiens (human)	Kd	16.6667	0.0110	1.5639	17.9840	AID1425045; AID435414; AID624866
BDNF/NT-3 growth factors receptor	Homo sapiens (human)	Kd	10.0000	0.0038	0.7875	7.2000	AID435564; AID625032
Mitogen-activated protein kinase 6	Homo sapiens (human)	Kd	10.0000	0.1700	1.9167	5.5000	AID435289; AID624887
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform	Homo sapiens (human)	Kd	10.0000	0.0004	1.5589	7.1000	AID436042; AID625035
Discoidin domain-containing receptor 2	Homo sapiens (human)	Kd	16.6667	0.0030	1.9888	42.2800	AID1424973; AID435154; AID624777
AP2-associated protein kinase 1	Homo sapiens (human)	Kd	20.0000	0.0012	1.3707	13.7110	AID1424889; AID435896; AID625089
Myosin light chain kinase 3	Homo sapiens (human)	Kd	20.0000	0.0020	1.6184	10.4240	AID1425082; AID624738
Uncharacterized aarF domain-containing protein kinase 5	Homo sapiens (human)	Kd	30.0000	0.2020	0.4990	0.7960	AID1424906
Serine/threonine-protein kinase SBK1	Homo sapiens (human)	Kd	10.0000	0.0032	0.9048	4.8000	AID624812
Mitogen-activated protein kinase kinase kinase 19	Homo sapiens (human)	Kd	10.0000	0.0005	0.8420	6.4000	AID625136
Putative heat shock protein HSP 90-beta 2	Homo sapiens (human)	Kd	30.0000	2.5660	2.5660	2.5660	AID1425019
Serine/threonine-protein kinase TNNI3K	Homo sapiens (human)	Kd	10.0000	0.0110	1.7345	7.2000	AID435200; AID625097
Rab-like protein 3	Homo sapiens (human)	Kd	30.0000	4.8300	4.8300	4.8300	AID1425151
Leucine-rich repeat serine/threonine-protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0004	1.2042	9.7000	AID624740; AID624741
Serine/threonine-protein kinase MRCK alpha	Homo sapiens (human)	Kd	16.6667	0.0570	4.5547	14.0200	AID1424933; AID436024; AID624920
Serine/threonine-protein kinase MRCK gamma	Homo sapiens (human)	Kd	16.6667	0.0370	1.9625	9.5000	AID1424935; AID436013; AID625107
Serine/threonine-protein kinase Nek5	Homo sapiens (human)	Kd	10.0000	0.0130	2.4114	7.3000	AID435534; AID624742
Serine/threonine-protein kinase N3	Homo sapiens (human)	Kd	30.0000	0.0990	0.7365	1.3740	AID1425119
Serine/threonine-protein kinase ULK3	Homo sapiens (human)	Kd	20.0000	0.0012	1.3350	9.9000	AID1425209; AID624818
Dual serine/threonine and tyrosine protein kinase	Homo sapiens (human)	Kd	10.0000	0.0053	1.7337	6.4000	AID624758
Mitogen-activated protein kinase kinase kinase 15	Homo sapiens (human)	Kd	10.0000	0.0025	0.9909	2.8000	AID624801
Uncharacterized protein FLJ45252	Homo sapiens (human)	Kd	30.0000	0.0030	1.2292	9.3110	AID1425147
Acyl-CoA dehydrogenase family member 11	Homo sapiens (human)	Kd	30.0000	1.9160	3.0730	4.1470	AID1424893
Serine/threonine-protein kinase/endoribonuclease IRE2	Homo sapiens (human)	Kd	30.0000	0.1160	0.7604	1.5000	AID1424998
Serine/threonine-protein kinase MARK2	Homo sapiens (human)	Kd	16.6667	0.0001	1.8425	11.1030	AID1425068; AID435296; AID625106
ATP-dependent RNA helicase DHX30	Homo sapiens (human)	Kd	30.0000	0.0060	0.0060	0.0060	AID1424979
Serine/threonine-protein kinase TAO1	Homo sapiens (human)	Kd	20.0000	0.0004	2.1612	18.7570	AID1425189; AID625126
STE20-related kinase adapter protein alpha	Homo sapiens (human)	Kd	30.0000	0.3160	1.7208	3.6720	AID1425186
AarF domain-containing protein kinase 1	Homo sapiens (human)	Kd	30.0000	0.0230	3.1137	22.7470	AID1424904
Serine/threonine-protein kinase tousled-like 2	Homo sapiens (human)	Kd	10.0000	0.0160	0.9012	2.6000	AID436054; AID624771
Serine/threonine-protein kinase 32C	Homo sapiens (human)	Kd	10.0000	0.0550	2.1688	8.0000	AID435834; AID624734
Serine/threonine-protein kinase pim-3	Homo sapiens (human)	Kd	10.0000	0.0005	1.3428	5.8000	AID435679; AID624802
Serine/threonine-protein kinase VRK2	Homo sapiens (human)	Kd	10.0000	0.0630	1.9933	4.0000	AID625058
Myosin light chain kinase family member 4	Homo sapiens (human)	Kd	10.0000	0.0150	0.6659	3.4000	AID435691; AID624809
Homeodomain-interacting protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0550	1.6626	6.8000	AID624726
Calcium/calmodulin-dependent protein kinase type 1D	Homo sapiens (human)	Kd	10.0000	0.0011	1.8547	5.9000	AID435393; AID625118
Mitogen-activated protein kinase kinase kinase kinase 3	Homo sapiens (human)	Kd	16.6667	0.0051	1.6413	15.4350	AID1425053; AID435295; AID624921
Cyclin-dependent kinase-like 3	Homo sapiens (human)	Kd	10.0000	0.0039	1.4549	5.1000	AID624822
MAP kinase-activated protein kinase 5	Homo sapiens (human)	Kd	16.6667	0.0080	1.1241	3.1180	AID1425067; AID435806; AID624923
Serine/threonine-protein kinase BRSK2	Homo sapiens (human)	Kd	10.0000	0.0035	1.9863	8.9000	AID435783; AID624929
Serine/threonine-protein kinase NIM1	Homo sapiens (human)	Kd	10.0000	0.1400	2.6188	8.7000	AID624728
Eukaryotic peptide chain release factor GTP-binding subunit ERF3B	Homo sapiens (human)	Kd	30.0000	0.0030	0.0030	0.0030	AID1425015
Serine/threonine-protein kinase ULK2	Homo sapiens (human)	Kd	10.0000	0.0008	1.0884	9.9000	AID625085
Misshapen-like kinase 1	Homo sapiens (human)	Kd	10.0000	0.0010	1.1425	8.9000	AID624813
Serine/threonine-protein kinase DCLK2	Homo sapiens (human)	Kd	10.0000	0.0160	1.6907	4.5000	AID435651; AID624814
Calcium/calmodulin-dependent protein kinase kinase 1	Homo sapiens (human)	Kd	10.0000	0.0000	1.1411	5.1000	AID435521; AID625143
Casein kinase I isoform alpha-like	Homo sapiens (human)	Kd	10.0000	0.2500	2.2056	7.1000	AID435281; AID624723
Homeodomain-interacting protein kinase 4	Homo sapiens (human)	Kd	10.0000	0.0005	1.3339	8.1000	AID624720
Myosin-IIIa	Homo sapiens (human)	Kd	10.0000	0.0410	1.6626	6.3000	AID435170; AID625104
Ankyrin repeat and protein kinase domain-containing protein 1	Homo sapiens (human)	Kd	10.0000	0.0320	1.6534	9.4000	AID436005; AID624735
Serine/threonine-protein kinase Nek11	Homo sapiens (human)	Kd	10.0000	0.1700	1.2350	3.1000	AID624725
Atypical kinase COQ8A, mitochondrial	Homo sapiens (human)	Kd	16.6667	0.0940	5.1673	65.3020	AID1424905; AID435516; AID625116
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Homo sapiens (human)	Kd	20.0000	0.0030	2.7522	8.8000	AID1425115; AID625134
Mitogen-activated protein kinase 15	Homo sapiens (human)	Kd	16.6667	0.0049	0.6880	4.5000	AID1425060; AID435405; AID624715
Serine/threonine-protein kinase Nek9	Homo sapiens (human)	Kd	16.6667	0.0160	2.7428	19.6170	AID1425089; AID435171; AID624704
Serine/threonine-protein kinase BRSK1	Homo sapiens (human)	Kd	10.0000	0.0140	2.3924	8.4000	AID435782; AID624702
Serine/threonine-protein kinase 35	Homo sapiens (human)	Kd	10.0000	0.0020	0.9706	5.4000	AID624711
Serine/threonine-protein kinase Nek7	Homo sapiens (human)	Kd	10.0000	0.0030	3.6719	8.7000	AID435666; AID624754
Rhodopsin kinase GRK7	Homo sapiens (human)	Kd	10.0000	0.0009	1.2793	7.5000	AID624719
Serine/threonine-protein kinase 32A	Homo sapiens (human)	Kd	10.0000	0.0130	2.2043	5.5000	AID624821
Myosin-IIIb	Homo sapiens (human)	Kd	10.0000	0.0810	2.4155	7.1000	AID436032; AID624817
ATP-dependent RNA helicase DDX1	Homo sapiens (human)	Kd	30.0000	0.0860	0.0860	0.0860	AID1424974
Dual specificity tyrosine-phosphorylation-regulated kinase 2	Homo sapiens (human)	Kd	10.0000	0.0220	2.3693	7.6000	AID624918
Cyclin-dependent kinase-like 2	Homo sapiens (human)	Kd	10.0000	0.0005	1.3519	5.9000	AID624928
Mitogen-activated protein kinase kinase kinase kinase 1	Homo sapiens (human)	Kd	16.6667	0.0010	0.9378	5.5000	AID1425051; AID435431; AID624816
Serine/threonine-protein kinase Sgk3	Homo sapiens (human)	Kd	10.0000	0.0034	1.3561	7.2000	AID625073
Atypical kinase COQ8B, mitochondrial	Homo sapiens (human)	Kd	10.0000	0.0270	2.3213	6.1000	AID435778; AID625135
Aurora kinase B	Homo sapiens (human)	Kd	16.6667	0.0020	1.0614	22.8520	AID1424918; AID435519; AID624772
MAP/microtubule affinity-regulating kinase 4	Homo sapiens (human)	Kd	10.0000	0.0054	1.1029	4.9000	AID435924; AID625140
Calcium/calmodulin-dependent protein kinase type 1G	Homo sapiens (human)	Kd	10.0000	0.0010	1.9148	6.8000	AID435151; AID625119
Serine/threonine-protein kinase Nek1	Homo sapiens (human)	Kd	16.6667	0.1700	2.4294	8.3000	AID1425085; AID435533; AID625068
Cyclin-dependent kinase 15	Homo sapiens (human)	Kd	10.0000	0.0320	1.8886	8.6000	AID624718
PAS domain-containing serine/threonine-protein kinase	Homo sapiens (human)	Kd	30.0000	1.0670	1.0670	1.0670	AID1425102
Calcium/calmodulin-dependent protein kinase kinase 2	Homo sapiens (human)	Kd	20.0000	0.0000	3.2331	52.8470	AID1424931; AID435648; AID625060
EKC/KEOPS complex subunit TP53RK	Homo sapiens (human)	Kd	30.0000	0.3110	1.9519	3.8400	AID1425204
SRSF protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0055	1.0891	5.2000	AID435936; AID624903
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase	Homo sapiens (human)	Kd	16.6667	0.0440	0.9285	2.9000	AID1425116; AID436043; AID624757
Mitogen-activated protein kinase kinase kinase 5	Homo sapiens (human)	Kd	16.6667	0.0700	6.5647	50.5360	AID1425049; AID435412; AID625028
Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha	Homo sapiens (human)	Kd	10.0000	0.0360	1.8381	9.7000	AID435190; AID624824
Mitogen-activated protein kinase kinase kinase 3	Homo sapiens (human)	Kd	20.0000	0.0060	1.5331	9.9000	AID1425047; AID624865
Eukaryotic translation initiation factor 2-alpha kinase 1	Homo sapiens (human)	Kd	20.0000	0.0580	1.9224	4.8360	AID1424984; AID625080
Serine/threonine-protein kinase RIO1	Homo sapiens (human)	Kd	10.0000	0.0090	1.3195	8.4000	AID435324; AID625141
MAP kinase-interacting serine/threonine-protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0260	1.9734	7.3000	AID435661; AID624823
Serine/threonine-protein kinase RIO2	Homo sapiens (human)	Kd	10.0000	0.0490	1.7667	9.1000	AID625111
Cyclin-dependent kinase 19	Homo sapiens (human)	Kd	10.0000	0.0015	1.9204	7.2000	AID435522; AID625094
Transient receptor potential cation channel subfamily M member 6	Homo sapiens (human)	Kd	10.0000	0.0079	0.0079	0.0079	AID625110
Testis-specific serine/threonine-protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0240	2.8577	6.3000	AID435940; AID625142
Serine/threonine-protein kinase 33	Homo sapiens (human)	Kd	10.0000	0.0018	1.3542	4.9000	AID436053; AID625138
Nucleolar GTP-binding protein 1	Homo sapiens (human)	Kd	30.0000	0.0090	4.1035	8.1980	AID1425016
Serine/threonine-protein kinase D2	Homo sapiens (human)	Kd	16.6667	0.0081	2.3723	25.0190	AID1425136; AID436046; AID625102
Serine/threonine-protein kinase DCLK3	Homo sapiens (human)	Kd	10.0000	0.0045	1.4011	6.5000	AID435399; AID624707
NUAK family SNF1-like kinase 2	Homo sapiens (human)	Kd	16.6667	0.0001	0.6774	4.6000	AID1425095; AID435559; AID625139
RNA cytidine acetyltransferase	Homo sapiens (human)	Kd	30.0000	1.2400	1.2400	1.2400	AID1425083
Serine/threonine-protein kinase SIK2	Homo sapiens (human)	Kd	16.6667	0.0011	1.8165	41.7950	AID1425166; AID436052; AID625095
Myosin light chain kinase 2, skeletal/cardiac muscle	Homo sapiens (human)	Kd	10.0000	0.0430	1.1312	5.4000	AID435415; AID624705
STE20-like serine/threonine-protein kinase	Homo sapiens (human)	Kd	13.1500	0.0000	3.8573	99.2320	AID1425171; AID256578; AID435832; AID625086
Serine/threonine-protein kinase TAO3	Homo sapiens (human)	Kd	20.0000	0.0002	2.7131	14.1960	AID1425191; AID625101
Homeodomain-interacting protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0073	1.3739	5.0000	AID625129
Tyrosine-protein kinase Srms	Homo sapiens (human)	Kd	10.0000	0.0130	2.6007	9.8000	AID435561; AID624710
Homeodomain-interacting protein kinase 3	Homo sapiens (human)	Kd	10.0000	0.0040	1.7046	9.7000	AID625023
Serine/threonine-protein kinase PLK3	Homo sapiens (human)	Kd	10.0000	0.0040	2.9056	8.5000	AID435183; AID624933
dCTP pyrophosphatase 1	Homo sapiens (human)	Kd	30.0000	0.5730	1.7403	3.0540	AID1424971
Dual specificity protein kinase CLK4	Homo sapiens (human)	Kd	16.6667	0.0020	1.4122	8.3000	AID1424958; AID435788; AID625125
MAP kinase-interacting serine/threonine-protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0014	1.4131	5.7000	AID435531; AID625108
Serine/threonine-protein kinase Nek6	Homo sapiens (human)	Kd	10.0000	0.0063	1.3385	4.4000	AID435545; AID625079
Casein kinase I isoform gamma-1	Homo sapiens (human)	Kd	16.6667	0.0530	2.0622	5.7000	AID1424964; AID435397; AID625128
Serine/threonine-protein kinase PAK 6	Homo sapiens (human)	Kd	10.0000	0.0004	1.9194	9.7000	AID435188; AID625115
SNF-related serine/threonine-protein kinase	Homo sapiens (human)	Kd	10.0000	0.0900	0.5520	1.5000	AID624752
Serine/threonine-protein kinase LATS2	Homo sapiens (human)	Kd	10.0000	0.0010	1.6879	8.0000	AID436021; AID625083
Serine/threonine-protein kinase 36	Homo sapiens (human)	Kd	10.0000	0.1800	2.7651	8.3000	AID435562; AID625096
Phenylalanine--tRNA ligase beta subunit	Homo sapiens (human)	Kd	30.0000	0.0030	0.0045	0.0060	AID1425000
Isoleucine--tRNA ligase, mitochondrial	Homo sapiens (human)	Kd	30.0000	0.0110	0.0110	0.0110	AID1425020
BMP-2-inducible protein kinase	Homo sapiens (human)	Kd	16.6667	0.0022	2.4097	56.0320	AID1424920; AID435275; AID625109
Obg-like ATPase 1	Homo sapiens (human)	Kd	30.0000	0.0030	0.0050	0.0070	AID1425096
Interleukin-1 receptor-associated kinase 4	Homo sapiens (human)	Kd	20.0000	0.0017	3.4719	34.1450	AID1425029; AID625098
Serine/threonine-protein kinase 32B	Homo sapiens (human)	Kd	10.0000	0.0240	2.7040	6.4000	AID436055; AID625112
Mitogen-activated protein kinase kinase kinase 20	Homo sapiens (human)	Kd	20.0000	0.0023	1.7034	13.6380	AID1425213; AID435941; AID624755
Cyclin-dependent kinase 12	Homo sapiens (human)	Kd	30.0000	0.0320	1.8032	5.6350	AID1424939
Serine/threonine-protein kinase PLK2	Homo sapiens (human)	Kd	10.0000	0.0008	1.8083	8.3000	AID625063
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13	Homo sapiens (human)	Kd	30.0000	3.9200	3.9200	3.9200	AID1425084
Serine/threonine-protein kinase MARK1	Homo sapiens (human)	Kd	10.0000	0.0040	1.2615	4.9000	AID435807; AID625113
Serine/threonine-protein kinase pim-2	Homo sapiens (human)	Kd	16.6667	0.0019	0.8415	5.0000	AID1425112; AID435440; AID625064
Serine/threonine-protein kinase PAK 5	Homo sapiens (human)	Kd	10.0000	0.0012	0.8801	3.3000	AID435687; AID625117
Serine/threonine-protein kinase 26	Homo sapiens (human)	Kd	16.6667	0.0074	1.7380	8.3000	AID1425181; AID435663; AID625103
eIF-2-alpha kinase GCN2	Homo sapiens (human)	Kd	10.0000	0.0033	1.1828	4.4000	AID436020; AID624810
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial	Homo sapiens (human)	Kd	30.0000	0.0070	0.0070	0.0070	AID1425187
Serine/threonine-protein kinase NLK	Homo sapiens (human)	Kd	16.6667	0.0060	1.0226	4.4000	AID1425090; AID435667; AID625100
Phosphatidylinositol 4-kinase beta	Homo sapiens (human)	Kd	0.9400	0.0390	1.1982	3.5000	AID624880
Serine/threonine-protein kinase 17A	Homo sapiens (human)	Kd	10.0000	0.0010	1.7218	9.0000	AID435790; AID624968
STE20/SPS1-related proline-alanine-rich protein kinase	Homo sapiens (human)	Kd	10.0000	0.1300	0.9879	3.7000	AID625071
Ephrin type-A receptor 6	Homo sapiens (human)	Kd	10.0000	0.0011	1.0255	9.1000	AID436015; AID624748
5'-AMP-activated protein kinase subunit gamma-2	Homo sapiens (human)	Kd	30.0000	0.0050	1.1581	9.1280	AID1425127
Serine/threonine-protein kinase TBK1	Homo sapiens (human)	Kd	20.0000	0.0009	1.7674	49.6010	AID1425192; AID625072
Septin-9	Homo sapiens (human)	Kd	30.0000	0.0100	0.2430	0.6350	AID1425165
Death-associated protein kinase 2	Homo sapiens (human)	Kd	10.0000	0.0016	1.1261	9.1000	AID435153; AID625077
Ribosomal protein S6 kinase alpha-6	Homo sapiens (human)	Kd	14.0000	0.0040	2.4153	23.7620	AID1425163; AID435193; AID435194; AID625081; AID625082
TRAF2 and NCK-interacting protein kinase	Homo sapiens (human)	Kd	16.6667	0.0047	1.3935	10.0000	AID1425199; AID435563; AID625093
Serine/threonine-protein kinase tousled-like 1	Homo sapiens (human)	Kd	10.0000	0.0270	1.0513	4.0000	AID435199; AID625069
Serine/threonine-protein kinase TAO2	Homo sapiens (human)	Kd	23.3333	0.0100	2.0176	12.9420	AID1425190; AID625099
Long-chain-fatty-acid--CoA ligase 5	Homo sapiens (human)	Kd	30.0000	0.0080	0.6353	1.6900	AID1424897
ALK tyrosine kinase receptor	Homo sapiens (human)	Kd	10.0000	0.0005	1.3507	7.7000	AID435779; AID624944
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	EC50 (µMol)	3.2000	0.0054	0.4220	3.2000	AID1904124
SRSF protein kinase 3	Homo sapiens (human)	Kd	10.0000	0.0120	2.1154	9.3000	AID625078
Serine/threonine-protein kinase ICK	Homo sapiens (human)	Kd	10.0000	0.0007	1.4717	9.3000	AID625090
Cyclin-dependent kinase 11A	Homo sapiens (human)	Kd	10.0000	0.0052	0.6617	1.3000	AID435649; AID625133
Aurora kinase C	Homo sapiens (human)	Kd	10.0000	0.0013	1.0848	8.7000	AID436006; AID624769
Calcium/calmodulin-dependent protein kinase type II subunit alpha	Homo sapiens (human)	Kd	10.0000	0.0001	1.6996	9.6000	AID435520; AID624730
RAC-gamma serine/threonine-protein kinase	Homo sapiens (human)	Kd	16.6667	0.0025	1.7646	6.2000	AID1424912; AID435900; AID625019
Serine/threonine-protein kinase 38-like	Homo sapiens (human)	Kd	10.0000	0.0280	1.4692	6.9000	AID436025; AID625092
Microtubule-associated serine/threonine-protein kinase 1	Homo sapiens (human)	Kd	10.0000	0.0190	1.5420	6.2000	AID625091
Serine/threonine-protein kinase SIK3	Homo sapiens (human)	Kd	20.0000	0.0005	1.5086	10.3180	AID1425167; AID624774
Mitogen-activated protein kinase kinase kinase 2	Homo sapiens (human)	Kd	20.0000	0.0024	1.3298	6.9000	AID1425046; AID625062
Thyroid hormone receptor-associated protein 3	Homo sapiens (human)	Kd	30.0000	2.7460	2.7460	2.7460	AID1425198
Dual specificity tyrosine-phosphorylation-regulated kinase 1B	Homo sapiens (human)	Kd	10.0000	0.0280	1.8129	9.5000	AID436014; AID624964
Mitogen-activated protein kinase kinase kinase kinase 5	Homo sapiens (human)	Kd	16.6667	0.0005	1.9494	50.2140	AID1425055; AID435805; AID625061
Receptor-interacting serine/threonine-protein kinase 3	Homo sapiens (human)	Kd	30.0000	0.0110	1.4797	6.7000	AID1425156
Serine/threonine-protein kinase MRCK beta	Homo sapiens (human)	Kd	16.6667	0.0340	3.6252	50.0050	AID1424934; AID435912; AID625031
Interleukin-1 receptor-associated kinase 3	Homo sapiens (human)	Kd	16.6667	0.0070	1.7137	25.5810	AID1425028; AID435528; AID625066
Serine/threonine-protein kinase 24	Homo sapiens (human)	Kd	16.6667	0.0065	0.8920	4.0840	AID1425180; AID435532; AID624917
Casein kinase I isoform gamma-3	Homo sapiens (human)	Kd	16.6667	0.0970	2.3978	8.7000	AID1424966; AID435905; AID624949
Mitogen-activated protein kinase kinase kinase 4	Homo sapiens (human)	Kd	16.6667	0.0390	2.3970	8.4000	AID1425048; AID435530; AID625027
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
dual specificity tyrosine-phosphorylation-regulated kinase 1A	Rattus norvegicus (Norway rat)	AC50	120.0000	0.0056	4.6932	26.6940	AID588449
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
positive regulation of gene expression	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
cartilage condensation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
ovarian cumulus expansion	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
osteoblast differentiation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
eye development	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
chondrocyte development	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
inflammatory response	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
central nervous system neuron differentiation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
proteoglycan biosynthetic process	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
positive regulation of bone mineralization	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
BMP signaling pathway	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
retinal ganglion cell axon guidance	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
positive regulation of chondrocyte differentiation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
ovulation cycle	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
positive regulation of osteoblast differentiation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
retina development in camera-type eye	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
endochondral bone morphogenesis	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
positive regulation of cartilage development	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
cellular response to BMP stimulus	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathway via death domain receptors	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
negative regulation of chondrocyte proliferation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
dorsal/ventral pattern formation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
protein phosphorylation	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
cellular response to growth factor stimulus	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
heme biosynthetic process	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
positive regulation of lipoprotein transport	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
G1/S transition of mitotic cell cycle	Cell division cycle 7-related protein kinase	Homo sapiens (human)
positive regulation of cell population proliferation	Cell division cycle 7-related protein kinase	Homo sapiens (human)
positive regulation of nuclear cell cycle DNA replication	Cell division cycle 7-related protein kinase	Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycle	Cell division cycle 7-related protein kinase	Homo sapiens (human)
cell cycle phase transition	Cell division cycle 7-related protein kinase	Homo sapiens (human)
cell division	Cell division cycle 7-related protein kinase	Homo sapiens (human)
peptidyl-serine phosphorylation	Cell division cycle 7-related protein kinase	Homo sapiens (human)
double-strand break repair via break-induced replication	Cell division cycle 7-related protein kinase	Homo sapiens (human)
signal transduction	Cell division cycle 7-related protein kinase	Homo sapiens (human)
phosphorylation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
natural killer cell differentiation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of cytokine production	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of endothelial cell proliferation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
adaptive immune response	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
mast cell chemotaxis	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
respiratory burst involved in defense response	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
protein phosphorylation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
inflammatory response	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
immune response	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
signal transduction	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of endothelial cell migration	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of gene expression	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
T cell chemotaxis	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
natural killer cell activation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
B cell differentiation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
T cell differentiation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of cell migration	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
neutrophil chemotaxis	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of neutrophil apoptotic process	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
natural killer cell chemotaxis	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
B cell chemotaxis	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
vascular endothelial growth factor signaling pathway	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
T cell activation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
B cell activation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
mast cell degranulation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
innate immune response	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of angiogenesis	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
T cell receptor signaling pathway	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
B cell receptor signaling pathway	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
mast cell differentiation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
neutrophil extravasation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of epithelial tube formation	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
cell migration	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic process	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
phosphatidylinositol-mediated signaling	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
positive regulation of centriole replication	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
centriole replication	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
positive regulation of centriole replication	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
cilium assembly	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
trophoblast giant cell differentiation	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
de novo centriole assembly involved in multi-ciliated epithelial cell differentiation	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase 25	Homo sapiens (human)
response to oxidative stress	Serine/threonine-protein kinase 25	Homo sapiens (human)
establishment or maintenance of cell polarity	Serine/threonine-protein kinase 25	Homo sapiens (human)
signal transduction	Serine/threonine-protein kinase 25	Homo sapiens (human)
axonogenesis	Serine/threonine-protein kinase 25	Homo sapiens (human)
positive regulation of stress-activated MAPK cascade	Serine/threonine-protein kinase 25	Homo sapiens (human)
cellular response to oxidative stress	Serine/threonine-protein kinase 25	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hydrogen peroxide	Serine/threonine-protein kinase 25	Homo sapiens (human)
protein autophosphorylation	Serine/threonine-protein kinase 25	Homo sapiens (human)
positive regulation of axonogenesis	Serine/threonine-protein kinase 25	Homo sapiens (human)
Golgi localization	Serine/threonine-protein kinase 25	Homo sapiens (human)
establishment of Golgi localization	Serine/threonine-protein kinase 25	Homo sapiens (human)
Golgi reassembly	Serine/threonine-protein kinase 25	Homo sapiens (human)
translational initiation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
chromosome segregation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptors	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
response to virus	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
RNA secondary structure unwinding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of gene expression	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
Wnt signaling pathway	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of translation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of cell growth	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of cell growth	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of protein-containing complex assembly	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of protein autophosphorylation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of type I interferon production	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
DNA duplex unwinding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of interferon-alpha production	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of interferon-beta production	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
stress granule assembly	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of toll-like receptor 7 signaling pathway	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of toll-like receptor 8 signaling pathway	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
intracellular signal transduction	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of translation in response to endoplasmic reticulum stress	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cytosolic ribosome assembly	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of apoptotic process	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of apoptotic process	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of viral genome replication	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
innate immune response	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of translation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of translational initiation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
lipid homeostasis	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cellular response to arsenic-containing substance	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cellular response to osmotic stress	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of chemokine (C-C motif) ligand 5 production	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of protein serine/threonine kinase activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of canonical Wnt signaling pathway	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
intrinsic apoptotic signaling pathway	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cellular response to virus	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycle	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assembly	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of non-canonical NF-kappaB signal transduction	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transduction	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of protein acetylation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptors	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
positive regulation of protein K63-linked ubiquitination	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
protein localization to cytoplasmic stress granule	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
negative regulation of gene expression	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
gamete generation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cell differentiation	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
biological_process	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
cellular response to starvation	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
autophagosome organization	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
cell migration	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
phosphatidylinositol-mediated signaling	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic process	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
pyridoxal 5'-phosphate salvage	Pyridoxal kinase	Homo sapiens (human)
pyridoxal metabolic process	Pyridoxal kinase	Homo sapiens (human)
pyridoxamine metabolic process	Pyridoxal kinase	Homo sapiens (human)
mitotic cell cycle	Citron Rho-interacting kinase	Homo sapiens (human)
mitotic cytokinesis	Citron Rho-interacting kinase	Homo sapiens (human)
positive regulation of cytokinesis	Citron Rho-interacting kinase	Homo sapiens (human)
negative regulation of hippo signaling	Citron Rho-interacting kinase	Homo sapiens (human)
generation of neurons	Citron Rho-interacting kinase	Homo sapiens (human)
neuron apoptotic process	Citron Rho-interacting kinase	Homo sapiens (human)
chromosome segregation	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
maturation of SSU-rRNA	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
negative regulation of protein-containing complex assembly	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
positive regulation of interferon-beta production	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
negative regulation of MDA-5 signaling pathway	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transduction	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
innate immune response	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
positive regulation of innate immune response	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
defense response to virus	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
cellular response to dsRNA	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
cellular response to virus	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
cellular response to dsDNA	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
apoptotic process	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
response to osmotic stress	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
signal transduction	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
JNK cascade	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
response to heat	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
response to UV	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
response to wounding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of telomere maintenance via telomerase	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
response to tumor necrosis factor	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
Fc-epsilon receptor signaling pathway	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of JUN kinase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of DNA-templated transcription	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of JNK cascade	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
stress-activated MAPK cascade	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of telomerase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
cellular response to lipopolysaccharide	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
cellular response to interleukin-1	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
cellular senescence	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
positive regulation of telomere capping	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
regulation of motor neuron apoptotic process	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
DNA damage checkpoint signaling	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
G2/M transition of mitotic cell cycle	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
inner cell mass cell proliferation	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
DNA replication	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
DNA repair	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
chromatin remodeling	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
apoptotic process	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
DNA damage response	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
nucleus organization	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
mitotic G2 DNA damage checkpoint signaling	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
regulation of double-strand break repair via homologous recombination	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
peptidyl-threonine phosphorylation	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
regulation of cell population proliferation	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
signal transduction in response to DNA damage	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
mitotic G2/M transition checkpoint	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
positive regulation of cell cycle	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
negative regulation of gene expression, epigenetic	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
negative regulation of mitotic nuclear division	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
regulation of mitotic centrosome separation	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
negative regulation of G0 to G1 transition	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
cellular response to mechanical stimulus	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
cellular response to caffeine	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
replicative senescence	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
regulation of signal transduction by p53 class mediator	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
apoptotic process involved in development	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
negative regulation of DNA biosynthetic process	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
stimulatory C-type lectin receptor signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependent	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
MyD88-dependent toll-like receptor signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein phosphorylation	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
inflammatory response	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
canonical NF-kappaB signal transduction	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
response to virus	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
regulation of tumor necrosis factor-mediated signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
peptidyl-serine phosphorylation	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
cortical actin cytoskeleton organization	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
toll-like receptor 3 signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
negative regulation of myosin-light-chain-phosphatase activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
TRIF-dependent toll-like receptor signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
Fc-epsilon receptor signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
regulation of phosphorylation	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
innate immune response	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
positive regulation of DNA-templated transcription	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
T cell receptor signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
stress-activated MAPK cascade	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein maturation	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
interleukin-1-mediated signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
cellular response to tumor necrosis factor	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein localization to plasma membrane	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
regulation of establishment of endothelial barrier	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
negative regulation of bicellular tight junction assembly	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
regulation of toll-like receptor signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
negative regulation of cell-matrix adhesion	Peripheral plasma membrane protein CASK	Homo sapiens (human)
cell adhesion	Peripheral plasma membrane protein CASK	Homo sapiens (human)
negative regulation of keratinocyte proliferation	Peripheral plasma membrane protein CASK	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Peripheral plasma membrane protein CASK	Homo sapiens (human)
GMP metabolic process	Peripheral plasma membrane protein CASK	Homo sapiens (human)
GDP metabolic process	Peripheral plasma membrane protein CASK	Homo sapiens (human)
establishment of localization in cell	Peripheral plasma membrane protein CASK	Homo sapiens (human)
negative regulation of wound healing	Peripheral plasma membrane protein CASK	Homo sapiens (human)
calcium ion import	Peripheral plasma membrane protein CASK	Homo sapiens (human)
positive regulation of calcium ion import	Peripheral plasma membrane protein CASK	Homo sapiens (human)
negative regulation of cellular response to growth factor stimulus	Peripheral plasma membrane protein CASK	Homo sapiens (human)
regulation of synaptic vesicle exocytosis	Peripheral plasma membrane protein CASK	Homo sapiens (human)
protein localization	Peripheral plasma membrane protein CASK	Homo sapiens (human)
regulation of neurotransmitter secretion	Peripheral plasma membrane protein CASK	Homo sapiens (human)
protein phosphorylation	Aurora kinase A	Homo sapiens (human)
response to wounding	Aurora kinase A	Homo sapiens (human)
liver regeneration	Aurora kinase A	Homo sapiens (human)
G2/M transition of mitotic cell cycle	Aurora kinase A	Homo sapiens (human)
mitotic cell cycle	Aurora kinase A	Homo sapiens (human)
chromatin remodeling	Aurora kinase A	Homo sapiens (human)
protein phosphorylation	Aurora kinase A	Homo sapiens (human)
apoptotic process	Aurora kinase A	Homo sapiens (human)
spindle organization	Aurora kinase A	Homo sapiens (human)
spindle assembly involved in female meiosis I	Aurora kinase A	Homo sapiens (human)
mitotic centrosome separation	Aurora kinase A	Homo sapiens (human)
anterior/posterior axis specification	Aurora kinase A	Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycle	Aurora kinase A	Homo sapiens (human)
negative regulation of gene expression	Aurora kinase A	Homo sapiens (human)
peptidyl-serine phosphorylation	Aurora kinase A	Homo sapiens (human)
regulation of protein stability	Aurora kinase A	Homo sapiens (human)
negative regulation of protein binding	Aurora kinase A	Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic process	Aurora kinase A	Homo sapiens (human)
negative regulation of apoptotic process	Aurora kinase A	Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic process	Aurora kinase A	Homo sapiens (human)
positive regulation of mitotic nuclear division	Aurora kinase A	Homo sapiens (human)
positive regulation of mitotic cell cycle	Aurora kinase A	Homo sapiens (human)
regulation of centrosome cycle	Aurora kinase A	Homo sapiens (human)
protein autophosphorylation	Aurora kinase A	Homo sapiens (human)
cell division	Aurora kinase A	Homo sapiens (human)
centrosome localization	Aurora kinase A	Homo sapiens (human)
cilium disassembly	Aurora kinase A	Homo sapiens (human)
protein localization to centrosome	Aurora kinase A	Homo sapiens (human)
positive regulation of mitochondrial fission	Aurora kinase A	Homo sapiens (human)
positive regulation of oocyte maturation	Aurora kinase A	Homo sapiens (human)
regulation of signal transduction by p53 class mediator	Aurora kinase A	Homo sapiens (human)
neuron projection extension	Aurora kinase A	Homo sapiens (human)
mitotic spindle organization	Aurora kinase A	Homo sapiens (human)
regulation of cytokinesis	Aurora kinase A	Homo sapiens (human)
receptor-mediated endocytosis	Cyclin-G-associated kinase	Homo sapiens (human)
endoplasmic reticulum organization	Cyclin-G-associated kinase	Homo sapiens (human)
Golgi organization	Cyclin-G-associated kinase	Homo sapiens (human)
negative regulation of neuron projection development	Cyclin-G-associated kinase	Homo sapiens (human)
synaptic vesicle uncoating	Cyclin-G-associated kinase	Homo sapiens (human)
protein localization to Golgi apparatus	Cyclin-G-associated kinase	Homo sapiens (human)
intracellular transport	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin coat assembly	Cyclin-G-associated kinase	Homo sapiens (human)
chaperone cofactor-dependent protein refolding	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin coat disassembly	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin-dependent endocytosis	Cyclin-G-associated kinase	Homo sapiens (human)
protein localization to plasma membrane	Cyclin-G-associated kinase	Homo sapiens (human)
Golgi to lysosome transport	Cyclin-G-associated kinase	Homo sapiens (human)
regulation of clathrin coat assembly	Cyclin-G-associated kinase	Homo sapiens (human)
neuron migration	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
protein phosphorylation	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
nervous system development	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
central nervous system development	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
response to virus	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
endosomal transport	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
central nervous system projection neuron axonogenesis	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
forebrain development	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
protein localization to nucleus	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
intracellular signal transduction	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
axon extension	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
dendrite morphogenesis	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
negative regulation of protein localization to nucleus	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
neuron projection morphogenesis	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
skeletal muscle contraction	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein phosphorylation	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
inflammatory response	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
immune response	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
canonical NF-kappaB signal transduction	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
I-kappaB phosphorylation	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
Rho protein signal transduction	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to xenobiotic stimulus	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to virus	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to toxic substance	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
anatomical structure morphogenesis	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to acetate	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to lipopolysaccharide	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
positive regulation of interferon-alpha production	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to hydroperoxide	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
toll-like receptor 4 signaling pathway	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cellular response to reactive oxygen species	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
non-canonical NF-kappaB signal transduction	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to amino acid	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
innate immune response	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
positive regulation of DNA-templated transcription	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
striated muscle cell differentiation	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
response to cholecystokinin	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cellular response to cadmium ion	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cellular response to tumor necrosis factor	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cellular response to virus	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
peptidyl-serine phosphorylation	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
positive regulation of protein phosphorylation	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
neuromuscular junction development	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
memory	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
regulation of synaptic assembly at neuromuscular junction	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
positive regulation of gene expression	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
cell differentiation	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
protein autophosphorylation	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
skeletal muscle acetylcholine-gated channel clustering	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
positive regulation of protein geranylgeranylation	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
multicellular organism development	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
positive regulation of kinase activity	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
positive regulation of neuron projection development	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
protein phosphorylation	Ephrin type-B receptor 6	Homo sapiens (human)
ephrin receptor signaling pathway	Ephrin type-B receptor 6	Homo sapiens (human)
axon guidance	Ephrin type-B receptor 6	Homo sapiens (human)
fatty acid beta-oxidation using acyl-CoA oxidase	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
lipid homeostasis	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
response to osmotic stress	Mitogen-activated protein kinase 13	Homo sapiens (human)
peptidyl-serine phosphorylation	Mitogen-activated protein kinase 13	Homo sapiens (human)
positive regulation of interleukin-6 production	Mitogen-activated protein kinase 13	Homo sapiens (human)
cellular response to UV	Mitogen-activated protein kinase 13	Homo sapiens (human)
positive regulation of inflammatory response	Mitogen-activated protein kinase 13	Homo sapiens (human)
stress-activated MAPK cascade	Mitogen-activated protein kinase 13	Homo sapiens (human)
cellular response to hydrogen peroxide	Mitogen-activated protein kinase 13	Homo sapiens (human)
cellular response to interleukin-1	Mitogen-activated protein kinase 13	Homo sapiens (human)
cellular response to sorbitol	Mitogen-activated protein kinase 13	Homo sapiens (human)
cellular response to anisomycin	Mitogen-activated protein kinase 13	Homo sapiens (human)
cellular response to sodium arsenite	Mitogen-activated protein kinase 13	Homo sapiens (human)
intracellular signal transduction	Mitogen-activated protein kinase 13	Homo sapiens (human)
negative regulation of myotube differentiation	Histone deacetylase 3	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Histone deacetylase 3	Homo sapiens (human)
establishment of mitotic spindle orientation	Histone deacetylase 3	Homo sapiens (human)
in utero embryonic development	Histone deacetylase 3	Homo sapiens (human)
positive regulation of protein phosphorylation	Histone deacetylase 3	Homo sapiens (human)
chromatin organization	Histone deacetylase 3	Homo sapiens (human)
transcription by RNA polymerase II	Histone deacetylase 3	Homo sapiens (human)
protein deacetylation	Histone deacetylase 3	Homo sapiens (human)
regulation of mitotic cell cycle	Histone deacetylase 3	Homo sapiens (human)
positive regulation of protein ubiquitination	Histone deacetylase 3	Homo sapiens (human)
regulation of protein stability	Histone deacetylase 3	Homo sapiens (human)
positive regulation of TOR signaling	Histone deacetylase 3	Homo sapiens (human)
circadian regulation of gene expression	Histone deacetylase 3	Homo sapiens (human)
regulation of multicellular organism growth	Histone deacetylase 3	Homo sapiens (human)
positive regulation of protein import into nucleus	Histone deacetylase 3	Homo sapiens (human)
regulation of circadian rhythm	Histone deacetylase 3	Homo sapiens (human)
negative regulation of apoptotic process	Histone deacetylase 3	Homo sapiens (human)
negative regulation of DNA-templated transcription	Histone deacetylase 3	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Histone deacetylase 3	Homo sapiens (human)
negative regulation of JNK cascade	Histone deacetylase 3	Homo sapiens (human)
spindle assembly	Histone deacetylase 3	Homo sapiens (human)
establishment of skin barrier	Histone deacetylase 3	Homo sapiens (human)
cellular response to fluid shear stress	Histone deacetylase 3	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Histone deacetylase 3	Homo sapiens (human)
DNA repair-dependent chromatin remodeling	Histone deacetylase 3	Homo sapiens (human)
cornified envelope assembly	Histone deacetylase 3	Homo sapiens (human)
negative regulation of cardiac muscle cell differentiation	Histone deacetylase 3	Homo sapiens (human)
epigenetic regulation of gene expression	Histone deacetylase 3	Homo sapiens (human)
intracellular signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
type B pancreatic cell development	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein phosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of protein kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
hyperosmotic response	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
epidermal growth factor receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
insulin receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of phospholipase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic process	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cell migration	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
peptidyl-threonine phosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
calcium-mediated signaling	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
actin cytoskeleton organization	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
T cell costimulation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
activation of protein kinase B activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cellular response to insulin stimulus	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of toll-like receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
regulation of mast cell degranulation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of angiogenesis	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein autophosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cellular response to epidermal growth factor stimulus	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
extrinsic apoptotic signaling pathway	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of protein localization to plasma membrane	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of sprouting angiogenesis	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
peptidyl-serine phosphorylation	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
intracellular signal transduction	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein phosphorylation	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
positive regulation of neuron maturation	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
peptidyl-serine phosphorylation	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
positive regulation of JUN kinase activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
positive regulation of axon extension	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein autophosphorylation	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
stress-activated MAPK cascade	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
positive regulation of neuron projection arborization	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
positive regulation of branching morphogenesis of a nerve	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
chromatin organization	Death-associated protein kinase 3	Homo sapiens (human)
regulation of DNA-templated transcription	Death-associated protein kinase 3	Homo sapiens (human)
protein phosphorylation	Death-associated protein kinase 3	Homo sapiens (human)
apoptotic process	Death-associated protein kinase 3	Homo sapiens (human)
regulation of smooth muscle contraction	Death-associated protein kinase 3	Homo sapiens (human)
regulation of mitotic nuclear division	Death-associated protein kinase 3	Homo sapiens (human)
regulation of mitotic cell cycle	Death-associated protein kinase 3	Homo sapiens (human)
regulation of cell shape	Death-associated protein kinase 3	Homo sapiens (human)
regulation of autophagy	Death-associated protein kinase 3	Homo sapiens (human)
negative regulation of translation	Death-associated protein kinase 3	Homo sapiens (human)
positive regulation of cell migration	Death-associated protein kinase 3	Homo sapiens (human)
regulation of actin cytoskeleton organization	Death-associated protein kinase 3	Homo sapiens (human)
intracellular signal transduction	Death-associated protein kinase 3	Homo sapiens (human)
regulation of apoptotic process	Death-associated protein kinase 3	Homo sapiens (human)
positive regulation of apoptotic process	Death-associated protein kinase 3	Homo sapiens (human)
regulation of myosin II filament organization	Death-associated protein kinase 3	Homo sapiens (human)
protein autophosphorylation	Death-associated protein kinase 3	Homo sapiens (human)
regulation of focal adhesion assembly	Death-associated protein kinase 3	Homo sapiens (human)
cellular response to type II interferon	Death-associated protein kinase 3	Homo sapiens (human)
positive regulation of canonical Wnt signaling pathway	Death-associated protein kinase 3	Homo sapiens (human)
apoptotic signaling pathway	Death-associated protein kinase 3	Homo sapiens (human)
regulation of cell motility	Death-associated protein kinase 3	Homo sapiens (human)
MAPK cascade	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
stimulatory C-type lectin receptor signaling pathway	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
positive regulation of T cell cytokine production	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathway	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
MyD88-dependent toll-like receptor signaling pathway	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
chromatin remodeling	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
inflammatory response	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
canonical NF-kappaB signal transduction	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
I-kappaB phosphorylation	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
JNK cascade	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
negative regulation of gene expression	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
positive regulation of macroautophagy	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)

Process	via Protein(s)	Taxonomy
protein serine/threonine kinase activity	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
transmembrane receptor protein serine/threonine kinase activity	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
transmembrane signaling receptor activity	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
protein binding	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
ATP binding	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
BMP binding	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
SMAD binding	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
metal ion binding	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
BMP receptor activity	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
transforming growth factor beta receptor activity, type I	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
amyloid-beta binding	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
steroid binding	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
protein binding	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
heme binding	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
protein homodimerization activity	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
metal ion binding	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
protein kinase activity	Cell division cycle 7-related protein kinase	Homo sapiens (human)
protein binding	Cell division cycle 7-related protein kinase	Homo sapiens (human)
ATP binding	Cell division cycle 7-related protein kinase	Homo sapiens (human)
kinase activity	Cell division cycle 7-related protein kinase	Homo sapiens (human)
metal ion binding	Cell division cycle 7-related protein kinase	Homo sapiens (human)
protein serine kinase activity	Cell division cycle 7-related protein kinase	Homo sapiens (human)
protein serine/threonine kinase activity	Cell division cycle 7-related protein kinase	Homo sapiens (human)
protein binding	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
ATP binding	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
kinase activity	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
1-phosphatidylinositol-3-kinase activity	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activity	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activity	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase 25	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase 25	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase 25	Homo sapiens (human)
protein homodimerization activity	Serine/threonine-protein kinase 25	Homo sapiens (human)
metal ion binding	Serine/threonine-protein kinase 25	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase 25	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase 25	Homo sapiens (human)
DNA binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
DNA helicase activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
RNA binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
RNA helicase activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
mRNA binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
GTPase activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
protein binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
ATP binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
transcription factor binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
poly(A) binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
eukaryotic initiation factor 4E binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
ATP hydrolysis activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
ribonucleoside triphosphate phosphatase activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
translation initiation factor binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
RNA strand annealing activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
signaling adaptor activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
RNA stem-loop binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
gamma-tubulin binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
ribosomal small subunit binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
CTPase activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
protein serine/threonine kinase activator activity	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cadherin binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
mRNA 5'-UTR binding	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
protein binding	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
ATP binding	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
1-phosphatidylinositol-3-kinase activity	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activity	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
phosphatidylinositol binding	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
magnesium ion binding	Pyridoxal kinase	Homo sapiens (human)
ATP binding	Pyridoxal kinase	Homo sapiens (human)
zinc ion binding	Pyridoxal kinase	Homo sapiens (human)
pyridoxal kinase activity	Pyridoxal kinase	Homo sapiens (human)
pyridoxal phosphate binding	Pyridoxal kinase	Homo sapiens (human)
potassium ion binding	Pyridoxal kinase	Homo sapiens (human)
sodium ion binding	Pyridoxal kinase	Homo sapiens (human)
lithium ion binding	Pyridoxal kinase	Homo sapiens (human)
protein homodimerization activity	Pyridoxal kinase	Homo sapiens (human)
transcription coactivator binding	Citron Rho-interacting kinase	Homo sapiens (human)
protein serine/threonine kinase activity	Citron Rho-interacting kinase	Homo sapiens (human)
protein binding	Citron Rho-interacting kinase	Homo sapiens (human)
ATP binding	Citron Rho-interacting kinase	Homo sapiens (human)
SH3 domain binding	Citron Rho-interacting kinase	Homo sapiens (human)
protein kinase binding	Citron Rho-interacting kinase	Homo sapiens (human)
PDZ domain binding	Citron Rho-interacting kinase	Homo sapiens (human)
protein serine/threonine kinase inhibitor activity	Citron Rho-interacting kinase	Homo sapiens (human)
metal ion binding	Citron Rho-interacting kinase	Homo sapiens (human)
scaffold protein binding	Citron Rho-interacting kinase	Homo sapiens (human)
protein serine kinase activity	Citron Rho-interacting kinase	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
metal ion binding	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
caspase binding	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
magnesium ion binding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
MAP kinase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
MAP kinase kinase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
protein tyrosine kinase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
protein binding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
ATP binding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
JUN kinase kinase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
enzyme binding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
protein kinase binding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
protein phosphatase binding	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
protein serine kinase activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
molecular function activator activity	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein domain specific binding	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
histone H3T11 kinase activity	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein serine/threonine kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein binding	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
ATP binding	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
IkappaB kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein kinase binding	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
identical protein binding	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein homodimerization activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein heterodimerization activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
scaffold protein binding	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
protein serine kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
transferrin receptor binding	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
guanylate kinase activity	Peripheral plasma membrane protein CASK	Homo sapiens (human)
protein serine/threonine kinase activity	Peripheral plasma membrane protein CASK	Homo sapiens (human)
protein binding	Peripheral plasma membrane protein CASK	Homo sapiens (human)
calmodulin binding	Peripheral plasma membrane protein CASK	Homo sapiens (human)
ATP binding	Peripheral plasma membrane protein CASK	Homo sapiens (human)
neurexin family protein binding	Peripheral plasma membrane protein CASK	Homo sapiens (human)
protein serine kinase activity	Peripheral plasma membrane protein CASK	Homo sapiens (human)
signaling receptor binding	Peripheral plasma membrane protein CASK	Homo sapiens (human)
protein kinase activity	Aurora kinase A	Homo sapiens (human)
protein serine/threonine kinase activity	Aurora kinase A	Homo sapiens (human)
protein serine/threonine/tyrosine kinase activity	Aurora kinase A	Homo sapiens (human)
protein binding	Aurora kinase A	Homo sapiens (human)
ATP binding	Aurora kinase A	Homo sapiens (human)
protein kinase binding	Aurora kinase A	Homo sapiens (human)
ubiquitin protein ligase binding	Aurora kinase A	Homo sapiens (human)
histone H3S10 kinase activity	Aurora kinase A	Homo sapiens (human)
protein heterodimerization activity	Aurora kinase A	Homo sapiens (human)
protein serine kinase activity	Aurora kinase A	Homo sapiens (human)
molecular function activator activity	Aurora kinase A	Homo sapiens (human)
protein serine/threonine kinase activity	Cyclin-G-associated kinase	Homo sapiens (human)
protein binding	Cyclin-G-associated kinase	Homo sapiens (human)
ATP binding	Cyclin-G-associated kinase	Homo sapiens (human)
cyclin binding	Cyclin-G-associated kinase	Homo sapiens (human)
protein-folding chaperone binding	Cyclin-G-associated kinase	Homo sapiens (human)
protein serine kinase activity	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin binding	Cyclin-G-associated kinase	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
protein kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein serine/threonine kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein binding	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
ATP binding	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
IkappaB kinase activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein homodimerization activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein-containing complex binding	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein heterodimerization activity	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
scaffold protein binding	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
transferrin receptor binding	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
protein tyrosine kinase activity	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
protein binding	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
ATP binding	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
metal ion binding	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
Wnt-protein binding	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
ephrin receptor activity	Ephrin type-B receptor 6	Homo sapiens (human)
protein binding	Ephrin type-B receptor 6	Homo sapiens (human)
ATP binding	Ephrin type-B receptor 6	Homo sapiens (human)
signaling receptor activity	Ephrin type-B receptor 6	Homo sapiens (human)
transmembrane-ephrin receptor activity	Ephrin type-B receptor 6	Homo sapiens (human)
FAD binding	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
flavin adenine dinucleotide binding	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
pristanoyl-CoA oxidase activity	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
fatty acid binding	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase 13	Homo sapiens (human)
MAP kinase activity	Mitogen-activated protein kinase 13	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase 13	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase 13	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase 13	Homo sapiens (human)
transcription corepressor binding	Histone deacetylase 3	Homo sapiens (human)
chromatin binding	Histone deacetylase 3	Homo sapiens (human)
transcription corepressor activity	Histone deacetylase 3	Homo sapiens (human)
histone deacetylase activity	Histone deacetylase 3	Homo sapiens (human)
protein binding	Histone deacetylase 3	Homo sapiens (human)
enzyme binding	Histone deacetylase 3	Homo sapiens (human)
cyclin binding	Histone deacetylase 3	Homo sapiens (human)
chromatin DNA binding	Histone deacetylase 3	Homo sapiens (human)
protein lysine deacetylase activity	Histone deacetylase 3	Homo sapiens (human)
histone deacetylase binding	Histone deacetylase 3	Homo sapiens (human)
NF-kappaB binding	Histone deacetylase 3	Homo sapiens (human)
DNA-binding transcription factor binding	Histone deacetylase 3	Homo sapiens (human)
protein decrotonylase activity	Histone deacetylase 3	Homo sapiens (human)
histone decrotonylase activity	Histone deacetylase 3	Homo sapiens (human)
protein de-2-hydroxyisobutyrylase activity	Histone deacetylase 3	Homo sapiens (human)
protein serine/threonine kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
3-phosphoinositide-dependent protein kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein binding	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
ATP binding	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
phospholipase activator activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
phospholipase binding	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein serine kinase activity	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
MAP kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
enzyme binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein kinase binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
identical protein binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein homodimerization activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein serine/threonine kinase activator activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
metal ion binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
IkappaB kinase complex binding	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
JUN kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
protein serine/threonine kinase activity	Death-associated protein kinase 3	Homo sapiens (human)
protein binding	Death-associated protein kinase 3	Homo sapiens (human)
ATP binding	Death-associated protein kinase 3	Homo sapiens (human)
cAMP response element binding protein binding	Death-associated protein kinase 3	Homo sapiens (human)
small GTPase binding	Death-associated protein kinase 3	Homo sapiens (human)
identical protein binding	Death-associated protein kinase 3	Homo sapiens (human)
protein homodimerization activity	Death-associated protein kinase 3	Homo sapiens (human)
leucine zipper domain binding	Death-associated protein kinase 3	Homo sapiens (human)
protein serine kinase activity	Death-associated protein kinase 3	Homo sapiens (human)
magnesium ion binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
transcription coactivator binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
MAP kinase activity	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
MAP kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
type II transforming growth factor beta receptor binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
MAP kinase kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
receptor tyrosine kinase binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
ubiquitin protein ligase binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
histone kinase activity	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
identical protein binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
scaffold protein binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
protein serine/threonine kinase binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
DNA-binding transcription factor binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
linear polyubiquitin binding	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
protein serine/threonine kinase activity	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
signaling receptor binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
protein binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
ATP binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
LIM domain binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
signaling adaptor activity	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
identical protein binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
protein homodimerization activity	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
CARD domain binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
caspase binding	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
protein serine kinase activity	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
JUN kinase kinase kinase activity	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
protein kinase activity	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
protein serine/threonine kinase activity	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
protein binding	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
ATP binding	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
protein serine kinase activity	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
histone H2A kinase activity	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
p53 binding	NUAK family SNF1-like kinase 1	Homo sapiens (human)
protein serine/threonine kinase activity	NUAK family SNF1-like kinase 1	Homo sapiens (human)
protein binding	NUAK family SNF1-like kinase 1	Homo sapiens (human)
ATP binding	NUAK family SNF1-like kinase 1	Homo sapiens (human)
metal ion binding	NUAK family SNF1-like kinase 1	Homo sapiens (human)
protein serine kinase activity	NUAK family SNF1-like kinase 1	Homo sapiens (human)
magnesium ion binding	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
GTPase activity	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
protein binding	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
GTP binding	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
phosphatidic acid binding	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
GTPase-dependent fusogenic activity	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
membrane bending activity	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
cardiolipin binding	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
microtubule binding	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
protein binding	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
ATP binding	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
1-phosphatidylinositol-4-phosphate 5-kinase activity	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
phosphatidylinositol kinase activity	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
protein kinase activity	Tyrosine-protein kinase JAK2	Homo sapiens (human)
protein tyrosine kinase activity	Tyrosine-protein kinase JAK2	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Tyrosine-protein kinase JAK2	Homo sapiens (human)
signaling receptor binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
growth hormone receptor binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
interleukin-12 receptor binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
protein binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
ATP binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
protein kinase binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
heme binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
type 1 angiotensin receptor binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
acetylcholine receptor binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
histone H3Y41 kinase activity	Tyrosine-protein kinase JAK2	Homo sapiens (human)
SH2 domain binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
histone binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
identical protein binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
phosphatidylinositol 3-kinase binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
insulin receptor substrate binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
metal ion binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
peptide hormone receptor binding	Tyrosine-protein kinase JAK2	Homo sapiens (human)
tRNA binding	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
RNA binding	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
translation initiation factor activity	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
GTPase activity	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
protein binding	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
GTP binding	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
metal ion binding	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
protease binding	Rho-associated protein kinase 2	Homo sapiens (human)
RNA binding	Rho-associated protein kinase 2	Homo sapiens (human)
protein serine/threonine kinase activity	Rho-associated protein kinase 2	Homo sapiens (human)
structural molecule activity	Rho-associated protein kinase 2	Homo sapiens (human)
protein binding	Rho-associated protein kinase 2	Homo sapiens (human)
ATP binding	Rho-associated protein kinase 2	Homo sapiens (human)
small GTPase binding	Rho-associated protein kinase 2	Homo sapiens (human)
metal ion binding	Rho-associated protein kinase 2	Homo sapiens (human)
tau protein binding	Rho-associated protein kinase 2	Homo sapiens (human)
tau-protein kinase activity	Rho-associated protein kinase 2	Homo sapiens (human)
endopeptidase activator activity	Rho-associated protein kinase 2	Homo sapiens (human)
Rho-dependent protein serine/threonine kinase activity	Rho-associated protein kinase 2	Homo sapiens (human)
protein serine kinase activity	Rho-associated protein kinase 2	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
small GTPase binding	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
protein-containing complex binding	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
GTPase binding	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
magnesium ion binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
RNA endonuclease activity	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
platelet-derived growth factor receptor binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
enzyme binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
Hsp70 protein binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
protein homodimerization activity	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
ADP binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
Hsp90 protein binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
unfolded protein binding	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
magnesium ion binding	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
protein serine/threonine kinase activity	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
protein tyrosine kinase activity	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
protein binding	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
ATP binding	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
histone H3S10 kinase activity	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
histone H3S28 kinase activity	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
histone H2AS1 kinase activity	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
protein serine kinase activity	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
RNA binding	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
RNA helicase activity	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
helicase activity	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
protein binding	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
ATP binding	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
ATP hydrolysis activity	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
identical protein binding	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
magnesium ion binding	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein serine/threonine kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
ribosomal protein S6 kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein binding	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
ATP binding	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
histone H3S10 kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
histone H3S28 kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
protein serine kinase activity	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Serine/threonine-protein kinase 16	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Serine/threonine-protein kinase 16	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase 16	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase 16	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase 16	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase 16	Homo sapiens (human)
ATP binding	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
1-phosphatidylinositol-3-kinase activity	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activity	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
phosphatidylinositol binding	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
phosphatidylinositol kinase activity	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
MAP kinase kinase activity	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
SH3 domain binding	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
small GTPase binding	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
metal ion binding	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
protein kinase activity	Cyclin-dependent kinase-like 5	Homo sapiens (human)
protein serine/threonine kinase activity	Cyclin-dependent kinase-like 5	Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activity	Cyclin-dependent kinase-like 5	Homo sapiens (human)
protein binding	Cyclin-dependent kinase-like 5	Homo sapiens (human)
ATP binding	Cyclin-dependent kinase-like 5	Homo sapiens (human)
kinase activity	Cyclin-dependent kinase-like 5	Homo sapiens (human)
small GTPase binding	Cyclin-dependent kinase-like 5	Homo sapiens (human)
protein serine kinase activity	Cyclin-dependent kinase-like 5	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase 17B	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase 17B	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase 17B	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase 17B	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase 10	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase 10	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase 10	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase 10	Homo sapiens (human)
protein homodimerization activity	Serine/threonine-protein kinase 10	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase 10	Homo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activity	Serine/threonine-protein kinase D3	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase D3	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase D3	Homo sapiens (human)
kinase activity	Serine/threonine-protein kinase D3	Homo sapiens (human)
metal ion binding	Serine/threonine-protein kinase D3	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase D3	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase D3	Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activity	Cyclin-dependent kinase 14	Homo sapiens (human)
protein binding	Cyclin-dependent kinase 14	Homo sapiens (human)
ATP binding	Cyclin-dependent kinase 14	Homo sapiens (human)
cyclin binding	Cyclin-dependent kinase 14	Homo sapiens (human)
protein serine kinase activity	Cyclin-dependent kinase 14	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
single-stranded DNA binding	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
protein binding	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
ATP binding	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
ATP hydrolysis activity	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
chromatin binding	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
magnesium ion binding	Mitogen-activated protein kinase kinase kinase 6	Homo sapiens (human)
MAP kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase 6	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase 6	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase 6	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase 6	Homo sapiens (human)
magnesium ion binding	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
protein kinase binding	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
creatine kinase activity	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
protein serine/threonine kinase activity	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
protein binding	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
ATP binding	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
microtubule binding	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
MAP kinase kinase kinase kinase activity	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
protein serine kinase activity	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
magnesium ion binding	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
protein kinase binding	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
nuclear estrogen receptor binding	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
protein kinase activity	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
cadherin binding involved in cell-cell adhesion	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
protein serine/threonine kinase activity	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
protein binding	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
ATP binding	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
protein kinase binding	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
ubiquitin protein ligase binding	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
identical protein binding	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
protein homodimerization activity	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
metal ion binding	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
protein serine kinase activity	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
supercoiled DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
magnesium ion binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
four-way junction DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
bubble DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
phosphotyrosine residue binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
transcription coactivator activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin monomer binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nicotinate-nucleotide adenylyltransferase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein tyrosine kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein kinase C binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
ATP binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
SH3 domain binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
syntaxin binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
manganese ion binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuropilin binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
SH2 domain binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
ephrin receptor binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin filament binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mitogen-activated protein kinase binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)

Process	via Protein(s)	Taxonomy
plasma membrane	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
dendrite	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
neuronal cell body	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
receptor complex	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
HFE-transferrin receptor complex	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
plasma membrane	Bone morphogenetic protein receptor type-1B	Homo sapiens (human)
plasma membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
extracellular region	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
mitochondrial outer membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
endoplasmic reticulum	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
plasma membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
smooth endoplasmic reticulum membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
specific granule membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
neuron projection	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
neuronal cell body	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
cell body	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
synapse	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
endoplasmic reticulum	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
endomembrane system	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
membrane	Membrane-associated progesterone receptor component 1	Homo sapiens (human)
nucleus	Cell division cycle 7-related protein kinase	Homo sapiens (human)
nucleoplasm	Cell division cycle 7-related protein kinase	Homo sapiens (human)
cytoplasm	Cell division cycle 7-related protein kinase	Homo sapiens (human)
intercellular bridge	Cell division cycle 7-related protein kinase	Homo sapiens (human)
mitotic spindle	Cell division cycle 7-related protein kinase	Homo sapiens (human)
nucleus	Cell division cycle 7-related protein kinase	Homo sapiens (human)
cytoplasm	Cell division cycle 7-related protein kinase	Homo sapiens (human)
cytosol	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
plasma membrane	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
phosphatidylinositol 3-kinase complex, class IA	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
phosphatidylinositol 3-kinase complex	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
cytoplasm	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
plasma membrane	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Homo sapiens (human)
XY body	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
nucleolus	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
centrosome	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
centriole	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
cleavage furrow	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
deuterosome	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
procentriole	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
procentriole replication complex	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase PLK4	Homo sapiens (human)
Golgi apparatus	Serine/threonine-protein kinase 25	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase 25	Homo sapiens (human)
extracellular exosome	Serine/threonine-protein kinase 25	Homo sapiens (human)
FAR/SIN/STRIPAK complex	Serine/threonine-protein kinase 25	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase 25	Homo sapiens (human)
eukaryotic translation initiation factor 3 complex	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cytosolic small ribosomal subunit	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cytoplasm	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
extracellular region	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
nucleus	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
nucleoplasm	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cytoplasm	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
centrosome	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cytosol	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
plasma membrane	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cytoplasmic stress granule	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
lamellipodium	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
cell leading edge	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
secretory granule lumen	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
extracellular exosome	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
ficolin-1-rich granule lumen	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
NLRP3 inflammasome complex	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
nucleus	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
P granule	ATP-dependent RNA helicase DDX3X	Homo sapiens (human)
nucleoplasm	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
endoplasmic reticulum	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
cytosol	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
plasma membrane	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
endocytic vesicle	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
intracellular membrane-bounded organelle	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
cytoplasm	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
plasma membrane	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
phosphatidylinositol 3-kinase complex	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta	Homo sapiens (human)
extracellular region	Pyridoxal kinase	Homo sapiens (human)
nucleus	Pyridoxal kinase	Homo sapiens (human)
nucleoplasm	Pyridoxal kinase	Homo sapiens (human)
cytosol	Pyridoxal kinase	Homo sapiens (human)
secretory granule lumen	Pyridoxal kinase	Homo sapiens (human)
specific granule lumen	Pyridoxal kinase	Homo sapiens (human)
extracellular exosome	Pyridoxal kinase	Homo sapiens (human)
cytosol	Pyridoxal kinase	Homo sapiens (human)
cytosol	Citron Rho-interacting kinase	Homo sapiens (human)
membrane	Citron Rho-interacting kinase	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
preribosome, small subunit precursor	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase RIO3	Homo sapiens (human)
nucleus	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
cytoplasm	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
cytosol	Dual specificity mitogen-activated protein kinase kinase 7	Homo sapiens (human)
chromosome, telomeric region	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
condensed nuclear chromosome	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
extracellular space	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
replication fork	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
centrosome	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
intracellular membrane-bounded organelle	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
chromatin	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
protein-containing complex	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase Chk1	Homo sapiens (human)
cytoplasm	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
nucleus	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
cytosol	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
IkappaB kinase complex	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
cytoplasmic side of plasma membrane	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
membrane raft	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
CD40 receptor complex	Inhibitor of nuclear factor kappa-B kinase subunit beta	Homo sapiens (human)
basement membrane	Peripheral plasma membrane protein CASK	Homo sapiens (human)
nuclear lamina	Peripheral plasma membrane protein CASK	Homo sapiens (human)
nucleolus	Peripheral plasma membrane protein CASK	Homo sapiens (human)
cytoplasm	Peripheral plasma membrane protein CASK	Homo sapiens (human)
cytosol	Peripheral plasma membrane protein CASK	Homo sapiens (human)
cell-cell junction	Peripheral plasma membrane protein CASK	Homo sapiens (human)
focal adhesion	Peripheral plasma membrane protein CASK	Homo sapiens (human)
actin cytoskeleton	Peripheral plasma membrane protein CASK	Homo sapiens (human)
nuclear matrix	Peripheral plasma membrane protein CASK	Homo sapiens (human)
vesicle	Peripheral plasma membrane protein CASK	Homo sapiens (human)
presynaptic membrane	Peripheral plasma membrane protein CASK	Homo sapiens (human)
ciliary membrane	Peripheral plasma membrane protein CASK	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Peripheral plasma membrane protein CASK	Homo sapiens (human)
basement membrane	Peripheral plasma membrane protein CASK	Homo sapiens (human)
cell-cell junction	Peripheral plasma membrane protein CASK	Homo sapiens (human)
basolateral plasma membrane	Peripheral plasma membrane protein CASK	Homo sapiens (human)
plasma membrane	Peripheral plasma membrane protein CASK	Homo sapiens (human)
spindle microtubule	Aurora kinase A	Homo sapiens (human)
nucleus	Aurora kinase A	Homo sapiens (human)
nucleoplasm	Aurora kinase A	Homo sapiens (human)
centrosome	Aurora kinase A	Homo sapiens (human)
centriole	Aurora kinase A	Homo sapiens (human)
spindle	Aurora kinase A	Homo sapiens (human)
cytosol	Aurora kinase A	Homo sapiens (human)
postsynaptic density	Aurora kinase A	Homo sapiens (human)
microtubule cytoskeleton	Aurora kinase A	Homo sapiens (human)
basolateral plasma membrane	Aurora kinase A	Homo sapiens (human)
midbody	Aurora kinase A	Homo sapiens (human)
spindle pole centrosome	Aurora kinase A	Homo sapiens (human)
ciliary basal body	Aurora kinase A	Homo sapiens (human)
germinal vesicle	Aurora kinase A	Homo sapiens (human)
axon hillock	Aurora kinase A	Homo sapiens (human)
pronucleus	Aurora kinase A	Homo sapiens (human)
perinuclear region of cytoplasm	Aurora kinase A	Homo sapiens (human)
mitotic spindle	Aurora kinase A	Homo sapiens (human)
meiotic spindle	Aurora kinase A	Homo sapiens (human)
mitotic spindle pole	Aurora kinase A	Homo sapiens (human)
glutamatergic synapse	Aurora kinase A	Homo sapiens (human)
spindle pole centrosome	Aurora kinase A	Homo sapiens (human)
chromosome passenger complex	Aurora kinase A	Homo sapiens (human)
spindle midzone	Aurora kinase A	Homo sapiens (human)
kinetochore	Aurora kinase A	Homo sapiens (human)
Golgi apparatus	Cyclin-G-associated kinase	Homo sapiens (human)
cytosol	Cyclin-G-associated kinase	Homo sapiens (human)
focal adhesion	Cyclin-G-associated kinase	Homo sapiens (human)
membrane	Cyclin-G-associated kinase	Homo sapiens (human)
clathrin-coated vesicle	Cyclin-G-associated kinase	Homo sapiens (human)
vesicle	Cyclin-G-associated kinase	Homo sapiens (human)
intracellular membrane-bounded organelle	Cyclin-G-associated kinase	Homo sapiens (human)
perinuclear region of cytoplasm	Cyclin-G-associated kinase	Homo sapiens (human)
presynapse	Cyclin-G-associated kinase	Homo sapiens (human)
vesicle	Cyclin-G-associated kinase	Homo sapiens (human)
cytoplasm	Cyclin-G-associated kinase	Homo sapiens (human)
intracellular membrane-bounded organelle	Cyclin-G-associated kinase	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
postsynaptic density	Serine/threonine-protein kinase DCLK1	Homo sapiens (human)
nucleoplasm	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cytoplasm	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cytosol	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
IkappaB kinase complex	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cytoplasmic side of plasma membrane	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
CD40 receptor complex	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
cytoplasm	Inhibitor of nuclear factor kappa-B kinase subunit alpha	Homo sapiens (human)
plasma membrane	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
neuromuscular junction	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
postsynaptic membrane	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
receptor complex	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
plasma membrane	Muscle, skeletal receptor tyrosine-protein kinase	Homo sapiens (human)
extracellular region	Ephrin type-B receptor 6	Homo sapiens (human)
cytosol	Ephrin type-B receptor 6	Homo sapiens (human)
plasma membrane	Ephrin type-B receptor 6	Homo sapiens (human)
plasma membrane	Ephrin type-B receptor 6	Homo sapiens (human)
dendrite	Ephrin type-B receptor 6	Homo sapiens (human)
peroxisome	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
peroxisomal matrix	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
cytosol	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
membrane	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
peroxisome	Peroxisomal acyl-coenzyme A oxidase 3	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase 13	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase 13	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase 13	Homo sapiens (human)
nucleus	Histone deacetylase 3	Homo sapiens (human)
nucleoplasm	Histone deacetylase 3	Homo sapiens (human)
cytoplasm	Histone deacetylase 3	Homo sapiens (human)
Golgi apparatus	Histone deacetylase 3	Homo sapiens (human)
cytosol	Histone deacetylase 3	Homo sapiens (human)
plasma membrane	Histone deacetylase 3	Homo sapiens (human)
mitotic spindle	Histone deacetylase 3	Homo sapiens (human)
histone deacetylase complex	Histone deacetylase 3	Homo sapiens (human)
transcription repressor complex	Histone deacetylase 3	Homo sapiens (human)
nucleus	Histone deacetylase 3	Homo sapiens (human)
nucleus	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytoplasm	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytosol	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
plasma membrane	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
focal adhesion	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
postsynaptic density	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytoplasmic vesicle	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cell projection	3-phosphoinositide-dependent protein kinase 1	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
membrane	Mitogen-activated protein kinase kinase kinase 13	Homo sapiens (human)
nucleus	Death-associated protein kinase 3	Homo sapiens (human)
nucleoplasm	Death-associated protein kinase 3	Homo sapiens (human)
cytosol	Death-associated protein kinase 3	Homo sapiens (human)
PML body	Death-associated protein kinase 3	Homo sapiens (human)
nucleus	Death-associated protein kinase 3	Homo sapiens (human)
cytoplasm	Death-associated protein kinase 3	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
nucleus	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
cytosol	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
plasma membrane	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
endosome membrane	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
ATAC complex	Mitogen-activated protein kinase kinase kinase 7	Homo sapiens (human)
plasma membrane	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
cytoplasm	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
endoplasmic reticulum	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
cytosol	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
cytoskeleton	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
vesicle	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
protein-containing complex	Receptor-interacting serine/threonine-protein kinase 2	Homo sapiens (human)
kinetochore	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
nucleoplasm	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
cytosol	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
membrane	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
intracellular membrane-bounded organelle	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
outer kinetochore	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
kinetochore	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
nucleus	Mitotic checkpoint serine/threonine-protein kinase BUB1	Homo sapiens (human)
fibrillar center	NUAK family SNF1-like kinase 1	Homo sapiens (human)
nucleus	NUAK family SNF1-like kinase 1	Homo sapiens (human)
nucleoplasm	NUAK family SNF1-like kinase 1	Homo sapiens (human)
cytoplasm	NUAK family SNF1-like kinase 1	Homo sapiens (human)
microtubule cytoskeleton	NUAK family SNF1-like kinase 1	Homo sapiens (human)
nucleoplasm	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrion	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrial outer membrane	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrial inner membrane	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrial intermembrane space	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
cytosol	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
membrane	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrial crista	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
dendrite	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
axon cytoplasm	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrial intermembrane space	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
cytoplasm	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
microtubule	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
mitochondrial membrane	Dynamin-like 120 kDa protein, mitochondrial	Homo sapiens (human)
phagocytic cup	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
uropod	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
nucleoplasm	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
cytosol	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
adherens junction	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
focal adhesion	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
endosome membrane	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
ruffle membrane	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
presynapse	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
plasma membrane	Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Homo sapiens (human)
extrinsic component of plasma membrane	Tyrosine-protein kinase JAK2	Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membrane	Tyrosine-protein kinase JAK2	Homo sapiens (human)
nucleus	Tyrosine-protein kinase JAK2	Homo sapiens (human)
nucleoplasm	Tyrosine-protein kinase JAK2	Homo sapiens (human)
cytoplasm	Tyrosine-protein kinase JAK2	Homo sapiens (human)
cytosol	Tyrosine-protein kinase JAK2	Homo sapiens (human)
cytoskeleton	Tyrosine-protein kinase JAK2	Homo sapiens (human)
plasma membrane	Tyrosine-protein kinase JAK2	Homo sapiens (human)
caveola	Tyrosine-protein kinase JAK2	Homo sapiens (human)
focal adhesion	Tyrosine-protein kinase JAK2	Homo sapiens (human)
granulocyte macrophage colony-stimulating factor receptor complex	Tyrosine-protein kinase JAK2	Homo sapiens (human)
endosome lumen	Tyrosine-protein kinase JAK2	Homo sapiens (human)
interleukin-12 receptor complex	Tyrosine-protein kinase JAK2	Homo sapiens (human)
membrane raft	Tyrosine-protein kinase JAK2	Homo sapiens (human)
interleukin-23 receptor complex	Tyrosine-protein kinase JAK2	Homo sapiens (human)
postsynapse	Tyrosine-protein kinase JAK2	Homo sapiens (human)
glutamatergic synapse	Tyrosine-protein kinase JAK2	Homo sapiens (human)
euchromatin	Tyrosine-protein kinase JAK2	Homo sapiens (human)
cytosol	Tyrosine-protein kinase JAK2	Homo sapiens (human)
nucleus	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
cytoplasm	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
cytosol	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
synapse	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
cytoplasm	Eukaryotic translation initiation factor 5B	Homo sapiens (human)
nucleus	Rho-associated protein kinase 2	Homo sapiens (human)
centrosome	Rho-associated protein kinase 2	Homo sapiens (human)
cytosol	Rho-associated protein kinase 2	Homo sapiens (human)
plasma membrane	Rho-associated protein kinase 2	Homo sapiens (human)
cytoplasmic ribonucleoprotein granule	Rho-associated protein kinase 2	Homo sapiens (human)
centrosome	Rho-associated protein kinase 2	Homo sapiens (human)
cytoskeleton	Rho-associated protein kinase 2	Homo sapiens (human)
cytoplasm	Rho-associated protein kinase 2	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
phagophore assembly site	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
autophagosome membrane	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
mitochondrial outer membrane	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
autophagosome	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
endoplasmic reticulum membrane	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
axon	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
phagophore assembly site membrane	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
recycling endosome	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
omegasome membrane	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
Atg1/ULK1 kinase complex	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
phagophore assembly site	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
autophagosome	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
phagophore assembly site membrane	Serine/threonine-protein kinase ULK1	Homo sapiens (human)
nuclear inner membrane	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
mitochondrion	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
endoplasmic reticulum	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
endoplasmic reticulum membrane	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
Ire1 complex	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
AIP1-IRE1 complex	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
IRE1-TRAF2-ASK1 complex	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
IRE1-RACK1-PP2A complex	Serine/threonine-protein kinase/endoribonuclease IRE1	Homo sapiens (human)
nucleus	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
cytoplasm	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
cytoplasm	Ribosomal protein S6 kinase alpha-5	Homo sapiens (human)
nucleus	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
nucleoplasm	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
membrane	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
U4/U6 x U5 tri-snRNP complex	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
spliceosomal complex	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
U5 snRNP	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
U2-type precatalytic spliceosome	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
U2-type catalytic step 1 spliceosome	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
catalytic step 2 spliceosome	U5 small nuclear ribonucleoprotein 200 kDa helicase	Homo sapiens (human)
nucleus	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
cytosol	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
synapse	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
cytoplasm	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-4	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein kinase 16	Homo sapiens (human)
Golgi-associated vesicle	Serine/threonine-protein kinase 16	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase 16	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase 16	Homo sapiens (human)
perinuclear region of cytoplasm	Serine/threonine-protein kinase 16	Homo sapiens (human)
Golgi apparatus	Serine/threonine-protein kinase 16	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase 16	Homo sapiens (human)
cytosol	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
membrane	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
phosphatidylinositol 3-kinase complex	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
cytoplasm	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
plasma membrane	Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
postsynaptic density	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
glutamatergic synapse	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase PAK 3	Homo sapiens (human)
ruffle membrane	Cyclin-dependent kinase-like 5	Homo sapiens (human)
glutamatergic synapse	Cyclin-dependent kinase-like 5	Homo sapiens (human)
nucleus	Cyclin-dependent kinase-like 5	Homo sapiens (human)
nucleoplasm	Cyclin-dependent kinase-like 5	Homo sapiens (human)
centrosome	Cyclin-dependent kinase-like 5	Homo sapiens (human)
dendrite cytoplasm	Cyclin-dependent kinase-like 5	Homo sapiens (human)
ciliary basal body	Cyclin-dependent kinase-like 5	Homo sapiens (human)
dendritic growth cone	Cyclin-dependent kinase-like 5	Homo sapiens (human)
perinuclear region of cytoplasm	Cyclin-dependent kinase-like 5	Homo sapiens (human)
ciliary tip	Cyclin-dependent kinase-like 5	Homo sapiens (human)
postsynaptic density, intracellular component	Cyclin-dependent kinase-like 5	Homo sapiens (human)
nucleus	Cyclin-dependent kinase-like 5	Homo sapiens (human)
dendrite cytoplasm	Cyclin-dependent kinase-like 5	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase 17B	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein kinase 17B	Homo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment	Serine/threonine-protein kinase 17B	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase 17B	Homo sapiens (human)
actin cytoskeleton	Serine/threonine-protein kinase 17B	Homo sapiens (human)
Flemming body	Serine/threonine-protein kinase 17B	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase 17B	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase 10	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase 10	Homo sapiens (human)
specific granule membrane	Serine/threonine-protein kinase 10	Homo sapiens (human)
extracellular exosome	Serine/threonine-protein kinase 10	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase 10	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein kinase D3	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase D3	Homo sapiens (human)
plasma membrane	Serine/threonine-protein kinase D3	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase D3	Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complex	Cyclin-dependent kinase 14	Homo sapiens (human)
nucleoplasm	Cyclin-dependent kinase 14	Homo sapiens (human)
cytosol	Cyclin-dependent kinase 14	Homo sapiens (human)
plasma membrane	Cyclin-dependent kinase 14	Homo sapiens (human)
cytoplasmic cyclin-dependent protein kinase holoenzyme complex	Cyclin-dependent kinase 14	Homo sapiens (human)
cytoplasm	Cyclin-dependent kinase 14	Homo sapiens (human)
cytosol	Cyclin-dependent kinase 14	Homo sapiens (human)
nucleus	Cyclin-dependent kinase 14	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
nuclear chromosome	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
condensed chromosome	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
condensed nuclear chromosome	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
condensin complex	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
nucleus	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
nucleoplasm	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
nucleolus	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
cytoplasm	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
cytosol	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
extracellular exosome	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
condensed chromosome	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
chromatin	Structural maintenance of chromosomes protein 2	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
extracellular exosome	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase OSR1	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
cytoplasm	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
focal adhesion	Mitogen-activated protein kinase kinase kinase kinase 4	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
spindle pole	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
centrosome	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
midbody	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
spindle pole	Serine/threonine-protein kinase LATS1	Homo sapiens (human)
Golgi apparatus	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
cytosol	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
adherens junction	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
focal adhesion	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase PAK 4	Homo sapiens (human)
chromosome, telomeric region	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
nucleoplasm	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
Golgi apparatus	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
PML body	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
cytoplasm	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
nucleus	Serine/threonine-protein kinase Chk2	Homo sapiens (human)
ruffle	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nucleus	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nucleoplasm	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nucleolus	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cytoplasm	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mitochondrion	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cytosol	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin cytoskeleton	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nuclear body	Tyrosine-protein kinase ABL1	Homo sapiens (human)
dendrite	Tyrosine-protein kinase ABL1	Homo sapiens (human)
growth cone	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nuclear membrane	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuronal cell body	Tyrosine-protein kinase ABL1	Homo sapiens (human)
perinuclear region of cytoplasm	Tyrosine-protein kinase ABL1	Homo sapiens (human)
postsynapse	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein-containing complex	Tyrosine-protein kinase ABL1	Homo sapiens (human)
plasma membrane	Tyrosine-protein kinase ABL1	Homo sapiens (human)
endosome	Epidermal growth factor receptor	Homo sapiens (human)
plasma membrane	Epidermal growth factor receptor	Homo sapiens (human)
ruffle membrane	Epidermal growth factor receptor	Homo sapiens (human)
Golgi membrane	Epidermal growth factor receptor	Homo sapiens (human)
extracellular space	Epidermal growth factor receptor	Homo sapiens (human)
nucleus	Epidermal growth factor receptor	Homo sapiens (human)
cytoplasm	Epidermal growth factor receptor	Homo sapiens (human)
endosome	Epidermal growth factor receptor	Homo sapiens (human)
endoplasmic reticulum membrane	Epidermal growth factor receptor	Homo sapiens (human)
plasma membrane	Epidermal growth factor receptor	Homo sapiens (human)
focal adhesion	Epidermal growth factor receptor	Homo sapiens (human)
cell surface	Epidermal growth factor receptor	Homo sapiens (human)
endosome membrane	Epidermal growth factor receptor	Homo sapiens (human)
membrane	Epidermal growth factor receptor	Homo sapiens (human)
basolateral plasma membrane	Epidermal growth factor receptor	Homo sapiens (human)
apical plasma membrane	Epidermal growth factor receptor	Homo sapiens (human)
cell junction	Epidermal growth factor receptor	Homo sapiens (human)
clathrin-coated endocytic vesicle membrane	Epidermal growth factor receptor	Homo sapiens (human)
early endosome membrane	Epidermal growth factor receptor	Homo sapiens (human)
nuclear membrane	Epidermal growth factor receptor	Homo sapiens (human)
membrane raft	Epidermal growth factor receptor	Homo sapiens (human)
perinuclear region of cytoplasm	Epidermal growth factor receptor	Homo sapiens (human)
multivesicular body, internal vesicle lumen	Epidermal growth factor receptor	Homo sapiens (human)
intracellular vesicle	Epidermal growth factor receptor	Homo sapiens (human)
protein-containing complex	Epidermal growth factor receptor	Homo sapiens (human)
receptor complex	Epidermal growth factor receptor	Homo sapiens (human)
Shc-EGFR complex	Epidermal growth factor receptor	Homo sapiens (human)
basal plasma membrane	Epidermal growth factor receptor	Homo sapiens (human)
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)

Bioassays (1934)

Assay ID	Title	Year	Journal	Article
AID493040	Navigating the Kinome	2011	Nature chemical biology, Apr, Volume: 7, Issue:4	Navigating the kinome.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID625070	Binding constant for PFTK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624832	Binding constant for IKK-alpha kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425130	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1378269	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay
AID256562	Average Binding Constant for PAK4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424895	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624797	Binding constant for PHKG2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256593	Average Binding Constant for NEK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435146	Binding constant for ABL1(H396P) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1378271	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
AID624769	Binding constant for AURKC kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1894160	Inhibition of HER2 (unknown origin)	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
AID1215643	Inhibition of human recombinant CYP3A5 using testosterone as substrate assessed as testosterone 6beta-hydroxylation at 50 uM preincubated up to 30 mins with NADPH followed by substrate addition measured after 10 mins by LC/MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID435200	Binding constant for full-length TNNI3K	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID270618	Inhibition of HN5 cell growth after 72 hrs	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID1426967	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1425159	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625018	Binding constant for YES kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625140	Binding constant for MARK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425187	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435791	Binding constant for EGFR(E746-A750del) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1676508	Stability of compound in human plasma assessed as parent compound remaining at 5 uM measured for 1 hr by LC-MS analysis	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1168588	Antitumor activity against human Calu3 cells xenografted in BALB/cA mouse assessed as tumor growth inhibition at 200 mg/kg, po	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID436046	Binding constant for PRKD2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID588210	Human drug-induced liver injury (DILI) modelling dataset from Ekins et al	2010	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12	A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1424940	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624843	Binding constant for CAMK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424979	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256563	Average Binding Constant for ULK3 m; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1215636	Inhibition of human recombinant CYP3A5 using testosterone as substrate assessed as testosterone 6-beta-hydroxylation preincubated up to 30 mins with NADPH followed by substrate addition measured after 10 mins by LC/MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1424959	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1667572	Antiproliferative activity against human BT474 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID625022	Binding constant for MUSK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256582	Average Binding Constant for NEK9; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435527	Binding constant for FGFR3(G697C) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636179	Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID256639	Average Binding Constant for PHkg1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624890	Binding constant for p38-beta kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625048	Binding constant for PRKCD kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435934	Binding constant for PLK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425002	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425113	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1268284	Inhibition of His-tagged EGFR cytoplasmic domain (645-1186 aa) (unknown origin) assessed as inhibition of autophosphorylation by TR-fluorometry	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID435153	Binding constant for full-length DAPK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625079	Binding constant for NEK6 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625081	Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636386	Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.
AID1425133	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424971	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425014	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1353457	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID436042	Binding constant for full-length PHKG1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436012	Binding constant for full-length CSNK2A1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID270616	Inhibition of ErbB2	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID1260767	Antiparasitic activity against bloodstream Trypanosoma brucei bruei CA427 after 48 hrs by cytometry	2015	MedChemComm, Feb, Volume: 6, Issue:2	EVALUATION OF AROMATIC 6-SUBSTITUTED THIENOPYRIMIDINES AS SCAFFOLDS AGAINST PARASITES THAT CAUSE TRYPANOSOMIASIS, LEISHMANIASIS, AND MALARIA.
AID1589079	Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 10 uM by luminescence based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID1718875	Effect on human recombinant N-terminal GST-tagged p38alpha expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID625012	Binding constant for GAK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1492834	Antiparasitic activity against bloodstream froms of Trypanosoma brucei brucei Lister 427 assessed as parasitic growth inhibition after 48 hrs by haemocytometer	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation.
AID1425085	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425193	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435184	Binding constant for PTK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425000	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436021	Binding constant for LATS2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435691	Binding constant for SgK085 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1219563	Activity of recombinant CYP3A4 (unknown origin) assessed as 6-(5-(aminomethyl)furan-2-yl)-N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)quinazolin-4-amine formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1424966	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435821	Binding constant for GAK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1202662	Growth inhibition of human MDA-MB-453 cells at 5 uM incubated for 72 hrs by ATP detection based luminescent assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Design and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors.
AID624979	Binding constant for ABL1(F317I)-non phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436053	Binding constant for full-length STK33	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424962	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1724908	Drug exposure in mouse brain at 80 mg/kg, po after 24 hrs	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID435936	Binding constant for full-length SRPK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256580	Average Binding Constant for CAMKK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID705604	Time dependent inhibition of CYP3A4 in human liver microsomes assessed as quasi-irreversible complex formation	2012	Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11	Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
AID624870	Binding constant for NEK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625005	Binding constant for EGFR(L861Q) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624711	Binding constant for STK35 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425169	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1219574	Activity of recombinant CYP3A4 (unknown origin) assessed as 2-chloro-4-(6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID625034	Binding constant for PDGFRA kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256650	Average Binding Constant for PIM1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435823	Binding constant for full-length PAK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID441961	Cytotoxicity against human A431 cells after 72 hrs by SRB assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID638912	Inhibition of c-Kit at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID435157	Binding constant for EGFR(G719C) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1543683	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID1219570	Drug metabolism in human liver microsomes assessed as (5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-yl)methanol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1664193	Inhibition of EGFR L858R/T790M mutant (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assay
AID1589080	Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 20 uM by luminescence based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID1425147	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435400	Binding constant for DDR1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID69892	Inhibitory activity against epidermal growth factor receptor	2004	Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1	Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
AID435285	Binding constant for DMPK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624800	Binding constant for IGF1R kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1443992	Total Cmax in human administered as single dose	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID624805	Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435661	Binding constant for full-length MKNK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425099	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624964	Binding constant for DYRK1B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435534	Binding constant for NEK5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624872	Binding constant for PAK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435650	Binding constant for full-length CSNK1E	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624778	Binding constant for ACVRL1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425100	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424997	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435395	Binding constant for CDC2L1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435147	Binding constant for ACVR2B kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624857	Binding constant for HCK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624885	Binding constant for ERK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425172	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624706	Binding constant for MLK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625133	Binding constant for CDC2L2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636169	Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1425098	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256559	Average Binding Constant for EPHB4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624730	Binding constant for CAMK2A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1426971	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1595629	Selectivity ratio of IC50 for human UCH2 cells to IC50 for human UCH1 cells	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID517323	Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
AID1207434	Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform
AID1424910	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1545923	Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Dec-01, Volume: 183	1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID767292	Antiproliferative activity against human HER2 deficient T47D cells expressing estrogen receptor and progesterone receptor after 72 hrs by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Synthesis and SAR studies of marine natural products ma'edamines A, B and their analogues.
AID1062003	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1425206	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624854	Binding constant for FLT4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1426968	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1215646	Inhibition of human recombinant CYP3A5 assessed as reduction of enzyme-CO complex formation at 50 uM preincubated for 3 to 5 mins with NADPH B followed by NADPH A addition measured after 30 mins by CO difference spectroscopy relative to control	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID624743	Binding constant for LTK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624856	Binding constant for GSK3B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425127	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435653	Binding constant for EGFR(L747-S752del, P753S) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435658	Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425180	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624702	Binding constant for BRSK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1315428	Cytotoxicity against human HELF assessed as reduction in cell viability after 48 hrs by MTT assay	2016	European journal of medicinal chemistry, Sep-14, Volume: 120	Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.
AID436034	Binding constant for PRKCH kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435645	Binding constant for ACVRL1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID664620	Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID624934	Binding constant for FLT3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168568	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G1 phase at 0.001 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 67%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1353484	Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 15 uM after 48 hrs by Annexin V-FITC/propidium iodide satining based FACS analysis (Rvb = 2.78%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID546548	Inhibition of human recombinant HDAC6 expressed in HEK293 cells	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID624710	Binding constant for SRMS kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636197	Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1330927	Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1425045	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1562674	Induction of cell cycle arrest in human A549 cells assessed as accumulation at S phase at 15 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 33.67%)
AID625090	Binding constant for ICK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624865	Binding constant for MAP3K3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1664188	Inhibition of wild type EGFR (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assay
AID1547473	Antileishmanial activity against Leishmania major	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.
AID1426969	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID435924	Binding constant for MARK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435929	Binding constant for PAK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435554	Binding constant for PRKD3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424989	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624745	Binding constant for PKN1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425082	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424915	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435284	Binding constant for DCAMKL1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID441965	Inhibition of Her1 T790M mutant by fluorescence polarization assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID1425156	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624703	Binding constant for MAPKAPK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1731400	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as spectral edge frequency at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID435407	Binding constant for FLT3(D835Y) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1360956	Cytotoxicity against human PBMC assessed as induction of cell death by cell Titer-Glo assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Identification of fused pyrimidines as interleukin 17 secretion inhibitors.
AID624829	Binding constant for CDK8 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625035	Binding constant for PHKG1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624808	Binding constant for TRKA kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435546	Binding constant for PRKG1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625026	Binding constant for MAP3K1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435288	Binding constant for EPHB2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1219555	Inhibition of recombinant CYP3A4 (unknown origin)-mediated midazolam 1-hydroxylation at 50 uM	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID410960	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activity.
AID624771	Binding constant for TLK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168564	Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624752	Binding constant for SNRK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624932	Binding constant for CLK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1268282	Cytotoxicity against human HEK293T cells for 24 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID1425145	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID662805	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.
AID624817	Binding constant for MYO3B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1219559	Inhibition of recombinant CYP3A5 (unknown origin)-mediated midazolam 1-hydroxylation at 50 uM in presence of 2 mM ferricyanide	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID68106	Inhibitory activity against ERBB2 receptor kinase	2004	Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1	Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
AID256633	Average Binding Constant for PRKACA; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424938	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425115	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256587	Average Binding Constant for ACK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1168583	Induction of apoptosis in human BT474 cells at 1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 1%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID636195	Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435644	Binding constant for ABL1(E255K) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1915535	Inhibition of EGFR (unknown origin) at 10 ug/ml using synthetic biotinylated peptide as substrate by Wallac Victor II 1420 microplate reader method relative to control	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID638914	Inhibition of PDGFRbeta at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1168591	Toxicity in human Calu3 cells xenografted BALB/cA mouse assessed as body weight loss at 200 mg/kg, po measured every other day for 21 days	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID435901	Binding constant for BRAF kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435937	Binding constant for TESK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1595620	Inhibition of EGFR in human A431 cells assessed as reduction in EGF-stimulated EGFR autophosphorylation preincuabted for 90 mins followed by EGF-stimulation by sandwich-ELISA	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID256584	Average Binding Constant for CAMK1D; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256618	Average Binding Constant for PHkg2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1718869	Inhibition of HER2 L755S mutant (unknown origin) at 5 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID256613	Average Binding Constant for Aurora2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624861	Binding constant for LIMK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1676506	Intrinsic clearance in human liver microsomes at 3 uM measured up to 50 mins by LC-MS analysis	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID436016	Binding constant for full-length ERK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624999	Binding constant for EGFR(G719S) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624782	Binding constant for FGFR3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435834	Binding constant for YANK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424912	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1532890	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID624869	Binding constant for NEK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624889	Binding constant for JNK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636184	Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435320	Binding constant for PRKCE kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256605	Average Binding Constant for STK17B; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624757	Binding constant for PKMYT1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636187	Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1555860	Drug concentration in NOD/SCID mouse blood xenografted with human A549 cells overexpressing EGFR at 86 micromol/kg, po administered once daily for 27 days and measured at day 27 at 2 hrs after last administered dose by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID1425004	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435197	Binding constant for TEC kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID664618	Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID435414	Binding constant for MLK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1595627	Antiproliferative activity against human UCH12 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID625083	Binding constant for LATS2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1463973	Inhibition of wild type recombinant EGFR (unknown origin) by ELISA	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase.
AID625096	Binding constant for STK36 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625063	Binding constant for PLK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624954	Binding constant for EPHB1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624822	Binding constant for CDKL3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID546554	Inhibition of INSR by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1424937	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168555	Inhibition of c-KIT phosphorylation (unknown origin) expressed in human NCI-H526 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624753	Binding constant for PKNB(M.tuberculosis) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425123	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624740	Binding constant for LRRK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256644	Average Binding Constant for CSNK1E; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424976	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID435514	Binding constant for ABL1(M351T) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624917	Binding constant for MST3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168567	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID625103	Binding constant for MST4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID345876	Inhibition of human recombinant EGFR	2009	Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4	Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.
AID1219566	Drug metabolism in human liver microsomes assessed as 2-chloro-4-(6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID256645	Average Binding Constant for JAK2 (Kin.Dom. 2); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624976	Binding constant for PRKX kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1353460	Inhibition of EGFR L858R mutant (unknown origin) using ULight-poly GT as substrate preincubated for 120 mins followed by substrate addition measured after 2 hrs by spectrophotometric method	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID435152	Binding constant for CAMK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625068	Binding constant for NEK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256566	Average Binding Constant for TNIK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID636180	Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID625111	Binding constant for RIOK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625106	Binding constant for MARK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1315425	Inhibition of His-tagged human HER2 (676 to 1255 residues) expressed in baculovirus after 1 hr by Z-lyte assay	2016	European journal of medicinal chemistry, Sep-14, Volume: 120	Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.
AID256664	Average Binding Constant for EGFR; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624941	Binding constant for CDKL1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624993	Binding constant for ABL2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1219571	Drug metabolism in human liver microsomes assessed as N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((hydroxy(2 (methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID636183	Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1424924	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435183	Binding constant for PLK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425204	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425011	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435530	Binding constant for MAP3K4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624786	Binding constant for KIT kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425119	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1667571	Antiproliferative activity against human A431 cells overexpressing EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID1168545	Inhibition of HER1 phosphorylation (unknown origin) expressed in human A431 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1809333	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
AID435902	Binding constant for BRAF(V600E) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624903	Binding constant for SRPK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718895	Effect on human recombinant N-terminal His-tagged ABL1 (27 to end residues) expressed in baculovirus-infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relat
AID624814	Binding constant for DCAMKL2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256602	Average Binding Constant for EPHA2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624846	Binding constant for CSNK1A1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1562610	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
AID1186995	Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by Cell-Titer Glo assay	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
AID636186	Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435785	Binding constant for full-length CDK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425093	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256630	Average Binding Constant for FYN; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425039	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435312	Binding constant for MET kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624760	Binding constant for PFPK5(P.falciparum) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256659	Average Binding Constant for DAPK3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624975	Binding constant for PLK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625025	Binding constant for MAK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436052	Binding constant for full-length SNF1LK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID729552	Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 5 uM by TR-FRET based binding assay	2013	European journal of medicinal chemistry, Mar, Volume: 61	Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
AID624951	Binding constant for EPHA2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435519	Binding constant for AURKB kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425191	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435690	Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435521	Binding constant for CAMKK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1426974	Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1407099	Inhibition of EGFR in human HepG2 cells	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID1915536	Inhibition of HER2 (unknown origin) at 10 ug/ml using synthetic biotinylated peptide as substrate by Wallac Victor II 1420 microplate reader method relative to control	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
AID642764	Antiproliferative activity against human NCI-H1975 cells over-expressing EGFR mutant gene after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Discovery of novel selective inhibitors for EGFR-T790M/L858R.
AID624922	Binding constant for CAMK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625124	Binding constant for RET(V804M) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425189	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624911	Binding constant for TXK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435520	Binding constant for CAMK2A kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425022	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424928	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1062007	Inhibition of HER2 (unknown origin) by ADP-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1168580	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G1 phase at 1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 67%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1664191	Selectivity index, ratio of IC50 for wild type EGFR (unknown origin) to IC50 for HER4 (unknown origin) by radioisotope filter binding assay
AID1424986	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718822	Inhibition of HER2 in human BT474 cells assessed as reduction in Akt phosphorylation at 0.5 IC50 incubated for 72 hrs by western blot analysis
AID435940	Binding constant for full-length TSSK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624886	Binding constant for ERK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436008	Binding constant for full-length BTK	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425025	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168570	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at S phase at 0.001 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 19%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID256594	Average Binding Constant for BMX; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID546551	Inhibition of EGFR by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1062005	Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1425047	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624960	Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID463638	Inhibition of EGFR	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Selectively nonselective kinase inhibition: striking the right balance.
AID256674	Average Binding Constant for PKMYT1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID546550	Inhibition of Flag tagged human recombinant HDAC8 expressed in Sf21 cells	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID625125	Binding constant for CLK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424922	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624842	Binding constant for BMX kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425140	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718819	Inhibition of HER2 in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.1 IC50 incubated for 72 hrs by western blot analysis
AID256628	Average Binding Constant for LYN; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624986	Binding constant for ABL1(Q252H)-non phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435154	Binding constant for DDR2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425167	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625053	Binding constant for PRKG2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1268303	Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID1718882	Inhibition of wild-type HER2 (unknown origin) at 0.01 to 25 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID624831	Binding constant for CHEK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168536	Inhibition of PDGFRbeta (unknown origin) by ELISA method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID435912	Binding constant for MRCKB kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624947	Binding constant for BRAF(V600E) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256627	Average Binding Constant for RPS6KA2 (Kin.Dom. 1); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID546547	Inhibition of human recombinant HDAC1 expressed in HEK293 cells	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID624826	Binding constant for BMPR2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625054	Binding constant for MST2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436007	Binding constant for AXL kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435182	Binding constant for full-length PKAC-beta	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168582	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at S phase at 1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 19%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1425095	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624713	Binding constant for ERK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435439	Binding constant for PAK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1215638	Inhibition of human recombinant CYP3A5 using midazolam as substrate assessed as midazolam 1'-hydroxylation at 2.5 to 50 uM preincubated up to 30 mins with NADPH followed by substrate addition measured after 10 mins by LC/MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1426972	Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1168535	Inhibition of HER1 (unknown origin) assessed as reduction in autophosphorylation by ELISA method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID435899	Binding constant for AKT1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424363	Binding affinity to human EGFR assessed as residence time	2017	European journal of medicinal chemistry, Dec-15, Volume: 142	How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.
AID1595631	Selectivity ratio of IC50 for human UMCHOR1 cells to IC50 for human UCH1 cells	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID625109	Binding constant for BIKE kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1678479	Inhibition of recombinant His6-tagged SARS-CoV-2 main protease using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay	2020	ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12	Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID1424994	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1366917	Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID1424999	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624736	Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435149	Binding constant for AMPK-alpha2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1407094	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID625019	Binding constant for AKT3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1315424	Inhibition of GST-tagged wild type recombinant human EGFR (668 to 1210 residues) expressed in baculovirus after 1 hr by Z-lyte assay	2016	European journal of medicinal chemistry, Sep-14, Volume: 120	Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.
AID435925	Binding constant for PCTK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1731406	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as delta at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID256604	Average Binding Constant for STK10; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID664746	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID435159	Binding constant for EPHB3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1589075	Cytotoxicity in human WS1 cells assessed as reduction in cell viability incubated fro 48 hrs by alamar blue dye based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID435926	Binding constant for PDGFRB kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1809336	Resistant factor, ratio of IC50 for antiproliferative activity against drug-tolerant human MDA-MB-231 cells to IC50 for human MDA-MB-231 cells
AID1425005	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID664744	Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID624708	Binding constant for CDC2L1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625122	Binding constant for RET(M918T) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625115	Binding constant for PAK6 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425067	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625137	Binding constant for MEK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624849	Binding constant for CSNK2A2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636162	Inhibition of MET using poly(Ala, Glu, Lys, Tyr) as substrate and [gamma33P]ATP at 1 uM after 60 mins by scintillation counting	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1589887	Inhibition of probe binding to EGFR L858R mutant (unknown origin) using rabbit reticulate lysate system after 1 hr by luminescence assay	2019	Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12	Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
AID624875	Binding constant for PDGFRB kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424955	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168590	Toxicity in human Calu3 cells xenografted BALB/cA mouse assessed as body weight loss at 100 mg/kg, po measured every other day for 21 days	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624982	Binding constant for ABL1(F317L)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624729	Binding constant for FAK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636173	Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1425166	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718820	Inhibition of HER2 in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.5 IC50 incubated for 72 hrs by western blot analysis
AID638068	Inhibition of Her-2 by time-resolved fluorescence assay	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
AID1306575	Inhibition of His-tagged human recombinant Her2 (676 to 1255 residues) expressed in baculovirus by fluorescence based assay	2016	Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16	Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
AID1366912	Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID625006	Binding constant for EGFR(S752-I759del) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1555856	Tmax in C57BL/6N mouse at 34 micromol/kg, po measured upto 24 hrs by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID1168587	Induction of apoptosis in human BT474 cells at 10 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 1%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1425208	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1731410	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as GSH level in brain at 20 mg/kg, po for 10 days by calorimetric method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID625121	Binding constant for RET kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424902	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435829	Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256631	Average Binding Constant for FLT4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256660	Average Binding Constant for KIT; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424911	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1562603	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
AID625007	Binding constant for EGFR(T790M) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1219584	Activity of recombinant CYP3A5 (unknown origin) assessed as (5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-yl)methanol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID435160	Binding constant for FER kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168572	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G1 phase at 0.01 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 67%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1425083	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1676513	Inhibition of human N-terminal GST-tagged EGFR L858R/T790M mutant (669 to 1210 residues) expressed in baculovirus infected Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 20 mins by HTRF as	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1724923	In vivo inhibition of EGFRvIII mutant in orthotopic patient derived GBM390 cells xenografted NSG mouse assessed as inhibition of PI3K-AKT-mTOR signaling by measuring reduction in S6 phosphorylation at 300 mg/kg, po administered twice daily for 3 days by G	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID1809360	Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44-positive cells measured after 24 hrs by MTT assay
AID1424973	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1219554	Inhibition of CYP3A4-mediated midazolam 1-hydroxylation in human liver microsomes at 50 uM	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID435663	Binding constant for full-length MST4	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID599959	Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
AID1425024	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625116	Binding constant for ADCK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435434	Binding constant for RET kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID441964	Inhibition of Her2 by fluorescence polarization assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID1168537	Inhibition of KDR (unknown origin) by ELISA method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID435799	Binding constant for FLT3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424893	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424917	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435441	Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424941	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425078	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625094	Binding constant for CDK11 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435794	Binding constant for EPHA3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256611	Average Binding Constant for RIPK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425110	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168576	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G1 phase at 0.1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 67%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID625049	Binding constant for PRKCH kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1353459	Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID624948	Binding constant for CSK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1186994	Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by Cell-Titer Glo assay	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
AID435786	Binding constant for full-length CLK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256621	Average Binding Constant for CAMK2A; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1402963	Inhibition of EGFR (unknown origin)	2018	European journal of medicinal chemistry, Jan-20, Volume: 144	Discovery of anilino-furo[2,3-d]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity.
AID1731362	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID624952	Binding constant for EPHA4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625120	Binding constant for EPHA8 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1664203	Inhibition of recombinant human wild type partial length HER4 (690 to 994 residues) expressed in bacterial expression system by competitive binding assay
AID624943	Binding constant for ACVR1B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636203	Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1636499	Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 150 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA	2016	Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16	Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1207374	Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform
AID624742	Binding constant for NEK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID638922	Inhibition of RON at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1424995	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1215641	Inhibition of human recombinant CYP3A5 at 50 uM preincubated up to 30 mins with NADPH in absence of GSH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1425171	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624728	Binding constant for NIM1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256617	Average Binding Constant for TEK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435277	Binding constant for full-length CDK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID546562	Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1424896	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625076	Binding constant for PLK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1674183	Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection method	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID624900	Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435795	Binding constant for EPHA4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425026	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1212341	Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay	2013	Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4	Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID1424905	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425154	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1676529	Inhibition of HER2-G776delinsVC mutant (unknown origin) expressed in human H1781 cells assessed as reduction in HER2 induced cell viability after 96 hrs by CellTiter-Glo assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID435444	Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425105	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1407097	Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID624988	Binding constant for ABL1(T315I)-non phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424936	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624944	Binding constant for ALK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436018	Binding constant for FLT4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1407096	Cytotoxicity against human Caco cells after 24 hrs by SRB assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID1425141	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256581	Average Binding Constant for CAMK1G; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1219578	Activity of recombinant CYP3A4 (unknown origin) assessed as 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde oxime formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID624919	Binding constant for AURKA kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1378273	Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA
AID1424983	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435802	Binding constant for KIT(V559D,V654A) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1219573	Drug metabolism in human liver microsomes assessed as N-((5-(4-(3-chloro-Drug metabolism in human liver microsomes assessed as 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde formation at 50 uM for 30 mins by LC/MS/MS	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1424984	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425153	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID546546	Inhibition of HDAC assessed as histone H3K'9+14 acetylation levels by cell based histone H3 hyperacetylation assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1638931	Inhibition of p38alpha MAPK (unknown origin) using ATF-2 as substrate after 1 hr by ELISA	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.
AID624980	Binding constant for ABL1(F317I)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1882632	Inhibition of EGFR (unknown origin)	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7	Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.
AID435323	Binding constant for RET(M918T) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435191	Binding constant for full-length RIOK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1724924	Inhibition of EGFRvII mutant in patient derived GBM39 cells assessed as effect on PI3K-AKT-mTOR signaling by measuring reduction in S6 phosphorylation by immunoblot analysis	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID435398	Binding constant for DAPK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425071	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1595622	Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells at 5 uM measured after 2 hrs by nanoBRET assay relative to control	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1425117	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1358761	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
AID624930	Binding constant for TNK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1439617	Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID435782	Binding constant for BRSK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID664740	Cytotoxicity against human MDA-MB-175 cells expressing Src, Ret and low HER-2 after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID1256452	Inhibition of EGFR (unknown origin) after 120 mins by HotSpot assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.
AID1718842	Inhibition of HER2 in human AU565 cells assessed as reduction in Akt phosphorylation at IC50 incubated after 24 to 72 hrs by Western blot analysis
AID463639	Inhibition of erbB2	2010	Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4	Selectively nonselective kinase inhibition: striking the right balance.
AID1425029	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425177	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435318	Binding constant for PAK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435900	Binding constant for AKT3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624734	Binding constant for YANK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID263983	Antiproliferative activity against human BT474 cell line	2006	Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9	Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.
AID624926	Binding constant for RIOK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID461251	Inhibition of EGFR	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID625045	Binding constant for PIK3CA(Q546K) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624724	Binding constant for TAK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624935	Binding constant for FLT3(D835H) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID441999	Toxicity in mouse bearing human A431 cells assessed as body weight loss at 10 mg/kg, po QD for 11 days	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID1219581	Activity of recombinant CYP3A5 (unknown origin) assessed as 2-chloro-4-(6-(5-(hydroxy(2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID624925	Binding constant for RIPK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424923	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1667573	Antiproliferative activity against human Calu3 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID1809367	Inhibition of Wnt/beta-Catenin signaling in drug-tolerant human MDA-MB-231/lapatinib cells assessed as reduction in p-GSK3beta level at 20 uM incubated for 24 hrs by Western blot analysis
AID624779	Binding constant for BTK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435827	Binding constant for PDGFRA kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424977	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID662803	Inhibition of EGFR at 10 uM after 50 mins by HTRF assay	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.
AID1168579	Induction of apoptosis in human BT474 cells at 0.1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 1%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID435429	Binding constant for FLT1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435941	Binding constant for ZAK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424898	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168559	Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1425097	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435291	Binding constant for FGFR3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1718879	Effect on human recombinant N-terminal GST-tagged MAPKAPK2 (46 to end residues) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay r
AID256649	Average Binding Constant for CSK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1426973	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1186992	Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 4 hrs by Cell-Titer Glo assay	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
AID1168549	Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID625066	Binding constant for IRAK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID263980	Inhibition of EGFR	2006	Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9	Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.
AID625067	Binding constant for NDR1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1731395	Inhibition of EGFR T790M mutant (unknown origin) at 10 uM relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID474116	Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
AID624921	Binding constant for MAP4K3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435408	Binding constant for INSR kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625101	Binding constant for TAOK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425065	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424929	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424920	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1256464	Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.
AID1158437	Cytotoxicity against human triple negative MDA-MB-231 cells	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1636388	Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 154.5 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of	2016	Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16	Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID625142	Binding constant for TSSK1B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624983	Binding constant for ABL1(H396P)-non phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624949	Binding constant for CSNK1G3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1667574	Inhibition of EGFR in human KB cells assessed as reduction in EGF-stimulated EGFR phosphorylation preincubated for 1 hr followed by EGF stimulation and measured after 6 mins by ELISA	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID1731411	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as GABA level in brain at 20 mg/kg, po for 10 days by ELISA relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID1425199	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425164	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256672	Average Binding Constant for CAMK2G; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424897	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424953	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624966	Binding constant for DCAMKL1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625021	Binding constant for LIMK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624820	Binding constant for ACVR2B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624965	Binding constant for LZK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425103	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435295	Binding constant for MAP4K3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435517	Binding constant for AKT2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435289	Binding constant for ERK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1718897	Antiproliferative activity against human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay
AID710534	Inhibition of ErbB2 at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID1425198	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID739090	Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei Lister 427 after 48 hrs by hemocytometer	2013	Journal of medicinal chemistry, May-23, Volume: 56, Issue:10	Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
AID435675	Binding constant for KIT(V559D,T670I) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425138	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624923	Binding constant for MAPKAPK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168562	Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624780	Binding constant for CDK4-cyclinD1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624773	Binding constant for AMPK-alpha1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625014	Binding constant for PRKCE kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625086	Binding constant for SLK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1212314	Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins	2013	Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4	Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
AID256571	Average Binding Constant for BIKE; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425038	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435830	Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1519083	Antiproliferative activity against human A2780 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
AID1718839	Down regulation of HER2 expression in human AU565 cells at IC50 incubated for 24 hrs by western blot analysis
AID1519084	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
AID1353462	Inhibition of EGFR T790M mutant (unknown origin) preincubated for 10 mins followed by TK substrate-botion addition measured after 1 hr by spectrophotometric method	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID1424990	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435553	Binding constant for PRKCD kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625000	Binding constant for EGFR(L747-E749del, A750P) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625102	Binding constant for PRKD2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624737	Binding constant for EPHA5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624755	Binding constant for ZAK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624939	Binding constant for FLT3(N841I) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256623	Average Binding Constant for MYLK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID638919	Inhibition of EPH-A2 at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1424894	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625143	Binding constant for CAMKK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624770	Binding constant for CAMK2D kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1158436	Cytotoxicity against human MDA-MB-435 cells	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID625065	Binding constant for CIT kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1545475	Inhibition of EGFR (unknown origin) expressed in baculovirus system assessed as reduction in phosphorylation of Peptide A incubated for 10 mins by scintillation counting	2019	European journal of medicinal chemistry, May-15, Volume: 170	Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
AID1718884	Effect on human recombinant N-terminal GST-tagged HER2 (676 to end residues) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay rela
AID625095	Binding constant for SIK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1674184	Toxicity in po dosed human assessed as maximum daily dose	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.
AID624768	Binding constant for SRPK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435193	Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1915714	Inhibition of HER2 (unknown origin)	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
AID638920	Inhibition of EPH-B2 at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID625107	Binding constant for DMPK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636192	Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1731363	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID624807	Binding constant for TNK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636188	Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID664631	Inhibition of wild-type EGFR preincubated for 10 mins followed by incubation for 30 mins by fluorescence polarization assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID624878	Binding constant for PIM1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425051	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1547466	Antiplasmodial activity against chloroquine-sensitive mefloquine resistant Plasmodium falciparum D6	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.
AID435290	Binding constant for FGFR2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625100	Binding constant for NLK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID634136	Inhibition of EGFR using poly(Glu,Tyr)4:1 as substrate and [gamma33P]ATP after 60 mins by scintillation counting	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435806	Binding constant for MAPKAPK5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625098	Binding constant for IRAK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435287	Binding constant for EPHA8 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435822	Binding constant for MEK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624749	Binding constant for CASK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625036	Binding constant for PIK3CA kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435281	Binding constant for full-length CSNK1A1L	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1894161	Inhibition of EGFR (unknown origin)	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
AID1168574	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at S phase at 0.01 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 19%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1424890	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424925	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1353504	Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 15 uM after 48 hrs by propidium iodide satining based FACS analysis (Rvb = 48.87%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID1425137	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436013	Binding constant for DMPK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424980	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436015	Binding constant for EPHA6 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624877	Binding constant for PIK3C2B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1215642	Irreversible inhibition of human recombinant CYP3A5 using testosterone as substrate assessed as residual enzyme activity at 50 uM preincubated up to 30 mins with NADPH followed by substrate addition measured after dialysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1424981	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625008	Binding constant for EPHA1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425111	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1532893	Inhibition of human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) T790M mutant expressed in baculovirus expression system after 1 hr in presence of ULight-labeled peptide substrate and ATP by LANCE ultra kinase assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID1904123	Inhibition of P-gp (unknown origin)	2022	European journal of medicinal chemistry, Apr-05, Volume: 233	Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID435805	Binding constant for MAP4K5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624789	Binding constant for KIT(D816V) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624765	Binding constant for TRKC kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256662	Average Binding Constant for ERBB2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425211	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435410	Binding constant for KIT kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624809	Binding constant for MYLK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625097	Binding constant for TNNI3K kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID270617	Inhibition of ErbB1	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID624762	Binding constant for DLK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1062013	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability at 10 uM after 48 hrs CellTiter-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID625093	Binding constant for TNIK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435276	Binding constant for BMPR1A kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256677	Average Binding Constant for STK38L; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425049	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1676514	Inhibition of human N-terminal GST-tagged EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus infected Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by HTRF assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1449628	Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method	2012	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12	Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1915705	Inhibition of EGFR (unknown origin)	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
AID435524	Binding constant for full-length CSNK1D	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1532896	Cytotoxicity against human A549 cells assessed as effect on intracellular ATP levels at 6 uM after 24 hrs by luciferase-luciferin based assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID1424934	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1330947	Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1532906	Cytotoxicity against mouse L929 cells assessed as cell growth inhibition at 1 uM after 72 hrs by MTT assay relative to control	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID1425176	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435694	Binding constant for TNK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1589077	Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 2.5 uM by luminescence based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID1595617	Antiproliferative activity against human UCH2 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1718872	Inhibition of HER2 L755S mutant (unknown origin) at 0.1 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID1718871	Inhibition of HER2 L755S mutant (unknown origin) at 0.5 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID1425125	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624830	Binding constant for CDK9 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435190	Binding constant for full-length PIP5K1A	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425174	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID638911	Inhibition of KDR at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1718883	Effect on human recombinant N-terminal GST-tagged HER4 (682 to 993) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to c
AID624893	Binding constant for MEK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424947	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256648	Average Binding Constant for RPS6KA5 (Kin.Dom 1); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424918	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425060	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425030	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435283	Binding constant for DAPK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435909	Binding constant for full-length LKB1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424974	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424978	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1731409	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as MDA level in brain at 20 mg/kg, po for 10 days by calorimetric method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID256612	Average Binding Constant for GAK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1738029	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by SRB assay	2020	European journal of medicinal chemistry, Jul-15, Volume: 198	Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
AID1676503	Ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells at 5 uM after 2 hrs by transwell assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID664633	Inhibition of HER2 preincubated for 10 mins followed by incubation for 30 mins by fluorescence polarization assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID624962	Binding constant for ASK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636196	Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID624862	Binding constant for LYN kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435662	Binding constant for MST2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624906	Binding constant for S6K1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425010	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625051	Binding constant for PRKCQ kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256590	Average Binding Constant for EPHB1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1353483	Induction of apoptosis in human A549 cells assessed as viable cells at 15 uM after 48 hrs by Annexin V-FITC/propidium iodide satining based FACS analysis (Rvb = 95.87%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID256654	Average Binding Constant for FGFR2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624991	Binding constant for ABL1-non phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1062012	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability at 10 uM after 48 hrs CellTiter-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID435189	Binding constant for full-length PDPK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1201367	Inhibition of EGFR (unknown origin) by Z'-LYTE assay	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	Truncated structures used in search for new lead compounds and in a retrospective analysis of thienopyrimidine-based EGFR inhibitors.
AID625088	Binding constant for ARK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID546545	Inhibition of HDAC in human HeLa cell nuclear extracts	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID625046	Binding constant for PIK3CB kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435525	Binding constant for EGFR(L858R) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424945	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425168	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625099	Binding constant for TAOK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425096	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425104	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435828	Binding constant for full-length PIP5K2B	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425058	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID634138	Inhibition of Erbb2 using poly(Glu,Tyr)4:1 as substrate and [gamma33P]ATP after 60 mins by scintillation counting	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1424970	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1678478	Inhibition of recombinant His6-tagged SARS-CoV-2 main protease assessed as residual enzyme activity at 100 uM using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay relative to con	2020	ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12	Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID1439623	Inhibition of EGFR phosphorylation at Y1068 in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID1425008	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1219557	Effect on CYP3A4-mediated midazolam 1-hydroxylation in human liver microsomes at 50 uM in presence of 2 mM ferricyanide	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID642761	Inhibition of EGFR T790M/L858R mutant expressed using baculovirus expression system by ELISA	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Discovery of novel selective inhibitors for EGFR-T790M/L858R.
AID1353505	Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 15 uM after 48 hrs by propidium iodide satining based FACS analysis (Rvb = 34.45%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID625072	Binding constant for TBK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1555852	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID1425018	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1207528	Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay
AID1425124	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624720	Binding constant for HIPK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624835	Binding constant for ERN1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624801	Binding constant for MAP3K15 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425001	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435528	Binding constant for IRAK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435651	Binding constant for DCAMKL2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425006	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256599	Average Binding Constant for TTK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425015	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1426975	Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID435325	Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168550	Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1268283	Inhibition of His-tagged human HER-2 cytoplasmic domain (676-1245 aa) (unknown origin) assessed as inhibition of autophosphorylation by TR-fluorometry	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID636385	Inhibition of human ErbB2 preincubated for 2 hrs prior addition of ATP by HTRF assay	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.
AID1555854	AUC (0 to 48 hrs) in human A549 cells overexpressing EGFR at 1 uM measured per 0.1 million cells by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID1168578	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at S phase at 0.1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 19%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624777	Binding constant for DDR2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435397	Binding constant for CSNK1G1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624850	Binding constant for DDR1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1407095	Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID1062010	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1425178	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1724902	In vivo inhibition of EGFRvIII mutant in orthotopic patient derived GBM390 cells xenografted NSG mouse assessed as inhibition of RAS-MAPK signaling by measuring reduction ERK phosphorylation at 300 mg/kg, po administered twice daily for 3 days by Gaussia	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID435203	Binding constant for TTK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636175	Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435279	Binding constant for full-length CDK9	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435158	Binding constant for EPHA5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624929	Binding constant for BRSK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1443989	Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1219575	Activity of recombinant CYP3A4 (unknown origin) assessed as N-((5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-yl)methylene)-2-(methylsulfonyl)ethanamine oxide formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1425112	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625087	Binding constant for MELK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID664634	Inhibition of HER4 preincubated for 10 mins followed by incubation for 30 mins by fluorescence polarization assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID435562	Binding constant for STK36 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1306589	Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay	2016	Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16	Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
AID1425017	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1366920	Cell cycle arrest in human K562 cells assessed as G1/G2-M ratio at GI50 concentration after 24 hrs by propidium iodide staining-based flow cytometry relative to control	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID1676512	Inhibiton of EGFR (unknown origin) expressed in human A431 cells assessed as reduction in EGFR induced cell viability after 96 hrs by CellTiter-Glo assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1207284	Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform
AID624785	Binding constant for JAK3(JH1domain-catalytic) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424916	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1724046	Inhibition of EGFR (unknown origin)	2020	Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18	Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.
AID625089	Binding constant for AAK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435687	Binding constant for PAK7/PAK5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624969	Binding constant for ROCK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256666	Average Binding Constant for ABL1(Q252H); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1809346	Inhibition of exogenous EGFR (unknown origin)
AID256665	Average Binding Constant for ABL1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1168575	Induction of apoptosis in human BT474 cells at 0.01 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 1%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID638082	Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor growth inhibition at 20 mg/kg, po QD for 14 days measured after 19 days	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
AID624931	Binding constant for CLK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425062	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168548	Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID636177	Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID256667	Average Binding Constant for ABL1(E255K); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1358763	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID435660	Binding constant for full-length MELK	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435393	Binding constant for CAMK1D kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435678	Binding constant for MUSK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID461261	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1718873	Effect on human recombinant N-terminal GST-tagged ROCK2 (5 to 554) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to co
AID1425163	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718823	Inhibition of HER2 in human BT474 cells assessed as reduction in Akt phosphorylation at IC50 incubated for 72 hrs by western blot analysis
AID435780	Binding constant for BMPR2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625003	Binding constant for EGFR(L858R) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624714	Binding constant for p38-alpha kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1492836	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation.
AID1424935	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624887	Binding constant for ERK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424987	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1595628	Antiproliferative activity against human UCH14 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID256625	Average Binding Constant for PAK3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID436049	Binding constant for PTK6 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID638917	Inhibition of ErbB2 at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1215637	Inhibition of human recombinant CYP3A5 using testosterone as substrate assessed as testosterone 6-beta-hydroxylation at 50 uM preincubated up to 30 mins without NADPH followed by substrate addition measured after 10 mins by LC/MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1425023	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1062008	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1724903	Antitumor activity against orthotopic patient derived GBM390 cells xenografted NSG mouse assessed as reduction in tumor growth at 300 mg/kg, po administered twice daily for 3 days by Gaussia luciferase reporter gene based immunoblotting analysis	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID1718836	Inhibition of HER2 in human AU565 cells assessed as reduction in expression of ERK phosphorylation at 0.5 IC50 incubated for 24 to 72 hrs by western blot analysis
AID624727	Binding constant for FYN kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718868	Inhibition of HER2 L755S mutant (unknown origin) at 10 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID1424968	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435399	Binding constant for DCAMKL3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1260760	Cytotoxicity against human HepG2 cells by MTT assay	2015	MedChemComm, Feb, Volume: 6, Issue:2	EVALUATION OF AROMATIC 6-SUBSTITUTED THIENOPYRIMIDINES AS SCAFFOLDS AGAINST PARASITES THAT CAUSE TRYPANOSOMIASIS, LEISHMANIASIS, AND MALARIA.
AID624799	Binding constant for TIE2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424926	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718891	Effect on human EGFR in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID436054	Binding constant for TLK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1463974	Inhibition of recombinant alpha-glucosidase (unknown origin) using PNP-G as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by spectrophotometric analysis	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase.
AID1676531	Inhibition of C-terminal His6-tagged HER2 (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 60 mins in presence of XL665-labeled streptavi	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID625069	Binding constant for TLK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624828	Binding constant for CDK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435793	Binding constant for EPHA1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1330926	Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID625136	Binding constant for YSK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1268281	Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID435171	Binding constant for NEK9 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436055	Binding constant for full-length YANK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1555849	Antiproliferative activity against human A549 cells overexpressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID662806	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.
AID1168534	Inhibition of HER2 (unknown origin) assessed as reduction in autophosphorylation by ELISA method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1555846	Inhibition of HER2 autophosphorylation in human HCC1954 cells overexpressing HER2 at 0.02 to 2 uM incubated for 1 hr by Western blot analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID435649	Binding constant for CDC2L2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID767293	Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Synthesis and SAR studies of marine natural products ma'edamines A, B and their analogues.
AID1168565	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624915	Binding constant for PIP5K2B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1562673	Induction of cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 15 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 51.73%)
AID624844	Binding constant for CDK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256657	Average Binding Constant for LCK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1718896	Antiproliferative activity against human BT474 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay
AID435664	Binding constant for MYLK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435201	Binding constant for TRKA kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425134	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718821	Inhibition of HER2 in human BT474 cells assessed as reduction in Akt phosphorylation at 0.1 IC50 incubated for 72 hrs by western blot analysis
AID636384	Inhibition of human EGFR preincubated 2 hrs prior addition of ATP by HTRF assay	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.
AID435907	Binding constant for EGFR(L861Q) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID546553	Inhibition of PDGFRbeta by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID435282	Binding constant for full-length CSNK1G2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425068	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625011	Binding constant for FGR kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424954	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID767291	Antiproliferative activity against human progesterone receptor and HER2 deficient CAMA1 cells expressing estrogen receptor after 72 hrs by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Synthesis and SAR studies of marine natural products ma'edamines A, B and their analogues.
AID1219583	Activity of recombinant CYP3A5 (unknown origin) assessed as N-((5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-yl)methylene)-2-(methylsulfonyl)ethanamine oxide formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID435199	Binding constant for TLK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435533	Binding constant for NEK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435322	Binding constant for PRKG2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID546563	Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID435693	Binding constant for TGFBR2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1330948	Antiproliferative activity against human NCI-H1975 expressing EGFR T790M/L858R mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID739089	Ratio of EC50 for human HepG2 cells to EC50 for bloodstream form Trypanosoma brucei brucei Lister 427	2013	Journal of medicinal chemistry, May-23, Volume: 56, Issue:10	Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
AID624898	Binding constant for GRK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425054	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436050	Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436051	Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1555845	Inhibition of human recombinant GST-tagged HER2 (catalytic domain 676 to end residues) autophosphorylation expressed in baculovirus infected Sf9 cells using poly( Glu, Tyr) 4:1 as substrate at 1 uM incubated for 60 mins by ELISA relative to control	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID624804	Binding constant for ERBB2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256626	Average Binding Constant for NTRK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID436044	Binding constant for PLK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425200	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256675	Average Binding Constant for PTK6; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425007	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1353461	Inhibition of EGFR L858R/T790M double mutant (unknown origin) using ULight-poly GT as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by spectrophotometric method	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID1547472	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes measured after 96 hrs by beta-galactosidase reporter gene assay	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.
AID1724921	Inhibition of EGFRvII mutant in patient derived GBM39 cells assessed as effect on PI3K-AKT-mTOR signaling by measuring reduction in AKT phosphorylation by immunoblot analysis	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID625042	Binding constant for PIK3CA(H1047Y) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718826	Inhibition of HER2 in human AU565 cells assessed as reduction in Akt expression level at 0.5 IC50 incubated for 72 hrs by western blot analysis
AID624836	Binding constant for IKK-beta kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID546552	Inhibition of HER2 by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1718835	Inhibition of HER2 in human AU565 cells assessed as reduction in Akt phosphorylation at 0.1 IC50 incubated for 24 hrs by western blot analysis
AID1667575	Inhibition of EGFR (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 40 mins in presence of ATP by caliper mobility shift assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID435297	Binding constant for MLK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256647	Average Binding Constant for SYK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624957	Binding constant for EPHB6 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435665	Binding constant for NEK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435939	Binding constant for TIE2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435442	Binding constant for SYK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636185	Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID624758	Binding constant for RIPK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425162	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID546559	Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID624933	Binding constant for PLK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1545925	Antiproliferative activity against human KG1a cells assessed as reduction in cell viability after 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Dec-01, Volume: 183	1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID624759	Binding constant for PFCDPK1(P.falciparum) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624741	Binding constant for LRRK2(G2019S) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435561	Binding constant for SRMS kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256576	Average Binding Constant for MKNK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID625113	Binding constant for MARK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1595624	Antiproliferative activity against human UCH7 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1731405	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as total power density at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID625001	Binding constant for EGFR(L747-S752del, P753S) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1202661	Growth inhibition of human SK/LapR1.0 cells at 5 uM incubated for 72 hrs by ATP detection based luminescent assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Design and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors.
AID256592	Average Binding Constant for LIMK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624781	Binding constant for CDK4-cyclinD3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624812	Binding constant for SBK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435405	Binding constant for ERK8 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624764	Binding constant for CLK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624897	Binding constant for RAF1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1330924	Inhibition of wild-type EGFR (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID624837	Binding constant for IRAK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625110	Binding constant for TRPM6 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435443	Binding constant for TXK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624909	Binding constant for TGFBR2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425155	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1244850	Inhibition of epidermal growth factor receptor kinase (unknown origin) using [33P]-ATP after 20 to 30 mins by radiometric assay	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
AID256567	Average Binding Constant for EPHA6; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID461252	Inhibition of HER2	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID624981	Binding constant for ABL1(F317L)-non phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624833	Binding constant for CSNK1G2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625039	Binding constant for PIK3CA(E545A) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436032	Binding constant for MYO3B kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624839	Binding constant for AKT2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624819	Binding constant for ACVR1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425052	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1731404	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as power pV2 at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID624992	Binding constant for ABL1-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424975	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624851	Binding constant for ERBB3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625013	Binding constant for LCK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425194	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425205	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624908	Binding constant for TEC kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435787	Binding constant for CLK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1731403	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as amplitude density at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID1731399	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as mean power frequency at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID435551	Binding constant for full-length p38-beta	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168586	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at S phase at 10 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 19%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1207314	Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID1425089	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168560	Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID435445	Binding constant for ZAP70 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425080	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1215634	Ratio of Kinact to Ki for recombinant human CYP3A4 using testosterone as substrate	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1425146	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435783	Binding constant for full-length BRSK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624945	Binding constant for BMPR1A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1439618	Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID636198	Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID624848	Binding constant for CSNK2A1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1426998	Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ig administered once daily for 28 days relative to control	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID1161351	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Synthesis and evaluation of 4-anilinoquinazoline bioisosteres as potential anti-breast cancer agents.
AID1425028	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1595616	Antiproliferative activity against human UCH1 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1424914	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424908	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1638929	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.
AID1425057	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625059	Binding constant for YSK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168573	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G2/M phase at 0.01 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 14%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID625020	Binding constant for ITK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID664632	Inhibition of EGFR T790M mutant preincubated for 10 mins followed by incubation for 30 mins by fluorescence polarization assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID1425143	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435804	Binding constant for LYN kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425102	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256560	Average Binding Constant for FGR; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435148	Binding constant for AMPK-alpha1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625139	Binding constant for SNARK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1215635	Inhibition of human recombinant CYP3A5 using testosterone as substrate assessed as testosterone 6-beta-hydroxylation at 2.5 to 50 uM preincubated up to 30 mins with NADPH followed by substrate addition by LC/MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID256573	Average Binding Constant for PAK6; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256608	Average Binding Constant for MARK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624907	Binding constant for SYK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1676510	Solubility of compound in aqueous buffer at pH 7.4 after 120 mins by turbidometric assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1425087	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625128	Binding constant for CSNK1G1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625091	Binding constant for MAST1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1219586	Activity of recombinant CYP3A5 (unknown origin) assessed as 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde oxime formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1425192	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718876	Effect on recombinant full-length human N-terminal GST-tagged SRC expressed in expressed in Escherichia coli in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID1207468	Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform
AID270621	Inhibition of HFF cell growth	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID435280	Binding constant for CSF1R kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1595634	Selectivity ratio of IC50 for human UCH14 cells to IC50 for human UCH1 cells	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1532894	Cytotoxicity against human A549 cells assessed as effect on intracellular ATP levels at 0 to 2 uM after 24 hrs by luciferase-luciferin based assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID1809361	Antiproliferative activity against drug-tolerant human MDA-MB-231/lapatinib cells assessed as CD44+/CD24- cells measured at 20 uM after 24 hrs by MTT assay
AID256658	Average Binding Constant for p38-beta; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1718887	Effect on human recombinant N-terminal GST-tagged FLT1 (784 to end residues) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay rela
AID624901	Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624994	Binding constant for AKT1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624811	Binding constant for PAK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1543688	Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID1555858	Antitumor activity against human A549 cells overexpressing EGFR xenografted in NOD/SCID mouse assessed as tumor volume at 86 micromol/kg, po administered once daily for 27 days measured at day 27 at 2 hrs after last administered dose (Rvb = 1869 +/- 134 m	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID546564	Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1463975	Inhibition of wild type recombinant EGFR (unknown origin) at 50 nM by ELISA relative to control	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase.
AID435293	Binding constant for JNK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256609	Average Binding Constant for AAK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1062011	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability at 10 uM after 48 hrs CellTiter-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID435674	Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1738027	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay	2020	European journal of medicinal chemistry, Jul-15, Volume: 198	Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
AID1425034	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1543664	Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID435294	Binding constant for full-length LIMK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1809331	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
AID636191	Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID256607	Average Binding Constant for STK18; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1062009	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1425175	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624891	Binding constant for JNK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1738032	Inhibition of EGFR L858R mutant (unknown origin) by FRET assay	2020	European journal of medicinal chemistry, Jul-15, Volume: 198	Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
AID625041	Binding constant for PIK3CA(H1047L) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435406	Binding constant for FLT3(D835H) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424993	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425179	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1202657	Growth inhibition of human BT474 cells at 5 uM incubated for 72 hrs by ATP detection based luminescent assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Design and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors.
AID546556	Inhibition of CDK2 by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID636165	Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1532891	Inhibition of wild type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system after 1 hr in presence of ULight-labeled peptide substrate and ATP by LANCE ultra kinase assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID1425118	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424939	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425053	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1595632	Selectivity ratio of IC50 for human CH22 cells to IC50 for human UCH1 cells	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1664200	Inhibition of recombinant human partial length EGFR L858R mutant (669 to 1011 residues) expressed in bacterial expression system by competitive binding assay
AID624746	Binding constant for WEE2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636161	Inhibition of ABL1 using poly(Ala, Glu, Lys, Tyr) as substrate and [gamma33P]ATP at 1 uM after 60 mins by scintillation counting	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1168589	Antitumor activity against human Calu3 cells xenografted in BALB/cA mouse assessed as tumor growth inhibition at 100 mg/kg, po	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID636189	Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1439615	Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID256561	Average Binding Constant for BTK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID636190	Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID624879	Binding constant for PIK3CG kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718889	Effect on recombinant full length human GST-tagged ERK2 expressed in Escherichia coli in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID435415	Binding constant for MYLK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1158442	Cytotoxicity against HUVEC	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID624937	Binding constant for FLT3(ITD) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624731	Binding constant for CAMK2G kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424933	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435432	Binding constant for MLK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1353485	Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 15 uM after 48 hrs by Annexin V-FITC/propidium iodide satining based FACS analysis (Rvb = 1.21%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID1425013	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID636387	Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay	2012	Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2	Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.
AID1219564	Activity of recombinant CYP3A4 (unknown origin) assessed as 2-chloro-4-(6-(5-(hydroxy(2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID435438	Binding constant for full-length p38-gamma	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1595630	Selectivity ratio of IC50 for human UCH7 cells to IC50 for human UCH1 cells	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID624795	Binding constant for MET(M1250T) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625033	Binding constant for PCTK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425009	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435777	Binding constant for ABL2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID664741	Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID1425181	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256601	Average Binding Constant for EPHA3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1525532	Inhibition of EGFR (unknown origin)	2019	Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22	Why Some Targets Benefit from beyond Rule of Five Drugs.
AID624845	Binding constant for CDK7 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718865	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay
AID345874	Inhibition of human recombinant EGFR at 100 uM	2009	Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4	Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.
AID1219577	Activity of recombinant CYP3A4 (unknown origin) assessed as N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((hydroxy(2 (methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID256598	Average Binding Constant for FRK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425186	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1873221	Inhibition of ABCG2 (unknown origin) expressed in human MCF7 cells membrane mediated [125I]iodoarylazidoprazosin photolabelling for 5 mins followed by UV light irradiation for 10 mins by radiometric scintillation analysis	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID625016	Binding constant for SRC kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1366918	Cell cycle arrest in human EOL-1 cells assessed as G1/G2-M ratio at GI50 concentration after 24 hrs by propidium iodide staining-based flow cytometry relative to control	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID256640	Average Binding Constant for PTK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435563	Binding constant for TNIK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425207	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID636166	Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1676504	Apparent permeability across apical side to basolateral side in human Caco-2 cells at 5 uM after 2 hrs by transwell assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID256642	Average Binding Constant for VEGFR2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID546558	Inhibition of PLK1 by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1718841	Inhibition of HER2 in human AU565 cells assessed as reduction in ERK phosphorylation at IC50 incubated for 72 hrs by western blot analysis
AID435789	Binding constant for full-length CSNK2A2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1215647	Drug metabolism assessed as recombinant human CYP3A5-mediated quinoneimine metabolite formation by measuring retention time at 50 uM after 60 mins by GSH trapping assay in presence of NADPH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1424906	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425012	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624766	Binding constant for p38-gamma kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168538	Inhibition of c-KIT (unknown origin) by ELISA method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624787	Binding constant for KIT(A829P) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625017	Binding constant for TIE1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID642762	Antiproliferative activity against human A549 cells over-expressing EGFR gene after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Discovery of novel selective inhibitors for EGFR-T790M/L858R.
AID1425121	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256616	Average Binding Constant for CDK5; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624784	Binding constant for INSR kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624860	Binding constant for VEGFR2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1443991	Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1425055	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256600	Average Binding Constant for EPHA8; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435327	Binding constant for VEGFR2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435166	Binding constant for full-length JNK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624896	Binding constant for PRKR kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1562608	Antiproliferative activity against human SW480 cells incubated for 72 hrs by MTT assay
AID1424988	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID636194	Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID624775	Binding constant for STK16 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624977	Binding constant for OSR1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1535425	Inhibition of EGF-induced EGFR phosphorylation at Tyr-residue in human HN5 cells preincubated for 24 hrs followed by EGF-stimulation and measured after 15 mins by Western blot analysis	2019	Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3	The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
AID1425150	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425182	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625044	Binding constant for PIK3CA(M1043I) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424942	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435904	Binding constant for full-length CSK	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435647	Binding constant for CAMK2D kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436048	Binding constant for full-length PTK2B	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625031	Binding constant for MRCKB kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1676507	Stability of compound in mouse plasma assessed as parent compound remaining at 5 uM measured for 1 hr by LC-MS analysis	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1425185	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435667	Binding constant for full-length NLK	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624847	Binding constant for CSNK1E kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424907	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624867	Binding constant for MLK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1207498	Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform
AID256597	Average Binding Constant for CLK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435328	Binding constant for YES kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1718874	Effect on human recombinant N-terminal GST-tagged PDGFRalpha (550 to end residues) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assa
AID256669	Average Binding Constant for ABL1(M351T); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1718870	Inhibition of HER2 L755S mutant (unknown origin) at 1 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID1424958	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624774	Binding constant for QSK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID638923	Inhibition of IGF1R at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1425072	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168563	Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624956	Binding constant for EPHB4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1062002	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2 at 10 uM after 2 hrs by Western blotting	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID624876	Binding constant for PDPK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624818	Binding constant for ULK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1062001	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2delta16 at 10 uM after 2 hrs by Western blotting	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID435204	Binding constant for WEE1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID270622	Selectivity for inhibition of averaged tumor cell growth over normal cell growth	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID436014	Binding constant for full-length DYRK1B	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1330944	Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID436005	Binding constant for ANKK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624873	Binding constant for PAK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1724898	Inhibition of EGFRvII mutant in patient derived GBM39 cells assessed as effect on RAS-MAPK signaling by measuring reduction ERK phosphorylation by immunoblot analysis	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID435779	Binding constant for ALK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624756	Binding constant for MAP4K4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID662802	Inhibition of EGFR at 100 uM after 50 mins by HTRF assay	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.
AID256651	Average Binding Constant for DAPK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425131	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624705	Binding constant for MYLK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625060	Binding constant for CAMKK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424957	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624840	Binding constant for AXL kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424967	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1664199	Inhibition of recombinant human wild type partial length EGFR (669 to 1011 residues) expressed in bacterial expression system by competitive binding assay
AID1330945	Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID625023	Binding constant for HIPK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624744	Binding constant for ZAP70 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424956	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID664742	Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID624942	Binding constant for DRAK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625119	Binding constant for CAMK1G kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435440	Binding constant for PIM2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625024	Binding constant for PRKD3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1186991	Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 4 hrs by Cell-Titer Glo assay	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
AID435151	Binding constant for CAMK1G kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256569	Average Binding Constant for PAK7/PAK5; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1118819	Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method	2011	MedChemComm, Jan-01, Volume: 2, Issue:8	Structure-activity relationship of conformationally constrained peptidomimetics for antiproliferative activity in HER2-overexpressing breast cancer cell lines.
AID1425149	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425048	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1543671	Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID1589081	Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 0.625 uM by luminescence based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID624910	Binding constant for TTK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435545	Binding constant for NEK6 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1439619	Inhibition of wild type recombinant EGFR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID1424969	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435659	Binding constant for full-length MARK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636182	Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1158440	Cytotoxicity against human taxoid-resistant MCF7 cells	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID435692	Binding constant for STK16 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624834	Binding constant for DAPK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624928	Binding constant for CDKL2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625078	Binding constant for SRPK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435778	Binding constant for full-length ADCK4	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID314993	Antitumor activity against human LoVo cells xenografted mouse at 100 mg/kg, bid	2008	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6	Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
AID1724907	Drug exposure in mouse plasma at 80 mg/kg, po after 24 hrs	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID624767	Binding constant for MERTK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425073	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435168	Binding constant for LTK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1219580	Activity of recombinant CYP3A5 (unknown origin) assessed as 2-chloro-4-(6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1724900	Growth inhibition of EGFRvII mutant patient derived GBM39 cells incubated at 100 to 300 nM for 72 hrs by Celltiter-Glo assay	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID461296	Antitumor activity against human MDA-MB-468 cells xenografted in nude CD1 mouse at 75 mg/kg, po daily relative to control	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID664743	Cytotoxicity against human JIMT1 cells expressing low HER-2 after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID435278	Binding constant for full-length CDK7	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID710535	Inhibition of EGFR at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA	2012	Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22	Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
AID1425188	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1366916	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID1422855	Cytotoxicity against human HepG2 cells	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.
AID435194	Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1676509	Kinetic solubility of compound in HEPES buffer a pH 7.4 at 500 uM after 90 mins	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID435559	Binding constant for SNARK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625050	Binding constant for PKN2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625132	Binding constant for FGFR1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624838	Binding constant for ACVR2A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424904	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425003	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256570	Average Binding Constant for PIM2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1168571	Induction of apoptosis in human BT474 cells at 0.001 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 1%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID256586	Average Binding Constant for STK4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425173	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425036	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425084	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID636181	Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID625074	Binding constant for IKK-epsilon kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1904124	Inhibition of BCRP (unknown origin)	2022	European journal of medicinal chemistry, Apr-05, Volume: 233	Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID638916	Inhibition of EGFR at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1424950	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1595650	Binding affinity to wild-type human partial length GAK (G13 to Y338 residues) expressed in bacterial expression system at 1 uM by Kinomescan method relative to control	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1330936	Inhibition of HER2 (unknown origin) expressed in baculovirus expression system using Biotin-(amino hexonoic acid)-EEEEYFELVAKKKCONH2 as substrate and [gamma32]-ATP measured after 10 mins by Topcount scintillation counting method	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID546555	Inhibition of ABL1 by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID624971	Binding constant for DAPK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID638067	Inhibition of EGFR by time-resolved fluorescence assay	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
AID435800	Binding constant for FYN kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1543686	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID435321	Binding constant for PRKCQ kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624864	Binding constant for CTK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID441962	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID624990	Binding constant for ABL1(Y253F)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624719	Binding constant for GRK7 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718898	Inhibition of HER2 (unknown origin) in presence of substrate incubated for 30 mins by ADP-Glo assay
AID1366911	Inhibition of recombinant human N-terminal GST-His6 tagged PDGFRalpha (Q551 to L1089 residues) expressed in Sf9 insect cells using poly(Ala,Glu,Lys,Tyr)6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID1439616	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID256578	Average Binding Constant for SLK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425157	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1358760	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
AID1724919	In vivo inhibition of EGFRvIII mutant in orthotopic patient derived GBM390 cells xenografted NSG mouse assessed as inhibition of PI3K-AKT-mTOR signaling by measuring reduction in AKT phosphorylation at 300 mg/kg, po administered twice daily for 3 days by	2020	ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10	Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
AID435286	Binding constant for EPHA7 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425197	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256603	Average Binding Constant for FER; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435526	Binding constant for FGFR1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436020	Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435652	Binding constant for EGFR(L747-E749del, A750P) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1244855	Inhibition of epidermal growth factor receptor kinase (unknown origin) using [33P]-ATP at 10 uM after 20 to 30 mins by radiometric assay	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
AID435319	Binding constant for PKN1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425202	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1219568	Drug metabolism in human liver microsomes assessed as 6-(5-(aminomethyl)furan-2-yl)-N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)quinazolin-4-amine formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID624914	Binding constant for WEE1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625027	Binding constant for MAP3K4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718838	Down regulation of HER2 expression in human AU565 cells at 0.5 IC50 incubated for 24 hrs by Western blot analysis
AID625092	Binding constant for NDR2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID638915	Inhibition of RET at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID435518	Binding constant for AURKA kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425059	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1667570	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID1424952	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256606	Average Binding Constant for STK16; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425209	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624788	Binding constant for KIT(D816H) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435326	Binding constant for TYRO3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624791	Binding constant for KIT(V559D) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1186996	Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by Cell-Titer Glo assay	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
AID1353455	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID256634	Average Binding Constant for CSNK1G2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID625057	Binding constant for TYRO3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435296	Binding constant for MARK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425040	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID636202	Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID638070	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
AID1219572	Drug metabolism in human liver microsomes assessed as 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde oxime formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID624987	Binding constant for ABL1(Q252H)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1904122	Inhibition of EGFR (unknown origin)	2022	European journal of medicinal chemistry, Apr-05, Volume: 233	Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
AID435908	Binding constant for EPHA2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624841	Binding constant for BLK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435677	Binding constant for LOK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168558	Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1315429	Antitumor activity against mouse LLC cells implanted in in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 14 days	2016	European journal of medicinal chemistry, Sep-14, Volume: 120	Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.
AID1168581	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G2/M phase at 1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 14%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID625114	Binding constant for GSK3A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624882	Binding constant for PKAC-beta kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424946	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424901	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624899	Binding constant for ROS1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435808	Binding constant for full-length MEK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624816	Binding constant for HPK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435311	Binding constant for HCK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625138	Binding constant for STK33 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1555844	Inhibition of human recombinant GST-tagged HER2 (catalytic domain 676 to end residues) autophosphorylation expressed in baculovirus infected Sf9 cells using poly( Glu, Tyr) 4:1 as substrate at 10 uM incubated for 60 mins by ELISA relative to control	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID435167	Binding constant for KIT(V559D) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435807	Binding constant for MARK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625037	Binding constant for PIK3CA(C420R) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636170	Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1425063	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1676528	Inhibition of HER2-A775_G776insYVMA mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in HER2 induced cell viability after 96 hrs by CellTiter-Glo assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID624883	Binding constant for PRKCI kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624747	Binding constant for SgK110 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1731396	Inhibition of HER2 (unknown origin) at 10 uM relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID624884	Binding constant for PRKD1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435910	Binding constant for MAP4K4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624970	Binding constant for CDK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435413	Binding constant for MLCK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625131	Binding constant for FGFR2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636172	Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID624855	Binding constant for FRK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256568	Average Binding Constant for STK17A; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1718890	Effect on human recombinant full-length ERK1 expressed in Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID1718878	Effect on recombinant full-length human N-terminal GST-tagged SYK expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to con
AID1424921	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1809334	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay
AID1425129	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID441966	Cytotoxicity against human NCI-H1975 cells after 24 hrs by MTT assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID624866	Binding constant for MLK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624825	Binding constant for BMPR1B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1168556	Inhibition of PDGFRbeta phosphorylation (unknown origin) expressed in human U87MG cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID436033	Binding constant for PIK3CA kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1545519	Inhibition of HER2 (unknown origin)	2019	European journal of medicinal chemistry, May-15, Volume: 170	Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
AID1219582	Activity of recombinant CYP3A5 (unknown origin) assessed as 6-(5-(aminomethyl)furan-2-yl)-N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)quinazolin-4-amine formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1425074	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425109	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256575	Average Binding Constant for NEK6; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1718824	Inhibition of HER2 in human BT474 cells assessed as reduction in HER2 expression at IC50 incubated for 24 hrs by western blot analysis
AID1425019	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435555	Binding constant for PRKR kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256610	Average Binding Constant for Aurora3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425210	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425027	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435196	Binding constant for full-length SRPK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424909	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624916	Binding constant for ULK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636205	Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID638921	Inhibition of c-Met at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID624997	Binding constant for EGFR(E746-A750del) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435165	Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435656	Binding constant for FGFR4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435198	Binding constant for TIE1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435531	Binding constant for MKNK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1407101	Inhibition of N-terminal GST-tagged recombinant human EGFR T790M mutant expressed in baculovirus infected Sf21 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID624790	Binding constant for KIT(L576P) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425158	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435930	Binding constant for PHKG2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636204	Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID546561	Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID624972	Binding constant for MTOR kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435164	Binding constant for IGF1R kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435431	Binding constant for MAP4K1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1407100	Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID435188	Binding constant for PAK6 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1676533	Apparent permeability across basolateral side to apical side in human Caco-2 cells at 5 uM after 2 hrs by transwell assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID624803	Binding constant for CHEK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256668	Average Binding Constant for ABL1(H396P); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624763	Binding constant for RIPK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435169	Binding constant for full-length MEK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625056	Binding constant for TESK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624968	Binding constant for DRAK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625117	Binding constant for PAK7 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1664201	Inhibition of recombinant human wild type partial length HER2 (646 to 1225 residues) expressed in mammalian expression system by competitive binding assay
AID624953	Binding constant for EPHA7 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435906	Binding constant for EGFR(L747-T751del,Sins) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435409	Binding constant for full-length JNK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1315427	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	2016	European journal of medicinal chemistry, Sep-14, Volume: 120	Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.
AID624739	Binding constant for GRK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624868	Binding constant for MST1R kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624754	Binding constant for NEK7 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624998	Binding constant for EGFR(G719C) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718866	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by WST8 assay
AID1219556	Inhibition of recombinant CYP3A5 (unknown origin)-mediated midazolam 1-hydroxylation at 50 uM	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID625141	Binding constant for RIOK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256624	Average Binding Constant for FGFR3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1215644	Inhibition of human recombinant CYP3A5 assessed as metabolite-inhibitor complex formation at 50 uM preincubated for 3 to 5 mins with NADPH A followed by NADPH B addition measured every 1 min for 10 mins by UV absorbance spectra analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID435275	Binding constant for BIKE kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID546565	Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1555857	AUC (0 to 24 hrs) in C57BL/6N mouse at 34 micromol/kg, po measured upto 24 hrs by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID624793	Binding constant for KIT(V559D,V654A) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625127	Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436022	Binding constant for full-length MEK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1562675	Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 15 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 14.36%)
AID624821	Binding constant for YANK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256635	Average Binding Constant for CAMK2D; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256589	Average Binding Constant for EPHA4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1215645	Inhibition of human recombinant CYP3A4 assessed as metabolite-inhibitor complex formation at 50 uM preincubated for 3 to 5 mins with NADPH A followed by NADPH B addition measured every 1 min for 10 mins by UV absorbance spectra analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID636171	Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1667576	Inhibition of HER2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 40 mins in presence of ATP by caliper mobility shift assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID435292	Binding constant for ITK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424960	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID638924	Inhibition of FGFR1 at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID256670	Average Binding Constant for ABL1(T315I); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624950	Binding constant for DMPK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425122	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID474117	Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
AID625038	Binding constant for PIK3CA(E542K) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256646	Average Binding Constant for JAK1 (Kin.Dom. 1); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID270619	Inhibition of BT474 cell growth after 72 hrs	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID624726	Binding constant for HIPK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718888	Effect on human recombinant N-terminal His-tagged FAK (393 to 698) expressed in Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID1728101	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs	2021	European journal of medicinal chemistry, Jan-15, Volume: 210	Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?
AID256632	Average Binding Constant for CDK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1407104	Inhibition of recombinant human FGFR preincubated for 5 mins followed by ATP addition and measured after 30 mind by HTRF assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID435897	Binding constant for ABL1(T315I) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624733	Binding constant for SIK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435430	Binding constant for INSRR kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435564	Binding constant for TRKB kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624735	Binding constant for ANKK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624806	Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718840	Inhibition of HER2 in human AU565 cells assessed as reduction in ERK phosphorylation at IC50 incubated for 24 hrs by western blot analysis
AID256574	Average Binding Constant for STK3_m; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435792	Binding constant for EGFR(S752-I759del) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1358764	Antiproliferative activity against human WM793B cells after 72 hrs by MTT assay
AID1595626	Antiproliferative activity against human CH22 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1532901	Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 8 uM after 72 hrs by FITC-annexin V/propidium iodide-double staining based flow cytometry (Rvb = 9.38%)	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID625129	Binding constant for HIPK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435404	Binding constant for EPHB4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636201	Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID410956	Cytotoxicity against human WI38 cells after 72 hrs by SRB assay	2009	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1	Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activity.
AID1366914	Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID1219585	Activity of recombinant CYP3A5 (unknown origin) assessed as N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((hydroxy(2 (methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID624938	Binding constant for FLT3(K663Q) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425107	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435784	Binding constant for CAMK2G kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624924	Binding constant for RIPK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624958	Binding constant for PIK3C2G kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1519082	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
AID624940	Binding constant for FLT3(R834Q) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425151	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436025	Binding constant for NDR2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424932	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624796	Binding constant for MET(Y1235D) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624776	Binding constant for PCTK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1158439	Cytotoxicity against human ER-positive MCF7 cells	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1215640	Inhibition of human recombinant CYP3A5 at 50 uM preincubated up to 30 mins with NADPH in presence of GSH	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID435522	Binding constant for CDK11 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425142	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID729550	Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay	2013	European journal of medicinal chemistry, Mar, Volume: 61	Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
AID435832	Binding constant for SLK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256629	Average Binding Constant for HCK; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID436010	Binding constant for full-length CDK5	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425190	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID441967	Cytotoxicity against human HS27 cells after 72 hrs by SRB assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID256638	Average Binding Constant for PRKAA1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624927	Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425037	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID509715	Inhibition of EGFR at 10 uM after 1 hr by ELISA	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Synthesis and biological evaluation of novel 2,4'-bis substituted diphenylamines as anticancer agents and potential epidermal growth factor receptor tyrosine kinase inhibitors.
AID624712	Binding constant for DYRK1A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID598797	Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines.
AID625112	Binding constant for YANK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1062006	Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID546557	Inhibition of PKA by flash plate based radioactive enzyme assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1424972	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1676530	Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins in presence of	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1315426	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	2016	European journal of medicinal chemistry, Sep-14, Volume: 120	Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.
AID435835	Selectivity for EGFR as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435688	Binding constant for full-length PCTK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1358762	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay
AID256643	Average Binding Constant for CAMK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624750	Binding constant for PRP4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436004	Binding constant for ACVR2A kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1562617	Inhibition of cell migration in CM-dil-labelled human A549 cells xenografted in 48 hrs post-fertilization zebrafish embryos at 15 uM incubated for 48 hrs by confocal microscopic method
AID636200	Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1425056	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435689	Binding constant for full-length PFTK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435798	Binding constant for FGR kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425035	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425120	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435905	Binding constant for full-length CSNK1G3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424889	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256637	Average Binding Constant for JNK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1168569	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G2/M phase at 0.001 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 14%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1425212	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1519085	Cytotoxicity against human MRC5 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
AID1545924	Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability after 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Dec-01, Volume: 183	1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
AID435679	Binding constant for PIM3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168557	Inhibition of KDR phosphorylation (unknown origin) expressed in human HUVEC at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1424930	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625276	FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI	2011	Drug discovery today, Aug, Volume: 16, Issue:15-16	FDA-approved drug labeling for the study of drug-induced liver injury.
AID1186993	Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 4 hrs by Cell-Titer Glo assay	2014	Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
AID1424951	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435532	Binding constant for MST3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624852	Binding constant for FES kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435411	Binding constant for KIT(D816V) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624913	Binding constant for TYK2(JH2domain-pseudokinase) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625082	Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1353506	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 15 uM after 48 hrs by propidium iodide satining based FACS analysis (Rvb = 16.09%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID625080	Binding constant for EIF2AK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636160	Inhibition of VEGFR2 using poly(Glu,Tyr)4:1 as substrate and [gamma33P]ATP after 60 mins by scintillation counting	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1595618	Binding affinity to wild-type human partial length EGFR (R669 to V1011 residues) expressed in bacterial expression system by Kinomescan method	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID625052	Binding constant for PRKG1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424931	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1664190	Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assay
AID664745	Cytotoxicity against human NCI-H1781 cells expressing HER-2 G776insV_G/C after 72 hrs by SRB assay	2012	Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6	Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.
AID624722	Binding constant for MKK7 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636178	Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1425213	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1168585	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G2/M phase at 10 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 14%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID256615	Average Binding Constant for p38-gamma; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424919	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425081	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1676505	Intrinsic clearance in mouse liver microsomes at 3 uM measured up to 60 mins by LC-MS analysis	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID624721	Binding constant for MEK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID599957	Binding affinity to human KIT incubated for 1 hr by kinase binding assay	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
AID1718880	Effect on human recombinant N-terminal GST-tagged KDR (789 to end) expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to co
AID1676515	Inhibition of human N-terminal GST-tagged EGFR (669 to 1210 residues) expressed in baculovirus infected Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 25 mins by HTRF assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID436017	Binding constant for ERK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID461257	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1425196	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1589076	Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 1.25 uM by luminescence based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID1168577	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G2/M phase at 0.1 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 14%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID256565	Average Binding Constant for MAP4K5; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1731407	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as theta at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID625104	Binding constant for MYO3A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636176	Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID625123	Binding constant for RET(V804L) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624963	Binding constant for LATS1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425016	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624715	Binding constant for ERK8 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1330925	Inhibition of HER2 (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysis	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID1555850	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID624798	Binding constant for LKB1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435833	Binding constant for full-length TNK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624723	Binding constant for CSNK1A1L kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID636199	Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID638910	Inhibition of Flt-1 at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID256661	Average Binding Constant for PDGFRB; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624892	Binding constant for p38-delta kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425165	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435676	Binding constant for LCK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1366919	Cell cycle arrest in human HCC827 cells assessed as G1/G2-M ratio at GI50 concentration after 24 hrs by propidium iodide staining-based flow cytometry relative to control	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID624802	Binding constant for PIM3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625040	Binding constant for PIK3CA(E545K) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625085	Binding constant for ULK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1532907	Cytotoxicity against mouse L929 cells assessed as cell growth inhibition after 72 hrs by MTT assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID461263	Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID624794	Binding constant for MET kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625055	Binding constant for MST1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624824	Binding constant for PIP5K1A kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256564	Average Binding Constant for MAP3K4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435412	Binding constant for MAP3K5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425033	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435433	Binding constant for full-length MST1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624888	Binding constant for ERK5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435826	Binding constant for full-length PCTK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1664192	Inhibition of EGFR L858R mutant (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assay
AID435180	Binding constant for MAPKAPK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624974	Binding constant for PIK3CD kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435932	Binding constant for PKAC-alpha kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435557	Binding constant for RIPK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1738033	Inhibition of EGFR T790M mutant (unknown origin) by FRET assay	2020	European journal of medicinal chemistry, Jul-15, Volume: 198	Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
AID638069	Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
AID1339612	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.
AID1424943	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1738028	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by SRB assay	2020	European journal of medicinal chemistry, Jul-15, Volume: 198	Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
AID1425090	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624973	Binding constant for JAK2(JH1domain-catalytic) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1330935	Inhibition of EGFR (unknown origin) expressed in baculovirus expression system using Biotin-(amino hexonoic acid)-EEEEYFELVAKKKCONH2 as substrate and [gamma32]-ATP measured after 10 mins by Topcount scintillation counting method	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID624985	Binding constant for ABL1(M351T)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1731364	Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 48 hrs by MTT assay	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID435788	Binding constant for CLK4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID638918	Inhibition of c-Src at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID1425042	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435170	Binding constant for MYO3A kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425126	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1757239	Inhibition of HER2 ECD in human A549 cells assessed as reduction in HER2 intracellular kinase domain phosphorylation at 2 uM incubated for 40 hrs by Western blot analysis	2021	European journal of medicinal chemistry, Apr-15, Volume: 216	A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models.
AID1731412	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as Glutamate level in brain at 20 mg/kg, po for 10 days by ELISA relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID624718	Binding constant for PFTAIRE2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435402	Binding constant for EGFR(G719S) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1202659	Growth inhibition of human MDA-MB-361 cells at 5 uM incubated for 72 hrs by ATP detection based luminescent assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Design and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors.
AID636167	Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435161	Binding constant for FES kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168561	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID625126	Binding constant for TAOK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624717	Binding constant for JNK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256572	Average Binding Constant for STK36; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624827	Binding constant for CAMK2B kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625073	Binding constant for SGK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718867	Inhibition of HER2 L755S mutant (unknown origin) at 25 uM in presence of substrate incubated for 30 mins by ADP-Glo assay relative to control
AID435324	Binding constant for full-length RIOK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624978	Binding constant for ABL1(E255K)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718881	Effect on human JAK2 in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID546560	Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1424992	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1443995	Hepatotoxicity in human assessed as drug-induced liver injury	2014	Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3	Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID436009	Binding constant for full-length CAMK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625002	Binding constant for EGFR(L747-T751del,Sins) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1207344	Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID625058	Binding constant for VRK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624725	Binding constant for NEK11 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435776	Binding constant for ABL1(Y253F) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436047	Binding constant for full-length PRKX	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435654	Binding constant for full-length ERK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435202	Binding constant for TRKC kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1543663	Antiproliferative activity against human DU145 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID435162	Binding constant for FLT3(N841I) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624859	Binding constant for JAK1(JH1domain-catalytic) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424944	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1718894	Effect on human recombinant N-terminal GST-tagged B-Raf (416 to 766) expressed in baculovirus-infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to
AID624815	Binding constant for ERBB4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625028	Binding constant for ASK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1219558	Effect on recombinant CYP3A4 (unknown origin)-mediated midazolam 1-hydroxylation at 50 uM in presence of 2 mM ferricyanide	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1202658	Growth inhibition of human BT/LapR1.0 cells at 5 uM incubated for 72 hrs by ATP detection based luminescent assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Design and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors.
AID1330946	Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.
AID435396	Binding constant for CHEK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID598799	Antiproliferative activity against human HCT116 cells by MTT assay	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines.
AID1882631	Inhibition of HER2 (unknown origin)	2022	Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7	Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.
AID624996	Binding constant for EGFR kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1215633	Ratio of Kinact to Ki for recombinant human CYP3A5 using testosterone as substrate	2012	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7	Interaction of lapatinib with cytochrome P450 3A5.
AID1219587	Activity of recombinant CYP3A5 (unknown origin) assessed as 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID435192	Binding constant for ROS1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435150	Binding constant for ARK5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1219579	Activity of recombinant CYP3A4 (unknown origin) assessed as 5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-carbaldehyde formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1168547	Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID624989	Binding constant for ABL1(T315I)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625108	Binding constant for MKNK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435155	Binding constant for full-length DLK	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425043	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424899	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624881	Binding constant for PKAC-alpha kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425079	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424948	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256591	Average Binding Constant for EPHA5; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1378270	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay
AID1424996	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625043	Binding constant for PIK3CA(I800L) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624902	Binding constant for MEK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435896	Binding constant for AAK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435560	Binding constant for SNF1LK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435310	Binding constant for FLT3(ITD) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID728990	Antiproliferative activity against human MCF7 cells assessed as inhibition of mammosphere formation at 1 uM after 5 to 7 days by microscopic analysis relative to control	2013	Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5	Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.
AID1425106	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425076	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256622	Average Binding Constant for JNK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256579	Average Binding Constant for MAP3K5; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1339614	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.
AID1353456	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID624732	Binding constant for PYK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624716	Binding constant for CSNK1D kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436043	Binding constant for PKMYT1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435556	Binding constant for RAF1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID256585	Average Binding Constant for EPHA7; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1424961	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624895	Binding constant for MEK6 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID598798	Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines.
AID624813	Binding constant for MINK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425135	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1443980	Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch	2010	Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2	Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID263982	Antiproliferative activity against human HN5 cell line	2006	Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9	Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.
AID1555851	Antiproliferative activity against human HCC1954 cells overexpressing HER2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID546549	Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID1543692	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID625077	Binding constant for DAPK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424991	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424949	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435529	Binding constant for LATS1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625010	Binding constant for FER kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424900	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625062	Binding constant for MAP3K2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625134	Binding constant for PIP5K2C kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1378272	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay
AID1532892	Inhibition of wild type human N-terminal His-tagged HER2 cytoplasmic domain (676 to 1255 residues) expressed in baculovirus expression system after 1 hr in presence of ULight-labeled peptide substrate and ATP by LANCE ultra kinase assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID256653	Average Binding Constant for FGFR1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1407102	Inhibition of GST-tagged recombinant human VEGFR (789-end) expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID1772926	Inhibition of ErbB4 in human T47D cells assessed as suppression of neuregulin 1-induced autophosphorylation incubated for 90 mins by sandwich ELISA	2021	European journal of medicinal chemistry, Nov-15, Volume: 224	Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.
AID1207404	Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform
AID1268304	Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID625004	Binding constant for EGFR(L858R,T790M) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1422854	Antiparasitic activity against Trypanosoma brucei	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.
AID256595	Average Binding Constant for CLK3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624704	Binding constant for NEK9 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1407103	Inhibition of recombinant human GST-tagged HER2 (676-end) expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
AID624904	Binding constant for NEK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425086	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID461262	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID435938	Binding constant for TGFBR1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1595625	Antiproliferative activity against human UMCHOR1 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1718877	Effect on rat recombinant N-terminal GST-tagged c-MET expressed in baculovirus infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID435803	Binding constant for full-length LIMK1	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425108	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID404519	Inhibition of HER2	2008	Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12	Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.
AID435274	Binding constant for ACVR1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624912	Binding constant for TYK2(JH1domain-catalytic) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1667569	Antiproliferative activity against human NCI-N87 cells overexpressing HER2 assessed as cell growth inhibition measured after 72 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
AID625130	Binding constant for FGFR4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425020	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436024	Binding constant for MRCKA kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID638913	Inhibition of PDGFRalpha at 10 uM	2012	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1	Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
AID625009	Binding constant for EPHA3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435394	Binding constant for CAMK2B kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625071	Binding constant for STK39 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624920	Binding constant for MRCKA kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624792	Binding constant for KIT(V559D,T670I) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718886	Effect on human FLT4 in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay relative to control
AID624961	Binding constant for TGFBR1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435790	Binding constant for DRAK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424964	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1424963	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624858	Binding constant for JAK1(JH2domain-pseudokinase) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624894	Binding constant for MEK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1532904	Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 8 uM after 72 hrs by FITC-annexin V/propidium iodide-double staining based flow cytometry (Rvb = 6.59%)	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID624810	Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425161	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435911	Binding constant for MEK6 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625084	Binding constant for HUNK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1562609	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay
AID624946	Binding constant for BRAF kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625030	Binding constant for LOK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1366915	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID256588	Average Binding Constant for PCTK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435558	Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1339613	Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream forms after 48 hrs by presto blue dye based fluorescence assay	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.
AID435401	Binding constant for full-length DRAK2	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435648	Binding constant for CAMKK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1256453	Inhibition of HER2 (unknown origin) after 120 mins by HotSpot assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.
AID256577	Average Binding Constant for CLK4; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1425160	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425128	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID436006	Binding constant for full-length AURKC	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1201370	Inhibition of EGFR (unknown origin) after 40 mins by scintillation proximity assay	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	Truncated structures used in search for new lead compounds and in a retrospective analysis of thienopyrimidine-based EGFR inhibitors.
AID256671	Average Binding Constant for ABL1(Y253F); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624880	Binding constant for PIK4CB kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID436045	Binding constant for PRKD1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624936	Binding constant for FLT3(D835Y) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624761	Binding constant for CDC2L5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1718893	Effect on human recombinant N-terminal GST-tagged c-KIT (544 to end residues) expressed in baculovirus-infected Sf9 insect cells in presence of substrate and [gamma-32ATP] at 10 uM incubated for 30 mins by scintillation counting based radiometry assay rel
AID624967	Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435646	Binding constant for BLK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1268302	Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
AID1638930	Antiproliferative activity against human MDA231 cells after 72 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds.
AID256663	Average Binding Constant for INSR; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID625061	Binding constant for MAP4K5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624772	Binding constant for AURKB kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID461256	Antiproliferative activity against human HepG2 cells after hrs by ATP content assay	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1425201	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1589078	Anti-tubercular activity against Mycobacterium tuberculosis H37Rv expressing LuxABCDE assessed as relative luminescence by measuring ratio of RLU (test compound)/RLU(no compound) at 5 uM by luminescence based assay	2019	Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18	Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
AID435775	Binding constant for ABL1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435329	Binding constant for YSK1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1532889	Antiproliferative activity against human A431 cells after 72 hrs by MTT assay	2018	Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24	Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.
AID263981	Inhibition of ErbB2	2006	Bioorganic & medicinal chemistry letters, May-01, Volume: 16, Issue:9	Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.
AID256656	Average Binding Constant for p38-alpha; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624707	Binding constant for DCAMKL3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624738	Binding constant for MLCK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435933	Binding constant for PKN2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID517324	Inhibition of ERBb2 phosphorylation in human BT474 cells by ELISA	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
AID624853	Binding constant for FLT1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1426970	Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.
AID624918	Binding constant for DYRK2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID474115	Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
AID435655	Binding constant for ERK5 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID436011	Binding constant for full-length CLK3	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435931	Binding constant for PIM1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624863	Binding constant for MARK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424362	Inhibition of HER2 (unknown origin)	2017	European journal of medicinal chemistry, Dec-15, Volume: 142	How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.
AID1676511	Inhibiton of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as reduction in EGFR induced cell viability after 96 hrs by CellTiter-Glo assay	2020	Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20	Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
AID1168546	Inhibition of HER2 phosphorylation (unknown origin) expressed in human BT474 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID636164	Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID625047	Binding constant for AMPK-alpha2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424985	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425144	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID517322	Inhibition of IGF1R phosphorylation in human MIAPaCa cells by ELISA	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
AID1555855	Cmax in C57BL/6N mouse at 34 micromol/kg, po measured upto 24 hrs by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID625135	Binding constant for ADCK4 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1339611	Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay	2017	ACS medicinal chemistry letters, Mar-09, Volume: 8, Issue:3	Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.
AID435801	Binding constant for full-length GSK3A	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625015	Binding constant for ROCK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1353458	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID1543670	Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID624709	Binding constant for MYLK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435516	Binding constant for ADCK3 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1664189	Inhibition of HER2 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assay
AID624905	Binding constant for CDKL5 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624751	Binding constant for PIP5K1C kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID642763	Antiproliferative activity against human A431 cells over-expressing EGFR gene after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Discovery of novel selective inhibitors for EGFR-T790M/L858R.
AID1202660	Growth inhibition of human SKBR3 cells at 5 uM incubated for 72 hrs by ATP detection based luminescent assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Design and synthesis of piperidine derivatives as novel human heat shock protein 70 inhibitors for the treatment of drug-resistant tumors.
AID1425170	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID625293	Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in LTKB-BD	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID436023	Binding constant for MERTK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1595633	Selectivity ratio of IC50 for human UCH12 cells to IC50 for human UCH1 cells	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1425116	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256619	Average Binding Constant for RPS6KA3 (Kin.Dom. 1); NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435666	Binding constant for full-length NEK7	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435156	Binding constant for EGFR kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435898	Binding constant for ACVR1B kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168566	Cytotoxicity against human NCI-H460 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID256583	Average Binding Constant for CAMKK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID636193	Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435181	Binding constant for full-length p38-alpha	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435935	Binding constant for RIPK2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1425061	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1809365	Inhibition of cell migration in human drug-tolerant MDA-MB-231/lapatinib cells at 20 uM
AID256652	Average Binding Constant for CAMK2B; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435403	Binding constant for EPHB1 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID461258	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay	2010	Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5	Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
AID1636446	Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 188.9 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of	2016	Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16	Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID435552	Binding constant for PIK3CA(E545K) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1168584	Induction of cell cycle arrest in human BT474 cells assessed as accumulation at G1 phase at 10 uM incubated for 12 hrs by propidium iodide staining based flow cytometry (Rvb = 67%)	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.
AID1425148	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624783	Binding constant for FGFR3(G697C) kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435163	Binding constant for full-length GSK3B	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1562604	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
AID436019	Binding constant for FRK kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1353454	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID361657	Antiproliferative activity against human BT474 cells overexpressing ErB2	2008	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16	4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.
AID624871	Binding constant for PAK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1353486	Induction of apoptosis in human A549 cells assessed as necrotic cells at 15 uM after 48 hrs by Annexin V-FITC/propidium iodide satining based FACS analysis (Rvb = 0.14%)	2018	European journal of medicinal chemistry, Mar-10, Volume: 147	6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.
AID1425044	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256596	Average Binding Constant for CLK2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID435796	Binding constant for ERBB2 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID624959	Binding constant for MAP4K2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID624995	Binding constant for CSF1R kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1731402	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as amplitude at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID441963	Inhibition of Her1 by fluorescence polarization assay	2009	Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21	Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
AID624874	Binding constant for PCTK3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1366913	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay	2017	Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24	Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
AID435657	Binding constant for full-length IKK-epsilon	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1424998	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID624984	Binding constant for ABL1(H396P)-phosphorylated kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425069	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1555842	Inhibition of human recombinant GST-tagged EGFR (catalytic domain 695 to end residues) autophosphorylation expressed in baculovirus infected Sf9 cells using poly( Glu,Tyr) 4:1 as substrate at 1 to 10 uM incubated for 60 mins by ELISA	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID624748	Binding constant for EPHA6 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1219576	Activity of recombinant CYP3A4 (unknown origin) assessed as (5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-yl)methanol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID625029	Binding constant for BRK kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425094	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1425136	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1207562	Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform
AID256676	Average Binding Constant for SRC; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID636168	Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID1062004	Inhibition of HER2 delta16 mutant autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting	2014	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1	Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.
AID1425064	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1439622	Inhibition of EGFR phosphorylation at Tyr residue in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method	2017	Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7	Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
AID256620	Average Binding Constant for FLT3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1158438	Cytotoxicity against human triple negative MDA-MB-468 cells	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1424361	Inhibition of EGFR (unknown origin)	2017	European journal of medicinal chemistry, Dec-15, Volume: 142	How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.
AID642760	Inhibition of wild-type EGFR expressed using baculovirus expression system by ELISA	2012	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3	Discovery of novel selective inhibitors for EGFR-T790M/L858R.
AID1751473	Inhibition of EGFR (unknown origin)	2021	Bioorganic & medicinal chemistry letters, 09-15, Volume: 48	Angiokinase inhibition of VEGFR-2, PDGFR and FGFR and cell growth inhibition in lung cancer: Design, synthesis, biological evaluation and molecular docking of novel azaheterocyclic coumarin derivatives.
AID625064	Binding constant for PIM2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID256655	Average Binding Constant for CSNK1G1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256641	Average Binding Constant for ABL2; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID256614	Average Binding Constant for YES; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1219569	Drug metabolism in human liver microsomes assessed as N-((5-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)furan-2-yl)methylene)-2-(methylsulfonyl)ethanamine oxide formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID270620	Inhibition of N87 cell growth after 72 hrs	2006	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17	Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
AID435797	Binding constant for ERBB4 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435515	Binding constant for ABL1(Q252H) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID636174	Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
AID435523	Binding constant for CIT kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID729551	Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 10 uM by TR-FRET based binding assay	2013	European journal of medicinal chemistry, Mar, Volume: 61	Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
AID625118	Binding constant for CAMK1D kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID435781	Binding constant for full-length BMX	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID625105	Binding constant for EPHB2 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1424891	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID435195	Binding constant for SRC kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID435903	Binding constant for CDK8 kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1555853	Drug uptake in human A549 cells overexpressing EGFR at 1 uM measured after 48 hrs by LC-MS/MS analysis	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Design, synthesis and biological evaluation of novel substituted purine isosters as EGFR kinase inhibitors, with promising pharmacokinetic profile and in vivo efficacy.
AID625032	Binding constant for TRKB kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID625075	Binding constant for INSRR kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1425046	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID1158441	Cytotoxicity against mouse triple negative 4T1 cells	2014	Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14	The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID546566	Inhibition of HADC in human CAL27 cells overexpressing EGFR assessed as effect on histone H2 acetylation after 16 hrs by Western blot	2010	Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24	Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
AID624955	Binding constant for EPHB3 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1738031	Inhibition of EGFR (unknown origin) by FRET assay	2020	European journal of medicinal chemistry, Jul-15, Volume: 198	Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
AID1731408	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as alpha at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID1425203	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry	2017	Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367	The target landscape of clinical kinase drugs.
AID256673	Average Binding Constant for PAK1; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID624823	Binding constant for MKNK1 kinase domain	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1809366	Inhibition of Wnt/beta-Catenin signaling in drug-tolerant human MDA-MB-231/lapatinib cells assessed as reduction in beta-catenin level at 20 uM incubated for 24 hrs by Western blot analysis
AID1809332	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
AID256636	Average Binding Constant for JNK3; NA=Not Active at 10 uM	2005	Nature biotechnology, Mar, Volume: 23, Issue:3	A small molecule-kinase interaction map for clinical kinase inhibitors.
AID1543674	Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
AID662804	Inhibition of EGFR after 50 mins by HTRF assay	2012	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12	Discovery of novel EGFR tyrosine kinase inhibitors by structure-based virtual screening.
AID435831	Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain	2008	Nature biotechnology, Jan, Volume: 26, Issue:1	A quantitative analysis of kinase inhibitor selectivity.
AID1219567	Drug metabolism in human liver microsomes assessed as 2-chloro-4-(6-(5-(hydroxy(2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-ylamino)phenol formation at 50 uM for 30 mins by LC/MS/MS analysis	2013	Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5	Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
AID1731401	Anticonvulsant activity against mouse model of LiCa/pilocarpine-induced status epilepticus assessed as total power at 20 mg/kg, po for 10 days by EEG method relative to control	2021	European journal of medicinal chemistry, Mar-15, Volume: 214	Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.
AID1595623	Cytotoxicity against human WS1 cells measured after 72 hrs by alamar blue assay	2019	Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9	Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508629	Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508628	Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508612	NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling	2017	Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3	Highly predictive and interpretable models for PAMPA permeability.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627	Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508591	NCATS Rat Liver Microsome Stability Profiling	2020	Scientific reports, 11-26, Volume: 10, Issue:1	Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347113	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID686947	qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen	2013	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15	Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1347126	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1645871	NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling in pH 5 buffer	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability.
AID1645848	NCATS Kinetic Aqueous Solubility Profiling	2019	Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14	Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1798859	Receptor Tyrosine Kinase Inhibition Assay from Article 10.1073/pnas.0708281105: \\6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.\\	2008	Proceedings of the National Academy of Sciences of the United States of America, Feb-26, Volume: 105, Issue:8	6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.
AID1795774	Kinase Inhibition Assay from Article 10.1016/j.bmcl.2003.10.010: \\Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.\\	2004	Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1	Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
AID1799771	Enzyme Assay from Article 10.1074/jbc.M110.206193: \\Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.\\	2011	The Journal of biological chemistry, May-27, Volume: 286, Issue:21	Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.
AID1345653	Human erb-b2 receptor tyrosine kinase 2 (Type I RTKs: ErbB (epidermal growth factor) receptor family)	2011	Nature biotechnology, Oct-30, Volume: 29, Issue:11	Comprehensive analysis of kinase inhibitor selectivity.
AID1345653	Human erb-b2 receptor tyrosine kinase 2 (Type I RTKs: ErbB (epidermal growth factor) receptor family)	2001	Molecular cancer therapeutics, Dec, Volume: 1, Issue:2	The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo.
AID1345502	Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family)	2001	Molecular cancer therapeutics, Dec, Volume: 1, Issue:2	The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo.
AID493017	Wombat Data for BeliefDocking	2004	Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1	Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
AID1811	Experimentally measured binding affinity data derived from PDB	2004	Cancer research, Sep-15, Volume: 64, Issue:18	A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells.
AID977610	Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB	2004	Cancer research, Sep-15, Volume: 64, Issue:18	A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	300 (16.09)	29.6817
2010's	1268 (67.99)	24.3611
2020's	297 (15.92)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	305 (15.89%)	5.53%
Reviews	331 (17.25%)	6.00%
Case Studies	82 (4.27%)	4.05%
Observational	9 (0.47%)	0.25%
Other	1,192 (62.12%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (286)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Phase II Clinical Study of Lapatinib (GW572016) in Patients With ErbB2 Over - Expressing Advanced or Metastatic Breast Cancer [NCT00320411]	Phase 2	62 participants (Actual)	Interventional	2005-11-28	Completed
Phase Ib Study of Preoperative Chemotherapy With Paclitaxel, Gemcitabine, and Lapatinib (Tykerb®) (PGT) in Patients With HER2 Positive Operable Breast Cancer [NCT01133912]	Phase 1	13 participants (Actual)	Interventional	2009-03-31	Completed
A Randomized, Multicenter, Double-Blind, Placebo-Controlled, 2-Arm, Phase III Study of Oral GW572016 in Combination With Paclitaxel in Subjects Previously Untreated or Advanced or Metastatic Breast Cancer [NCT00075270]	Phase 3	580 participants (Actual)	Interventional	2004-01-31	Completed
A Phase II Study Evaluating the Efficacy and Safety of Lapatinib + Vinorelbine in ErbB2 Positive Metastatic Breast Cancer Patients Pretreated With Chemotherapy or Hormonal Treatment in Combination With Lapatinib for Metastatic Disease [NCT01161368]	Phase 2	9 participants (Actual)	Interventional	2010-09-30	Terminated(stopped due to poor recruitment)
A Phase 2 Multicenter Trial Comparing Two Schedules of GW572016 as First or Second Line Monotherapy in Subjects With Advanced or Metastatic Non-Small Cell Lung Cancer With Either Bronchioloalveolar Carcinoma or No Smoking History [NCT00073008]	Phase 2	131 participants (Actual)	Interventional	2003-11-30	Terminated(stopped due to Based on interim analysis at the end of Stage 1, and predefined stopping rules for futility, further enrollment was stopped due to lack of efficacy)
A Randomized, Double Blind, Placebo-Controlled, Multicenter, Phase III Study Comparing the Activity of Paclitaxel Plus Trastuzumab Plus Lapatinib to Paclitaxel Plus Trastuzumab Plus Placebo in Women With ErbB2 Overexpressing Metastatic Breast Cancer [NCT00272987]	Phase 3	63 participants (Actual)	Interventional	2005-12-13	Terminated(stopped due to Enrollment was closed after the open label stage due to poor recruitment rate (randomized stage never opened).)
Pilot Study of Lapatinib (Tyverb®) in Neoadjuvant Treatment for Patients With Locally Bladder Carcinoma Before Cystectomy [NCT01245660]	Early Phase 1	3 participants (Actual)	Interventional	2011-01-31	Terminated(stopped due to The rythm of enrollment was not compatible with the objective of recruitement in the research.)
Phase II Trial of Pulse Dosing of Lapatinib in Combination With Temozolomide and Regional Radiation Therapy for Upfront Treatment of Patients With Newly-Diagnosed Glioblastoma Multiforme [NCT01591577]	Phase 2	50 participants (Actual)	Interventional	2012-12-07	Active, not recruiting
An Open-label Positron Emission Tomography Study to Investigate and Quantify Brain and Tumour Penetration of [11C]Lapatinib in Subjects With HER2-overexpressing Breast Cancer [NCT01290354]	Phase 1	10 participants (Actual)	Interventional	2011-09-12	Completed
A Phase 1 and Pharmacologic Study of MM-111 in Combination With Multiple Treatment Regimens in Patients With Advanced HER2 Positive Solid Tumors [NCT01304784]	Phase 1	100 participants (Anticipated)	Interventional	2011-01-31	Completed
A Phase II Evaluation Of Lapatinib (GW572016) (NCI-Supplied Agent, NSC #727989) In The Treatment Of Persistent Or Recurrent Endometrial Carcinoma [NCT00096447]	Phase 2	31 participants (Actual)	Interventional	2004-11-30	Completed
Effectiveness of First Line Treatment With Lapatinib and ECF/X in Histologically Proven Adenocarcinoma of the Stomach or the Esophagogastric Junction, Metastatic or Not Amenable to Curative Surgery According to HER2 and EGFR Status: a Randomized Phase II [NCT01123473]	Phase 2	29 participants (Actual)	Interventional	2010-12-31	Terminated(stopped due to company withdrew interest)
PHASE II STUDY Evaluating the Toxicity and Activity of the Combination Lapatinib + Capecitabine in Elderly Patients Aged 70 and Over With Metastatic Breast Cancer Over Expressing HER2 [NCT01262469]	Phase 2	4 participants (Actual)	Interventional	2009-12-31	Completed
Phase I/II Trial of Primary Chemotherapy With Non-pegylated Liposomal Doxorubicin, Paclitaxel and Lapatinib in Patients With HER2-positive Early [NCT01172223]	Phase 1/Phase 2	81 participants (Actual)	Interventional	2007-09-30	Completed
Targeted Therapy Selection Based on Tumor Tissue Kinase Activity Profiles for Patients With Advanced Solid Malignancies, an Exploratory Study [NCT01190241]		45 participants (Actual)	Interventional	2010-08-31	Terminated
A Phase 1/2 Study to Evaluate the Safety, Tolerability, and Preliminary Efficacy of KW-2450 in Combination With Lapatinib and Letrozole in Subjects With Advanced or Metastatic Breast Cancer Whose Tumors Overexpress HER2 [NCT01199367]	Phase 1	11 participants (Actual)	Interventional	2010-12-31	Terminated(stopped due to The results of the dose escalation phase did not identify a well-tolerated dose that would permit further study in Phase 2.)
Randomized Study of Efficacy & Safety of Lapatinib & Epirubicin & Cyclophosphamide (EC90) Followed by Paclitaxel & Lapatinib Compared With EC90 Followed by Paclitaxel & Trastuzumab, as Neoadjuvant Therapy in Patients With Previously Untreated ErbB2-overex [NCT01205217]	Phase 2	0 participants (Actual)	Interventional	2010-12-31	Withdrawn(stopped due to Data presented at SABCS 2010 showing that dual blockade is superior to monotherapy)
A Randomized Trial With Factorial Design Comparing Fulvestrant ± Lapatinib ± Aromatase Inhibitor in Metastatic Breast Cancer Progressing After Aromatase Inhibitor Therapy [NCT02394496]	Phase 3	396 participants (Anticipated)	Interventional	2007-11-30	Recruiting
Single Arm Phase II Study of Docetaxel and Lapatinib in Metastatic Transitional Cell Carcinoma in Bladder as Second Line Treatment [NCT01382706]	Phase 2	15 participants (Actual)	Interventional	2011-06-13	Terminated(stopped due to Trial not progressing toward scientific goals)
An Open-Label Randomized, Parallel, Two-Arm Phase II Study Comparing BMS-690514 + Letrozole With Lapatinib + Letrozole in Recurrent and Metastatic Breast Cancer Patients Who Are Hormone Receptor Positive Despite HER2 Status And Who Relapsed While Receivin [NCT01068704]	Phase 2	4 participants (Actual)	Interventional	2010-06-30	Completed
Phase Ib Trial of Trastuzumab Emtansine In Combination With Lapatinib Plus Abraxane In Metastatic Her 2 Neu Over-Expressed Breast Cancer Patients [NCT02073916]	Phase 1	24 participants (Actual)	Interventional	2013-10-31	Completed
Occurrence of Brain Metastasis in Breast Cancer Patients Diagnosed at Advanced Stages of the Disease [NCT01077648]		1 participants (Actual)	Observational	2010-02-28	Completed
A Phase I Study of Lapatinib and Cetuximab in Patients With Solid Tumors [NCT01184482]	Phase 1	22 participants (Actual)	Interventional	2010-06-30	Completed
Molecular Biology and Phase II Study of Lapatinib (GW572016) in Pediatric Patients With Recurrent or Refractory Medulloblastoma, Malignant Glioma or Ependymoma [NCT00095940]	Phase 1/Phase 2	52 participants (Actual)	Interventional	2004-10-31	Completed
Endocrine Therapy With or Without Inhibition of EGF and HER2 Growth Factor Receptors: A Randomized, Double-Blind, Placebo-Controlled Phase III Trial of Fulvestrant With or Without Lapatinib (GW572016) for Postmenopausal Women With Hormone Receptor Positiv [NCT00390455]	Phase 3	295 participants (Actual)	Interventional	2006-09-15	Completed
A Multicenter Open-label, Phase I/II Dose Escalation Study of Oral Lapatinib in Combination With Docetaxel in Patients With HER-2 Positive Advanced or Metastatic Breast Cancer [NCT01044485]	Phase 1/Phase 2	17 participants (Actual)	Interventional	2008-11-30	Completed
A Phase 1 Trial of Lapatinib in Combination With 1) Sirolimus or 2) Metformin in Advanced Cancer [NCT01087983]	Phase 1	111 participants (Actual)	Interventional	2010-03-31	Completed
Sun Yat-sen University Cancer Center [NCT02362958]	Phase 2	159 participants (Actual)	Interventional	2015-01-09	Completed
A Phase III Trial to Compare the Safety and Efficacy of Lapatinib Plus Trastuzumab Plus an Aromatase Inhibitor (AI) vs. Trastuzumab Plus an AI vs. Lapatinib Plus an AI as 1st- or 2nd- Line Therapy in Postmenopausal Subjects With Hormone Receptor+, HER2-po [NCT01160211]	Phase 3	369 participants (Actual)	Interventional	2011-05-05	Completed
A Multicenter, Open Label, Randomized Phase II Trial of Presurgical Treatment With Single-Agent Trastuzumab (H) or Lapatinib (Ty) or the Combination of Trastuzumab and Lapatinib (H+Ty), Followed by Six Cycles of Docetaxel (T) and Carboplatin (C) With Tras [NCT00769470]	Phase 2	18 participants (Actual)	Interventional	2009-04-30	Completed
A Multi-centre, Open-label, Randomized Clinical Trial Comparing the Efficacy and Safety of the Antibody-drug Conjugate SYD985 to Physician's Choice in Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer [NCT03262935]	Phase 3	437 participants (Actual)	Interventional	2017-12-15	Completed
A Phase Ib Study of Lapatinib in Combination With Caelyx in Patients With Advanced HER2 Positive Pretreated Breast Cancer [NCT02131506]	Phase 1	11 participants (Actual)	Interventional	2009-12-31	Terminated(stopped due to Safety reasons)
A Phase II/III, Randomised, Two-Arm, Comparison of Maintenance Lapatinib Versus Placebo After First-Line Chemotherapy in Patients With HER1 and/or HER2 Overexpressing Locally Advanced or Metastatic Bladder Cancer [LaMB] [NCT00949455]	Phase 2/Phase 3	204 participants (Anticipated)	Interventional	2009-03-31	Active, not recruiting
N-of-1 Trial of Actionable Target Identification in Metastatic Cancer for Palliative Systemic Therapy [NCT02142036]	Phase 2	50 participants (Actual)	Interventional	2014-05-31	Completed
An Open Label Study to Examine the Effects of Low-Fat and High-Fat Meals on the Pharmacokinetics of Orally Administered Lapatinib in Metastatic ErbB2 Positive Breast Cancer Patients [NCT00821054]	Phase 1	24 participants (Actual)	Interventional	2009-03-06	Completed
The Role of Circulating Tumor DNA in Decision-making of Patients With Metastatic Colorectal Cancer After Failure of First-line Treatment Containing Cetuximab - a Single-center, Phase II Clinical Study [NCT04831528]		100 participants (Anticipated)	Observational	2021-04-10	Not yet recruiting
A Phase IV, Placebo-controlled Single Sequence Crossover Study to Evaluate the Effect of Repeat Oral Doses of Lapatinib on Cardiac Repolarization in Patients With Advanced Cancer [NCT01328054]	Phase 4	58 participants (Actual)	Interventional	2011-12-31	Completed
A Randomized, Double-Blind, Placebo-Controlled, Multicenter Phase III Study Comparing GW572016 and Letrozole Versus Letrozole in Subjects With Estrogen/Progesterone Receptor- Positive Advanced or Metastatic Breast Cancer [NCT00073528]	Phase 3	1,286 participants (Actual)	Interventional	2003-12-09	Completed
Lapatinib in Endocrine-Resistant Metastatic Breast Cancer [NCT00225758]	Phase 2	27 participants (Actual)	Interventional	2006-01-31	Terminated(stopped due to slow accrual)
A Phase II, Randomized, Open-label Study of Lapatinib Plus Chemotherapy Versus Trastuzumab Plus Chemotherapy as First-line Treatment for Women With HER2-positive and p95HER2-positive Metastatic Breast Cancer [NCT01137994]	Phase 2	0 participants (Actual)	Interventional	2011-10-31	Withdrawn
A Phase II Evaluation of Lapatinib (GW572016) (NCI-Supplied Agent, NSC #727989) in the Treatment of Persistent or Recurrent Epithelial Ovarian or Primary Peritoneal Carcinoma [NCT00113373]	Phase 2	28 participants (Actual)	Interventional	2005-05-31	Completed
Lapatinib Versus Lapatinib With Capecitabine as Second-line Treatment in Her2-Overexpressing Metastatic Gastro-Esophageal Cancer: A Randomized Phase II Trial [NCT01145404]	Phase 2	76 participants (Anticipated)	Interventional	2010-06-30	Terminated(stopped due to Changes of SoC for third line therapy resulting in poor recruitment)
Letrozole Versus Letrozole Plus Lapatinib (GW572016) in Hormone-sensitive, HER-2 Negative Operable Breast Cancer. A Double Blind Randomized Phase II Study With Biomarker Evaluation. [NCT00422903]	Phase 2	92 participants (Actual)	Interventional	2007-04-30	Completed
A Phase II Open Label, Multicenter Study to Evaluate the Efficacy and Safety of Daily Dose of Lapatinib in Advanced Breast Cancer Patients With HER-2 Non-amplified Primary Tumours and HER-2 Positive Circulating Tumour Cells or EGFR Positive Circulating Tu [NCT00820924]	Phase 2	23 participants (Actual)	Interventional	2008-06-30	Terminated
Effect of Perioperative AntiHER-2 Therapy on Early Breast Cancer Study - Biological Phase (EPHOS-B) [NCT01104571]	Phase 3	257 participants (Actual)	Interventional	2010-04-30	Active, not recruiting
Lapatinib and Whole Brain Radiotherapy for Patients With Brain Metastases From Lung and Breast Tumors. A Phase II Study of the Hellenic Cooperative Oncology Group (HeCOG). [NCT01218529]	Phase 2	82 participants (Actual)	Interventional	2010-10-31	Completed
Randomized Phase III Trial of Paclitaxel +Trastuzumab + Lapatinib Versus Paclitaxel + Trastuzumab as Neoadjuvant Treatment of HER2-Positive Primary Breast Cancer [NCT00770809]	Phase 3	305 participants (Actual)	Interventional	2008-12-01	Active, not recruiting
Combinational Therapy of Capecitabine, Lapatinib and Vinorelbine for the Treatment of Patients With her2/Neu Positive, Relapsed or Metastatic Breast Carcinoma Following Treatment Failure With Trastuzumab [NCT01238029]	Phase 1	12 participants (Actual)	Interventional	2010-10-31	Terminated(stopped due to new methods of treatment, no more patients appilicable for study)
An Open-Label Study of AMG 386 in Combination With Either Paclitaxel and Trastuzumab or Capecitabine and Lapatinib in Subjects With HER2-positive Locally Recurrent or Metastatic Breast Cancer [NCT00807859]	Phase 1	65 participants (Actual)	Interventional	2009-03-09	Completed
A Phase 1b Dose-Escalation Study of the AKT Inhibitor MK-2206 (NSC# 749607) Plus Lapatinib (NSC# 727989) Administered in Patients With HER2 Positive Metastatic Breast Cancer [NCT01281163]	Phase 1	4 participants (Actual)	Interventional	2011-01-31	Terminated
Phase II Trial of Lapatinib and RAD-001 for HER2 Positive Metastatic Breast Cancer [NCT01283789]	Phase 2	23 participants (Actual)	Interventional	2011-02-28	Active, not recruiting
A Phase II, Single-Arm, Multi-Center Study Evaluating the Combination of Vinorelbine and Lapatinib in Women With ErbB2 Overexpressing Metastatic Breast Cancer [NCT00709618]	Phase 2	44 participants (Actual)	Interventional	2008-06-30	Terminated(stopped due to Evolving standard of care practices in this disease setting was limiting enrolment and leading to a delay in delivering this study information to the public.)
Drug Use Investigation for TYKERB Tablet (All Case Investigation) [NCT01332396]		4,054 participants (Actual)	Observational	2009-06-30	Completed
Phase II Open-Label Study of Preoperative Weekly Paclitaxel and Carboplatin With Lapatinib (Tykerb®) in Patients With ErbB2-Positive Stage I-III Breast Cancer [NCT01309607]	Phase 2	34 participants (Anticipated)	Interventional	2011-04-30	Active, not recruiting
The Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy [NCT04591431]	Phase 2	400 participants (Actual)	Interventional	2020-10-07	Active, not recruiting
A Phase II, Randomised, Multi-Centre Study Evaluating Lapatinib in Combination With Vinorelbine or Capecitabine in Women With ErbB2 Overexpressing Metastatic Breast Cancer [NCT01013740]	Phase 2	112 participants (Actual)	Interventional	2009-11-25	Completed
A Phase I/II Trial of Ketoconazole, Hydrocortisone, Dutasteride and Lapatinib (KHAD-L) in Castration Resistant Prostate Cancer With Pre- and Post-therapy Tumor Biopsies [NCT00953576]	Phase 1/Phase 2	11 participants (Actual)	Interventional	2009-09-29	Terminated(stopped due to The study terminated early due to concerns about drug toxicity.)
Phase II Study of a Novel Capecitabine Dosing Schedule in Combination With Lapatinib, Based on the Norton-Simon Mathematical Method in Patients With HER2 Overexpressed/Amplified, Trastuzumab (Herceptin) -Refractory, Metastatic Breast Cancer [NCT00721630]	Phase 2	24 participants (Actual)	Interventional	2008-07-31	Completed
A Phase I/II Study of Foretinib in Combination With Lapatinib in Patients With Human Epidermal Growth Factor Receptor 2(HER2)Over-Expressing Metastatic Breast Cancer [NCT01138384]	Phase 1/Phase 2	19 participants (Actual)	Interventional	2010-10-27	Completed
LPT 111111- A Single-arm, Multicenter Phase II Study to Evaluate The Combination of Weekly Nanoparticle Albumin Bound Paclitaxel (Nab-Paclitaxel or ABRAXANE®) and Lapatinib (TYKERB®) in Women With No More Than One Prior Treatment for ErbB2 Overexpressing [NCT00709761]	Phase 2	60 participants (Actual)	Interventional	2008-07-02	Completed
A Randomised, Multicentre, Open-label Phase II Trial Investigating Activity of Chemotherapy and Lapatinib and Trastuzumab in Patients With HER2-positive Metastatic Breast Cancer (MBC) Refractory to Anti HER2 Therapies [NCT02238509]	Phase 2	154 participants (Anticipated)	Interventional	2014-11-30	Recruiting
Lapatinib Plus Caelyx in Patients With Advanced Metastatic Breast Cancer Following Failure of Trastuzumab Therapy - a Phase II Study [NCT00903656]	Phase 2	24 participants (Actual)	Interventional	2009-05-31	Terminated(stopped due to Caelyx was not available anymore)
A Phase II, Placebo Controlled, Double-Blind, Randomized, Discontinuation Study of Lapatinib Administered Orally to Subjects With ErbB2 Positive Ovarian, Gastric/Esophageal Adenocarcinoma, Uterine Serous Papillary, or Bladder Cancer [NCT00447226]	Phase 2	32 participants (Actual)	Interventional	2007-05-31	Terminated(stopped due to The study had failed to meet the primary objective of tumor response rate at 12 weeks from first dose.)
A Phase II Trial of Lapatinib and Trastuzumab With or Without Endocrine Therapy in Locally Advanced HER2 Overexpressing Breast Cancer Patients [NCT00548184]	Phase 2	65 participants (Actual)	Interventional	2008-05-31	Completed
Neo ALTTO (Neoadjuvant Lapatinib and/or Trastuzumab Treatment Optimisation) Study: A Randomised, Multicenter Open-label Phase III Study of Neoadjuvant Lapatinib, Trastuzumab and Their Combination Plus Paclitaxel in Women With HER2/ErbB2 Positive Primary B [NCT00553358]	Phase 3	455 participants (Actual)	Interventional	2008-01-05	Completed
A Phase II Study of Lapatinib and Capecitabine in the Treatment of Metastatic Pancreatic Cancer. [NCT00962312]	Phase 2	9 participants (Actual)	Interventional	2009-01-31	Completed
A Phase 3, Multicenter, Randomized, Open-label, Active-controlled Study of Trastuzumab Deruxtecan (DS-8201a), an Anti-HER2-antibody Drug Conjugate, Versus Treatment of Investigator's Choice for HER2-positive, Unresectable and/or Metastatic Breast Cancer S [NCT03523585]	Phase 3	608 participants (Actual)	Interventional	2018-08-01	Active, not recruiting
Phase II Study of Dose-Dense Doxorubicin and Cyclophosphamide (AC) Followed by Weekly Paclitaxel With Trastuzumab and Lapatinib in HER2/NEU-Overexpressed/Amplified Breast Cancer: Feasibility [NCT00482391]	Phase 2	95 participants (Actual)	Interventional	2007-03-31	Completed
A Randomized, Single Blinded, Placebo-controlled, Multi-centre, Phase II Study of Lapatinib in Patients With Locally Advanced Squamous Cell Carcinoma of the Head and Neck (SCCHN) [NCT00371566]	Phase 2	107 participants (Actual)	Interventional	2006-03-31	Completed
Study EGF107671 - a Phase II Study of Lapatinib Plus Topotecan or Lapatinib Plus Capecitabine in the Treatment of Recurrent Brain Metastases From ErbB2-Positive Breast Cancer Following Cranial Radiotherapy [NCT00437073]	Phase 2	22 participants (Actual)	Interventional	2007-05-31	Terminated(stopped due to Lapatinib-topotecan arm enrollment closed early per protocol amendment 2. Then enrollment into remaining arm terminated due to operational issues.)
An Open-label, Randomized, Adaptive Design, Two-period Crossover Study in Cancer Patients to Evaluate the Bioequivalence of Alternative Formulations of Lapatinib Compared to the Commercial Tablet [NCT00996762]	Phase 1	158 participants (Actual)	Interventional	2009-11-12	Completed
A Randomized Open-Label, Phase II Study of Lapatinib-capecitabine or Lapatinib-vinorelbine or Lapatinib/Gemcitabine in Subjects With Her2/Neu Amplified Metastatic Breast Cancer Patients Progression After Taxanes Treatment [NCT01050322]	Phase 2	142 participants (Actual)	Interventional	2009-11-30	Completed
A Phase II, Open-Label, Randomized, Multicenter Trial of Pazopanib (GW786034) in Combination With Lapatinib (GW572016) Compared to Pazopanib Monotherapy and Lapatinib Monotherapy in Subjects With FIGO Stage IVB or Recurrent or Persistent Cervical Cancer W [NCT00430781]	Phase 2	228 participants (Actual)	Interventional	2006-11-30	Completed
Chemotherapy Plus Lapatinib or Trastuzumab or Both in Her2+ Primary Breast Cancer. A Randomized Phase IIb Study With Biomarker Evaluation. [NCT00429299]	Phase 2	121 participants (Actual)	Interventional	2006-08-31	Completed
A Phase II Study of Lapatinib for Brain Metastases in Subjects With ErbB2-Positive Breast Cancer Following Trastuzumab-based Systemic Therapy and Cranial Radiotherapy [NCT00263588]	Phase 2	242 participants (Actual)	Interventional	2005-12-02	Completed
A Pilot Feasibility Study to Evaluate the Efficacy of Lapatinib in Eliminating Cytokeratin-positive Tumour Cells Circulating in the Blood of Women With Breast Cancer [NCT00694252]	Phase 2	20 participants (Actual)	Interventional	2008-07-31	Completed
Study of Resistance Mechanisms Against Lapatinib in Patients With ErbB-2-Positive Breast Cancers [NCT00898573]		0 participants (Actual)	Observational	2008-07-31	Withdrawn
Phase I Study Evaluating the Combination of Lapatinib + Vinorelbine in Patients With Locally Advanced or Metastatic Breast Cancer Overexpressing HER2 [NCT00513058]	Phase 1	33 participants (Actual)	Interventional	2007-06-30	Completed
Phase 1 Study of the Combination of Lapatinib and Temozolomide for the Treatment of Progressive Brain Disease in HER-2 Positive Breast Cancer [NCT00614978]	Phase 1	18 participants (Actual)	Interventional	2008-01-31	Completed
A Multicentre, Open-label, Randomised, Controlled Study of Molecularly Precision Target Therapy Based on Tumor Molecular Profiling With GEMOX in Advanced or Recurrent Extrahepatic Cholangiocarcinoma and Gallbladder Carcinoma [NCT02836847]	Phase 2	152 participants (Anticipated)	Interventional	2016-07-31	Recruiting
Phase I Study of Intermittent High-Dose Lapatinib in Tandem With Capecitabine for HER2 Overexpressed/Amplified Metastatic Breast Cancer With Central Nervous System (CNS) Metastases [NCT02650752]	Phase 1	11 participants (Actual)	Interventional	2016-01-06	Completed
An Open-Label, Two-Part, Single Sequence Study to Examine the Effects of Lapatinib on the Pharmacokinetics of Orally Administered Digoxin in Subjects With Metastatic ErbB2 Positive Breast Cancer [NCT00650910]	Phase 1	17 participants (Actual)	Interventional	2008-04-23	Completed
A Phase I/II Study of Lapatinib in Combination With Oxaliplatin and Capecitabine in Subjects With Advanced or Metastatic Colorectal Cancer [NCT00536809]	Phase 1	12 participants (Actual)	Interventional	2007-09-26	Completed
An Open-Label, Two-Part, Single Sequence Study to Examine the Effects of Esomeprazole on the Pharmacokinetics of Orally Administered Lapatinib in Subjects With Metastatic ErbB2 [NCT00849329]	Phase 1	12 participants (Actual)	Interventional	2009-03-10	Completed
A Randomized, Multicenter, Open-label, Phase III Study of Lapatinib (GW572016) in Combination With Weekly Paclitaxel Versus Weekly Paclitaxel Alone in the Second Line Treatment of ErbB2 Amplified Advanced Gastric Cancer [NCT00486954]	Phase 3	273 participants (Actual)	Interventional	2007-07-31	Completed
Pilot Neoadjuvant Trial in Breast Cancer With Combination of ABI-007 (Abraxane) and GW572016 (Lapatinib) [NCT00331630]	Early Phase 1	30 participants (Actual)	Interventional	2006-05-04	Completed
An Open-Label Multicenter Study Administering Lapatinib and Capecitabine (Xeloda) in Women With Advanced or Metastatic Breast Cancer [NCT00508274]	Phase 3	52 participants (Actual)	Interventional	2007-07-18	Terminated(stopped due to Primary analysis was completed in 2015 and data collection post 1-Jul-2019 was not reportable due to local regulations in China.)
A Multicenter Phase II Clinical Trial Assessing the Efficacy of the Combination of Lapatinib and Capecitabine in Patients With Non Pretreated Brain Metastasis From HER2 Positive Breast Cancer [NCT00967031]	Phase 2	45 participants (Actual)	Interventional	2009-04-30	Completed
Phase I and Pharmacokinetics Study of Lapatinib in Combination With Sorafenib in Patients With Advanced Refractory Solid Tumors [NCT00984425]	Phase 1	30 participants (Actual)	Interventional	2009-09-30	Completed
An Open-label, Single-arm, Multi-centre, Phase II Study of Oral Lapatinib in Combination With Paclitaxel as First-line Treatment for ErbB2-amplified Metastatic Breast Cancer Patients [NCT00356811]	Phase 2	57 participants (Actual)	Interventional	2006-05-31	Completed
A Phase II, Open-Label, Randomized, Multicenter Trial of GW786034 (Pazopanib) in Combination With Lapatinib (GW572016) Compared to Lapatinib Alone as First Line Therapy in Subjects With Advanced or Metastatic Breast Cancer With ErbB2 Fluorescence In Situ [NCT00347919]	Phase 2	189 participants (Actual)	Interventional	2006-07-31	Completed
A Phase II Study of GW572016 and Tamoxifen in Patients With Metastatic Breast Cancer Resistant to Single-Agent Tamoxifen [NCT00118157]	Phase 2	19 participants (Actual)	Interventional	2005-05-31	Completed
A Phase II, Open-Label Study of the Clinical Activity, Safety, and Tolerability of Lapatinib in Combination With Bevacizumab in Subjects With Advanced or Metastatic ErbB2-Overexpressing Breast Cancer [NCT00444535]	Phase 2	52 participants (Actual)	Interventional	2007-02-27	Completed
A Phase 1 Study of Dabrafenib in Combination With Lapatinib in BRAF Mutant Thyroid Cancer [NCT01947023]	Phase 1	21 participants (Anticipated)	Interventional	2013-09-27	Active, not recruiting
A Phase 2 Study of Lapatinib in Combination With Trastuzumab in Patients With HER2-Positive, Metastatic Breast Cancer [NCT00470704]	Phase 2	87 participants (Actual)	Interventional	2007-05-14	Active, not recruiting
A Phase II Neo-Adjuvant Study of Letrozole in Combination With Lapatinib in Post -Menopausal Patients With HER2-Positive and Hormone Receptor-Positive Operable Breast Cancer [NCT00499681]	Phase 2	6 participants (Actual)	Interventional	2007-07-31	Terminated(stopped due to slow accrual)
A Phase II Study of Dose-Dense Temozolomide and Lapatinib for Recurrent Low-Grade and Anaplastic Supratentorial, Infratentorial and Spinal Cord Ependymoma [NCT00826241]	Phase 2	58 participants (Actual)	Interventional	2009-01-31	Completed
Phase I/II Study of Lapatinib in Combination With Oral Vinorelbine for Metastatic Breast Cancer [NCT00912275]	Phase 1/Phase 2	46 participants (Actual)	Interventional	2008-11-24	Completed
Phase II Study of Lapatinib and Capecitabine in 2nd Line Treatment of Locally Advanced/Metastatic Pancreatic Cancer [NCT00881621]	Phase 2	17 participants (Actual)	Interventional	2009-08-31	Terminated(stopped due to slow enrollment)
A Phase 2 Study of the Efficacy and Safety of Apricoxib in Combination With Lapatinib and Capecitabine in the Treatment of Patients With HER2/Neu+ Breast Cancer Who Have Failed Trastuzumab and Chemotherapy Including a Taxane [NCT00657137]	Phase 2	12 participants (Actual)	Interventional	2008-04-30	Terminated(stopped due to Slow accrual)
An Open-Label Phase Ib Continuation Study of Lapatinib Monotherapy or Lapatinib in Combination With Other Anti-Cancer Treatment in Patients With Solid Tumors [NCT00790816]	Phase 1	500 participants (Actual)	Interventional	2008-10-31	Completed
A Phase II Study of Neoadjuvant Lapatinib Plus Chemotherapy (Sequential FEC75 and Paclitaxel) in Women With Inflammatory Breast Cancer Whose Tumors Overexpress ErbB2 (Her2/Neu) [NCT00756470]	Phase 2	15 participants (Actual)	Interventional	2008-10-31	Terminated(stopped due to Slow accrual.)
Phase I Study of Lapatinib (GW572016) in Combination With Weekly Ixabepilone (BMS 247550) in Advanced Solid Tumors [NCT00804310]	Phase 1	5 participants (Actual)	Interventional	2009-08-31	Terminated(stopped due to Lack of funding)
A Randomized, Multicenter, Phase III Open-label Study of the Efficacy and Safety of Trastuzumab MCC-DM1 vs. Capecitabine + Lapatinib in Patients With HER2-Positive Locally Advanced or Metastatic Breast Cancer Who Have Received Prior Trastuzumab-Based Ther [NCT00829166]	Phase 3	991 participants (Actual)	Interventional	2009-02-28	Completed
An Open-Label Phase I Study of Fixed Dose Lapatinib in Combination With an Escalating Dose of Epirubicin in Metastatic Breast Cancer [NCT00753207]	Phase 1	10 participants (Actual)	Interventional	2007-10-31	Completed
A Phase 1, Open-label Study to Evaluate the Effect of Lapatinib, a BCRP Inhibitor, on the Pharmacokinetics of JTZ-951 in Subjects With End-stage Renal Disease Receiving Hemodialysis [NCT02581124]	Phase 1	10 participants (Actual)	Interventional	2015-10-31	Completed
Tolerability of the Combination of Lapatinib and Trastuzumab in Adults Age 60 or Older With HER2 Positive Locally Advanced or Metastatic Breast Cancer [NCT01273610]	Phase 2	40 participants (Actual)	Interventional	2011-04-20	Active, not recruiting
A Phase II, Randomized Trial With Single Agent Trastuzumab or Lapatinib in Patients With Metastatic HER2-Overexpressing Breast Cancer [NCT00842998]	Phase 2	120 participants (Anticipated)	Interventional	2009-02-28	Recruiting
A Randomised, Double-Blind, Placebo-Controlled, Multi-centre, Phase III Study of Post-Operative Adjuvant Lapatinib or Placebo and Concurrent Chemoradiotherapy Followed by Maintenance Lapatinib or Placebo Monotherapy in High-Risk Subjects With Resected Squ [NCT00424255]	Phase 3	688 participants (Actual)	Interventional	2006-12-31	Completed
A Randomized, Controlled, Multi-center Phase II Clinical Study to Evaluate the Efficacy and Safety of Recombinant Humanized Anti-HER2 Monoclonal Antibody-MMAE Conjugate for Injection in the Treatment of HER2-positive Locally Advanced or Metastatic Breast [NCT03500380]	Phase 2/Phase 3	301 participants (Anticipated)	Interventional	2018-04-24	Active, not recruiting
A Phase I, Open-label Study of the Safety, Tolerability, and Pharmacokinetics of Oral Topotecan in Combination With Lapatinib in Subjects With Advanced Solid Tumors [NCT00682279]	Phase 1	0 participants (Actual)	Interventional	2008-09-30	Withdrawn(stopped due to Cancelled before enrollment)
GCC 0845: Pilot and Phase II- Vorinostat and Lapatinib in Patients With Advanced Solid Tumor Malignancies and Women With Recurrent Local-Regional or Metastatic Breast Cancer to Evaluate Response and Biomarkers of EMT and Breast Cancer Stem Cells [NCT01118975]	Phase 1/Phase 2	12 participants (Actual)	Interventional	2010-03-31	Terminated(stopped due to Lost sponsorship for study drug)
A Randomized, Double-blind, Placebo Controlled, Multicentre, Phase II Study of Oral Lapatinib in Combination With Concurrent Radiotherapy and Cisplatin Versus Radiotherapy and Cisplatin Alone, in Subjects With Stage III, IVA, B Squamous Cell Carcinoma of [NCT00387127]	Phase 2	67 participants (Actual)	Interventional	2006-11-30	Completed
BrUOG-PA-209: Lapatinib and Gemcitabine for Metastatic Pancreaticobiliary Cancer: A Phase I Study #108181 [NCT00447122]	Phase 1	25 participants (Actual)	Interventional	2007-03-31	Terminated(stopped due to slow enrollment and lack of funding)
An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance (PMS) to Monitor the Safety and Effectiveness of TYKERB® Tablets Administered in Korean Patients According to the Prescribing Information [NCT00975988]		750 participants (Actual)	Observational	2010-01-31	Completed
Phase II Trial of Capecitabine (Xeloda) and Lapatinib (Tykerb) as First-line Therapy in Patients With HER2/Neu-Overexpressing Advanced or Metastatic Breast Cancer [NCT00496366]	Phase 2	11 participants (Actual)	Interventional	2007-07-23	Terminated
Clinical Study to Assess Entry of Chemotherapeutic Agents Into Brain Metastases in Women With Breast Cancer [NCT00795678]		10 participants (Actual)	Observational	2008-09-30	Completed
A Randomized, Multicentre, Open-Label, Phase III Study of Lapatinib Plus Capecitabine Versus Trastuzumab Plus Capecitabine in Patients With Anthracycline- or Taxane-Exposed ErbB2-Positive Metastatic Breast Cancer [NCT00820222]	Phase 3	540 participants (Actual)	Interventional	2009-04-14	Completed
A Phase 2 Randomized Open-Label Study of Neratinib Versus Lapatinib Plus Capecitabine For The Treatment Of ErbB-2 Positive Locally Advanced Or Metastatic Breast Cancer [NCT00777101]	Phase 2	233 participants (Actual)	Interventional	2009-02-04	Completed
An Open Label, Phase 1b Rollover Study to Assess the Long-Term Safety Profile of Lapatinib (GW572016) in Cancer Patients. [NCT00169533]	Phase 1	31 participants (Actual)	Interventional	2004-08-19	Completed
A Phase II Study Evaluating the Association of Topotecan and Lapatinib in Early Recurrent (Less Than 12 Months)Ovarian or Peritoneal Cancer Patients After First Line of Platinum-Based Chemotherapy [NCT00888810]	Phase 2	39 participants (Actual)	Interventional	2008-03-31	Terminated(stopped due to lack of efficacy (intermediate analysis))
A Phase I Dose Escalation Study of 5-Day Intermittent Oral Lapatinib Therapy With Biomarker Analysis in Patients With HER2-Overexpressing Breast Cancer [NCT00544804]	Phase 1	41 participants (Actual)	Interventional	2007-08-31	Completed
A Phase II Trial of Lapatinib in Combination With Weekly Topotecan in Patients With Platinum-Refractory/Resistant Ovarian and Primary Peritoneal Carcinoma [NCT00436644]	Phase 2	18 participants (Actual)	Interventional	2007-03-31	Completed
Phase II Study of Cardiac Safety and Tolerability of an Adjuvant Chemotherapy Plus Trastuzumab With Lapatinib in Patients With Resected HER2 + Breast Cancer [NCT00436566]	Phase 2	122 participants (Actual)	Interventional	2007-03-16	Completed
Phase II Multicentered Study of Exemestane and Lapatinib in Advanced Hormone-responsive Breast Cancer [NCT01005641]	Phase 2	0 participants (Actual)	Interventional	2009-12-31	Withdrawn(stopped due to Study not started for administrative reasons)
Phase I and II, Open-Label, Multi-Center Trials of Pazopanib in Combination With Lapatinib in Adult Patients With Relapsed Malignant Glioma [NCT00350727]	Phase 2	75 participants (Actual)	Interventional	2006-12-31	Completed
A Randomized, Multicenter, Open-Label, Phase III Study of Lapatinib in Combination With Trastuzumab Versus Lapatinib Monotherapy in Subjects With HER2-positive Metastatic Breast Cancer Whose Disease Has Progressed on Trastuzumab-Containing Regimens [NCT00320385]	Phase 3	296 participants (Actual)	Interventional	2005-11-30	Completed
A Randomized, Double-blind, Multicenter, Placebo-controlled Study of Adjuvant Lapatinib (GW572016) in Women With Early-Stage ErbB2 Overexpressing Breast Cancer [NCT00374322]	Phase 3	3,166 participants (Actual)	Interventional	2006-08-31	Completed
Phase II Neoadjuvant Chemotherapy Trial in Clinical Stage II/III Her2Neu Positive Breast Cancer With Sequential AC -> Docetaxel With Concurrent Dual EGFR Kinase Blockade by GW572016 (Lapatinib) Followed by 1 Year Adjuvant Trastuzumab [NCT00404066]	Phase 2	21 participants (Actual)	Interventional	2006-10-31	Completed
A Neoadjuvant Phase II Trial of GW572016 in HER2 Overexpressing Breast Cancer Patients: Biologic Correlative Study [NCT00206427]	Phase 2	49 participants (Actual)	Interventional	2004-08-31	Completed
Phase II Randomized Trial of Neoadjuvant Trastuzumab and/or Lapatinib Plus Chemotherapy (Sequential FEC75 and Paclitaxel) in Women With ErbB2- (HER2/Neu-) Overexpressing Invasive Breast Cancer [NCT00524303]	Phase 2	100 participants (Actual)	Interventional	2007-08-31	Completed
A Randomised, Multi-centre, Open-label, Phase III Study of Adjuvant Lapatinib, Trastuzumab, Their Sequence and Their Combination in Patients With HER2/ErbB2 Positive Primary Breast Cancer [NCT00490139]	Phase 3	8,382 participants (Actual)	Interventional	2007-05-16	Completed
A Multi-Institutional Phase II Study of Radiation and GW572016 (Lapatinib) for Patients With Stage III-IV Head and Neck Cancer Who Cannot Tolerate Concurrent Chemoradiotherapy. [NCT00490061]	Phase 2	17 participants (Actual)	Interventional	2007-07-31	Terminated(stopped due to Poor accrual.)
Defining the HER2 Positive (+) Breast Cancer Kinome Response to Trastuzumab, Pertuzumab, Combination Trastuzumab +Pertuzumab, or Combination Trastuzumab + Lapatinib [NCT01875666]	Early Phase 1	26 participants (Actual)	Interventional	2013-08-05	Completed
PAMELA: PAM50 HER2-enriched Phenotype as a Predictor of Early Response to Neoadjuvant Lapatinib Plus Trastuzumab in Stage I to IIIA HER2-positive Breast Cancer [NCT01973660]	Phase 2	151 participants (Actual)	Interventional	2013-10-31	Completed
Randomised, Open-label Phase II Study to Compare the Safety and Efficacy of Lapatinib Plus Trastuzumab or Lapatinib Plus Capecitabine in Trastuzumab-resistant HER2-overexpressing Metastatic Breast Cancer [NCT01985893]	Phase 2	0 participants (Actual)	Interventional	2013-09-30	Withdrawn(stopped due to Due to missing patient recruitment, the financial support was stopped.)
Phase II Study of Neoadjuvant XELOX + Lapatinib in HER2(+) Gastric Cancer Patients With Liver Metastasis [NCT02015169]	Phase 2	32 participants (Actual)	Interventional	2012-07-09	Completed
An Open Label, Pilot Study of Veliparib (ABT-888) and Lapatinib (Tykerb) in Patients With Metastatic, Triple Negative (ER, PR, and HER-2 Negative) Breast Cancer [NCT02158507]		23 participants (Actual)	Interventional	2014-09-30	Active, not recruiting
A Phase III Trials Program Exploring the Integration of Bevacizumab, Everolimus (RAD001), and Lapatinib Into Current Neoadjuvant Chemotherapy Regimes for Primary Breast Cancer [NCT00567554]	Phase 3	2,600 participants (Actual)	Interventional	2007-10-31	Completed
A Phase I Study of Lapatinib in Combination With Radiation Therapy in Patients With Brain Metastases From HER2-Positive Breast Cancer [NCT00470847]	Phase 1	35 participants (Actual)	Interventional	2007-04-30	Completed
Clinical Evaluation of Lapatinib Administered With Capecitabine in Japanese Patients With ErbB2 Overexpressing Advanced or Metastatic Breast Cancer [NCT00477464]	Phase 2	51 participants (Actual)	Interventional	2007-06-30	Completed
An Open-label, Multi-centre Study of Lapatinib in Combinationwith Chemotherapy in Patients With ErbB2 Overexpressing Breastcancer After Trastuzumab Failure in the Neoadjuvant or Adjuvantsetting. [NCT00479856]	Phase 2	9 participants (Actual)	Interventional	2007-11-30	Terminated(stopped due to Study was terminated due to difficulty in identifying eligible subjects)
A Phase III Study for ErbB2 Positive Advanced or Metastatic Gastric, Esophageal, or Gastroesophageal Junction Adenocarcinoma Treated With Capecitabine Plus Oxaliplatin With or Without Lapatinib [NCT00680901]	Phase 3	545 participants (Actual)	Interventional	2008-06-04	Active, not recruiting
Vinorelbine Metronomic Plus Lapatinib as Salvage Therapy for Patients With Overexpressing HER-2 Metastatic Breast Cancer. A Multicenter Phase II Study [NCT00754702]	Phase 2	16 participants (Actual)	Interventional	2008-10-31	Terminated(stopped due to Poor accrual)
Phase I Study of Cisplatin, Gemcitabine and Lapatinib as First Line Treatment in Advanced/Metastatic Urothelial Cancer [NCT00623064]	Phase 1	18 participants (Actual)	Interventional	2007-11-30	Completed
A Randomized, Open-Label, Phase III Study of Taxane Based Chemotherapy With Lapatinib or Trastuzumab as First-Line Therapy for Women With HER2/Neu Positive Metastatic Breast Cancer [NCT00667251]	Phase 3	652 participants (Actual)	Interventional	2008-10-07	Completed
Overcoming Endocrine Resistance in Metastatic Breast Cancer: A Randomized Trial With Factorial Design Comparing Fulvestrant ± Lapatinib ± Aromatase Inhibitor in Metastatic Breast Cancer Progressing After Aromatase Inhibitor Therapy [NCT00688194]	Phase 3	396 participants (Anticipated)	Interventional	2008-05-31	Recruiting
A Phase I Dose Escalation Study of a 2 Day Oral Lapatinib Chemosensitization Pulse Given Prior To Weekly Intravenous Abraxane™ in Patients With Advanced Solid Tumors [NCT00313599]	Phase 1	28 participants (Actual)	Interventional	2006-02-28	Completed
A Phase II Study of Bevacizumab and Lapatinib in Children With Recurrent or Refractory Ependymoma [NCT00883688]	Phase 2	24 participants (Actual)	Interventional	2009-07-31	Completed
An Exploratory, Phase II Trial to Determine the Association of Lapatinib Induced Fluoropyrimidine Gene Changes With Efficacy Parameters of Lapatinib and Capecitabine in First Line Gastric Cancer [NCT00526669]	Phase 2	68 participants (Actual)	Interventional	2008-03-31	Completed
Phase I Trial of the Combination of Dasatinib and Lapatinib [NCT00662636]	Phase 1	27 participants (Actual)	Interventional	2008-08-31	Completed
A Clinical Study Evaluating the Efficacy and Safety of BAT8001 Injection for the Treatment of HER2-positive Advanced Breast Cancer - A Multicenter, Randomized, Open-label, Positive-controlled, Superiority Phase III Clinical Trial in China [NCT04185649]	Phase 3	410 participants (Anticipated)	Interventional	2018-07-01	Active, not recruiting
TBCRC 023: A Randomized Multicenter Phase II Neoadjuvant Trial of Lapatinib Pus Trastuzumab, With or Without Endocrine Therapy for 12 Weeks vs. 24 Weeks in Patients With HER2 Overexpressing Breast Cancer [NCT00999804]	Phase 2	128 participants (Actual)	Interventional	2011-10-31	Active, not recruiting
Randomised Phase II Study of Neoadjuvant BIBW 2992 Versus Herceptin Versus Lapatinib in Her2 Positive Breast Cancer Patients [NCT00826267]	Phase 2	29 participants (Actual)	Interventional	2009-01-31	Completed
A Randomized, Phase III, Open-label Study of Lapatinib Plus Trastuzumab Versus Trastuzumab as Continued HER2 Suppression Therapy After Completion of First- or Second-line Trastuzumab Plus Chemotherapy in Subjects With HER2-positive Metastatic Breast Cance [NCT00968968]	Phase 3	37 participants (Actual)	Interventional	2010-01-20	Terminated
An Open-label, Single-arm, Phase I/II Study of Lapatinib in Combination With Weekly Paclitaxel as First-line Chemotherapy for ErbB2-overexpressing Metastatic Breast Cancer Patients [NCT01138046]	Phase 2	12 participants (Actual)	Interventional	2010-04-30	Completed
A Randomized Phase II Trial Investigating the Addition of Carboplatin to Neoadjuvant Therapy for Triple-negative and HER2-positive Early Breast Cancer [NCT01426880]	Phase 2/Phase 3	595 participants (Actual)	Interventional	2011-08-31	Completed
A Randomized Study of Lapatinib With Radiation Versus Radiation Alone in Advanced Solid Tumor Cancer Patients Receiving Radiation Therapy for Metastatic Disease [NCT01427322]	Early Phase 1	6 participants (Actual)	Interventional	2011-09-30	Terminated(stopped due to Slow accrual)
Phase I Study of Two Different Schedules of Lapatinib (GW572016) in Combination With Vinorelbine in Advanced Solid Tumors [NCT00389922]	Phase 1	22 participants (Actual)	Interventional	2005-12-31	Completed
Pilot Trial of Molecular Profiling and Targeted Therapy for Advanced Non-Small Cell Lung Cancer, Small Cell Lung Cancer, and Thymic Malignancies [NCT01306045]	Phase 2	647 participants (Actual)	Interventional	2011-02-08	Active, not recruiting
Relative Bioavailability of Four Alternative Oral Formulations Versus the Current Tablet Formulation of Lapatinib [NCT00513253]	Phase 1	0 participants (Actual)	Interventional	2008-04-30	Withdrawn(stopped due to It was determined not to be needed based on the clinical development plan of Tykerb.)
Implementation of a Therapeutic Educational Program Applicated to Adherence of Patients Treated by Capecitabine Alone or in Combination With Lapatinib [NCT01847599]		65 participants (Actual)	Interventional	2011-09-06	Terminated(stopped due to interim analysis : discontinuation for efficacy of the intervention)
A Phase I, Open-Label Study of the Safety, Tolerability and Pharmacokinetics of GW572016 in Combination With Trastuzumab [Herceptin†] [NCT00085020]	Phase 1	13 participants (Actual)	Interventional	2004-03-31	Completed
TRYHARD: A Phase II, Randomized, Double Blind, Placebo-Controlled Study of Lapatinib (Tykerb®) for Non-HPV Locally Advanced Head and Neck Cancer With Concurrent Chemoradiation [NCT01711658]	Phase 2	142 participants (Actual)	Interventional	2013-03-15	Completed
Phase II Randomized Study of Whole Brain Radiotherapy/Stereotactic Radiosurgery in Combination With Concurrent Lapatinib in Patients With Brain Metastasis From HER2-Positive Breast Cancer - A Collaborative Study of NRG Oncology and KROG [NCT01622868]	Phase 2	143 participants (Actual)	Interventional	2012-12-06	Completed
A Phase I Study of LBH589 in Combination With Capecitabine ± Lapatinib [NCT00632489]	Phase 1	20 participants (Actual)	Interventional	2008-05-31	Completed
Modulation of Response to Hormonal Therapy With Lapatinib and/or Metformin in Patients With HER2-negative, ER and/or PgR Positive Metastatic Brest Cancer With Progressive Disease After First-line Therapy [NCT01477060]	Phase 2	32 participants (Actual)	Interventional	2011-11-30	Terminated(stopped due to The study was stopped due to insufficient accrual)
Phase II Clinical Study of GW572016 in Patients With Advanced or Metastatic Breast Cancer [NCT00462956]	Phase 1	59 participants (Actual)	Interventional	2004-06-30	Completed
A Randomized Phase III Trial of Neoadjuvant Therapy for Patients With Palpable and Operable HER2-Positive Breast Cancer Comparing the Combination of Trastuzumab Plus Lapatinib to Trastuzumab and to Lapatinib Administered With Weekly Paclitaxel Following A [NCT00486668]	Phase 3	529 participants (Actual)	Interventional	2007-07-31	Active, not recruiting
Phase I/II Study on Induction Chemotherapy Followed by Chemoradiation With or Without Lapatinib, a Dual EGFR/ErbB2 Kinase Inhibitor, in Patients With Locally Advanced Larynx and Hypopharynx Squamous Cell Carcinoma [NCT00498953]	Phase 1/Phase 2	7 participants (Actual)	Interventional	2007-05-31	Completed
A Phase I, Open-Label, Multiple Dose of Pazopanib Alone and In Combination With Lapatinib in Japanese Patients With Solid Tumors [NCT00516672]	Phase 1	30 participants (Actual)	Interventional	2007-09-10	Completed
A Single-arm, Two-stage Phase II Study of Lapatinib and Pemetrexed in the Second Line Treatment of Advanced or Metastatic Non-Small Cell Lung Cancer [NCT00528281]	Phase 1	18 participants (Actual)	Interventional	2007-09-20	Completed
A Phase II Study of Lapatinib for the Treatment of Stage IV Melanoma Harboring ERBB4 Mutations [NCT01264081]	Phase 2	34 participants (Actual)	Interventional	2011-05-20	Terminated(stopped due to Protocol would not be able to reach stated accrual.)
A Phase 1 Study of Bevacizumab in Combination With 1) Sunitinib, 2) Sorafenib, 3) Erlotinib and Cetuximab, 4) Trastuzumab and Lapatinib [NCT00543504]	Phase 1	343 participants (Actual)	Interventional	2007-10-10	Completed
A Randomised Phase II/III Trial of Peri-Operative Chemotherapy With or Without Bevacizumab in Operable Oesophagogastric Adenocarcinoma and A Feasibility Study Evaluating Lapatinib in HER-2 Positive Oesophagogastric Adenocarcinomas and (in Selected Centres [NCT00450203]	Phase 2/Phase 3	1,103 participants (Anticipated)	Interventional	2007-10-31	Recruiting
A Phase I, Open Label Study of the Safety, Pharmacokinetics and Pharmacodynamics of GW572016 in Once Daily Versus Twice Daily Dosing Regimens in Patients With Treatment- Naive Breast Cancer [NCT00359190]	Phase 1	28 participants (Actual)	Interventional	2004-06-29	Completed
A Phase Ib/Randomized Phase II Study of BEZ235 and Trastuzumab Versus Lapatinib and Capecitabine in Patients With HER2-positive Locally Advanced or Metastatic Breast Cancer Who Failed Prior to Trastuzumab [NCT01471847]	Phase 1	5 participants (Actual)	Interventional	2012-02-29	Completed
A Phase II Neo-adjuvant Study Assessing TCH (Docetaxel, Carboplatin and Trastuzumab) and TCHL (Docetaxel, Carboplatin, Trastuzumab and Lapatinib) in HER-2 Positive Breast Cancer Patients. [NCT01485926]	Phase 2	120 participants (Anticipated)	Interventional	2010-10-31	Completed
Lapatinib (GW572016) a Dual Inhibitor of EGFR and ErbB2, for Metastatic or Recurrent Squamous Cell Carcinoma of the Esophagus [NCT00239200]	Phase 2	29 participants (Anticipated)	Interventional	2005-10-31	Terminated(stopped due to notification from sponsor)
A Phase II Study Of GW572016 In Squamous Cell Carcinoma Of The Head And Neck (SCCHN) [NCT00098631]	Phase 2	88 participants (Anticipated)	Interventional	2004-10-31	Completed
A Phase I/II Study of GW572016 in Patients With Recurrent Malignant Glioma [NCT00099060]	Phase 1/Phase 2	24 participants (Actual)	Interventional	2004-12-31	Completed
A Phase II, Open-Label Study Evaluating Clinical Efficacy, Safety, Pharmacokinetic and Pharmacodynamic Effects of Lapatinib (GW572016) in Patients With Relapsed Adenocarcinoma of the Esophagus, Including Tumors of the Gastroesophageal Junction and Gastric [NCT00259987]	Phase 2	24 participants (Actual)	Interventional	2005-11-30	Completed
A Phase III, Randomized, Open-label, Multicenter Study Comparing GW572016 and Capecitabine (XELODA) Versus Capecitabine in Women With Refractory Advanced or Metastatic Breast Cancer [NCT00078572]	Phase 3	408 participants (Actual)	Interventional	2004-03-31	Completed
A Phase I Trial of Lapatinib in Combination With Carboplatin in Patients With Platinum Sensitive Recurrent Epithelial Ovarian Cancer [NCT00317434]	Phase 1	12 participants (Actual)	Interventional	2005-11-30	Terminated(stopped due to Due to unacceptable non-dose limiting toxicities, excessive treatment delays and limited clinical responses.)
[NCT00343759]	Phase 2	0 participants (Actual)	Interventional	2006-06-30	Withdrawn
A Phase II Study to Evaluate the Efficacy, Safety and Pharmacodynamics of Lapatinib in Patients With Relapsed or Refractory Inflammatory Breast Cancer [NCT00105950]	Phase 2	126 participants (Actual)	Interventional	2005-03-31	Completed
A Biomarker and Phase II Study of GW572016 in Recurrent Malignant Glioma [NCT00107003]	Phase 2	9 participants (Actual)	Interventional	2005-03-30	Completed
A Phase I-II Study of Lapatinib and Docetaxel as Neoadjuvant Treatment for HER-2 Positive Locally Advanced/Inflammatory or Large Operable Breast Cancer [NCT00450892]	Phase 1/Phase 2	129 participants (Actual)	Interventional	2007-02-28	Completed
A Prospective, Open-label，Multicentre，Real-word Study of Lapatinib Plus Chemotherapy Versus Trastuzumab Plus Chemotherapy as Neoadjuvant Therapy for Women With HER2-positive and p95HER2-positive，PI3K Mutation，or PTEN Loss Breast Cancer [NCT03273595]	Phase 2	100 participants (Anticipated)	Interventional	2016-07-31	Recruiting
A Phase I Study of MK-2206 in Combination With Lapatinib in Refractory Solid Tumors Followed by Dose-Expansion in Advanced HER2+ Breast Cancer [NCT01245205]	Phase 1	28 participants (Actual)	Interventional	2010-11-30	Completed
Pharmacokinetics Study of Combined Treatment Lapatinib and Tamoxifen in Advanced/Metastatic Breast Cancer [NCT00424164]	Phase 1	20 participants (Anticipated)	Interventional	2006-11-30	Active, not recruiting
A Phase I, Open-Label Study of the Safety, Tolerability and Pharmacokinetics of GW572016 in Combination With Docetaxel (Taxotere) [NCT00148902]	Phase 1	52 participants (Actual)	Interventional	2003-04-28	Completed
Phase II Trial of Lapatinib in Women With Hormone Receptor Positive (Estrogen Receptor [ER] and/or Progesterone Receptor [PR] +) Human Epidermal Growth Factor Receptor 2 (HER-2) Negative Metastatic Breast Cancer Who Have Failed Prior Antihormone Therapy [NCT00759642]	Phase 2	33 participants (Actual)	Interventional	2009-03-31	Terminated(stopped due to IRB decision)
Phase II Safety Study of Docetaxel and Carboplatin in Combination With Trastuzumab and Lapatinib in Early Breast Cancer [NCT00820872]	Phase 2	30 participants (Actual)	Interventional	2009-02-28	Completed
Population Pharmacokinetics, Effectiveness and Safety of Antineoplastic Drugs in Elderly Patients [NCT05467189]		500 participants (Anticipated)	Observational [Patient Registry]	2021-01-01	Recruiting
A Phase I Investigation of the Combination of MK-2206, Trastuzumab and Lapatinib in HER2+ Solid Tumors [NCT00963547]	Phase 1	33 participants (Actual)	Interventional	2009-09-15	Terminated
Targeted Therapy With Lapatinib in Patients With Recurrent Pituitary Tumors Resistant to Standard Therapy [NCT00939523]	Phase 2	9 participants (Actual)	Interventional	2009-07-31	Completed
A Multicenter, Open-Label, Phase II Study of Lapatinib in Combination With Vinorelbine in Subjects With ErbB2 Amplified Recurrent and Metastatic Breast Cancer [NCT01128543]	Phase 2	29 participants (Actual)	Interventional	2009-04-30	Completed
A Multi-Arm Complete Phase 1 Trial of Valproic Acid-Based 2-Agent Oral Regimens for Patients With Advanced Solid Tumor [NCT00495872]	Phase 1	204 participants (Actual)	Interventional	2007-06-30	Completed
A Four Part, Phase I Dose-Escalation Study of the Combinations of Concurrent BKM120 and Capecitabine, or Concurrent BYL719 and Capecitabine, or Concurrent BKM120 and Capecitabine and Trastuzumab, or Concurrent BKM120 and Capecitabine and Lapatinib in Pati [NCT01300962]	Phase 1	47 participants (Actual)	Interventional	2011-08-31	Completed
A Phase III Randomized Study of TH (Paclitaxel and Trastuzumab) Versus THL (Paclitaxel, Trastuzumab and Lapatinib) in First Line Treatment of HER2-positive Metastatic Breast Cancer [NCT01526369]	Phase 3	75 participants (Actual)	Interventional	2012-02-13	Completed
A Randomized Phase II Study to Determine the Efficacy and Tolerability of Two Doses of Eribulin Plus Lapatinib in Trastuzumab Pre-treated Patients With HER2-positive Metastatic Breast Cancer (E-VITA) [NCT01534455]	Phase 2	43 participants (Actual)	Interventional	2012-02-29	Terminated(stopped due to very slow patient recruitment and concerns about the actuality of the study design)
A Phase 2 Study of GW572016 for Brain Metastases in Patients With HER2-Positive Breast Cancer [NCT00098605]	Phase 2	37 participants (Actual)	Interventional	2004-10-31	Completed
Phase II Study of GW572016 (NSC-727989) as First Line Therapy in Patients With Advanced or Metastatic Gastric Cancer [NCT00103324]	Phase 2	40 participants (Actual)	Interventional	2004-12-31	Completed
A Phase I, Open-Label, Study of the Safety, Tolerability, and Pharmacokinetics of Pazopanib in Combination With Paclitaxel on a Weekly Schedule for Three Consecutive Weeks of a 28-Day Cycle, Paclitaxel and Carboplatin on an Every 21 Days Schedule and Lapa [NCT00388076]	Phase 1	86 participants (Actual)	Interventional	2006-04-28	Completed
A Phase II Study to Evaluate the Efficacy, Safety, and Pharmacodynamics of Lapatinib in Combination With Paclitaxel as Neoadjuvant Therapy in Patients With Newly Diagnosed Inflammatory Breast Cancer [NCT00111787]	Phase 2	49 participants (Actual)	Interventional	2005-04-11	Completed
A Phase 2 Trial of GW572016 in Patients With Metastatic and Recurrent Squamous Cell Carcinomas of the Head and Neck [NCT00114283]	Phase 2	30 participants (Anticipated)	Interventional	2005-03-31	Completed
A Randomized, Multicenter, Phase III Study Comparing the Combination of Pazopanib and Lapatinib Versus Lapatinib Monotherapy in Patients With ErbB2 Over-expressing Inflammatory Breast Cancer [NCT00558103]	Phase 2	163 participants (Actual)	Interventional	2007-12-31	Completed
An Open-Label, Multicenter, Single Arm Phase II Study of Oral GW572016 as Single Agent Therapy in Subjects With Advanced or Metastatic Breast Cancer Who Have Progressed While Receiving HERCEPTIN-Containing Regimens [NCT00062686]	Phase 2	200 participants	Interventional	2003-11-30	Completed
An Open-Label, Multicenter, Phase II Study of Oral Lapatinib (GW572016) as Single Agent, Second-Line Therapy in Subjects With Metastatic Colorectal Cancer Who Have Progressed on First-Line Therapy With 5-Fluorouracil in Combination With Irinotecan or Oxal [NCT00044343]	Phase 2	80 participants (Actual)	Interventional	2002-09-30	Completed
An Open-Label, Safety, Pharmacokinetic and Pharmacodynamic Study of Multiple Doses of GW786034 and Lapatinib Concomitantly Administered in Cancer Patients [NCT00158782]	Phase 1	75 participants (Actual)	Interventional	2004-09-28	Completed
A Phase II Study of Lapatinib in Combination With Trastuzumab in Metastatic HER2 Non-amplified But HER2 Mutant Breast Cancer [NCT01557764]	Phase 2	0 participants (Actual)	Interventional	2012-09-30	Withdrawn
Molecular Profiling of Advanced Soft-tissue Sarcomas. A Phase III Study [NCT03784014]	Phase 3	960 participants (Anticipated)	Interventional	2019-10-19	Recruiting
A Phase 2 Study of GW572016 in Hormone Naive Recurrent or Metastatic Hormone Sensitive Prostate Cancer [NCT00095667]	Phase 2	41 participants (Anticipated)	Interventional	2004-11-30	Completed
Phase II Trial of Metronomic Capecitabine and Cyclophosphamide With Lapatinib and Trastuzumab in Patients With HER2 Positive Metastatic Breast Cancer Who Have Progressed on a Previous Trastuzumab-Based Regimen [NCT01873833]	Phase 2	10 participants (Actual)	Interventional	2013-07-29	Terminated(stopped due to Insufficient accrual)
Safety and Clinical Activity of Lapatinib in Patients With HER2-positive Refractory Advanced Cancer: A Phase II Single Arm Prospective Study [NCT02342587]	Phase 2	7 participants (Actual)	Interventional	2014-12-03	Completed
Neoadjuvant Letrozole and Lapatinib in Postmenopausal Women With ER and Her2 Positive Breast Cancer [NCT01275859]	Phase 2	25 participants (Actual)	Interventional	2010-09-30	Completed
Randomized Phase II Trial of Capecitabine and Lapatinib With or Without IMC-A12 in Patients With HER2 Positive Breast Cancer Previously Treated With Trastuzumab and an Anthracycline and/or a Taxane [NCT00684983]	Phase 2	64 participants (Actual)	Interventional	2008-07-30	Completed
Neoadjuvant Trial of Lapatinib for the Treatment of Women With DCIS Breast Cancer [NCT00555152]		22 participants (Actual)	Interventional	2009-08-19	Completed
Phase I Study of Lapatinib in Combination With Trastuzumab [NCT00371488]	Phase 1	11 participants (Actual)	Interventional	2006-04-06	Completed
A Phase II Study of Capecitabine and Lapatinib in Squamous Cell Carcinoma of the Head and Neck [NCT01044433]	Phase 2	44 participants (Actual)	Interventional	2009-10-31	Completed
A Phase II Trial of Lapatinib and Capectiabine for Patients With Refractory Advanced Colorectal Adenocarcinoma (LAP109859) [NCT00574171]	Phase 2	29 participants (Actual)	Interventional	2007-09-30	Completed
A Randomized, Multicenter, Double-Blind, Placebo-Controlled, Phase III Study of Lapatinib (GW572016) in Combination With Paclitaxel Versus Paclitaxel Plus Placebo in Subjects With ErbB2 Amplified Metastatic Breast Cancer [NCT00281658]	Phase 3	444 participants (Actual)	Interventional	2006-01-02	Completed
Phase I Radiosensitization Study of GW572016 With Biologic Correlates in Locoregionally Recurrent Breast Cancer [NCT00379509]	Phase 1	20 participants (Actual)	Interventional	2006-04-30	Completed
A Randomized, Multicenter, Parallel,Phase III Open-label Study of the Efficacy and Safety of Hemay022 + AI in Patients With ER+/HER2+ Advanced or Metastatic Breast Cancer Who Have Received Prior Trastuzumab-Based Therapy [NCT05122494]	Phase 3	339 participants (Anticipated)	Interventional	2022-01-19	Recruiting
A Four-Way Cross-Over Study to Examine the Effects of Lapatinib on the Pharmacokinetics of Orally and Intravenously Administered Midazolam in Cancer Patients [NCT00258050]	Phase 1	24 participants (Actual)	Interventional	2005-11-21	Completed
A Double Blind Short-Term Presurgical Study Assessing the Molecular Antiproliferative Predictors of Lapatinib's Effects in Breast Cancer [NCT00299286]	Phase 2	121 participants (Actual)	Interventional	2007-06-30	Completed
Phase I/II Lapatinib Plus Carboplatin and Paclitaxel in Stage III or IV Relapsed Ovarian or Stage IV Breast Cancer Patients [NCT00316407]	Phase 1/Phase 2	30 participants (Actual)	Interventional	2005-08-31	Completed
A Phase I, Open-Label Study of the Safety, Tolerability and Pharmacokinetics of Lapatinib in Combination With Liposomal Doxorubicin in Patients With Metastatic Breast Cancer [NCT00316875]	Phase 1	23 participants (Actual)	Interventional	2006-05-31	Completed
An Open-Label Expanded Access Study of Lapatinib and Capecitabine Therapy in Subjects With ErbB2 Overexpressing Locally Advanced or Metastatic Breast Cancer [NCT00338247]		0 participants	Expanded Access	2006-07-31	Approved for marketing
A Phase I/II Study of Lapatinib Plus Myocet TM in Patients With HER2+ve Metastatic Breast Cancer Following Disease Progression During, or After, Treatment With Trastuzumab and Taxanes [NCT01495884]	Phase 1/Phase 2	11 participants (Actual)	Interventional	2011-03-31	Terminated(stopped due to Slower than anticipated accrual)
A Phase I Study of the HER1, HER2 Dual Kinase Inhibitor, Lapatinib Plus the Proteosomal Inhibitor Bortezomib in Patients With Advanced Malignancies [NCT01497626]	Phase 1	15 participants (Actual)	Interventional	2011-09-30	Terminated(stopped due to Drug support withdrawn)
Pilot Study on the Determination of Intratumoral Concentrations of Kinase Inhibitors in Patients With Advanced Solid Malignancies. [NCT01636908]		43 participants (Actual)	Interventional	2011-08-31	Completed
A Phase I/II Study of Lapatinib (Tykerb) Plus Liposomal Doxorubicin Hydrochloride ( Lipo-Dox) for Patients With ErbB2 Positive Metastatic Breast Cancer [NCT01658358]	Phase 1/Phase 2	15 participants (Anticipated)	Interventional	2012-07-31	Terminated
[NCT01666431]	Phase 2	10 participants (Actual)	Interventional	2012-06-30	Terminated
Phase II Trial of Lapatinib and Weekly Paclitaxel for Advanced Platinum Refractory Urothelial Cancer [NCT01700010]	Phase 2	0 participants (Actual)	Interventional	2012-11-30	Withdrawn(stopped due to Funding issues.)
A Phase I Study of MK-2206 in Combination With Trastuzumab and Lapatinib in HER2-Positive Breast and Gastric Cancer [NCT01705340]	Phase 1	60 participants (Actual)	Interventional	2012-09-30	Terminated
Randomized Phase II Study of Lapatinib Plus Vinorelbine Versus Vinorelbine in Patients With HER2 Positive Metastatic Breast Cancer Progressed After Lapatinib and Trastuzumab Treatment [NCT01730677]	Phase 2	150 participants (Anticipated)	Interventional	2012-07-31	Recruiting
A Randomized Proof-of-concept Phase II Trial Comparing Therapy Based on Tumor Molecular Profiling Versus Conventional Therapy in Patients With Refractory Cancer. [NCT01771458]	Phase 2	742 participants (Actual)	Interventional	2012-10-31	Active, not recruiting
Treatment Options in Human Epidermal Growth Factor Receptor 2 (HER2) Positive Metastatic Breast Cancer Patients [NCT01782651]		1 participants (Actual)	Observational	2014-08-31	Completed
Phase 1b/2 Single-arm Trial Evaluating the Combination of Lapatinib, Everolimus and Capecitabine for the Treatment of Patients With HER2-positive Metastatic Breast Cancer With CNS Progression After Trastuzumab [NCT01783756]	Phase 1/Phase 2	9 participants (Actual)	Interventional	2013-06-26	Completed
A Phase II Study With Lead-in Safety Cohort of 5-Fluorouracil, Oxaliplatin and Lapatinib in Combination With Radiation Therapy as Neoadjuvant Treatment for Patients With Localized HER2 Positive Esophagogastric Adenocarcinomas [NCT01769508]	Phase 2	12 participants (Actual)	Interventional	2013-02-28	Terminated(stopped due to Study closed due to slow accrual.)
Phase II Trial of Lapatinib in Combination With Everolimus in Triple Negative Metastatic or Locally Advanced Breast Cancer [NCT01272141]	Phase 2	5 participants (Actual)	Interventional	2010-12-31	Terminated(stopped due to Slow accrual, Funding stopped)
Phase I and Phase I Trastuzumab Cohort Study of Entinostat, Lapatinib and Trastuzumab in Patients With HER2-Positive Metastatic Breast Cancer in Whom Trastuzumab Has Failed [NCT01434303]	Phase 1	37 participants (Actual)	Interventional	2012-01-10	Completed
Multimodality Risk Adapted Therapy Including Carboplatin/Paclitaxel/Lapatinib as Induction for Squamous Cell Carcinoma of the Head and Neck Amenable to Transoral Surgical Approaches [NCT01612351]	Phase 2	40 participants (Actual)	Interventional	2012-06-30	Active, not recruiting
Parallel Phase I Study of Ixabepilone Plus Lapatinib and Ixabepilone Plus Lapatinib Plus Capecitabine in Subjects With HER2 Positive Locally Advanced or Metastatic Breast Cancer [NCT00634088]	Phase 1	13 participants (Actual)	Interventional	2008-06-30	Terminated(stopped due to Slow Accrual)
Randomized Phase 2A/2B Study to Compare the Efficacy and Safety of ASLAN001 + Capecitabine to Lapatinib + Capecitabine in Patients With HER 2-Positive MBC That Has Failed on Prior Trastuzumab Therapy [NCT02338245]	Phase 2	200 participants (Anticipated)	Interventional	2014-12-29	Completed
Phase II Study of Lapatinib in Children and Adults With Neurofibromatosis Type 2(NF2) and NF2-related Tumors [NCT00973739]	Phase 2	21 participants (Actual)	Interventional	2009-09-30	Completed
Phase I Study of Pazopanib in Combination With Lapatinib or Trastuzumab in Subjects With Solid Tumors [NCT01454804]	Phase 1	43 participants (Actual)	Interventional	2011-10-31	Completed
A Phase II Study of GW572016 (Lapatanib) in Locally Advanced or Metastatic Hepato-Biliary Cancers [NCT00101036]	Phase 2	57 participants (Actual)	Interventional	2004-11-30	Completed
A Phase II Study of Oral Once Daily GW572016 (Lapatinib) In Patients With Hormone Refractory Prostate Cancer [NCT00246753]	Phase 2	29 participants (Actual)	Interventional	2005-10-31	Completed
A Phase II, Open-Label, Randomized, Parallel-Group Multicenter Trial Comparing Two Schedules of GW572016 as First-Line Monotherapy in Patients With Advanced or Metastatic Breast Cancer [NCT00089999]	Phase 2	138 participants (Actual)	Interventional	2004-06-30	Completed
An Open-label, Multicenter, Phase I/II Dose Escalation Study of Oral GW572016 in Combination With Docetaxel (Taxotere) Plus Trastuzumab (Herceptin) in Subjects Previously Untreated for ErbB2-overexpressing Metastatic Breast Cancer [NCT00251433]	Phase 1	53 participants (Actual)	Interventional	2005-09-26	Terminated(stopped due to EGF100161 (NCT00251433) was terminated in Phase I (Phase II expansion portion of the study was never initiated) by sponsor decision.)
A Phase I Study of Lapatinib (Tykerb) Plus Ixabepilone (Ixempra) as 2nd-line Treatment for Patients With HER-2 Overexpressed Recurrent or Persistent Endometrial Carcinoma or Carcinosarcoma [NCT01454479]	Phase 1	24 participants (Anticipated)	Interventional	2011-03-31	Enrolling by invitation
Phase I/II Pilot Study of Lapatinib in Combination With Carboplatin and Paclitaxel in the Treatment of Recurrent/Metastatic Adenocarcinoma of the Esophagus and Gastroesophageal Junction (GEJ) [NCT01395537]	Phase 1/Phase 2	13 participants (Actual)	Interventional	2011-08-31	Terminated(stopped due to Research Cancelled)
A Phase 2 Study of GW572016 in Recurrent and/or Metastatic Adenoid Cystic Carcinoma, and Other EGFR-and/or erbB2-expressing Malignant Tumors of the Salivary Glands [NCT00095563]	Phase 2	40 participants (Actual)	Interventional	2004-09-30	Completed
DETECT III - A Multicenter, Randomized, Phase III Study to Compare Standard Therapy Alone Versus Standard Therapy Plus Lapatinib in Patients With Initially HER2-negative Metastatic Breast Cancer and HER2-positive Circulating Tumor Cells [NCT01619111]	Phase 3	105 participants (Actual)	Interventional	2012-02-29	Completed
A Randomized, Multicenter, Phase III Open-Label Study of the Efficacy and Safety of Trastuzumab Emtansine Versus Lapatinib Plus Capecitabine in Chinese Patients With HER2-Positive Locally Advanced or Metastatic Breast Cancer Who Have Received Prior Trastu [NCT03084939]	Phase 3	351 participants (Actual)	Interventional	2017-04-24	Completed
A Phase Ib/II Open-label Study Evaluating Safety and Efficacy of Oral BKM120 in Combination With Lapatinib in HER2+/PI3K-activated, Trastuzumab-resistant Locally Advanced, Recurrent and Metastatic Breast Cancer. PIKHER2/IPC 2011-001 [NCT01589861]	Phase 1/Phase 2	106 participants (Anticipated)	Interventional	2011-12-31	Suspended(stopped due to Data analysis)
A Randomized Controlled Trial of HER-2 Positive Breast Cancer Patients Treated With Lapatinib and Paclitaxel vs Herceptin and Paclitaxel With Sequential and Synchronous Anthracycline [NCT03085368]	Phase 2/Phase 3	482 participants (Anticipated)	Interventional	2017-03-01	Recruiting
A Monocentric, Open-label Phase I/II Study to Assess dHER2+AS15 Cancer Immunotherapeutic Given in Combination With Lapatinib to Patients With ErbB2 Overexpressing Metastatic Breast Cancer Refractory to Trastuzumab [NCT00952692]	Phase 1/Phase 2	12 participants (Actual)	Interventional	2009-07-31	Completed
Phase II Trial of GW572016 in Patients With Recurrent Prostate Cancer as Evident by a Rising PSA [NCT00103194]	Phase 2	49 participants (Actual)	Interventional	2005-09-30	Completed
Phase I Study Evaluating the Combination of Lapatinib (GW572016; NSC-727989) and Everolimus (RAD001) in Patients With Advanced Solid Tumors [NCT00352443]	Phase 1	66 participants (Actual)	Interventional	2006-09-30	Completed
A Phase I Dose-Escalation Study on the Safety of Lapatinib With Dose-Dense Paclitaxel in Patients With Platinum-Resistant Ovarian Cancer [NCT04608409]	Phase 1	15 participants (Anticipated)	Interventional	2021-03-17	Recruiting
INST 0514C- A Neoadjuvant Phase II Trial of GW572016 in HER2 Overexpressing Breast Cancer Patients: Biologic Correlative Study [NCT00455039]	Phase 1/Phase 2	0 participants (Actual)	Interventional	2023-07-31	Withdrawn(stopped due to This is a duplicate record and the sponsor has submitted under NCT00206427.)
A Phase I, Dose Escalation Study to Assess the Safety and Tolerability of Lapatinib in Combination With Carboplatin, Paclitaxel, With and Without Trastuzumab in Subjects With Metastatic Breast Cancer [NCT00367471]	Phase 1	31 participants (Actual)	Interventional	2006-12-07	Completed
Open-Label, Phase II Study of Trastuzumab in Combination With Lapatinib (Cohort A) or Pertuzumab in Combination With Trastuzumab-emtansine (Cohort B) in Patients With HER2-positive Metastatic Colorectal Cancer: the HERACLES (HER2 Amplification for Colo-re [NCT03225937]	Phase 2	54 participants (Anticipated)	Interventional	2012-08-31	Active, not recruiting
A Study of Pyrotinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+Metastatic Breast Cancer Who Have Prior Received Anthracyclin, Taxane or Trastuzumab [NCT02422199]	Phase 1/Phase 2	128 participants (Anticipated)	Interventional	2015-05-31	Active, not recruiting
Randomized Open Label PhII Trial of Neoadjuvant Trastuzumab Emtansine(Te) in Combination w/Lapatinib(L) Followed by Abraxane (A) Compared w/Trastuzumab Plus Pertuzumab Followed by Paclitaxel in Her2/Neu Over-Expressed Breast Cancer Patients [NCT02073487]	Phase 2	32 participants (Actual)	Interventional	2014-02-28	Completed
Phase II Study of Lapatinib and Trastuzumab Followed by Concurrent Lapatinib, Trastuzumab, and Paclitaxel Followed by Surgery for Primary HER2-positive (HER2+) Breast Cancer [NCT01688609]	Phase 2	18 participants (Actual)	Interventional	2012-07-31	Completed
An Open-Label, Phase II, Study to Evaluate Biomarkers Associated With Response to Subsequent Therapies in Subjects With HER2-Positive Metastatic Breast Cancer Receiving Treatment With Trastuzumab in Combination With Lapatinib or Chemotherapy (EGF117165) [NCT02213042]	Phase 2	42 participants (Actual)	Interventional	2014-10-24	Terminated(stopped due to Primary analysis was completed in 2018 and continued minimal data collection from the one participant active in the study was not expected to add meaningful knowledge to the understanding of lapatinib)
A Phase II Study of Efficacy and Tolerability of GW572016 in Patients With Advanced Hepatocellular and Biliary Carcinomas [NCT00107536]	Phase 2	26 participants (Actual)	Interventional	2005-10-31	Completed
A Multicenter Site, Open Label, Phase II Trial to Validate Predictive Markers for the Response Evaluation of a Combined Chemo-immunotherapy in Patients With HER2-positive Early Breast Cancer [NCT01891357]	Phase 2	64 participants (Actual)	Interventional	2013-09-30	Terminated(stopped due to Early termination due to significant lack of relevant patient data for evaluation of objectives.)
The Feasibility of Paclitaxel With Trastuzumab and Lapatinib in HER2-Positive Early Stage Breast Cancer [NCT01827163]	Phase 2	20 participants (Actual)	Interventional	2013-04-30	Completed
Phase II Study to Investigate Concurrent Lapatinib and Radiotherapy in Locally Advanced or Locally Recurrent Breast Cancer and the Impact on Breast Cancer Stem Cells [NCT01868503]	Phase 2	7 participants (Actual)	Interventional	2013-07-31	Terminated(stopped due to Protocol modification)
A Multicentre, Randomised Phase II to Compare Epirubicin (E) & Cyclophosphamide (C) Treatment Plus Docetaxel (D) & Trastuzumab vs. E & C Treatment Plus D & Lapatinib in Women With Primary Resectable or Locally Advanced HER2+ Breast Cancer [NCT00841828]	Phase 2	102 participants (Actual)	Interventional	2009-02-28	Completed
Exploration and Estimation of Intratumoral Concentration and Activity of Lapatinib in Vivo in Vestibular Schwannomas [NCT00863122]	Early Phase 1	26 participants (Actual)	Interventional	2009-06-30	Completed
A Randomised, Open-label, Parallel Controlled, Multicentre, Phase 3 Clinical Trial of Pyrotinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in Patients With HER2+ Metastatic Breast Cancer: [NCT03080805]	Phase 3	240 participants (Anticipated)	Interventional	2017-05-03	Active, not recruiting
Lapatinib in the Treatment of Ductal Carcinoma in Situ of the Breast [NCT00857714]		1 participants (Actual)	Interventional	2009-04-30	Terminated(stopped due to Terminated due to low accrual)
Phase II Study With Lead-in Safety Cohort of Cabazitaxel Plus Lapatinib as Therapy for HER2-Positive Metastatic Breast Cancer Patients With Intracranial Metastases [NCT01934894]	Phase 2	11 participants (Actual)	Interventional	2014-05-31	Terminated(stopped due to Study was terminated due to lack of significant signal of efficacy)
A STUDY OF NERATINIB PLUS CAPECITABINE VERSUS LAPATINIB PLUS CAPECITABINE IN PATIENTS WITH HER2+ METASTATIC BREAST CANCER WHO HAVE RECEIVED TWO OR MORE PRIOR HER2-DIRECTED REGIMENS IN THE METASTATIC SETTING (NALA) [NCT01808573]	Phase 3	621 participants (Actual)	Interventional	2013-03-29	Completed
GCC 0901- A Phase II Study of Letrozole in Combination With Lapatinib Followed by an Addition of Everolimus in Postmenopausal Women With Advanced Endocrine Resistant Breast Cancer [NCT01499160]	Phase 2	7 participants (Actual)	Interventional	2012-05-31	Terminated(stopped due to low accrual)
Phase I/II Study With Lapatinib Plus Trametinib in Patients With Metastatic KRAS Mutant Non-small Cell Lung Cancer [NCT02230553]	Phase 1/Phase 2	30 participants (Anticipated)	Interventional	2014-10-31	Recruiting
Drug Distribution and Pharmacodynamic Study of Pulsatile Lapatinib in Surgically Accessible EGFR-Amplified Recurrent High-Grade Glioma [NCT02101905]	Phase 1	29 participants (Actual)	Interventional	2014-03-13	Active, not recruiting
A Two-period, Multicenter, Randomized, Open-label, Phase II Study Evaluating the Clinical Benefit of a Maintenance Treatment Targeting Tumor Molecular Alterations in Patients With Progressive Locally-advanced or Metastatic Solid Tumors [NCT02029001]	Phase 2	560 participants (Anticipated)	Interventional	2014-03-31	Recruiting
A Randomised, Multicentre, Open Label, Phase II Study of Prophylactic Octreotide to Prevent or Reduce the Frequency and Severity of Diarrhoea in Subjects Receiving Lapatinib With Capecitabine for the Treatment of Metastatic Breast Cancer [NCT02294786]	Phase 2	62 participants (Actual)	Interventional	2014-12-17	Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00073008 (4) [back to overview]	Tumor Response in the Targeted Population Through the End of Treatment
NCT00073008 (4) [back to overview]	Progression-free Survival (PFS) at Four Months in the Non-Targeted Population
NCT00073008 (4) [back to overview]	Progression-free Survival (PFS) at Four Months in the Targeted Population
NCT00073008 (4) [back to overview]	Tumor Response in the Non-Targeted Population Through the End of Treatment
NCT00073528 (34) [back to overview]	Overall Tumor Response (OR) for Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Adjusted Mean Change From Baseline for the FACT-B Total Score Using Observed Data
NCT00073528 (34) [back to overview]	TTP for Participants From the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Time to Seroconversion for Participants Who Were HER2 Negative at Baseline But Became HER2 Positive
NCT00073528 (34) [back to overview]	Time to Progression (TTP) for the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Progression Free Survival (PFS) of Participants in the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	PFS in Participants in the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Overall Tumor Response (OR) for Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Overall Survival in the ITT Population
NCT00073528 (34) [back to overview]	Overall Survival in the HER2-Positive Population
NCT00073528 (34) [back to overview]	Number of Participants With Progression Free Survival (PFS) in the Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced or Metastatic Breast Cancer as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With PFS in the Intent-To-Treat (ITT) Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With Evidence of Brain Metastases in the HER2-Positive Population
NCT00073528 (34) [back to overview]	Number of Participants With Evidence of Brain Metastases From the ITT Population
NCT00073528 (34) [back to overview]	Duration of Response for the Participants With CR or PR in the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Clinical Benefit (CB) in the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Clinical Benefit (CB) in the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With the Indicated Time to Response for CR or PR in the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With the Indicated Expression of Tumor by Epidermal Growth Factor Receptor (ErbB1/HER1/EGFR) at Baseline
NCT00073528 (34) [back to overview]	Duration of Response for the Participants With CR or PR in the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With the Indicated Best Response From the Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the ITT Population as Assessed by the Investigator.
NCT00073528 (34) [back to overview]	Number of Participants With the Indicated Best Response From the Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the HER2-Positive Population as Assessed by the Investigator.
NCT00073528 (34) [back to overview]	Number of Participants With Response in Participants With Baseline Serum HER2 Extracellular Domain (ECD) Baseline Values Greater Than 15 Nanograms Per Milliliter (ng/mL) and 15 ng/mL or Lower
NCT00073528 (34) [back to overview]	Number of Participants With Overall Tumor Response (OR) by Stratification Factors With Measurable Disease, Including Bone Scans, in the ITT Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With Overall Tumor Response (OR) by Stratification Factors With Measurable Disease, Including Bone Scans, in the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With Clinical Benefit Categorized by HER2 ImmunoHistoChemistry (IHC) Intensity
NCT00073528 (34) [back to overview]	Number of Participants With the Indicated Time to Response for CR or PR in the HER2-Positive Population as Assessed by the Investigator
NCT00073528 (34) [back to overview]	Number of Participants With Clinical Benefit Categorized by HER2 Fluorescence in Situ Hybridization (FISH) Status
NCT00073528 (34) [back to overview]	Number of Participants Completing the Functional Assessment of Cancer Therapy-breast (FACT-B) Questionnaire at the Scheduled Visits
NCT00073528 (34) [back to overview]	Number of Participants Classified as QOL Responders Based on the FACT-B, FACT-G, and TOI Total Scores
NCT00073528 (34) [back to overview]	Number of HER2-Negative Participants at Baseline With and Without Seroconversion to a Status of HER2 Positive
NCT00073528 (34) [back to overview]	All Collected Deaths
NCT00073528 (34) [back to overview]	Adjusted Mean Change From Baseline for the Trial Outcome Index (TOI) Score Using Observed Data
NCT00073528 (34) [back to overview]	Adjusted Mean Change From Baseline for the Functional Assessment of Cancer Therapy-General (FACT-G) Score Using Observed Data
NCT00075270 (20) [back to overview]	Overall Survival
NCT00075270 (20) [back to overview]	Percentage of Participants With Clinical Benefit (CB) as Assessed by the Investigator
NCT00075270 (20) [back to overview]	Progression-Free Survival (PFS)
NCT00075270 (20) [back to overview]	Time to Progression as Evaluated by the Independent Review Committee (IRC)
NCT00075270 (20) [back to overview]	Time to Progression as Evaluated by the Investigator
NCT00075270 (20) [back to overview]	Change From Baseline in Functional Assessment of Cancer Therapy-Breast Cancer (FACT-B) Questionnaire Scores
NCT00075270 (20) [back to overview]	Change From Baseline in Functional Assessment of Cancer Therapy-General (FACT-G) Questionnaire Scores
NCT00075270 (20) [back to overview]	Change From Baseline in Trial Outcome Index (TOI) Questionnaire Scores
NCT00075270 (20) [back to overview]	Number of Participants With a Response of CR or PR by the Indicated Study Week
NCT00075270 (20) [back to overview]	Number of Participants With the Indicated ErbB2 Fluorescence in Situ Hybridization (FISH) Results
NCT00075270 (20) [back to overview]	Number of Participants With the Indicated ErbB2 Status at Baseline
NCT00075270 (20) [back to overview]	Number of Participants With the Indicated Immunohistochemistry (IHC) Results at Screening
NCT00075270 (20) [back to overview]	Number of Participants With Tumor Response as Evaluated by the Independent Review Committee
NCT00075270 (20) [back to overview]	Number of Participants With Tumor Response as Evaluated by the Investigator
NCT00075270 (20) [back to overview]	Serum ErbB1 Concentration
NCT00075270 (20) [back to overview]	Serum ErbB2 Concentration
NCT00075270 (20) [back to overview]	Number of Participants With the Indicated Adverse Events (AEs) With a Maximum Toxicity Grade of 3 or 4
NCT00075270 (20) [back to overview]	Duration of Response (DOR)
NCT00075270 (20) [back to overview]	ErbB2 Ratio
NCT00075270 (20) [back to overview]	Number of Participants Who Progressed or Died at or Prior to 6 Months, as a Measure of Six Months Progression-free Survival (PFS)
NCT00089999 (8) [back to overview]	Progression-free Survival, as Assessed by the IRC and Investigator
NCT00089999 (8) [back to overview]	Time to Treatment Failure, as Assessed by IRC and Investigator
NCT00089999 (8) [back to overview]	Time to Response, as Assessed by the IRC and Investigator
NCT00089999 (8) [back to overview]	Duration of Response (DoR), as Assessed by the IRC and Investigator
NCT00089999 (8) [back to overview]	Percentage of Participants With Clinical Benefit (CR or PR or Stable Disease [SD] for at Least 24 Weeks), as Assessed by the IRC and Investigator
NCT00089999 (8) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT00089999 (8) [back to overview]	Number of Participants With a Best Overall Response (OR) of Confirmed Complete Response (CR) or Partial Response (PR), as Assessed by the Investigator
NCT00089999 (8) [back to overview]	Number of Participants With a Best Overall Response (OR) of Confirmed Complete Response (CR) or Partial Response (PR), as Assessed by the Independent Review Committee (IRC)
NCT00095563 (5) [back to overview]	Objective Response Rates (Partial and Complete Responses)
NCT00095563 (5) [back to overview]	Overall Survival (OS)
NCT00095563 (5) [back to overview]	Most Frequent Adverse Events of Grade 1-2 by CTCAE Grading
NCT00095563 (5) [back to overview]	Rate of Stable Disease
NCT00095563 (5) [back to overview]	Progression-free Survival (PFS) According to RECIST
NCT00095940 (6) [back to overview]	Relative Phosphorylation of ERBB2 (Molecular Biology Objective)
NCT00095940 (6) [back to overview]	Tumor to Plasma Lapatinib Concentration (Molecular Biology Objective)
NCT00095940 (6) [back to overview]	Number of Participants With a Sustained Objective Response (Complete or Partial Response) (Phase II Objective)
NCT00095940 (6) [back to overview]	Maximum Concentration of Lapatinib in Plasma (Phase II Objective)
NCT00095940 (6) [back to overview]	Number of Participants With Tumors Expressing Total ERBB2
NCT00095940 (6) [back to overview]	Number of Participants With Tumors Expressing Phosphorylated ERBB2 (Phase II Objective)
NCT00096447 (6) [back to overview]	Overall Survival
NCT00096447 (6) [back to overview]	Frequency and Severity of Adverse Events as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) v 3.0
NCT00096447 (6) [back to overview]	Prognostic Factors (Performance Status)
NCT00096447 (6) [back to overview]	Percentage of Patients With Tumor Response
NCT00096447 (6) [back to overview]	Duration of Progression-free Survival
NCT00096447 (6) [back to overview]	Percentage of Patients With Progression-free Survival > 6 Months
NCT00101036 (4) [back to overview]	Disease Control Rate.
NCT00101036 (4) [back to overview]	Overall Survival
NCT00101036 (4) [back to overview]	Progression-free Survival
NCT00101036 (4) [back to overview]	Response Rate
NCT00103194 (4) [back to overview]	Number of Patients With PSA Response, Defined as a 50% or Greater Decline in the Serum PSA Level
NCT00103194 (4) [back to overview]	Progression-free Survival Rate at 2 Years
NCT00103194 (4) [back to overview]	The Change in PSA Slope With GW572016 (Lapatinib)
NCT00103194 (4) [back to overview]	Relationship Between Progression-free Survival and EGFR Expression Levels
NCT00107536 (7) [back to overview]	Progression-free Survival
NCT00107536 (7) [back to overview]	Overall Survival
NCT00107536 (7) [back to overview]	Toxicity Profile Assessed Using NCI CTCAE Version 3.0
NCT00107536 (7) [back to overview]	Target-EGFR/EGFR-P Protein Expression
NCT00107536 (7) [back to overview]	Proportion of Patients Demonstrating Objective Response (PR+CR) as Defined by RECIST
NCT00107536 (7) [back to overview]	Expression Profile and Mutations of Genes Critical for EGFR and ERBB2 Signaling Pathways
NCT00107536 (7) [back to overview]	Median Overall Survival
NCT00113373 (6) [back to overview]	Prognostic Variable: Cellular Histology
NCT00113373 (6) [back to overview]	Frequency and Severity of Adverse Effects as Assessed by Common Toxicity Criteria for Adverse Events (CTCAE) v3.0
NCT00113373 (6) [back to overview]	Tumor Response
NCT00113373 (6) [back to overview]	Progression-free Survival (PFS) > 6 Months
NCT00113373 (6) [back to overview]	Overall Survival
NCT00113373 (6) [back to overview]	Duration of Progression-free Survival
NCT00118157 (1) [back to overview]	Tumor Response Rate (Complete and Partial) Assessed by Response Evaluation Criteria in Solid Tumors (RECIST)
NCT00206427 (3) [back to overview]	Inhibition of HER1 and HER2 Signaling as Determined by ki67 and CC3
NCT00206427 (3) [back to overview]	Clinical Response
NCT00206427 (3) [back to overview]	Inhibition of HER1 and HER2 Signaling as Determined by EGFR, HER2, and pHER2
NCT00225758 (3) [back to overview]	Determine the Toxicities of the Combination of the Hormonal Agent and Lapatinib in Patients With Metastatic Breast Cancer
NCT00225758 (3) [back to overview]	Determine the Response Rate and Progression Free Survival of Hormone Therapy-resistant Patients With Metastatic Breast Cancer Treated With the Same Continued Hormonal Agent With the Addition of Lapatinib.
NCT00225758 (3) [back to overview]	Progression-free Survival
NCT00246753 (2) [back to overview]	Number of Patients Experiencing Decline in Prostate-specific Antigen
NCT00246753 (2) [back to overview]	Time to Prostate-Specific Antigen (PSA) Progression
NCT00263588 (10) [back to overview]	Percentage of Subjects With a CNS Objective Response or Improvement in Baseline Neurological Signs and Symptoms (NSS)
NCT00263588 (10) [back to overview]	The Percentage of Participants With Central Nervous System (CNS) Objective Response Rate - Response Rate (CR + PR)
NCT00263588 (10) [back to overview]	Percentage of Patients With CNS Disease Control (Complete Response, Partial Response or Stable Disease) at 6 Months of Lapatinib Therapy
NCT00263588 (10) [back to overview]	Overall Survival (OS)
NCT00263588 (10) [back to overview]	Duration of Central Nervous System (CNS) Objective Response
NCT00263588 (10) [back to overview]	Percentage of Participants With Improvement in Neurological Signs and Symptoms (NSS) Measured Using the Neurological Examination Worksheet
NCT00263588 (10) [back to overview]	Time to Progression (TTP) at Any Site
NCT00263588 (10) [back to overview]	The Number of Participants With Central Nervous System (CNS) Best Overall Response
NCT00263588 (10) [back to overview]	Summary of Site of First Progression
NCT00263588 (10) [back to overview]	Primary Cause of Death
NCT00272987 (28) [back to overview]	Number of Participants With the Indicated Eastern Cooperative Oncology Group (ECOG) Performance Status Value
NCT00272987 (28) [back to overview]	Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure at the Indicated Time Points
NCT00272987 (28) [back to overview]	Time to Response as Assessed by the Investigator
NCT00272987 (28) [back to overview]	Number of Participants With the Maximum Toxicity Grade for the Indicated Clinical Hematology Parameters
NCT00272987 (28) [back to overview]	Number of Participants With the Maximum Toxicity Grade for the Indicated Clinical Chemistry Parameters
NCT00272987 (28) [back to overview]	Number of Events of Rash With the Indicated Characteristics
NCT00272987 (28) [back to overview]	Number of Participants With the Indicated Eastern Cooperative Oncology Group (ECOG) Performance Status Value
NCT00272987 (28) [back to overview]	Number of Participants With the Indicated Eastern Cooperative Oncology Group (ECOG) Performance Status Value
NCT00272987 (28) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT00272987 (28) [back to overview]	Change From Baseline in Heart Rate at the Indicated Time Points
NCT00272987 (28) [back to overview]	Change From Baseline in Heart Rate at the Indicated Time Points
NCT00272987 (28) [back to overview]	Number of Events of Hepatotoxicity With the Indicated Characteristics
NCT00272987 (28) [back to overview]	Number of Events of Diarrhea With the Indicated Characteristics
NCT00272987 (28) [back to overview]	Change From Baseline in Body Temperature at the Indicated Time Points
NCT00272987 (28) [back to overview]	Extent of Exposure to Lapatinib, Trastuzumab and Paclitaxel by Median/Min-Max
NCT00272987 (28) [back to overview]	Change From Baseline in Body Temperature at the Indicated Time Points
NCT00272987 (28) [back to overview]	Percentage of Participants With Clinical Benefit (Complete Response (CR), Partial Response (PR), and Stable Disease [SD] for at Least 24 Weeks) as Assessed by Investigator
NCT00272987 (28) [back to overview]	Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure at the Indicated Time Points
NCT00272987 (28) [back to overview]	Extent of Exposure to Lapatinib, Trastuzumab and Paclitaxel by Mean/Standard Deviation
NCT00272987 (28) [back to overview]	Overall Response (OR): Percentage of Participants With a Best Overall Response (OR) of Confirmed Complete Response (CR) or Confirmed Partial Response (PR) as Assessed by the Investigator
NCT00272987 (28) [back to overview]	Number of Participants With at Least 1 Event of Left Ventricular Ejection Fraction Decrease With the Indicated Characteristics
NCT00272987 (28) [back to overview]	Number of Participants Who Received Any Concomitant Medications During the Study Period
NCT00272987 (28) [back to overview]	Number of Participants Who Died Due to Any Cause
NCT00272987 (28) [back to overview]	Change From Baseline in Systolic Blood Pressure and Diastolic Blood Pressure at the Indicated Time Points
NCT00272987 (28) [back to overview]	Change From Baseline in Heart Rate at the Indicated Time Points
NCT00272987 (28) [back to overview]	Change From Baseline in Body Temperature at the Indicated Time Points
NCT00272987 (28) [back to overview]	Duration of Response (DoR), as Assessed by the Investigator
NCT00272987 (28) [back to overview]	Progression-free Survival as Assessed by the Investigator
NCT00281658 (11) [back to overview]	Number of Participants With a CR or PR at Weeks 8, 12, 16, 24, 32, 40, 48, 56, 64, and 72
NCT00281658 (11) [back to overview]	Clinical Benefit Rate (CBR)
NCT00281658 (11) [back to overview]	Overall Survival (OS) at 190 Months
NCT00281658 (11) [back to overview]	Overall Survival (OS) at 53 Months
NCT00281658 (11) [back to overview]	Predictive Effect of PIK3CA Mutations Status on Clinical Benefit Rate (CBR)
NCT00281658 (11) [back to overview]	Predictive Effect of PIK3CA Mutations Status on Overall Response Rate (ORR)
NCT00281658 (11) [back to overview]	Predictive Effect of PTEN Low on Clinical Benefit Rate (CBR)
NCT00281658 (11) [back to overview]	Duration of Response (DOR)
NCT00281658 (11) [back to overview]	Progression-free Survival (PFS) by Investigator Assessment
NCT00281658 (11) [back to overview]	Predictive Effect of PTEN Low on Overall Response Rate (ORR)
NCT00281658 (11) [back to overview]	Overall Response Rate (ORR) by Investigator Assessment
NCT00320385 (5) [back to overview]	Overall Tumor Response (OR)
NCT00320385 (5) [back to overview]	Progression-Free Survival (PFS)
NCT00320385 (5) [back to overview]	Change From Baseline in Functional Assessment of Cancer Therapy-Breast (FACT-B) Scores at Week 4, Week 12, Week 16, Week 24, and Conclusion or Withdrawal From Study
NCT00320385 (5) [back to overview]	Overall Survival (OS)
NCT00320385 (5) [back to overview]	Clinical Benefit Response (CBR)
NCT00320411 (18) [back to overview]	Mean Insulin-like Growth Factor 1 Receptor (IGF1R) H Score for All Participants
NCT00320411 (18) [back to overview]	Mean p-BAD H Score for All Participants
NCT00320411 (18) [back to overview]	Mean Phosphorylated 58 kDa Serine/Threonine Protein Kinase (p-AKT) H Score for All Participants
NCT00320411 (18) [back to overview]	Mean Survivin H Score for All Participants
NCT00320411 (18) [back to overview]	Mean Terminal Deoxynucleotidyl Transferase Biotin-dUTP Nick End Labeling (TUNEL) H Score for All Participants
NCT00320411 (18) [back to overview]	Overall Survival
NCT00320411 (18) [back to overview]	Time to Progression
NCT00320411 (18) [back to overview]	Time to Response
NCT00320411 (18) [back to overview]	Mean Phosphorylated Extracellular Signal-regulated Kinase (p-ERK) H Score for All Participants
NCT00320411 (18) [back to overview]	6-month Progression Free Survival
NCT00320411 (18) [back to overview]	Clinical Benefit
NCT00320411 (18) [back to overview]	Duration of Response
NCT00320411 (18) [back to overview]	Mean Bcl-2 H Score for All Participants
NCT00320411 (18) [back to overview]	Mean Epidermal Growth Factor Receptor 3 (ErbB3) H Score for All Participants
NCT00320411 (18) [back to overview]	Mean Epidermal Growth Factor Receptor 4 (ErbB4) H Score for All Participants
NCT00320411 (18) [back to overview]	4-month Progression Free Survival
NCT00320411 (18) [back to overview]	Mean Heregulin H Score for All Participants
NCT00320411 (18) [back to overview]	Overall Tumor Response
NCT00331630 (7) [back to overview]	Pathologic Complete Response (pCR)
NCT00331630 (7) [back to overview]	Proliferation (Ki67) Measured at Baseline and After Completion of Study Treatment
NCT00331630 (7) [back to overview]	Side Effects From the Combination of Abraxane and Lapatinib
NCT00331630 (7) [back to overview]	Epidermal Growth Factor Receptor (EGFR), and Matrix Metalloproteinases (MMPs), Measured at Baseline and After Completion of Study Treatment
NCT00331630 (7) [back to overview]	Clinical Response Rate (cRR)
NCT00331630 (7) [back to overview]	Apoptosis (Cleaved Caspase-3) Measured at Baseline and After Completion of Study Treatment
NCT00331630 (7) [back to overview]	Angiogenesis (vW, CD34) Markers as Measured at Baseline and After Completion of Study Treatment
NCT00347919 (6) [back to overview]	Overall Survival for Cohort 1
NCT00347919 (6) [back to overview]	Duration of Response in Cohort 1
NCT00347919 (6) [back to overview]	Percentage of Participants With Progressive Disease at Week 12 in Cohort 1
NCT00347919 (6) [back to overview]	Response at Week 12 for Cohort 1 and Cohort 2
NCT00347919 (6) [back to overview]	Time to Response (Complete or Partial Response) in Cohort 1 and Cohort 2
NCT00347919 (6) [back to overview]	Percentage of Participants With Progressive Disease at Week 12
NCT00350727 (37) [back to overview]	Overall Response (OR) in Phase II Based GlaxoSmithKline's Evaluation
NCT00350727 (37) [back to overview]	Overall Response (OR) in Phase II Based on an Independent Radiologist's Review
NCT00350727 (37) [back to overview]	Overall Response (OR) in Phase II Based on the Investigator-assigned Response
NCT00350727 (37) [back to overview]	Progression-free Survival at 6 Months
NCT00350727 (37) [back to overview]	Progression-free Survival
NCT00350727 (37) [back to overview]	Number of Participants With the Indicated Change From Baseline to Study Completion in Diastolic Blood Pressure
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in the Study for Lymphocytes, Neutrophils, Platelet Count, and White Blood Count
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Total Bilirubin and Creatinine
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Thyroxine and Free T3 (Triiodothyronine)
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Thyroid Stimulating Hormone
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Partial Thromboplastin Time and Prothrombin Time
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Lymphocytes, Neutrophils, Platelet Count, and White Blood Count
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Calcium, Glucose, Potassium, Magnesium, Inorganic Phosphorus, Sodium, and Urea
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Amylase and Lipase
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Calcium, Glucose, Potassium, Magnesium, Inorganic Phosphorus, Sodium, and Urea
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Alkaline Phosphatase, Alanine Aminotransferase, Aspartate Aminotransferase, and Lactate Dehydrogenase
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Total Bilirubin and Creatinine
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for International Normalized Ratio (Prothrombin Time)
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Hemoglobin
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Hematocrit
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Free T3 (Triiodothyronine)
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Albumin
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Partial Thromboplastin Time and Prothrombin Time
NCT00350727 (37) [back to overview]	Number of Participants With the Indicated Change From Baseline to Study Completion in Heart Rate
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Amylase and Lipase
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Alkaline Phosphatase, Alanine Aminotransferase, Aspartate Aminotransferase, and Lactate Dehydrogenase
NCT00350727 (37) [back to overview]	Time to Disease Progression or Death Due to Any Cause
NCT00350727 (37) [back to overview]	Number of Participants Experiencing a Dose-limiting Toxicity at the Indicated Dose
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Total T3
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Thyroid Stimulating Hormone
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for International Normalized Ratio (Prothrombin Time)
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Hemoglobin
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Hematocrit
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase II of the Study for Albumin
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Total T3
NCT00350727 (37) [back to overview]	Mean Change From Baseline to Maximum Value in Phase I of the Study for Thyroxine
NCT00350727 (37) [back to overview]	Number of Participants With the Indicated Change From Baseline to Study Completion in Systolic Blood Pressure
NCT00356811 (10) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT00356811 (10) [back to overview]	Number of Participants With a Best Overall Response (OR) of Confirmed Complete Response (CR) or Partial Response (PR), as Assessed by the Investigator
NCT00356811 (10) [back to overview]	Number of Participants With a Best Overall Response (OR) of Confirmed Complete Response (CR) or Partial Response (PR), as Assessed by the Independent Review Committee (IRC)
NCT00356811 (10) [back to overview]	Time to Response, as Assessed by the IRC
NCT00356811 (10) [back to overview]	Time to Response, as Assessed by the Investigator
NCT00356811 (10) [back to overview]	Overall Survival
NCT00356811 (10) [back to overview]	Duration of Response (DoR), as Assessed by the IRC
NCT00356811 (10) [back to overview]	Duration of Response (DoR), as Assessed by the Investigator
NCT00356811 (10) [back to overview]	Time to Progression, as Assessed by the IRC and the Investigator
NCT00356811 (10) [back to overview]	Progression-free Survival, as Assessed by the IRC and the Investigator
NCT00371566 (33) [back to overview]	Adverse Events (AEs) by Maximum Toxicity Grade 4 During or After Chemoradiotherapy Phase
NCT00371566 (33) [back to overview]	Adverse Events by Maximum Toxicity Grade 3 During or After Chemoradiotherapy Phase
NCT00371566 (33) [back to overview]	Adverse Events by Maximum Toxicity Grade 5 During or After Chemoradiotherapy Phase
NCT00371566 (33) [back to overview]	Comparison of Overall Response During Follow up Phase Using CT/MRI and PET Information
NCT00371566 (33) [back to overview]	Comparison of Overall Response During Treatment Phase Using CT/MRI and PET Information
NCT00371566 (33) [back to overview]	Number of Biomarkers Including ErbB1, ErbB2, pErbB1, and pErb2 at Baseline and During Treatment Phase
NCT00371566 (33) [back to overview]	Number of Biomarkers Including Tumor Protein 53 and HPV During Treatment Phase
NCT00371566 (33) [back to overview]	Number of Circulating Tumor Cells at Baseline in mITT Population
NCT00371566 (33) [back to overview]	Number of Participants With Circulating Tumor Cells After Chemoradiotherapy Phase in mITT Population
NCT00371566 (33) [back to overview]	Number of Participants With Circulating Tumor Cells After Treatment Phase in mITT Population
NCT00371566 (33) [back to overview]	Overall Radiological Response After Follow-up Phase in ITT Population
NCT00371566 (33) [back to overview]	Overall Radiological Response After Follow-up Phase in mITT Population
NCT00371566 (33) [back to overview]	Overall Radiological Response After Treatment Phase in ITT Population
NCT00371566 (33) [back to overview]	Overall Radiological Response After Treatment Phase in mITT Population
NCT00371566 (33) [back to overview]	Summary of Adverse Events by Maximum Toxicity Grade (Grade 3 or Higher) Started During or After the Chemoradiotherapy Phase
NCT00371566 (33) [back to overview]	Summary of Adverse Events by Maximum Toxicity Grade Started During Treatment Phase
NCT00371566 (33) [back to overview]	Summary of Adverse Events Experienced by 15% or More Subjects in Either Treatment Group
NCT00371566 (33) [back to overview]	Summary of Fatal/Serious Adverse Events During or After Chemoradiotherapy Phase
NCT00371566 (33) [back to overview]	Summary of Serious Adverse Events During or After Chemoradiotherapy Phase
NCT00371566 (33) [back to overview]	Change From Baseline of Cell Proliferation Rate of the Ki-67 Proliferative Index in Tumour Biopsy Samples During Treatment Phase
NCT00371566 (33) [back to overview]	Change From Baseline of the Apoptotic Index During Treatment Phase
NCT00371566 (33) [back to overview]	Relative Change From Baseline of IAUC Mean (90) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of IAUC Median (90) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Kep Mean (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Kep Median (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Kep Perfused (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Kep Whole (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Ktrans Mean (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Ktrans Median (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Ktrans Perfused (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Ktrans Whole (1/Min) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Perfused IAUC (90) After 2 - 4 Weeks of Treatment
NCT00371566 (33) [back to overview]	Relative Change From Baseline of Whole IAUC(90) After 2 - 4 Weeks of Treatment
NCT00374322 (14) [back to overview]	Number of Participants With Any Recurrence of the Initial Disease, Contralateral Breast Cancer, or Death (Disease-free Survival [DFS])
NCT00374322 (14) [back to overview]	Number of Participants With CNS Recurrence
NCT00374322 (14) [back to overview]	Number of Participants With Clinical Chemistry Values Outside the Reference Range for the Indicated Parameters
NCT00374322 (14) [back to overview]	Percentage of Participants With the Indicated Period of Recurrence-free Survival (Time to First Recurrence)
NCT00374322 (14) [back to overview]	Change From Baseline in Short Form-36 Version 2 (SF-36 v2) Scores for the Physical Component Summary (PCS)
NCT00374322 (14) [back to overview]	Change From Baseline in SF-36 v2 Scores for the Mental Component Summary (MCS)
NCT00374322 (14) [back to overview]	Percentage of Participants With the Indicated Period of Distant Recurrence-free Survival (Time to Distant Recurrence)
NCT00374322 (14) [back to overview]	Number of Participants With the Indicated Electrocardiogram (ECG) Findings
NCT00374322 (14) [back to overview]	Number of Participants With Non-laboratory Toxicities of the Indicated Toxicity Grades
NCT00374322 (14) [back to overview]	Number of Participants With Hematology Values Outside the Reference Range for the Indicated Parameters
NCT00374322 (14) [back to overview]	Number of Participants Who Died (Overall Survival)
NCT00374322 (14) [back to overview]	Number of Participants Experiencing Primary or Secondary Cardiac Events
NCT00374322 (14) [back to overview]	Number of Participants (Par.) With Any Recurrence of the Initial Disease, Second Primary Cancer, Contralateral Breast Cancer, or Death (Disease-free Survival [DFS])
NCT00374322 (14) [back to overview]	Change From Baseline in the SF-36 v2 Domain Scores for Physical Functioning (PF), Role-Physical (RP), Bodily Pain (BP), General Health (GH), Vitality (VT), Social Functioning (SF), Role-Emotional (RE), and Mental Health (MH)
NCT00387127 (14) [back to overview]	Number of Participants With Distant Recurrence of Initial Disease
NCT00387127 (14) [back to overview]	Number of Participants Positive and Negative for the Expression of Biomarkers in Tumor Tissue: Human Epidermal Growth Factor Receptor (HER)-1, HER2, HER3, HER4, P16, and Transforming Growth Factor (TGF-alpha)
NCT00387127 (14) [back to overview]	Number of Participants (Par.) With Complete Response (CR), as Assessed by Independent Radiological Review
NCT00387127 (14) [back to overview]	Number of Participants With CR, as Assessed by the Investigator
NCT00387127 (14) [back to overview]	Disease-specific Survival
NCT00387127 (14) [back to overview]	Number of Participants With Loco-regional Recurrence of Initial Disease
NCT00387127 (14) [back to overview]	Number of Participants With Overall Response (OR), as Assessed by the Investigator
NCT00387127 (14) [back to overview]	Overall Survival (OS)
NCT00387127 (14) [back to overview]	Distant Relapse
NCT00387127 (14) [back to overview]	Number of Participants Positive and Negative for Biomarker HER1/ErbB1 Categorized in the Indicated Independent Review Panel-assessed Tumor Responses by Expression of Biomarkers From Tumor Tissues: Sensitivity Analysis - 0, 1, 2 Versus 3
NCT00387127 (14) [back to overview]	Number of Participants Who Died Due to Progressive Disease
NCT00387127 (14) [back to overview]	Progression-Free Survival (PFS), as Assessed by the Investigator
NCT00387127 (14) [back to overview]	Number of Participants Negative and Positive for Human Papilloma Virus (HPV) Infection, as Determined From Tumor Samples
NCT00387127 (14) [back to overview]	Number of Participants Positive and Negative for Biomarker HER1/ErbB1 Categorized in the Indicated Independent Review Panel-assessed Tumor Responses by Expression of Biomarkers From Tumor Tissue: Sensitivity Analysis - 0 Versus (1, 2, 3)
NCT00390455 (7) [back to overview]	Progression-free Survival (PFS)
NCT00390455 (7) [back to overview]	Objective Tumor Response Rate for Participants With HER2-positive Tumors
NCT00390455 (7) [back to overview]	Objective Tumor Response Rate
NCT00390455 (7) [back to overview]	Progression-free Survival for Participants With HER2-positive Tumors
NCT00390455 (7) [back to overview]	Progression-free Survival for Participants With HER2-negative Tumors
NCT00390455 (7) [back to overview]	Objective Tumor Response Rate for Participants With HER2-negative Tumors
NCT00390455 (7) [back to overview]	Overall Survival (OS)
NCT00404066 (2) [back to overview]	Percentage of Participants With Pathologic Complete Response (pCR)
NCT00404066 (2) [back to overview]	Disease-free Survival (DFS)
NCT00422903 (10) [back to overview]	Number of Participants With Breast Tumors Per Pathological Stage at Surgery
NCT00422903 (10) [back to overview]	Number of Participants With the Indicated Adverse Events With a Classification of >=Grade 2
NCT00422903 (10) [back to overview]	Number of Participants With the Indicated Nodal Status at Surgery
NCT00422903 (10) [back to overview]	Time to Treatment Failure From the Start of the Primary Therapy
NCT00422903 (10) [back to overview]	Number of Participants With the Indicated Type of Surgery
NCT00422903 (10) [back to overview]	Mean Left Ventricular Ejection Fraction (LVEF)
NCT00422903 (10) [back to overview]	Percentage of Participants With Conversion From Planned Mastectomy at Baseline to BCS at Surgery
NCT00422903 (10) [back to overview]	Percentage of Participants With Pathological Complete Response (pCR) in the Breast and Axillary Nodes, Evaluated Using Miller and Payne Criteria
NCT00422903 (10) [back to overview]	Percentage of Participants With Various Responses in the Breast, Evaluated Using Per Protocol Criteria
NCT00422903 (10) [back to overview]	Percentage of Participants With Clinical Objective Response (cOR) in the Breast, Evaluated by an Independent Radiological Evaluation Monitoring Committee
NCT00424255 (21) [back to overview]	Number of Participants With Abnormal 12-lead Electrocardiogram (ECG) Findings at the Indicated Time Points
NCT00424255 (21) [back to overview]	Change From Baseline in Quality of Life Status as Assessed by the Functional Assessement of Cancer Therapy-Head and Neck (FACT-H&N) Questionnaire
NCT00424255 (21) [back to overview]	Change From Baseline in Heart Rate at the Indicated Time Points
NCT00424255 (21) [back to overview]	Change From Baseline in Quality of Life Status as Assessed by the EuroQol-5D (EQ-5D) Scale
NCT00424255 (21) [back to overview]	Change From Baseline in Body Temperature at the Indicated Time Points
NCT00424255 (21) [back to overview]	Change From Baseline in Blood Pressure at the Indicated Time Points
NCT00424255 (21) [back to overview]	Time to Locoregional Recurrence (TTLR)
NCT00424255 (21) [back to overview]	Time to Distant Relapse (TTDR)
NCT00424255 (21) [back to overview]	Number of Participants With the Indicated Worst-case On-therapy Left Ventricular Ejection Fraction (LVEF) Change From Baseline
NCT00424255 (21) [back to overview]	Overall Survival (OS)
NCT00424255 (21) [back to overview]	Disease Specific Survival (DSS)
NCT00424255 (21) [back to overview]	Disease Free Survival (DFS)
NCT00424255 (21) [back to overview]	Change From Baseline in Body Weight at the Indicated Time Points
NCT00424255 (21) [back to overview]	Number of Participants With the Indicated Hematological Toxicities by Maximum Toxicity Grade (G3 and G4) at the Worst-case On-therapy Visit
NCT00424255 (21) [back to overview]	Number of Participants With the Indicated Eastern Cooperative Oncology Group (ECOG) Performance Status Value
NCT00424255 (21) [back to overview]	Number of Participants With the Indicated Chemistry Toxicities by Maximum Toxicity Grade (G3 and G4) at the Worst-case On-therapy Visit
NCT00424255 (21) [back to overview]	Number of Participants With the Indicated Biomarker Expression Status
NCT00424255 (21) [back to overview]	Number of Participants With On-therapy and Follow-up Late Radiation Morbidity Events
NCT00424255 (21) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT00424255 (21) [back to overview]	Extent of Exposure
NCT00424255 (21) [back to overview]	Number of Participants With a Second Primary Tumor
NCT00429299 (8) [back to overview]	Percentage of Participants With Pathological Complete Response (pCR) in the Breast and in the Lymph Nodes
NCT00429299 (8) [back to overview]	Time to Treatment Failure From the Start of Primary Therapy
NCT00429299 (8) [back to overview]	Percentage of Participants With the Indicated Clinical Objective Response (Complete Response and Partial Response), Stable Disease, and Progressive Disease, as Assessed by Ultrasonography
NCT00429299 (8) [back to overview]	Percentage of Participants Who Had Breast-conserving Surgery (BCS), Mastectomy, and Conversion From Mastectomy to BCS
NCT00429299 (8) [back to overview]	Percentage of Inhibition of Biomarkers Ki67, pAKT, pMAPK, Tunel Test, PTEN, and pEGFR After Treatment
NCT00429299 (8) [back to overview]	Number of Participants With Any Adverse Event (AE), Including Serious Adverse Events (SAEs), Occurring in >=5% of Participants
NCT00429299 (8) [back to overview]	Number of Participants With Treatment Failure
NCT00429299 (8) [back to overview]	Number of Variations/Somatic Mutation in PI3KCA at Baseline
NCT00430781 (8) [back to overview]	Progression-free Survival (PFS) in Interim Analysis
NCT00430781 (8) [back to overview]	Response
NCT00430781 (8) [back to overview]	Time to Response
NCT00430781 (8) [back to overview]	Safety and Tolerability of Pazopanib, Lapatinib and the Combination of Pazopanib and Lapatinib
NCT00430781 (8) [back to overview]	Progression-free Survival (PFS) in Final Analysis
NCT00430781 (8) [back to overview]	Clinical Benefit Response
NCT00430781 (8) [back to overview]	Duration of Response
NCT00430781 (8) [back to overview]	Overall Survival
NCT00436566 (9) [back to overview]	Cumulative Incidence (CI) of Cardiac Events
NCT00436566 (9) [back to overview]	Number of Patients With Congestive Heart Failure (CHF) While on Active Treatment
NCT00436566 (9) [back to overview]	Percentage of Participants With Disease-Free Survival (DFS)
NCT00436566 (9) [back to overview]	Percentage of Participants With Overall Survival (OS)
NCT00436566 (9) [back to overview]	Incidence of Pulmonary Events
NCT00436566 (9) [back to overview]	Adverse Event Profile as Measured by NCI CTCAE v 3.0
NCT00436566 (9) [back to overview]	Change in Overall LINEAR ANALOGUE SELF ASSESSMENT (LASA) and Change in Symptom Distress Scale (SDS) Overall QOL
NCT00436566 (9) [back to overview]	Number of Patients Who Experience >= 10 Percent Drop in Left Ventricular Ejection Fraction (LVEF)
NCT00436566 (9) [back to overview]	Proportion of Patients Experienced a Significant Decline in LINEAR ANALOGUE SELF ASSESSMENT (LASA) and a Overall Symptom Distress Scale (SDS) QOL Measurements
NCT00436644 (4) [back to overview]	Time to Progression
NCT00436644 (4) [back to overview]	Adverse Event Profile
NCT00436644 (4) [back to overview]	Response Rate (Complete Response (CR) or Partial Response (PR))
NCT00436644 (4) [back to overview]	Overall Survival
NCT00437073 (2) [back to overview]	Number of Participants With the Indicated Central Nervous System (CNS) Objective Response (OR)
NCT00437073 (2) [back to overview]	Number of Participants With the Indicated CNS Responses
NCT00444535 (7) [back to overview]	Progression-free Survival - Kaplan-Meier Estimates for Progression-free Survival (Weeks) - 1st and 3rd Quartile
NCT00444535 (7) [back to overview]	Overall Tumor Response Rate Per Investigator Assessment (RECIST)
NCT00444535 (7) [back to overview]	Investigator-Assessed Clinical Benefit Response Rate (%) (RECIST)
NCT00444535 (7) [back to overview]	Progression-free Survival - Kaplan-Meier Estimates for Progression-free Survival (Weeks) - Median
NCT00444535 (7) [back to overview]	Investigator-evaluated Crude Progression-free Survival Rate After 12 Weeks of Study Treatment
NCT00444535 (7) [back to overview]	Overall Tumor Response - Best Response Per Investigator Assessment (RECIST)
NCT00444535 (7) [back to overview]	Progression-free Survival
NCT00447122 (1) [back to overview]	Overall Survival for Patients With Metastatic Pancreatic Cancer.
NCT00447226 (4) [back to overview]	Percentage of Participants Who Remained Progression-free 12 Weeks After Randomization
NCT00447226 (4) [back to overview]	Time to Disease Progression (TTP)
NCT00447226 (4) [back to overview]	Number of Participants With the Indicated Tumor Response at 12 Weeks From First Dose
NCT00447226 (4) [back to overview]	Number of Participants With the Indicated Change in Cancer Antigen-125 (CA-125) Levels From Day 1
NCT00470704 (6) [back to overview]	Top 3 Most Common Treatment RelatedToxicities
NCT00470704 (6) [back to overview]	Sites of First Progression
NCT00470704 (6) [back to overview]	Objective Response Rate
NCT00470704 (6) [back to overview]	Median Time to Progression
NCT00470704 (6) [back to overview]	Clinical Benefit Rate
NCT00470704 (6) [back to overview]	3-Year Overall Survival
NCT00470847 (6) [back to overview]	Overall Survival
NCT00470847 (6) [back to overview]	Percentage of Participants Having Non-Central Nervous System Sites as the Site of First Progression
NCT00470847 (6) [back to overview]	Percentage of Participants Having Central Nervous System as the Site of the First Progression
NCT00470847 (6) [back to overview]	Objective Response Rate in Central Nervous System Sites
NCT00470847 (6) [back to overview]	The Maximum Tolerated Dose of Lapatinib When Combined With Cranial Radiation in Patients With CNS Metastases From HER2-positive Breast Cancer.
NCT00470847 (6) [back to overview]	Progression Free Survival
NCT00477464 (20) [back to overview]	Objective Response (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Maximum Plasma Concentration (Cmax) of Lapatinib
NCT00477464 (20) [back to overview]	Duration of Response (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Clinical Benefit Response (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Trough Concentration of Capecitabine, 5-FU, and FBAL
NCT00477464 (20) [back to overview]	Trough Concentration of Lapatinib
NCT00477464 (20) [back to overview]	AUC0-tau of Capecitabine, 5'-Fluorouracil (5-FU), and Alpha-fluoro-beta-alanine (FBAL)
NCT00477464 (20) [back to overview]	Area Under the Plasma Concentration-time Curve From Zero to 12 Hours (AUC0-12) of Capecitabine, 5'-Fluorouracil (5-FU), and Alpha-fluoro-beta-alanine (FBAL)
NCT00477464 (20) [back to overview]	Time to Response (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Time to Progression (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Area Under the Plasma Concentration-time Curve Within the Dosing Interval AUC0-tau of Lapatinib
NCT00477464 (20) [back to overview]	Area Under the Plasma Concentration-time Curve From Zero to 24 Hours AUC0-24 of Lapatinib
NCT00477464 (20) [back to overview]	6-Month Progression-free Survival (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Time to Maximum Plasma Concentration (Tmax) of Lapatinib
NCT00477464 (20) [back to overview]	Terminal Elimination Half-life (t1/2) of Lapatinib
NCT00477464 (20) [back to overview]	Progression-free Survival (PFS) (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Overall Survival (Independent Reviewer-assessed)
NCT00477464 (20) [back to overview]	Cmax of Capecitabine, 5'-Fluorouracil (5-FU), and Alpha-fluoro-beta-alanine (FBAL)
NCT00477464 (20) [back to overview]	t1/2 of Capecitabine, 5'-Fluorouracil (5-FU), and Alpha-fluoro-beta-alanine (FBAL)
NCT00477464 (20) [back to overview]	Tmax of Capecitabine, 5'-Fluorouracil (5-FU), and Alpha-fluoro-beta-alanine (FBAL)
NCT00479856 (1) [back to overview]	Overall Tumor Response
NCT00482391 (2) [back to overview]	Number of Patients Who Completed All Planned Therapy
NCT00482391 (2) [back to overview]	Number of Patients Who Were Evaluated for Toxicity
NCT00486954 (44) [back to overview]	Number of Participants With the Indicated Epidermal Growth Factor Receptor (EGFR) Immunohistochemistry Intensity in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Appetite Loss Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Cognitive Functioning Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Constipation Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Anxiety Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Number of Participants With the Indicated Time to Response in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Area Under the Concentration-time Curve From Time Zero to 24 Hours (AUC[0-24]) of Lapatinib in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Body Image Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Tmax of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Time to Cmax (Tmax) of Lapatinib in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Social Functioning Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Financial Difficulties Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Number of Participants With the Indicated Human Epidermal Growth Factor Receptor 2 (HER2) Immunohistochemistry Intensity in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Number of Participants With the Indicated Grade 3 and Grade 4 Adverse Events (AEs) for Which All Grades of the AE Were Reported in >=10% of Participants, Regardless of Causality in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Role Functioning Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Physical Functioning Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Pain Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Nausea and Vomiting Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Insomnia Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Fatigue Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Emotional Functioning Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Dyspnea Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-C30 Diarrhea Symptom Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Maximum Plasma Concentration (Cmax) of Lapatinib in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Half-life of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Area Under the Concentration-time Curve From Time Zero to Infinity (AUC[0-inf]) of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Distribution Volume at Steady State (Vss) of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Cmax of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Clearance of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	AUC(0-24) of Paclitaxel in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Time to Progression in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Progression-free Survival (PFS) in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Percentage of Participants With Overall Response in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Overall Survival (OS) in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Number of Participants With Dose Limiting Toxicities (DLTs) in the Pilot Part of the Study
NCT00486954 (44) [back to overview]	Duration of Response in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the European Organization for Research and Treatment of Cancer Quality of Life (QOL) Questionnaire (EORTC QLQ-C30) Global Health Status (GHS)/QOL Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Taste Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Reflux Symptoms Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Pain Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Hair Loss Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Eating Restrictions Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Dysphagia Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00486954 (44) [back to overview]	Change From Baseline in the EORTC QLQ-STO22 Dry Mouth Scale Score at the End of Therapy in the Randomized Part of the Study
NCT00490061 (2) [back to overview]	Progression Free Survival
NCT00490061 (2) [back to overview]	Overall Survival.
NCT00490139 (6) [back to overview]	Time to Central Nervous System Recurrence
NCT00490139 (6) [back to overview]	DFS Ignoring Non-breast Second Primary Malignancies
NCT00490139 (6) [back to overview]	Disease-free Survival (DFS)
NCT00490139 (6) [back to overview]	Overall Survival (OS)
NCT00490139 (6) [back to overview]	Time to Distant Recurrence
NCT00490139 (6) [back to overview]	Time to Recurrence
NCT00496366 (2) [back to overview]	Determine the Response Rate (as Determined by RECIST Criteria) of Capecitabine and Lapatinib as First-line Therapy in Patients With Advanced or Metastatic Breast Cancer That Overexpress HER2.
NCT00496366 (2) [back to overview]	-Determine the Clinical Benefit Rate (Complete Response, Partial Response, or Stable Disease for at Least 6 Months) of Capecitabine and Lapatinib. -Determine Time to Disease Progression After Treatment With Capecitabine and Lapatinib. -Evaluate Overall
NCT00499681 (1) [back to overview]	Number of Participants With a Pathological Complete Response
NCT00508274 (7) [back to overview]	All Collected Deaths
NCT00508274 (7) [back to overview]	Duration of Response (DOR)
NCT00508274 (7) [back to overview]	Number of Participants With Central Nervous System (CNS) as First Site of Relapse
NCT00508274 (7) [back to overview]	Clinical Benefit Rate (CBR)
NCT00508274 (7) [back to overview]	Time to Response (TTR)
NCT00508274 (7) [back to overview]	Six Months Progression-Free Survival
NCT00508274 (7) [back to overview]	Progression-Free Survival (PFS)
NCT00524303 (6) [back to overview]	Mean Intra-tumoral Expression of the Indicated Proteins at Baseline and Day 14
NCT00524303 (6) [back to overview]	Number of Participants With the Indicated Electrocardiogram (ECG) Status at Baseline and at EOT or Early Withdrawal
NCT00524303 (6) [back to overview]	Cumulative Number of Participants With at Least One Decrease of More Than or Equal to 20% in Left Ventricular Ejection Fraction (LVEF) at the Indicated Time Points Compared to LVEF at Baseline
NCT00524303 (6) [back to overview]	Percentage of Participants With Overall Pathological Complete Response (pCR) After 26 Weeks of Therapy
NCT00524303 (6) [back to overview]	Percentage of Participants With Clinical Complete Response (cCR) at 26 Weeks or at End of Treatment (EOT) or Early Withdrawal
NCT00524303 (6) [back to overview]	Percentage of Participants (Par.) With Disease-free Survival (DFS) at the End of 5 Years From Randomization
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for White Blood Cell (WBC) Count at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as Any Grade Increase [AGI], Increase to Grade 3 [ItoG3], and Increase to Grade 4 [ItoG4]) in Toxicity Grades for Albumin at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Total Neutrophils at the Indicated Time Points
NCT00526669 (26) [back to overview]	Time to Progression (All Deaths Due to Non-PD Are Treated as Competing Risk)
NCT00526669 (26) [back to overview]	Duration of Response
NCT00526669 (26) [back to overview]	Percentage of Participants (Par.) With 5-month Progression-free Survival (PFS)
NCT00526669 (26) [back to overview]	PFS
NCT00526669 (26) [back to overview]	Response Rate (Measured as the Percentage of Participants With Response [Complete Response or Partial Response])
NCT00526669 (26) [back to overview]	Time to Progression (All Deaths Are Treated as Competing Risk)
NCT00526669 (26) [back to overview]	Time to Response
NCT00526669 (26) [back to overview]	Change From Start of Run-in Period in Biomarker Expression Levels at Day 0
NCT00526669 (26) [back to overview]	Number of Participants in the Indicated Categories for Best Overall Response (BOR)
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4 ) in Toxicity Grades for Alanine Aminotransferase (ALT) at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Alkaline Phosphatase (ALP) at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Aspartate Aminotransferase (AST) at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Calcium at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Creatinine at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Glucose at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Hemoglobin at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Lymphocytes at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Magnesium at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Platelet Count at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Potassium at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Sodium at the Indicated Time Points
NCT00526669 (26) [back to overview]	Number of Participants With Change From Baseline (Measured as AGI, ItoG3, and ItoG4) in Toxicity Grades for Total Bilirubin at the Indicated Time Points
NCT00526669 (26) [back to overview]	Overall Survival (OS)
NCT00536809 (1) [back to overview]	Overall Response in Phase II
NCT00548184 (1) [back to overview]	Pathologic Assessment After Study Treatment
NCT00553358 (22) [back to overview]	Event-free Survival (EFS) - Events and Censoring
NCT00553358 (22) [back to overview]	Event-free Survival (EFS) - Median Clinical Follow-up
NCT00553358 (22) [back to overview]	Number of Participants Starting Paclitaxel Before Completing 6 Weeks of Treatment With Either Lapatinib or Trastuzumab
NCT00553358 (22) [back to overview]	Number of Participants With Negative Lymph Nodes at the Time of Surgery
NCT00553358 (22) [back to overview]	Number of Participants With Pathological Complete Response (pCR) at the Time of Surgery
NCT00553358 (22) [back to overview]	Overall Survival (OS) - Median Survival Follow-up
NCT00553358 (22) [back to overview]	Percentage of Participants With Circulating Tumor Cells (CTC) in the Bloodstream
NCT00553358 (22) [back to overview]	Percentage of Participants With the Indicated Biomarker Expression - PIK3CA.
NCT00553358 (22) [back to overview]	Ratio (95% CI) of Geometric Means in p95HER2 Expression in HR Positive Patients With pCR vs no pCR
NCT00553358 (22) [back to overview]	To Assess Safety Via a Comparison of the Three Treatment Arms - to Measure On-treatment Primary Cardiac Endpoints
NCT00553358 (22) [back to overview]	All Collected Deaths
NCT00553358 (22) [back to overview]	Assess Associations Between Locoregional Pathological Complete Response (pCR) and and Overall Survival (OS) - Median Clinical Follow-up (OS Landmark Population)
NCT00553358 (22) [back to overview]	Assess Associations Between Locoregional Pathological Complete Response (pCR) and and Overall Survival (OS) - Number of Participants Who Died (OS Landmark Population)
NCT00553358 (22) [back to overview]	Assess Associations Between Locoregional Pathological Complete Response (pCR) and Event-free Survival (EFS) - Median Clinical Follow-up (EFS Landmark Population)
NCT00553358 (22) [back to overview]	Assess Associations Between Locoregional Pathological Complete Response (pCR) and Event-free Survival (EFS) - Number of Participants With EFS Events (EFS Landmark Population)
NCT00553358 (22) [back to overview]	Mean Change From Baseline in Tumor Size at Week 6 and at Surgery
NCT00553358 (22) [back to overview]	Metabolic Response Rate Determined by Positron Emission Tomography/Computed Tomography (PET/CT)
NCT00553358 (22) [back to overview]	Number of Participants With Actual Indicated Surgery
NCT00553358 (22) [back to overview]	Number of Participants With Overall Response at Week 6
NCT00553358 (22) [back to overview]	Overall Response at the Time of Surgery
NCT00553358 (22) [back to overview]	Overall Survival (OS) - Deaths and Censoring
NCT00553358 (22) [back to overview]	Percentage of Participants With the Indicated Biomarker Expression - PTEN.
NCT00555152 (2) [back to overview]	Incidence of Adverse Events Graded According to the National Cancer Institute (NCI) Common Terminology Criteria (CTCAE) Version 3.0
NCT00555152 (2) [back to overview]	Incidence of Ductal Carcinoma in Situ Remaining at Resection
NCT00558103 (4) [back to overview]	Progression-free Survival, Defined as the Interval Between the Date of Randomization and the Earliest Date of Disease Progression (PD) or Death Due to Any Cause (Defined by an Investigator Review of Lesions Based on RECIST and Cutaneous Disease)
NCT00558103 (4) [back to overview]	Overall Survival
NCT00558103 (4) [back to overview]	Number of Participants With Overall Response (OR), Defined as Those Participants Achieving Complete Response (CR) or Partial Response (PR), Assessed Per Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.0 and Cutaneous Lesions
NCT00558103 (4) [back to overview]	Median Duration of Response,Defined as the First Documented Evidence of CR or PR Until the First Documentation of Disease Progression
NCT00574171 (1) [back to overview]	Response Rate of Lapatinib/Capecitabine.
NCT00632489 (2) [back to overview]	To Determine the Maximum Tolerated Doses (MTD) and Dose-limiting Toxicities (DLT) of LBH589 in Combination With Capecitabine When Administered to Patients With Refractory and Advanced Tumor Types That Are Sensitive to 5-fluorouracil
NCT00632489 (2) [back to overview]	To Determine the Maximum Tolerated Doses (MTD) and Dose-limiting Toxicities (DLT) of LBH589 in Combination With Capecitabine When Administered to Patients With Refractory and Advanced Tumor Types That Are Sensitive to 5-fluorouracil
NCT00634088 (10) [back to overview]	Number of Participants With Abnormalities in Serum Chemistry Laboratory Results by Worst CTC Grade
NCT00634088 (10) [back to overview]	Number of Participants With Abnormalities in Hematology Laboratory Results by Worst CTC Grade
NCT00634088 (10) [back to overview]	Area Under the Concentration-time Curve From 0 to Infinity (AUC[INF]) and AUC From 0 to Last Quantifiable Concentration (AUC[O-T] of Ixabepilone
NCT00634088 (10) [back to overview]	Volume of Distribution at Steady State of Ixabepilone
NCT00634088 (10) [back to overview]	Time to Peak Concentration of Ixabepilone
NCT00634088 (10) [back to overview]	Overall Tumor Response By Number of Participants
NCT00634088 (10) [back to overview]	Terminal Half-life of Ixabepilone
NCT00634088 (10) [back to overview]	Maximum Concentration of Ixabepilone
NCT00634088 (10) [back to overview]	Number of Participants With DLT
NCT00634088 (10) [back to overview]	Number of Participants With Death, Serious Adverse Events (SAEs), Adverse Events (AEs) Leading to Discontinuation, Treatment-related AEs, Treatment-related AEs (Grade 3 or 4), Peripheral Neuropathy (PN), PN (Grade 3 or 4)
NCT00667251 (10) [back to overview]	Time to CNS Metastases at the Time of First Progression
NCT00667251 (10) [back to overview]	Progression-free Survival
NCT00667251 (10) [back to overview]	Quality of Life as Measured by the EORTC QLQ-C30 Global Score From Baseline to 12 Weeks
NCT00667251 (10) [back to overview]	Overall Survival
NCT00667251 (10) [back to overview]	Overall Objective Response Rate (Complete or Partial) ITT
NCT00667251 (10) [back to overview]	Overall Objective Response Rate (Complete or Partial) HER2/Neu+
NCT00667251 (10) [back to overview]	CNS Metastases at the Time of Progression (HER2+)
NCT00667251 (10) [back to overview]	Clinical Benefit Response Rate (ITT)
NCT00667251 (10) [back to overview]	CNS Metastases at the Time of Progression (ITT)
NCT00667251 (10) [back to overview]	Clinical Benefit Response Rate (HER2/Neu+))
NCT00680901 (15) [back to overview]	Number of Participants With Adverse Events of the Indicated Severity, Per the National Cancer Institute (NCI) Common Terminology Criteria in Adverse Events (CTCAE)
NCT00680901 (15) [back to overview]	Time to Response (TTR)
NCT00680901 (15) [back to overview]	Number of Participants With a Worst-case on Therapy Grade 3 or Grade 4 for the Indicated Hematology Parameters
NCT00680901 (15) [back to overview]	Mean Change in Scores on the EORTC Quality of Life (QOL) Questionnaire of Stomach 22 (QLQ-STO22) From Baseline to Week 36
NCT00680901 (15) [back to overview]	Mean Change in Scores on the European Organization for Research and Treatment of Cancer (EORTC) Quality of Life (QOL) Questionnaire Core 30 (QLQ-C30) From Baseline to Week 36
NCT00680901 (15) [back to overview]	Mean Change in Scores on the Questionnaire EuroQoL-5 Dimensions (EQ-5D) From Baseline to Week 36
NCT00680901 (15) [back to overview]	Number of Participants With a Worst-case on Therapy Grade 3 or Grade 4 for the Indicated Clinical Chemistry Parameters
NCT00680901 (15) [back to overview]	Progression Free Survival (PFS)
NCT00680901 (15) [back to overview]	Number of Participants With Any Non-serious Adverse Event (AE: Occurring in >=5% Participants in Any Treatment Arm) or Any Serious Adverse Event (SAE)
NCT00680901 (15) [back to overview]	Duration of Response (DOR)
NCT00680901 (15) [back to overview]	Number of Participants With a Response of Confirmed Complete Response (CR) or Confirmed Partial Response (PR)
NCT00680901 (15) [back to overview]	Number of Participants With Clinical Benefit (CB)
NCT00680901 (15) [back to overview]	Overall Survival
NCT00680901 (15) [back to overview]	Overall Survival in All Randomized Participants
NCT00680901 (15) [back to overview]	Mean Change in Scores on the EORTC Quality of Life (QOL) Questionnaire of Stomach 22 (QLQ-STO22) From Baseline to Week 36
NCT00684983 (6) [back to overview]	Adverse Event Profile of Capecitabine and Lapatinib With and Without IMC-A12 (Using NCI CTCAE v3.0)
NCT00684983 (6) [back to overview]	Confirmed Tumor Response, Defined as Either a Complete Response (CR) or Partial Response (PR) Noted as the Objective Status on 2 Consecutive Evaluations at Least 6 Weeks Apart, Assessed by Response Evaluation Criteria for Solid Tumors (RECIST)
NCT00684983 (6) [back to overview]	Duration of Response
NCT00684983 (6) [back to overview]	Overall Survival
NCT00684983 (6) [back to overview]	Progression-free Survival (PFS)
NCT00684983 (6) [back to overview]	Time to Treatment Failure
NCT00709618 (6) [back to overview]	Number of Participants With the Indicated Adverse Events Occurring in at Least 5 Participants and Related to the Combination of Lapatinib and Vinorelbine
NCT00709618 (6) [back to overview]	Time to Response, as Assessed by the Investigator
NCT00709618 (6) [back to overview]	Progression-Free Survival (PFS), as Assessed by the Investigator
NCT00709618 (6) [back to overview]	Number of Participants With Overall Response (OR), as Assessed by the Investigator
NCT00709618 (6) [back to overview]	Duration of Response, as Assessed by the Investigator
NCT00709618 (6) [back to overview]	Time to Progression (TTP), as Assessed by the Investigator
NCT00709761 (5) [back to overview]	Time to Response (TTR)
NCT00709761 (5) [back to overview]	Progression-Free Survival (PFS)
NCT00709761 (5) [back to overview]	Overall Tumor Response (OR)
NCT00709761 (5) [back to overview]	Duration of Response (DOR)
NCT00709761 (5) [back to overview]	Time to Progression (TTP)
NCT00721630 (1) [back to overview]	Number of Participants With Toxicities Associated With Capecitabine and Lapatinib
NCT00756470 (2) [back to overview]	Number of Participants With pCR After Completion of All Protocol Specified Therapy & Surgery (Surgical Population)
NCT00756470 (2) [back to overview]	Rate of Pathologic Complete Response (pCR) Following Neoadjuvant Chemotherapy
NCT00759642 (1) [back to overview]	Progression Free Survival
NCT00770809 (1) [back to overview]	pCR Rate
NCT00777101 (7) [back to overview]	Clinical Benefit Rate
NCT00777101 (7) [back to overview]	Time to CNS Metastases
NCT00777101 (7) [back to overview]	Progression Free Survival
NCT00777101 (7) [back to overview]	Overall Survival (OS)
NCT00777101 (7) [back to overview]	Objective Response Rate (ORR).
NCT00777101 (7) [back to overview]	Frequency of CNS Metastases (Frequency)
NCT00777101 (7) [back to overview]	Duration of Response
NCT00820222 (9) [back to overview]	Duration of Response
NCT00820222 (9) [back to overview]	Number of Participants With Central Nervous System (CNS) Metastases (as Assessed by Independent Review) as the Site of First Relapse
NCT00820222 (9) [back to overview]	Number of Participants With CNS Progression at Any Time
NCT00820222 (9) [back to overview]	Overall Survival
NCT00820222 (9) [back to overview]	Progression Free Survival (PFS), as Assessed by the Investigator
NCT00820222 (9) [back to overview]	Time to First CNS Progression, Defined as the Time From Randomization Until the Date of Documented CNS Progression as the First Site of Relapse
NCT00820222 (9) [back to overview]	Number of Participants With Overall Response (OR), as Assessed by the Investigator
NCT00820222 (9) [back to overview]	Number of Participants With Clinical Benefit (CB)
NCT00820222 (9) [back to overview]	Number of Participants With the Indicated Grade 3 or Grade 4 Adverse Events (AEs) Occurring in >=2% of Participants in Either Treatment Arm
NCT00820872 (1) [back to overview]	Proportion of Patients Experiencing Grade 3 or 4 Diarrhea as Measured by NCI CTCAE v3.0
NCT00826241 (3) [back to overview]	Number of Participants With an Overall Response (Complete Response or Partial Response) Assessed by the MacDonald Criteria
NCT00826241 (3) [back to overview]	Time to Progression
NCT00826241 (3) [back to overview]	Number of Participants With Serious and Non-Serious Adverse Events Assessed by the Common Terminology Criteria in Adverse Events (CTCAE v4.0)
NCT00826267 (4) [back to overview]	Plasma Concentration of Afatinib
NCT00826267 (4) [back to overview]	Objective Response (OR)
NCT00826267 (4) [back to overview]	Change From Baseline in the Diameter of the Primary Target Lesion.
NCT00826267 (4) [back to overview]	Number of Participants Who Achieved Clinical Benefit (CB)
NCT00829166 (17) [back to overview]	Percentage of Participants Who Were Alive at Year 1
NCT00829166 (17) [back to overview]	Percentage of Participants Who Were Alive at Year 2
NCT00829166 (17) [back to overview]	Percentage of Participants With Clinical Benefit as Assessed by an IRC
NCT00829166 (17) [back to overview]	Percentage of Participants With PD or Death as Assessed by an Independent Review Committee (IRC)
NCT00829166 (17) [back to overview]	Percentage of Participants With PD or Death as Assessed by the Investigator
NCT00829166 (17) [back to overview]	Percentage of Participants With Symptom Progression
NCT00829166 (17) [back to overview]	Percentage of Participants With Treatment Failure
NCT00829166 (17) [back to overview]	PFS as Assessed by the Investigator
NCT00829166 (17) [back to overview]	Progression-free Survival (PFS) as Assessed by an IRC (Co-primary Endpoint)
NCT00829166 (17) [back to overview]	Time to Symptom Progression
NCT00829166 (17) [back to overview]	Time to Treatment Failure
NCT00829166 (17) [back to overview]	Duration of Objective Response (DOR) as Assessed by an IRC
NCT00829166 (17) [back to overview]	Overall Survival: Final Analysis
NCT00829166 (17) [back to overview]	Overall Survival: Second Interim Analysis (Co-primary Endpoint)
NCT00829166 (17) [back to overview]	Percentage of Participants Who Died: Final Analysis
NCT00829166 (17) [back to overview]	Percentage of Participants With Objective Response (OR) as Assessed by an IRC
NCT00829166 (17) [back to overview]	Percentage of Participants Who Died: Second Interim Analysis
NCT00841828 (2) [back to overview]	Complete Pathological Response (pCR) Rate in Breast and Axilla According to the Miller&Payne Criteria (G5-A and G5-D).
NCT00841828 (2) [back to overview]	Overall Clinical Response Rate (ORR)
NCT00857714 (2) [back to overview]	Number of Patients With Toxicity Associated With Short Therapy With Lapatinib.
NCT00857714 (2) [back to overview]	Number of Patients Where Gene Signature Was Obtained.
NCT00863122 (5) [back to overview]	Perform NF2 Gene Mutation Analysis Via Exon Scanning and MLPA as Well as Protein Expression in All VS and Explore Differences Between Sporadic and NF2 Related VS.
NCT00863122 (5) [back to overview]	To Assess Whether Lapatinib Can Reach a Minimum Tumor Concentration Level of >3uM in VS After Oral Dosing.
NCT00863122 (5) [back to overview]	Median Steady-state Lapatinib Plasma Concentrations at the Time of Surgical Resection
NCT00863122 (5) [back to overview]	Explore the Difference in the Concentration of Lapatinib Achieved in NF2-related Versus Idiopathic VS.
NCT00863122 (5) [back to overview]	Assess the Level of ErbB2 Phosphorylation in VS.
NCT00881621 (4) [back to overview]	Adverse Events
NCT00881621 (4) [back to overview]	Clinical Benefit Response
NCT00881621 (4) [back to overview]	Progression Free Survival
NCT00881621 (4) [back to overview]	Overall Survival
NCT00883688 (1) [back to overview]	Objective Response Rate
NCT00939523 (4) [back to overview]	Number of Participants With 50% Reduction in Prolactin Levels
NCT00939523 (4) [back to overview]	% Change in Prolactin From Baseline to Study End
NCT00939523 (4) [back to overview]	Change in Tumor Volume
NCT00939523 (4) [back to overview]	ErbB Receptor Expression
NCT00952692 (4) [back to overview]	Occurrence of Objective Clinical Response (CR or PR) as Best Overall Response.
NCT00952692 (4) [back to overview]	Number of Participants With T-cell Response
NCT00952692 (4) [back to overview]	Time to Progression
NCT00952692 (4) [back to overview]	The Safety of dHER2+AS15 ASCI When Administered in Combination With Lapatinib Measured by Occurrence of Severe Toxicities (According to CTCAE, Version 3.0)
NCT00953576 (4) [back to overview]	Grade 3-4 Treatment-Related Adverse Events Rate
NCT00953576 (4) [back to overview]	Lapatinib Dose Limiting Toxicity (DLT) [Phase I]
NCT00953576 (4) [back to overview]	Lapatinib Maximum Tolerated Dose (MTD) [Phase I]
NCT00953576 (4) [back to overview]	Plasma Lapatinib Levels [Phase I]
NCT00963547 (5) [back to overview]	Maximum Tolerated Dose of MK-2206 in Combination With Trastuzumab (Part 1) and With Trastuzumab/Lapatinib (Part 2)
NCT00963547 (5) [back to overview]	Number of Participants Discontinuing Study Drug Due to an Adverse Event
NCT00963547 (5) [back to overview]	Number of Participants Experiencing ≥1 Adverse Event
NCT00963547 (5) [back to overview]	Number of Participants Experiencing ≥1 Dose-Limiting Toxicity (DLT) in Cycle 1
NCT00963547 (5) [back to overview]	Recommended Phase 2 Dose of MK-2206 in Combination With Trastuzumab (Part 1) and With Trastuzumab/Lapatinib (Part 2)
NCT00968968 (5) [back to overview]	Best Overall Response
NCT00968968 (5) [back to overview]	Adverse Event Profile of the Two Treatment Arms
NCT00968968 (5) [back to overview]	Progression-free Survival
NCT00968968 (5) [back to overview]	Clinical Benefit Response Rate (CR, PR or SD ≥24 Weeks)
NCT00968968 (5) [back to overview]	Overall Survival
NCT00973739 (4) [back to overview]	Estimated Volumetric Progression Free Survival at 12 Months
NCT00973739 (4) [back to overview]	Estimated Volumetric Progression Free Survival for Hearing at 12 Months
NCT00973739 (4) [back to overview]	Participants Experiencing Grades 1 or 2 Toxicities (CTCAE)
NCT00973739 (4) [back to overview]	Participants Experiencing Grade 3 Toxicities (CTCAE)
NCT00999804 (4) [back to overview]	Clinical Response
NCT00999804 (4) [back to overview]	Number of Participants With Adverse Events
NCT00999804 (4) [back to overview]	Total Pathologic Complete Response
NCT00999804 (4) [back to overview]	Pathologic Complete Response
NCT01013740 (7) [back to overview]	Number of Participants With Clinical Benefit (CB) in the Randomized Phase
NCT01013740 (7) [back to overview]	Number of Participants With Overall Response (OR), as Assessed by the Investigator in the Randomized Phase
NCT01013740 (7) [back to overview]	Number of Participants With Grade 4 and Grade 5 Adverse Events (AE)
NCT01013740 (7) [back to overview]	Duration of Response (DOR) in the Randomized Phase
NCT01013740 (7) [back to overview]	Time to Response in the Randomized Phase
NCT01013740 (7) [back to overview]	Progression Free Survival (PFS) in the Randomized Phase
NCT01013740 (7) [back to overview]	Overall Survival (OS)
NCT01044433 (5) [back to overview]	Progression-free Survival
NCT01044433 (5) [back to overview]	Response Rate
NCT01044433 (5) [back to overview]	Number of Participants With Adverse Events and Serious Adverse Events
NCT01044433 (5) [back to overview]	Overall Survival
NCT01044433 (5) [back to overview]	Disease Control Rate
NCT01118975 (2) [back to overview]	Dose Limiting Toxicities
NCT01118975 (2) [back to overview]	Clinical Benefit Rate
NCT01128543 (3) [back to overview]	Number of Participants (Par.) With Clinical Benefit (CB) at Week 12 and Week 24
NCT01128543 (3) [back to overview]	Duration of Response
NCT01128543 (3) [back to overview]	Progression-free Survival
NCT01138046 (14) [back to overview]	Number of Partcipants With a Best Overall Response (OR) as Determined by the Response Evaluation Criteria in Solid Tumors (RECIST)
NCT01138046 (14) [back to overview]	Time to the Maximum Drug Concentration (Tmax) of Lapatinib and Paclitaxel
NCT01138046 (14) [back to overview]	Duration of Response
NCT01138046 (14) [back to overview]	Number of Participants With Intolerable Toxicities in Phase I of the Study
NCT01138046 (14) [back to overview]	Number of Participants With Clinical Benefit Response (CBR)
NCT01138046 (14) [back to overview]	AUC From Time Zero to Infinity (0-INF) of Paclitaxel
NCT01138046 (14) [back to overview]	Distribution Volume at Steady State (Vss) of Paclitaxel
NCT01138046 (14) [back to overview]	Overall Survival
NCT01138046 (14) [back to overview]	Progression-free Survival (PFS)
NCT01138046 (14) [back to overview]	Drug Clearance (CL) of Paclitaxel
NCT01138046 (14) [back to overview]	Half-life (t1/2) of Paclitaxel
NCT01138046 (14) [back to overview]	Maximum Plasma Concentration (Cmax) of Lapatinib and Paclitaxel
NCT01138046 (14) [back to overview]	Area Under the Concentration-time Curve (AUC) (0-24) of Lapatinib and Paclitaxel
NCT01138046 (14) [back to overview]	Time to Response
NCT01160211 (9) [back to overview]	Time to Response in Lapatinib+Trastuzumab+AI vs. Trastuzumab+AI and Lapatinib+AI vs. Trastuzumab+AI
NCT01160211 (9) [back to overview]	Overall Response Rate (ORR; Complete or Partial Response) in Lapatinib+Trastuzumab+AI vs. Trastuzumab+AI and Lapatinib+AI vs. Trastuzumab+AI
NCT01160211 (9) [back to overview]	Duration of Response in Lapatinib+Trastuzumab+AI vs. Trastuzumab+AI and Lapatinib+AI vs. Trastuzumab+AI
NCT01160211 (9) [back to overview]	Median Kaplan Meier Estimates for PFS of Lapatinib+Trastuzumab+AI Combination vs. Trastuzumab+AI Combination
NCT01160211 (9) [back to overview]	PFS of Trastuzumab/AI vs. Lapatinib/AI and Trastuzumab/Lapatinib/AI vs. Lapatinib/AI
NCT01160211 (9) [back to overview]	PFS of Lapatinib+Trastuzumab+AI Combination vs. Trastuzumab+AI Combination
NCT01160211 (9) [back to overview]	Overall Survival (OS) Events of Lapatinib+Trastuzumab+AI vs. Trastuzumab+AI and Lapatinib+AI vs. Trastuzumab+AI
NCT01160211 (9) [back to overview]	Changes in the Quality of Life (QoL) Status Relative to Baseline FACT-B Overall and Subscale Scores at Last On-treatment Assessment
NCT01160211 (9) [back to overview]	Clinical Benefit Rate (CBR; Complete Response, Partial Response, or Stable Disease for at Least 6 Months) in Lapatinib+Trastuzumab+AI vs. Trastuzumab+AI and Lapatinib+AI vs. Trastuzumab+AI
NCT01264081 (2) [back to overview]	Number of Participants With Serious and Non-Serious Adverse Events
NCT01264081 (2) [back to overview]	Count of Participants With a Partial Response (PR) and Complete Response (CR) to Lapatinib Who Have Metastatic Melanoma Harboring ERBB4 Mutations.
NCT01273610 (4) [back to overview]	Percent of Participants With a Dose Modifications
NCT01273610 (4) [back to overview]	Median Progression-free Survival (PFS)
NCT01273610 (4) [back to overview]	Median Overall Survival (OS)
NCT01273610 (4) [back to overview]	Percent of Participants With Grade 3 or Higher Non-hematological Toxicities and Symptomatic Congestive Heart Failure
NCT01306045 (10) [back to overview]	Percentage of Enrolled Participants Testing Positive for Genomic Abnormality
NCT01306045 (10) [back to overview]	Percentage of Evaluable Participants Overall Response Rate (ORR) Based on the Drug Selected for Their Particular Profile
NCT01306045 (10) [back to overview]	Percentage of Evaluable Participants Overall Response Rate (ORR) Based on the Drug Selected for Their Particular Profile
NCT01306045 (10) [back to overview]	Percentage of Evaluable Participants Overall Response Rate (ORR) Based on the Drug Selected for Their Particular Profile
NCT01306045 (10) [back to overview]	Number of Evaluable Participants With a Response Based on Molecular Profile Directed Treatments in Non-Small Cell Lung Cancer, (NSCLC), Small Cell Lung Cancer (SCLC), and Thymic Malignancies
NCT01306045 (10) [back to overview]	Here is the Number of Participants With Serious and/or Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0)
NCT01306045 (10) [back to overview]	Number of Evaluable Participants With a Response Based on Molecular Profile Directed Treatments in Non-Small Cell Lung Cancer, (NSCLC), Small Cell Lung Cancer (SCLC), and Thymic Malignancies
NCT01306045 (10) [back to overview]	Number of Evaluable Participants With a Response Based on Molecular Profile Directed Treatments in Non-Small Cell Lung Cancer, (NSCLC), Small Cell Lung Cancer (SCLC), and Thymic Malignancies
NCT01306045 (10) [back to overview]	Percentage of Enrolled Participants Testing Positive for Genomic Abnormality
NCT01306045 (10) [back to overview]	Percentage of Enrolled Participants Testing Positive for Genomic Abnormality
NCT01328054 (16) [back to overview]	Mean Calcium, Chloride, Carbon Dioxide (CO2), Potassium, Sodium, Magnesium and Urea at the Indicated Time Points
NCT01328054 (16) [back to overview]	Median Time to Cmax (Tmax) and the Time Prior to the First Quantifiable (Non-zero) Lapatinib Plasma Concentration (Tlag) Following the Last (3rd) Lapatinib Dose
NCT01328054 (16) [back to overview]	Number of Participants With 12-lead ECG Findings at Indicated Time Points
NCT01328054 (16) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT01328054 (16) [back to overview]	Treatment Difference in Duration of Cardiac Ventricular Depolarization and Repolarization Interval (QT) in Fridericia-corrected QT Interval (QTcF) Values Between Placebo and Lapatinib 2000mg
NCT01328054 (16) [back to overview]	Mean Direct Bilirubin, Total Bilirubin, and Creatinine at the Indicated Time Points
NCT01328054 (16) [back to overview]	Number of Participants With the Worst-case Post-Baseline 12-lead Holter ECG Findings With Significant ST, T Wave, and U Wave Abnormalities
NCT01328054 (16) [back to overview]	Change From Baseline in Heart Rate at the Indicated Time Points
NCT01328054 (16) [back to overview]	Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at the Indicated Time Points
NCT01328054 (16) [back to overview]	Change From Baseline in the Holter ECG Parameters of QT Interval, Corrected QT Interval (QTc), Bazett Corrected QTc Interval (QTcB), Individual-corrected QT Interval (QTcI), RR Interval, PR Interval, and QRS Duration at Indicated Time Points
NCT01328054 (16) [back to overview]	Mean Alkaline Phosphatase (ALP), Alanine Aminotransferase (ALT), and Aspartate Aminotransferase (AST) at the Indicated Time Points
NCT01328054 (16) [back to overview]	Mean Area Under the Plasma Drug Concentration-time Curve (AUC) From Time Zero (Pre-dose) to the Last Time of Quantifiable Concentration (AUC[0-t]) and From Time Zero (Pre-dose) to 24 Hours Post Dose (AUC[0-24]) for Lapatinib
NCT01328054 (16) [back to overview]	Mean Maximum Plasma Concentration (Cmax) and Observed Plasma Concentration at 24 Hours Post-dose (C24) of Lapatinib
NCT01328054 (16) [back to overview]	Mean Total Neutrophils (ANC [Absolute Neutrophil Count]), Platelets and Leukocyte Count at the Indicated Time Points
NCT01328054 (16) [back to overview]	Number of Participants With 12-lead Holter ECG Findings at the Indicated Time Points
NCT01328054 (16) [back to overview]	Mean Albumin, and Hemoglobin at the Indicated Time Points
NCT01395537 (3) [back to overview]	To Determine the Overall Survival
NCT01395537 (3) [back to overview]	PHASE I: Number of Patients That Experience a Grade 3-4 Dose Limiting Toxicity
NCT01395537 (3) [back to overview]	PHASE II: To Assess the Response Rate to This Regimen.
NCT01499160 (2) [back to overview]	PROGRESSION FREE SURVIVAL TUMOR ASSESSMENT
NCT01499160 (2) [back to overview]	Clinical Benefit Rate of Patients Treated With the Combination of Letrozole and Lapatinib and Then After Progression, Treated With Everolimus, Letrozole and Lapatinib.
NCT01612351 (9) [back to overview]	Voice and Swallowing Function- MD Anderson Dysphagia Inventory (MDADI)
NCT01612351 (9) [back to overview]	Estimate the Pathologic Complete Response Rate at the Primary Site and in the Neck Following Induction Chemotherapy
NCT01612351 (9) [back to overview]	Feasibility of 3 Part Therapy
NCT01612351 (9) [back to overview]	Voice and Swallowing Function - Voice-Related Quality of Life Assessment (VRQOL)
NCT01612351 (9) [back to overview]	Response Rates at the Primary Site
NCT01612351 (9) [back to overview]	Response Rates at the Neck.
NCT01612351 (9) [back to overview]	Number of Subjects Who Experience Grade 3/4 Adverse Events According to CTCAE 4.0
NCT01612351 (9) [back to overview]	Number of Patients Who Decreased in Risk Level Post Induction Chemotherapy.
NCT01612351 (9) [back to overview]	Overall Response Rate
NCT01622868 (11) [back to overview]	Overall Survival (OS)
NCT01622868 (11) [back to overview]	Complete Response Rate in the Brain at 4 Weeks Post-RT Using the RECIST 1.1 Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Overall Complete Response Rate in the Brain Using the RECIST 1.1 Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Complete Response (CR) Rate in the Brain at 12 Weeks Post-radiation Therapy (RT) Using the RECIST 1.1 Criteria Based on Brain Magnetic Resonance Imaging (MRI)
NCT01622868 (11) [back to overview]	Overall Progression Rate in the Brain Using the RECIST 1.1 Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Targeted Lesion-specific Progression Rate Using the RECIST 1.1 Measurement Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Complete Response Rate in the Brain Using the World Health Organization (WHO)/Modified McDonald Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Frequency of Highest Treatment-related Adverse Event Per Participant
NCT01622868 (11) [back to overview]	Objective Response Rate in the Brain Using the RECIST 1.1 Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Targeted Lesion-specific Objective Response Rate Using the RECIST 1.1 Measurement Criteria Based on Brain MRI
NCT01622868 (11) [back to overview]	Percentage of Participants With Progression in the Brain Outside the Targeted Measurable Disease Using the RECIST 1.1 Criteria Based on Brain MRI
NCT01688609 (4) [back to overview]	Number of Participants With Pathological Complete Response (pCR)
NCT01688609 (4) [back to overview]	Cellular Response Rate, Defined as Patients With an Epithelial Phenotype Having Eradication of CTCs; Patients With a Mesenchymal Phenotype Having Eradication of Tumor Cells; Patients With a Mesenchymal Phenotype Converting to an Epithelial Phenotype
NCT01688609 (4) [back to overview]	Expression of ALDH1 and CD44v Change in the Binary Biomarkers From Baseline to 6 Weeks and 18 Weeks
NCT01688609 (4) [back to overview]	Number of Participants With Treatment-Related Toxicities
NCT01711658 (6) [back to overview]	Percentage of Participants Alive Without Progression (Progression-free Survival)
NCT01711658 (6) [back to overview]	Percentage of Participants Alive (Overall Survival)
NCT01711658 (6) [back to overview]	Percentage of Participants Who Complied With Protocol Treatment
NCT01711658 (6) [back to overview]	Percentage of Participants With Treatment-related Grade 3 or Higher Adverse Events
NCT01711658 (6) [back to overview]	Percentage of Participants With Local-regional Progression
NCT01711658 (6) [back to overview]	Percentage of Participants With Distant Metastases
NCT01769508 (6) [back to overview]	Overall Survival (OS)
NCT01769508 (6) [back to overview]	Progression Free Survival (PFS)
NCT01769508 (6) [back to overview]	Safety and Optimal Dose of Regimen
NCT01769508 (6) [back to overview]	Time to Progression (TTP)
NCT01769508 (6) [back to overview]	Toxicity Profile for Treated Patients
NCT01769508 (6) [back to overview]	Pathologic Complete Response Rate (pCR Rate)
NCT01808573 (7) [back to overview]	Centrally Assessed Progression Free Survival
NCT01808573 (7) [back to overview]	Clinical Benefit Rate (CBR) - Central Assessment (ITT Population With Measurable Disease at Screening)
NCT01808573 (7) [back to overview]	Duration of Response (DOR) - Central Assessment (Population That Had a Response With Measurable Disease at Screening)
NCT01808573 (7) [back to overview]	Intervention for Symptomatic Metastatic Central Nervous System Disease
NCT01808573 (7) [back to overview]	Objective Response Rate (ORR) - Central Assessment (ITT Population With Measurable Disease at Screening)
NCT01808573 (7) [back to overview]	Overall Survival
NCT01808573 (7) [back to overview]	Percentage of Participants With Treatment-Emergent Adverse Events (Adverse Events and Serious Adverse Events)
NCT01827163 (1) [back to overview]	Participants Toxicity Evaluated While on Study Treatment
NCT01868503 (3) [back to overview]	Pathologic Complete Response Rate for Those Patients Undergoing Surgical Resection Defined as no Evidence of Residual Tumor in the Breast and Lymph Nodes
NCT01868503 (3) [back to overview]	Percentage of Patients Achieving Complete Clinical Response
NCT01868503 (3) [back to overview]	Incidence of Adverse Events Graded According to Common Terminology Criteria for Adverse Events (CTCAE) Version 4.0
NCT01873833 (5) [back to overview]	Progression Free Survival (PFS)
NCT01873833 (5) [back to overview]	Overall Survival (OS)
NCT01873833 (5) [back to overview]	Overall Response Rate (ORR)
NCT01873833 (5) [back to overview]	Number of Participants With Any Adverse Events as a Measure of Safety and Tolerability
NCT01873833 (5) [back to overview]	Clinical Benefit Rate (CBR)
NCT01891357 (1) [back to overview]	Pathological Complete Response (pCR)
NCT01934894 (5) [back to overview]	CNS Clinical Benefit Response
NCT01934894 (5) [back to overview]	CNS Objective Response
NCT01934894 (5) [back to overview]	Extra-Cranial Objective Response
NCT01934894 (5) [back to overview]	Number of Participants Who Experience Dose-Limiting Toxicities (DLTs) as a Measure of Safety
NCT01934894 (5) [back to overview]	Maximum Tolerated Dose of Cabazitaxel With Lapatinib
NCT02073487 (2) [back to overview]	Breast Imaging Response to Treatment: Number of Eventual Responders in Standard Arm
NCT02073487 (2) [back to overview]	Pathological Complete Response (pCR) RCB-0 or RCB-1
NCT02213042 (7) [back to overview]	All-Collected Deaths
NCT02213042 (7) [back to overview]	Fold Change in Expression Profile of Genes and /or Proteins for Arm B (TRAS+CHEM±AI (HER2-Enriched)) From Screening to Approx. 3.5 Years
NCT02213042 (7) [back to overview]	Fold Change in Expression Profile of Genes and /or Proteins for Arm C (Non-HER2- Enriched) From Screening to Approx. 3.5 Years
NCT02213042 (7) [back to overview]	Fold Change in Expression Profile of Genes and/or Proteins for Arm A (LAP+TRAS±AI (HER2-Enriched)) From Screening to Approx. 3.5 Years
NCT02213042 (7) [back to overview]	Clinical Benefit Rate (CBR)
NCT02213042 (7) [back to overview]	Overall Response Rate (ORR)
NCT02213042 (7) [back to overview]	Progression-free Survival (PFS)
NCT02294786 (17) [back to overview]	Clinical Benefit Response (up to 24 Weeks)
NCT02294786 (17) [back to overview]	Duration of Diarrhoea of Any Grade of Severity
NCT02294786 (17) [back to overview]	Proportion of Subjects Contacting Other Non-hospital Healthcare Professionals to Discuss Diarrhoea as Recorded in the DMD
NCT02294786 (17) [back to overview]	Proportion of Subjects Experiencing Diarrhoea of Any Grade of Severity (up to 24 Weeks)
NCT02294786 (17) [back to overview]	Proportion of Subjects Experiencing Diarrhoea of Grade 3 and Above (up to 24 Weeks)
NCT02294786 (17) [back to overview]	Proportion of Subjects Making Dietary Changes Due to Diarrhoea as Recorded in the DMD
NCT02294786 (17) [back to overview]	Proportion of Subjects Reporting Changes in Bowel Movements From Baseline (Frequency and/or Consistency) as Recorded in the Diarrhoea Management Diary (DMD)
NCT02294786 (17) [back to overview]	Proportion of Subjects Reporting Stopping Completely or Missing Doses of Anti-cancer Tablets Due to Diarrhoea as Recorded in the DMD
NCT02294786 (17) [back to overview]	Proportion of Subjects Taking Anti-diarrhoeal Medication
NCT02294786 (17) [back to overview]	Proportion of Subjects Taking Anti-diarrhoeal Medication as Recorded in the DMD
NCT02294786 (17) [back to overview]	Time to Onset of the First Episode of Diarrhoea of Any Grade of Severity
NCT02294786 (17) [back to overview]	Time to the First Subject Reported Change in Frequency and/or Consistency of Bowel Movements From Baseline as Recorded in the DMD
NCT02294786 (17) [back to overview]	Number of Lapatinib and Capecitabine Tablets Dispensed and Returned
NCT02294786 (17) [back to overview]	Proportion of Subjects Experiencing Diarrhoea of Grade 2 and Above (up to 24 Weeks)
NCT02294786 (17) [back to overview]	Proportion of Subjects Requiring Dose Delay in Lapatinib and Capecitabine
NCT02294786 (17) [back to overview]	Proportion of Subjects Requiring Dose Reduction in Lapatinib and Capecitabine
NCT02294786 (17) [back to overview]	Proportion of Subjects Requiring Treatment Withdrawal in Lapatinib and Capecitabine
NCT03262935 (6) [back to overview]	Investigator Assessed Progression Free Survival
NCT03262935 (6) [back to overview]	Objective Response Rate
NCT03262935 (6) [back to overview]	Overall Survival
NCT03262935 (6) [back to overview]	Progression Free Survival
NCT03262935 (6) [back to overview]	Patient Reported Outcomes for Health Related Quality of Life
NCT03262935 (6) [back to overview]	Patient Reported Outcomes for Health Related Quality of Life
NCT03523585 (5) [back to overview]	Progression-Free Survival (PFS) Based on Blinded Independent Central Review (BICR) in Participants With HER2-positive, Unresectable and/or Metastatic Breast Cancer Participants Previously Treated With Trastuzumab Emtansine
NCT03523585 (5) [back to overview]	Overall Survival (OS) in Participants With HER2-positive, Unresectable and/or Metastatic Breast Cancer Participants Previously Treated With Trastuzumab Emtansine
NCT03523585 (5) [back to overview]	Duration of Response (DoR) Based on BICR in Participants With HER2-positive, Unresectable and/or Metastatic Breast Cancer Participants Previously Treated With Trastuzumab Emtansine
NCT03523585 (5) [back to overview]	Percentage of Participants With Objective Response Rate (ORR) in Participants With HER2-positive, Unresectable and/or Metastatic Breast Cancer Participants Previously Treated With Trastuzumab Emtansine
NCT03523585 (5) [back to overview]	Progression-Free Survival (PFS) Based on Investigator Assessment in Participants With HER2-positive, Unresectable and/or Metastatic Breast Cancer Participants Previously Treated With Trastuzumab Emtansine

Tumor Response in the Targeted Population Through the End of Treatment

Disease progression and tumor response (number of participants achieving a complete response [CR] or partial response [PR]), using standardized criteria (Response evaluation criteria in solid tumors). CR, disappearance of all target lesions; PR, 30% decrease in the sum of the longest diameter of target lesions; progressive disease, 20% increase in the sum of the longest diameter of target lesions; stable disease, small changes that do not meet above criteria. Disease assessment was done at baseline and then every 8 weeks after starting treatment, until the participant discontinued treatment. (NCT00073008)
Timeframe: Baseline and then every 8 weeks through end of treatment

Intervention	participants (Number)
	Complete response	Partial response	Stable disease	Progressive disease	Missing
Lapatinib 1500 mg QD	0	0	5	18	1
Lapatinib 500 mg BID	0	0	9	20	3

Intervention	Percent response rate (Number)
Placebo + Letrozole 2.5 mg	14.8
Lapatinib 1500 mg + Letrozole 2.5 mg	27.9

Intervention	Adjusted mean change (Number)
	Week 12	Week 24	Week 36	Week 48	Conclusion/WD
Lapatinib 1500 mg + Letrozole 2.5 mg	3.3	1.9	1.4	0.3	-9.0
Placebo + Letrozole 2.5 mg	1.5	3.8	3.3	2.9	-9.4

Intervention	weeks (Median)
Placebo + Letrozole 2.5 mg	47.0
Lapatinib 1500 mg + Letrozole 2.5 mg	51.7

Intervention	Weeks (Median)
Placebo + Letrozole 2.5 mg	NA
Lapatinib 1500 mg + Letrozole 2.5 mg	36.1

Intervention	weeks (Median)
Placebo + Letrozole 2.5 mg	13.0
Lapatinib 1500 mg + Letrozole 2.5 mg	35.4

Intervention	percentage of participants (Number)
Placebo + Letrozole 2.5 mg	27.8
Lapatinib 1500 mg + Letrozole 2.5 mg	30.5

Intervention	weeks (Median)
Placebo + Letrozole 2.5 mg	176.3
Lapatinib 1500 mg + Letrozole 2.5 mg	170.9

Intervention	Weeks (Median)
Placebo + Letrozole 2.5 mg	140.3
Lapatinib 1500 mg + Letrozole 2.5 mg	144.7

Intervention	weeks (Median)
Placebo + Letrozole 2.5 mg	72.6
Lapatinib 1500 mg + Letrozole 2.5 mg	60.1

Intervention	Months (Number)
Placebo + Letrozole 2.5 mg	28.7
Lapatinib 1500 mg + Letrozole 2.5 mg	47.7

Intervention	percentage of participants (Number)
Placebo + Letrozole 2.5 mg	50.6
Lapatinib 1500 mg + Letrozole 2.5 mg	55.8

Intervention	participants (Number)
	Week 12	Week 16	Week 24	Week 28	Week 36 or longer
Lapatinib 1500 mg + Letrozole 2.5 mg	94	18	28	14	42
Placebo + Letrozole 2.5 mg	76	21	28	17	37

Intervention	Participants (Count of Participants)
	EGFR, 0	EGFR, 1+	EGFR, 2+	EGFR, 3+
Lapatinib 1500 mg + Letrozole 2.5 mg	522	45	12	1
Placebo + Letrozole 2.5 mg	513	43	17	3

Intervention	weeks (Median)
Placebo + Letrozole 2.5 mg	84.4
Lapatinib 1500 mg + Letrozole 2.5 mg	47.4

Intervention	Participants (Count of Participants)
	CR	PR	SD	PD	Unknown
Lapatinib 1500 mg + Letrozole 2.5 mg	28	168	280	113	53
Placebo + Letrozole 2.5 mg	26	153	243	174	48

Intervention	Participants (Count of Participants)
	>15 ng/mL, CR/PR	>15 ng/mL, SD	>15 ng/mL, PD/NE	=<15 ng/mL, CR/PR	=<15 ng/mL, SD	=<15 ng/mL, PD/NE
Lapatinib 1500 mg + Letrozole 2.5 mg	9	13	12	17	30	23
Placebo + Letrozole 2.5 mg	3	11	39	12	23	16

Intervention	participants (Number)
	SDS, Soft tissue or visceral	PAET, DI =>6 months	PAET, DI <6 months
Lapatinib 1500 mg + Letrozole 2.5 mg	190	168	22
Placebo + Letrozole 2.5 mg	170	151	19

Intervention	Participants (Count of Participants)
	SDS, Soft tissue or visceral	SDS, Bone-only disease	PAET, DI =>6 months	PAET, DI <6 months
Lapatinib 1500 mg + Letrozole 2.5 mg	31	0	24	7
Placebo + Letrozole 2.5 mg	14	0	12	2

Intervention	Participants (Count of Participants)
	IHC Intensity 0	IHC Intensity 1	IHC Intensity 2	IHC Intensity 3	IHC Intensity Missing
Lapatinib 1500 mg + Letrozole 2.5 mg	106	106	85	26	35
Placebo + Letrozole 2.5 mg	74	108	94	16	34

Intervention	Participants (Count of Participants)
	Week 12	Week 16	Week 24 or longer
Lapatinib 1500 mg + Letrozole 2.5 mg	23	3	5
Placebo + Letrozole 2.5 mg	11	1	4

lapatinib

Cross-References

Synonyms (116)

Research Excerpts

Overview

Effects

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Bioavailability

Dosage Studied

Roles (2)

Drug Classes (4)

Pathways (6)

Protein Targets (549)

Potency Measurements

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Biological Processes (3233)

Molecular Functions (638)

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Research

Studies (1,865)

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Research Demand Index: 64.50

Study Types

Clinical Trials (286)

Trial Overview

Trial Outcomes

Tumor Response in the Targeted Population Through the End of Treatment

Progression-free Survival (PFS) at Four Months in the Non-Targeted Population

Progression-free Survival (PFS) at Four Months in the Targeted Population

Tumor Response in the Non-Targeted Population Through the End of Treatment

Overall Tumor Response (OR) for Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the HER2-Positive Population as Assessed by the Investigator

Adjusted Mean Change From Baseline for the FACT-B Total Score Using Observed Data

TTP for Participants From the ITT Population as Assessed by the Investigator

Time to Seroconversion for Participants Who Were HER2 Negative at Baseline But Became HER2 Positive

Time to Progression (TTP) for the HER2-Positive Population as Assessed by the Investigator

Progression Free Survival (PFS) of Participants in the HER2-Positive Population as Assessed by the Investigator

PFS in Participants in the ITT Population as Assessed by the Investigator

Overall Tumor Response (OR) for Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the ITT Population as Assessed by the Investigator

Overall Survival in the ITT Population

Overall Survival in the HER2-Positive Population

Number of Participants With Progression Free Survival (PFS) in the Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced or Metastatic Breast Cancer as Assessed by the Investigator

Number of Participants With PFS in the Intent-To-Treat (ITT) Population as Assessed by the Investigator

Number of Participants With Evidence of Brain Metastases in the HER2-Positive Population

Number of Participants With Evidence of Brain Metastases From the ITT Population

Duration of Response for the Participants With CR or PR in the ITT Population as Assessed by the Investigator

Clinical Benefit (CB) in the HER2-Positive Population as Assessed by the Investigator

Clinical Benefit (CB) in the ITT Population as Assessed by the Investigator

Number of Participants With the Indicated Time to Response for CR or PR in the ITT Population as Assessed by the Investigator

Number of Participants With the Indicated Expression of Tumor by Epidermal Growth Factor Receptor (ErbB1/HER1/EGFR) at Baseline

Duration of Response for the Participants With CR or PR in the HER2-Positive Population as Assessed by the Investigator

Number of Participants With the Indicated Best Response From the Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the ITT Population as Assessed by the Investigator.

Number of Participants With the Indicated Best Response From the Participants With Measurable and Non-measurable Disease, Including Bone Scans, in the HER2-Positive Population as Assessed by the Investigator.

Number of Participants With Response in Participants With Baseline Serum HER2 Extracellular Domain (ECD) Baseline Values Greater Than 15 Nanograms Per Milliliter (ng/mL) and 15 ng/mL or Lower

Number of Participants With Overall Tumor Response (OR) by Stratification Factors With Measurable Disease, Including Bone Scans, in the ITT Population as Assessed by the Investigator

Number of Participants With Overall Tumor Response (OR) by Stratification Factors With Measurable Disease, Including Bone Scans, in the HER2-Positive Population as Assessed by the Investigator

Number of Participants With Clinical Benefit Categorized by HER2 ImmunoHistoChemistry (IHC) Intensity

Number of Participants With the Indicated Time to Response for CR or PR in the HER2-Positive Population as Assessed by the Investigator

Number of Participants With Clinical Benefit Categorized by HER2 Fluorescence in Situ Hybridization (FISH) Status

Number of Participants Completing the Functional Assessment of Cancer Therapy-breast (FACT-B) Questionnaire at the Scheduled Visits

Number of Participants Classified as QOL Responders Based on the FACT-B, FACT-G, and TOI Total Scores

Number of HER2-Negative Participants at Baseline With and Without Seroconversion to a Status of HER2 Positive

All Collected Deaths

Adjusted Mean Change From Baseline for the Trial Outcome Index (TOI) Score Using Observed Data

Adjusted Mean Change From Baseline for the Functional Assessment of Cancer Therapy-General (FACT-G) Score Using Observed Data

Overall Survival

Percentage of Participants With Clinical Benefit (CB) as Assessed by the Investigator

Progression-Free Survival (PFS)

Time to Progression as Evaluated by the Independent Review Committee (IRC)

Time to Progression as Evaluated by the Investigator

Change From Baseline in Functional Assessment of Cancer Therapy-Breast Cancer (FACT-B) Questionnaire Scores

Change From Baseline in Functional Assessment of Cancer Therapy-General (FACT-G) Questionnaire Scores

Change From Baseline in Trial Outcome Index (TOI) Questionnaire Scores

Number of Participants With a Response of CR or PR by the Indicated Study Week

Intervention	Participants (Count of Participants)
	FISH status, Positive	FISH status, Negative	FISH status, missing
Lapatinib 1500 mg + Letrozole 2.5 mg	49	245	64
Placebo + Letrozole 2.5 mg	28	237	61

Intervention	Participants (Count of Participants)
	Day 1, baseline	Week 12	Week 24	Week 36	Week 48	Week 60	Week 72	Week 84	Week 96	Week 108	Week 120	Week 132	Week 144	Week 156	Week 168	Week 180	Week 192	Conclusion/withdrawal
Lapatinib 1500 mg + Letrozole 2.5 mg	605	476	382	294	243	183	153	119	98	62	56	43	33	21	11	5	1	359
Placebo + Letrozole 2.5 mg	605	460	350	291	254	199	181	144	117	80	59	43	33	22	15	11	6	327

Intervention	Participants (Count of Participants)
	FACT-B total, =>8 (MID upper bound)	FACT-G, =>6 (MID upper bound)	TOI, =>6 (MID upper bound)
Lapatinib 1500 mg + Letrozole 2.5 mg	33	38	33
Placebo + Letrozole 2.5 mg	29	29	29

Intervention	Participants (Count of Participants)
	Seroconversion, No	Seroconversion, Yes	Missing
Lapatinib 1500 mg + Letrozole 2.5 mg	140	219	119
Placebo + Letrozole 2.5 mg	323	52	99

Intervention	Participants (Count of Participants)
	On-treatment deaths	All deaths
Lapatinib 1500 mg + Letrozole 2.5 mg	18	488
Placebo + Letrozole 2.5 mg	23	484

Intervention	Scores on a scale (Mean)
	Week 9, n=208, 230	Week 21, n=126, 125	Week 33, n=72, 64	Week 45, n=35, 38	Withdrawal, n=190, 212
Lapatinib With Paclitaxel	-1.1	1.0	1.4	2.3	-5.0
Placebo With Paclitaxel	-2.3	-1.3	-2.0	-1.4	-8.4

Intervention	Scores on a scale (Mean)
	Week 9, n=213, 232	Week 21, n=127, 125	Week 33, n=71, 65	Week 45, n=34, 39	Withdrawal, n=193, 214
Lapatinib With Paclitaxel	-0.7	0.4	1.1	0.9	-4.4
Placebo With Paclitaxel	-1.3	-0.2	-1.7	-1.6	-7.5

Intervention	Scores on a scale (Mean)
	Week 9, n=208, 232	Week 21, n=126, 125	Week 33, n=72, 65	Week 45, n=36, 38	Withdrawal, n=190, 212
Lapatinib With Paclitaxel	-2.3	-0.5	-0.1	1.5	-4.4
Placebo With Paclitaxel	-2.6	-2.7	-2.9	-2.8	-6.1

Intervention	participants (Number)
	Week 6	Week 12	Week 18	Week 24	Week 30	Week 36	Week 42	Week 48	Week 54	Week 60	Week 66	Week 72
Lapatinib With Paclitaxel	3	83	86	98	98	101	102	102	102	102	102	102
Placebo With Paclitaxel	0	55	57	69	69	71	72	72	72	72	72	73

Intervention	participants (Number)
	Amplified	Non-amplified	Assay not done
Lapatinib With Paclitaxel	45	175	71
Placebo With Paclitaxel	35	165	88