ID Source | ID |
---|---|
PubMed CID | 46220502 |
CHEMBL ID | 3301610 |
SCHEMBL ID | 2487229 |
MeSH ID | M000596583 |
Synonym |
---|
ly2835219 |
UZWDCWONPYILKI-UHFFFAOYSA-N |
[5-(4-ethyl-piperazin-1-ylmethyl)-pyridin-2-yl]-[5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3h-benzoimidazol-5-yl)-pyrimidin-2-yl]-amine |
abemaciclib , |
HY-16297A , |
CS-1230 , |
S5716 |
gtpl7382 |
verzenios |
n-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine |
ly-2835219 |
verzenio |
ly 2835219 |
abemaciclib [usan] |
abemaciclib [inn] |
abemaciclib [mi] |
abemaciclib [jan] |
2-pyrimidinamine, n-(5-((4-ethyl-1-piperazinyl)methyl)-2-pyridinyl)-5-fluoro-4-(4-fluoro-2-methyl-1-(1-methylethyl)-1h-benzimidazol-6-yl) |
60UAB198HK , |
abemaciclib [who-dd] |
abemaciclib [orange book] |
CHEMBL3301610 |
5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3h-benzimidazol-5-yl)pyrimidin-2-yl)amine |
5-(4-ethylpiperazin-1-ylmethyl)pyridin-2-yl)-(5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-3h-benzoimidazol-5-yl)pyrimidin-2-yl)amine |
ly 2835210 |
unii-60uab198hk |
abemaciclib [usan:inn] |
ly2835210 |
1231929-97-7 |
ly2835219 (free base) |
SCHEMBL2487229 |
c27h32f2n8 |
n-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1h-benzo[d]imidazol-6-yl)pyrimidin-2-amine |
verzenio (tn) |
abemaciclib (jan/usan) |
D10688 |
ly 2835219 (free base) |
ly2835219 free base |
AC-30666 |
6zv , |
AKOS025404907 |
J-690083 |
DTXSID20673119 |
n-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-[4-fluoro-2-methyl-1-(propan-2-yl)-1h-benzimidazol-6-yl]pyrimidin-2-amine |
EX-A521 |
cdk4/6 dual inhibitor |
mfcd22665744 |
bdbm50110183 |
NCGC00351599-06 |
n-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-(7-fluoro-3-isopropyl-2-methyl-1,3-benzodiazol-5-yl)pyrimidin-2-amine |
ly2835219 free base (abemaciclib) |
DB12001 |
rimidin-2-amine |
n-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-[4-fluoro-2-methyl-1-(propan-2-yl)-1h-benzimidazol-6-yl]py |
1231929-97-7, verzenio, |
FT-0700134 |
ly2835219 ms salt, abemaciclib ms salt |
EX-A1588 |
Q23901483 |
AS-10230 |
BCP13079 |
SB16476 |
HMS3673I05 |
2-pyrimidinamine, n-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1h-benzimidazol-6-yl]- |
CCG-269750 |
NCGC00351599-02 |
nsc783671 |
nsc-783671 |
nsc768073 |
nsc-768073 |
n-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-[4-fluoro-2-methyl-1-(propan-2-yl)-1h-benzimidazol-6-yl]py rimidin-2-amine |
abemaciclibum |
n-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-2-methyl-1-(1-methylethyl)-1h-benzimidazol-6-yl)pyrimidin-2-amine |
l01xe50 |
n-{5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl}-5-fluoro-4-[4-fluoro-2-methyl-1-(propan-2-yl)-1h-1,3-benzodiazol-6-yl]pyrimidin-2-amine |
EN300-7406007 |
Abemaciclib is a selective cyclin-dependent kinase(CDK)4 & 6 inhibitor, which induces G1 cell cycle arrest and tumour growth inhibition. It is approved for hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer.
Abemaciclib has been approved in the USA for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.
Excerpt | Reference | Relevance |
---|---|---|
"Abemaciclib has a lower incidence of neutropenia and a much greater incidence of all grades of diarrhea compared with other CDK4/6i, making diarrhea the key toxicity for abemaciclib." | ( CDK4/6 Inhibitors Expand the Therapeutic Options in Breast Cancer: Palbociclib, Ribociclib and Abemaciclib. Degenhardt, T; Eggersmann, TK; Gluz, O; Harbeck, N; Wuerstlein, R, 2019) | 1.45 |
"Abemaciclib has been developed for use in hormone receptor positive(HR+)breast cancer, dosed daily in combination with endocrine therapy." | ( [Development of CDK4 & 6 Inhibitor Abemaciclib in Breast Cancer]. Chen, Y; Kawaguchi, T; Masuda, N; Ohno, S; Saji, S, 2021) | 1.62 |
"Abemaciclib has been approved in the USA for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer, in combination with fulvestrant in women with disease progression following endocrine therapy, and as monotherapy in adult patients with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting." | ( Abemaciclib: First Global Approval. Kim, ES, 2017) | 2.62 |
Abemaciclib has a lower incidence of neutropenia and a much greater incidence of all grades of diarrhea compared with other CDK4/6i, making diarrhea the key toxicity for abemacIClib. AbemACiclib can also increase the expression of PD-L1 in SCLC.
Excerpt | Reference | Relevance |
---|---|---|
"Abemaciclib can also increase the expression of PD-L1 in SCLC." | ( [Study on the Biological Function of Abemecilib in Inhibiting the Proliferation, Invasion and
Migration of Small Cell Lung Cancer with High c-Myc Expression]. Guo, J; Han, Y; Mu, D; Ren, X; Sun, L; Yu, W; Zhang, J, 2023) | 1.63 |
"Abemaciclib has a lower incidence of neutropenia and a much greater incidence of all grades of diarrhea compared with other CDK4/6i, making diarrhea the key toxicity for abemaciclib." | ( CDK4/6 Inhibitors Expand the Therapeutic Options in Breast Cancer: Palbociclib, Ribociclib and Abemaciclib. Degenhardt, T; Eggersmann, TK; Gluz, O; Harbeck, N; Wuerstlein, R, 2019) | 1.45 |
Abemaciclib plus fulvestrant resulted in a statistically significant and clinically meaningful median OS improvement of 9.4 months for patients with HR-positive, ERBB2-negative ABC who progressed after prior ET. Treatment is associated with a potential complication of interstitial lung disease, regardless of age.
The CKD4/6 inhibitor abemaciclib is related to adverse events such as hematological toxicity and increase in serum creatinine levels. Neutropenia is observed at varying incidences in patients treated with these drugs.
A phase I study was conducted in cancer patients which incorporated intensive pharmacokinetic sampling after single and multiple oral doses of abemaciclib.
Excerpt | Reference | Relevance |
---|---|---|
" The objectives of this study were to characterize the pharmacokinetics of abemaciclib in cancer patients using population pharmacokinetic (popPK) modeling, and to evaluate target engagement at clinically relevant dose levels." | ( A Population Pharmacokinetic and Pharmacodynamic Analysis of Abemaciclib in a Phase I Clinical Trial in Cancer Patients. Chan, EM; Cronier, DM; Kulanthaivel, P; Sykes, AK; Tate, SC; Turner, PK, 2018) | 0.95 |
"A phase I study was conducted in cancer patients which incorporated intensive pharmacokinetic sampling after single and multiple oral doses of abemaciclib." | ( A Population Pharmacokinetic and Pharmacodynamic Analysis of Abemaciclib in a Phase I Clinical Trial in Cancer Patients. Chan, EM; Cronier, DM; Kulanthaivel, P; Sykes, AK; Tate, SC; Turner, PK, 2018) | 0.92 |
"The proportion of abemaciclib pharmacokinetic variability that can be attributed to patient demographics is negligible, and as such there are currently no dose adjustments recommended for adult patients of different sex, age, or body weight." | ( A Population Pharmacokinetic and Pharmacodynamic Analysis of Abemaciclib in a Phase I Clinical Trial in Cancer Patients. Chan, EM; Cronier, DM; Kulanthaivel, P; Sykes, AK; Tate, SC; Turner, PK, 2018) | 1.06 |
" A physiologically based pharmacokinetic (PBPK) model incorporating the metabolites was developed to predict the effect of other strong and moderate CYP3A4 inhibitors and inducers." | ( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling. Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020) | 0.81 |
" In this review, we provide an overview of the available clinical pharmacokinetic and pharmacodynamic characteristics of these novel drugs, summarize the results of food-effect and drug-drug interaction studies, and highlight exposure-response and exposure-toxicity relationships." | ( Clinical Pharmacokinetics and Pharmacodynamics of the Cyclin-Dependent Kinase 4 and 6 Inhibitors Palbociclib, Ribociclib, and Abemaciclib. Beijnen, JH; Groenland, SL; Huitema, ADR; Martínez-Chávez, A; Schinkel, AH; Steeghs, N; van Dongen, MGJ, 2020) | 0.76 |
" Therefore, we evaluated whether ABCB1 and ABCG2 polymorphisms are pharmacokinetic predictive factors of abemaciclib." | ( Effects of ABCB1 and ABCG2 polymorphisms on the pharmacokinetics of abemaciclib. Ando, H; Ebi, H; Fukushima, S; Hashimoto, N; Irie, K; Iwata, H; Maeda, A; Matsuzaki, M; Morishige, JI; Okada, A; Sawaki, M, 2022) | 1.17 |
The National Institute for Health and Care Excellence (NICE) invited the manufacturer (Eli Lilly) of abemaciclib (Verzenios) to submit evidence for the clinical and cost effectiveness of this drug in combination with endocrine therapy (ET)
Abemaciclib (LY2835219) is an orally bioavailable CDK4/6 inhibitor under phase III clinical trials. Palbociclib was recently approved by the U.S. FDA.
Abemaciclib has been developed for use in hormone receptor positive(HR+)breast cancer, dosed daily in combination with endocrine therapy. Preclinical difference in selectivity for CDK4 vs CDK6 could help explain its safety profile and ability to be dosed on a continuous schedule.
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
PPM1D protein | Homo sapiens (human) | Potency | 10.4353 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 11.9877 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 18.9991 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
Interferon beta | Homo sapiens (human) | Potency | 10.4353 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 1.1869 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
[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) |
---|---|---|---|---|---|---|---|
Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 0.0734 | 0.0010 | 0.5585 | 8.0000 | AID1277161; AID1382365; AID1513684; AID1737182 |
Cyclin-T1 | Homo sapiens (human) | Ki | 0.0570 | 0.0030 | 0.2768 | 0.7900 | AID1317308 |
Cyclin-K | Homo sapiens (human) | IC50 (µMol) | 0.0650 | 0.0030 | 0.2656 | 1.3700 | AID1648273 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.7569 | 0.0004 | 1.3452 | 10.0000 | AID1239760; AID1277156; AID1366692; AID1374353; AID1382343; AID1513678; AID1551211; AID1653003; AID1732687; AID1737228 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | Ki | 1.6270 | 0.0010 | 1.2551 | 5.0000 | AID1317305 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 6.6200 | 0.0002 | 2.4585 | 9.9600 | AID1804171 |
Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | Ki | 0.0100 | 0.0000 | 0.0084 | 0.0160 | AID1551238 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 0.0097 | 0.0006 | 0.5706 | 10.0000 | AID1239759; AID1239761; AID1277158; AID1366691; AID1374354; AID1374364; AID1382342; AID1424508; AID1509614; AID1513680; AID1551213; AID1653034; AID1732739; AID1737183; AID1737184; AID1909254; AID1915587 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | Ki | 0.0013 | 0.0006 | 0.7369 | 3.6000 | AID1239763; AID1317329 |
G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 0.7484 | 0.0013 | 1.4518 | 10.0000 | AID1239760; AID1277156; AID1382343; AID1513678; AID1732687; AID1737228 |
G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | Ki | 1.6270 | 0.1900 | 2.3292 | 5.0000 | AID1317305 |
Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 0.1036 | 0.0004 | 1.0339 | 10.0000 | AID1509616; AID1513681; AID1648274; AID1737229 |
G1/S-specific cyclin-D1 | Homo sapiens (human) | IC50 (µMol) | 0.0048 | 0.0006 | 0.5479 | 9.5000 | AID1239759; AID1277158; AID1374364; AID1374365; AID1513680; AID1732739 |
G1/S-specific cyclin-D1 | Homo sapiens (human) | Ki | 0.0042 | 0.0006 | 0.6654 | 3.6000 | AID1239763; AID1317329; AID1317331 |
G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 0.2320 | 0.0010 | 1.0404 | 10.0000 | AID1382342; AID1513679; AID1732740 |
G1/S-specific cyclin-E1 | Homo sapiens (human) | Ki | 0.5040 | 0.0005 | 0.5633 | 1.4850 | AID1317332 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 0.2635 | 0.0004 | 1.0444 | 10.0000 | AID1509616; AID1513679; AID1513681; AID1551212; AID1648274; AID1653004; AID1732740; AID1737229 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | Ki | 0.5040 | 0.0005 | 0.6427 | 5.0000 | AID1317332 |
G1/S-specific cyclin-D3 | Homo sapiens (human) | IC50 (µMol) | 0.0112 | 0.0015 | 0.0862 | 0.9250 | AID1374353; AID1382364; AID1402379; AID1509614; AID1509615; AID1648272; AID1737183; AID1737184; AID1909254 |
G1/S-specific cyclin-D3 | Homo sapiens (human) | Ki | 0.0082 | 0.0082 | 0.0176 | 0.0270 | AID1239764 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 2.0270 | 0.0001 | 0.9106 | 9.2000 | AID1277160; AID1513683; AID1551216; AID1737230 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | Ki | 3.9100 | 2.8000 | 3.3550 | 3.9100 | AID1317353 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 0.0693 | 0.0010 | 0.6236 | 8.0000 | AID1277161; AID1382365; AID1513684; AID1551217; AID1648273; AID1737182 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | Ki | 0.0570 | 0.0030 | 0.2482 | 0.7900 | AID1317308 |
Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 2.6027 | 0.0005 | 1.0823 | 9.2000 | AID1277160; AID1513683; AID1737230 |
Cyclin-H | Homo sapiens (human) | Ki | 3.9100 | 2.8000 | 3.3550 | 3.9100 | AID1317353 |
CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | IC50 (µMol) | 3.1060 | 0.0030 | 1.6892 | 9.2000 | AID1277160; AID1513683 |
CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | Ki | 3.9100 | 2.8000 | 3.3550 | 3.9100 | AID1317353 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | IC50 (µMol) | 0.0168 | 0.0019 | 0.8654 | 7.2000 | AID1239761; AID1366690; AID1374355; AID1374365; AID1382364; AID1402379; AID1424509; AID1509615; AID1551215; AID1648272; AID1653035; AID1915588 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | Ki | 0.0091 | 0.0082 | 0.0151 | 0.0270 | AID1239764; AID1317331 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 0.4050 | 0.0002 | 1.1832 | 10.0000 | AID1277159; AID1513682 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 10.9000 | 0.0009 | 1.9014 | 10.0000 | AID1374357 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Ki | 0.0100 | 0.0100 | 0.4108 | 1.5000 | AID1551237 |
Calcium/calmodulin-dependent protein kinase type 1 | Homo sapiens (human) | Ki | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID1551240 |
Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 0.4050 | 0.0010 | 1.2898 | 10.0000 | AID1277159; AID1513682 |
Homeodomain-interacting protein kinase 1 | Homo sapiens (human) | Ki | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID1551239 |
[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) |
---|---|---|---|---|---|---|---|
Bone morphogenetic protein receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.1413 | 3.7000 | AID1424922 |
Cell division cycle 7-related protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.5110 | 0.5110 | 0.5110 | AID1424936 |
Serine/threonine-protein kinase PLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.5144 | 9.0000 | AID1425121 |
ATP-dependent RNA helicase DDX3X | Homo sapiens (human) | Kd | 30.0000 | 0.4350 | 0.4350 | 0.4350 | AID1424975 |
Pyridoxal kinase | Homo sapiens (human) | Kd | 30.0000 | 0.2860 | 5.0765 | 16.4040 | AID1425106 |
Citron Rho-interacting kinase | Homo sapiens (human) | Kd | 0.7980 | 0.0330 | 3.0646 | 48.8760 | AID1424954 |
Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | Kd | 30.0000 | 0.0028 | 1.4744 | 8.7000 | AID1424953 |
Aurora kinase A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.7342 | 9.3000 | AID1424917 |
Cyclin-G-associated kinase | Homo sapiens (human) | Kd | 2.1940 | 0.0003 | 0.9086 | 28.6510 | AID1425009 |
Ephrin type-B receptor 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0768 | 9.0000 | AID1424995 |
Peroxisomal acyl-coenzyme A oxidase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.3140 | 2.6020 | AID1424896 |
Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6212 | 11.4330 | AID1425155 |
Mitotic checkpoint serine/threonine-protein kinase BUB1 | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 1.3910 | 3.5070 | AID1424926 |
Dynamin-like 120 kDa protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 0.3610 | 0.7050 | AID1425097 |
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 | 30.0000 | 0.0002 | 2.7105 | 56.0660 | AID1425158 |
Serine/threonine-protein kinase ULK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.8410 | 23.2730 | AID1425208 |
Serine/threonine-protein kinase/endoribonuclease IRE1 | Homo sapiens (human) | Kd | 30.0000 | 0.0057 | 2.0095 | 12.2010 | AID1424997 |
Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 1.9737 | 29.9570 | AID1425162 |
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 | 30.0000 | 0.0120 | 1.6396 | 7.2000 | AID1425161 |
Serine/threonine-protein kinase 16 | Homo sapiens (human) | Kd | 0.4950 | 0.0017 | 1.2483 | 9.9690 | AID1425179 |
Cyclin-dependent kinase-like 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.4788 | 7.3000 | AID1424951 |
Serine/threonine-protein kinase 10 | Homo sapiens (human) | Kd | 2.4700 | 0.0000 | 2.9234 | 57.4530 | AID1425177 |
Serine/threonine-protein kinase D3 | Homo sapiens (human) | Kd | 1.8410 | 0.0089 | 2.2738 | 23.3410 | AID1425137 |
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 | 30.0000 | 0.1700 | 1.5781 | 8.0000 | AID1425050 |
Mitogen-activated protein kinase kinase kinase kinase 4 | Homo sapiens (human) | Kd | 1.3220 | 0.0082 | 2.3645 | 62.7720 | AID1425054 |
Serine/threonine-protein kinase LATS1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 1.8393 | 10.7330 | AID1425033 |
Serine/threonine-protein kinase PAK 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0027 | 2.5694 | 30.3710 | AID1425100 |
Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0411 | 13.4530 | AID1424890 |
Epidermal growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.3514 | 20.8270 | AID1424983 |
High affinity nerve growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.3484 | 9.2000 | AID1425094 |
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 | 1.6240 | 0.0013 | 2.7081 | 26.3240 | AID1425130 |
Insulin receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.0823 | 7.9060 | AID1425026 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1174 | 24.2210 | AID1425034 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.4238 | 8.4000 | AID1425008 |
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 | 30.0000 | 0.0048 | 1.0986 | 7.4000 | AID1425003 |
Tyrosine-protein kinase Yes | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.3708 | 17.1520 | AID1425212 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0485 | 5.7000 | AID1425037 |
Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 0.8642 | 27.5420 | AID1425154 |
Insulin-like growth factor 1 receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.9211 | 19.2170 | AID1425022 |
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 | 30.0000 | 0.0002 | 1.6297 | 8.5000 | AID1425076 |
Tyrosine-protein kinase HCK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0343 | 15.9930 | AID1425017 |
Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.0050 | 11.1070 | AID1425104 |
Serine/threonine-protein kinase A-Raf | Homo sapiens (human) | Kd | 30.0000 | 0.0470 | 9.6832 | 33.6550 | AID1424915 |
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 | 0.0070 | 0.0010 | 1.1393 | 19.3160 | AID1425111 |
Fibroblast growth factor receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5581 | 6.2000 | AID1425004 |
DNA topoisomerase 2-alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0640 | 0.2750 | 0.4860 | AID1425202 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | Kd | 0.0970 | 0.0033 | 1.6050 | 8.6000 | AID1424946 |
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 | 30.0000 | 0.0002 | 1.5077 | 9.6000 | AID1425175 |
cAMP-dependent protein kinase type II-alpha regulatory subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0520 | 1.7535 | 3.4550 | AID1425128 |
Serine/threonine-protein kinase B-raf | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6258 | 26.0180 | AID1424924 |
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.0569 | 9.5000 | AID1425110 |
Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 6.7556 | 88.9030 | AID1425093 |
Tyrosine-protein kinase Fer | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 1.3604 | 8.8000 | AID1425002 |
Protein kinase C alpha type | Homo sapiens (human) | Kd | 0.5300 | 0.0003 | 1.7922 | 21.3520 | AID1425129 |
cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 2.9479 | 23.2450 | AID1425123 |
General transcription and DNA repair factor IIH helicase subunit XPD | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6906 | 12.0220 | AID1424996 |
Casein kinase II subunit alpha' | Homo sapiens (human) | Kd | 0.0190 | 0.0010 | 2.5309 | 28.8720 | AID1424968 |
Ras-related protein Rab-6A | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 0.0330 | 0.0330 | AID1425150 |
Ephrin type-A receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0041 | 1.8000 | 9.8000 | AID1424987 |
Multifunctional protein ADE2 | Homo sapiens (human) | Kd | 30.0000 | 5.4810 | 5.4810 | 5.4810 | AID1425098 |
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 | 30.0000 | 0.0130 | 0.7408 | 4.1000 | AID1425124 |
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 | 30.0000 | 0.0013 | 1.1805 | 4.8000 | AID1425164 |
Tyrosine-protein kinase JAK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 1.2166 | 7.8000 | AID1425030 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 10.4870 | 0.0070 | 1.5179 | 10.4870 | AID1424944 |
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 |
Mitogen-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.4300 | 5.2743 | 9.8000 | AID1425061 |
MAP/microtubule affinity-regulating kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.9689 | 58.2400 | AID1425069 |
Deoxycytidine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.0875 | 2.1630 | AID1424970 |
Mitogen-activated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.7441 | 7.3000 | AID1425056 |
Ephrin type-A receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.0752 | 8.1980 | AID1424988 |
Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 3.1536 | 53.1980 | AID1424992 |
Non-receptor tyrosine-protein kinase TYK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.5575 | 8.7000 | AID1425207 |
Wee1-like protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 3.5389 | 65.1580 | AID1425210 |
Heme oxygenase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.1190 | 0.1190 | 0.1190 | AID1425018 |
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 | 30.0000 | 0.0006 | 1.0621 | 4.4000 | AID1424910 |
RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0021 | 1.6196 | 8.7000 | AID1424911 |
Dual specificity protein kinase TTK | Homo sapiens (human) | Kd | 30.0000 | 0.0065 | 1.6269 | 8.5000 | AID1425205 |
DNA replication licensing factor MCM4 | Homo sapiens (human) | Kd | 30.0000 | 0.6290 | 0.6290 | 0.6290 | AID1425072 |
Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 1.6429 | 9.6000 | AID1425039 |
Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 0.9559 | 9.9000 | AID1425006 |
Bone morphogenetic protein receptor type-1A | Homo sapiens (human) | Kd | 30.0000 | 0.0600 | 1.5010 | 7.0000 | AID1424921 |
Activin receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.5110 | 15.2580 | AID1424901 |
TGF-beta receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.2785 | 9.6000 | AID1425196 |
TGF-beta receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0800 | 1.8351 | 6.9000 | AID1425197 |
Tyrosine-protein kinase CSK | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 3.4578 | 39.5530 | AID1424960 |
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 | 30.0000 | 0.0260 | 9.3316 | 51.0180 | AID1425133 |
Exosome RNA helicase MTR4 | Homo sapiens (human) | Kd | 30.0000 | 2.6070 | 2.6070 | 2.6070 | AID1425168 |
Tyrosine-protein kinase Tec | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.0095 | 8.7000 | AID1425193 |
Tyrosine-protein kinase ABL2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1249 | 14.9240 | AID1424891 |
Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.2424 | 10.8370 | AID1425007 |
Tyrosine-protein kinase SYK | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 2.0052 | 9.2260 | AID1425188 |
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 | 3.7560 | 0.0110 | 2.0965 | 26.0590 | AID1425063 |
Mitogen-activated protein kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4596 | 8.1000 | AID1425064 |
Dual specificity mitogen-activated protein kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.0462 | 6.6000 | AID1425040 |
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 | 30.0000 | 0.0010 | 2.5756 | 19.3520 | AID1424961 |
Casein kinase I isoform delta | Homo sapiens (human) | Kd | 30.0000 | 0.0150 | 2.2270 | 18.3960 | AID1424962 |
MAP kinase-activated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0274 | 14.7420 | AID1425065 |
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 |
Casein kinase I isoform epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.4086 | 12.4090 | AID1424963 |
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 | 0.0070 | 0.0020 | 1.8791 | 29.8810 | AID1424955 |
Dual specificity protein kinase CLK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.4499 | 9.0000 | AID1424957 |
Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 0.0130 | 0.0060 | 2.4754 | 22.5430 | AID1425013 |
Glycogen synthase kinase-3 beta | Homo sapiens (human) | Kd | 0.0130 | 0.0070 | 1.0057 | 6.1680 | AID1425014 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.6783 | 7.7000 | AID1424949 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | Kd | 0.1740 | 0.0010 | 1.6166 | 9.9010 | AID1424950 |
Ras-related protein Rab-27A | Homo sapiens (human) | Kd | 30.0000 | 4.4930 | 4.4930 | 4.4930 | AID1425149 |
Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 0.1260 | 0.0061 | 1.5252 | 8.5000 | AID1425027 |
Ribosomal protein S6 kinase alpha-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 2.8896 | 37.6050 | AID1425160 |
Serine/threonine-protein kinase Nek2 | Homo sapiens (human) | Kd | 30.0000 | 0.1100 | 1.5649 | 6.5000 | AID1425086 |
Serine/threonine-protein kinase Nek3 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.9368 | 38.0880 | AID1425087 |
Dual specificity mitogen-activated protein kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0034 | 2.3943 | 6.5000 | AID1425043 |
LIM domain kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.7840 | 21.0890 | AID1425035 |
LIM domain kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.9717 | 52.0560 | AID1425036 |
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 |
Ephrin type-B receptor 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0069 | 2.1713 | 6.4100 | AID1424993 |
Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.2100 | 5.9000 | AID1424990 |
Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.1678 | 26.3990 | AID1424994 |
Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 3.1525 | 43.9420 | AID1424989 |
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 |
Ras-related protein Rab-10 | Homo sapiens (human) | Kd | 30.0000 | 1.3480 | 1.3480 | 1.3480 | AID1425148 |
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 |
GTP-binding nuclear protein Ran | Homo sapiens (human) | Kd | 30.0000 | 0.7590 | 0.7590 | 0.7590 | AID1425153 |
Casein kinase I isoform gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0460 | 1.4506 | 6.6000 | AID1424965 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | Kd | 0.0590 | 0.0320 | 1.2007 | 3.3560 | AID1424948 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0430 | 1.3757 | 8.3000 | AID1424947 |
Cyclin-dependent kinase 16 | Homo sapiens (human) | Kd | 0.0500 | 0.0011 | 1.5855 | 10.0000 | AID1424941 |
Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.8233 | 5.6000 | AID1424942 |
ATP-dependent 6-phosphofructokinase, platelet type | Homo sapiens (human) | Kd | 30.0000 | 0.9830 | 0.9830 | 0.9830 | AID1425108 |
Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1386 | 8.7730 | AID1425038 |
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 | 30.0000 | 0.0007 | 1.6140 | 7.2000 | AID1425134 |
Activin receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.4853 | 16.1210 | AID1424900 |
Macrophage-stimulating protein receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.0718 | 8.4000 | AID1425078 |
Focal adhesion kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.2255 | 13.0390 | AID1425142 |
Protein kinase C delta type | Homo sapiens (human) | Kd | 0.7950 | 0.0002 | 1.1261 | 9.2060 | AID1425131 |
Tyrosine-protein kinase BTK | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.5299 | 10.1530 | AID1424925 |
Activated CDC42 kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.7138 | 9.6000 | AID1425201 |
Epithelial discoidin domain-containing receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6314 | 71.4840 | AID1424972 |
Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 1.4681 | 14.0430 | AID1425052 |
Serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.7120 | 25.9020 | AID1425185 |
5'-AMP-activated protein kinase catalytic subunit alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0037 | 1.8913 | 15.3890 | AID1425122 |
Dual specificity mitogen-activated protein kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.6590 | 65.6770 | AID1425042 |
Mitogen-activated protein kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0420 | 2.0073 | 9.9000 | AID1425062 |
Serine/threonine-protein kinase PAK 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 2.3045 | 6.0000 | AID1425099 |
Serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.8602 | 17.5260 | AID1425182 |
Mitogen-activated protein kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.5995 | 12.4730 | AID1425044 |
Rho-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7555 | 13.4620 | AID1425157 |
Non-receptor tyrosine-protein kinase TNK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.0064 | 11.2690 | AID1425200 |
Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | Kd | 0.0180 | 0.0005 | 1.0209 | 7.8000 | AID1424929 |
Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | Kd | 0.0190 | 0.0003 | 1.5044 | 20.3010 | AID1424928 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 0.2040 | 0.0001 | 2.1016 | 40.2910 | AID1424981 |
Activin receptor type-2B | Homo sapiens (human) | Kd | 30.0000 | 0.0076 | 2.7328 | 9.9000 | AID1424902 |
Bone morphogenetic protein receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0190 | 2.5917 | 14.3770 | AID1424923 |
Protein-tyrosine kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0043 | 1.7430 | 9.0000 | AID1425144 |
cGMP-dependent protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 0.7072 | 3.8000 | AID1425138 |
Cyclin-dependent kinase 13 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.2571 | 4.5180 | AID1424940 |
Inhibitor of nuclear factor kappa-B kinase subunit epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.1093 | 8.3000 | AID1425023 |
Protein-tyrosine kinase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.9450 | 30.4140 | AID1425143 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 2.2835 | 29.9330 | AID1425074 |
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 |
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 | 30.0000 | 0.0280 | 2.5286 | 22.7260 | AID1425159 |
Dual specificity testis-specific protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 1.7568 | 5.6000 | AID1425194 |
Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2088 | 7.9000 | AID1425081 |
Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.4610 | 3.7430 | AID1425058 |
Serine/threonine-protein kinase STK11 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.9949 | 5.9000 | AID1425178 |
Serine/threonine-protein kinase N1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 3.1729 | 49.8130 | AID1425117 |
Serine/threonine-protein kinase N2 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.7527 | 9.9000 | AID1425118 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 0.5036 | 8.5000 | AID1425059 |
Calcium/calmodulin-dependent protein kinase type IV | Homo sapiens (human) | Kd | 30.0000 | 0.0300 | 1.9215 | 5.4600 | AID1424930 |
Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.5639 | 17.9840 | AID1425045 |
MAP kinase-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0170 | 0.0260 | AID1425066 |
Discoidin domain-containing receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.9888 | 42.2800 | AID1424973 |
AP2-associated protein kinase 1 | Homo sapiens (human) | Kd | 0.1020 | 0.0012 | 1.3707 | 13.7110 | AID1424889 |
Myosin light chain kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6184 | 10.4240 | AID1425082 |
Uncharacterized aarF domain-containing protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.4990 | 0.7960 | AID1424906 |
Putative heat shock protein HSP 90-beta 2 | Homo sapiens (human) | Kd | 30.0000 | 2.5660 | 2.5660 | 2.5660 | AID1425019 |
Rab-like protein 3 | Homo sapiens (human) | Kd | 30.0000 | 4.8300 | 4.8300 | 4.8300 | AID1425151 |
Serine/threonine-protein kinase MRCK alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.5547 | 14.0200 | AID1424933 |
Serine/threonine-protein kinase MRCK gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0370 | 1.9625 | 9.5000 | AID1424935 |
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 | 30.0000 | 0.0012 | 1.3350 | 9.9000 | AID1425209 |
Uncharacterized protein FLJ45252 | Homo sapiens (human) | Kd | 0.0880 | 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 | 30.0000 | 0.0001 | 1.8425 | 11.1030 | AID1425068 |
Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 0.1070 | 0.0004 | 2.1612 | 18.7570 | AID1425189 |
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 | 0.0400 | 0.0230 | 3.1137 | 22.7470 | AID1424904 |
Mitogen-activated protein kinase kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.6413 | 15.4350 | AID1425053 |
MAP kinase-activated protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 1.1241 | 3.1180 | AID1425067 |
Atypical kinase COQ8A, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 5.1673 | 65.3020 | AID1424905 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.7522 | 8.8000 | AID1425115 |
Mitogen-activated protein kinase 15 | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 0.6880 | 4.5000 | AID1425060 |
Serine/threonine-protein kinase Nek9 | Homo sapiens (human) | Kd | 30.0000 | 0.0160 | 2.7428 | 19.6170 | AID1425089 |
ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 30.0000 | 0.0860 | 0.0860 | 0.0860 | AID1424974 |
Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.9378 | 5.5000 | AID1425051 |
Aurora kinase B | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.0614 | 22.8520 | AID1424918 |
MAP/microtubule affinity-regulating kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0054 | 1.1029 | 4.9000 | AID1425070 |
Serine/threonine-protein kinase Nek1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 2.4294 | 8.3000 | AID1425085 |
Calcium/calmodulin-dependent protein kinase kinase 2 | Homo sapiens (human) | Kd | 2.5980 | 0.0000 | 3.2331 | 52.8470 | AID1424931 |
EKC/KEOPS complex subunit TP53RK | Homo sapiens (human) | Kd | 30.0000 | 0.3110 | 1.9519 | 3.8400 | AID1425204 |
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0440 | 0.9285 | 2.9000 | AID1425116 |
Mitogen-activated protein kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0700 | 6.5647 | 50.5360 | AID1425049 |
Mitogen-activated protein kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.5331 | 9.9000 | AID1425047 |
Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | Kd | 4.8360 | 0.0580 | 1.9224 | 4.8360 | AID1424984 |
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 | 2.0640 | 0.0081 | 2.3723 | 25.0190 | AID1425136 |
NUAK family SNF1-like kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.6774 | 4.6000 | AID1425095 |
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 | 30.0000 | 0.0011 | 1.8165 | 41.7950 | AID1425166 |
STE20-like serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.8573 | 99.2320 | AID1425171 |
Serine/threonine-protein kinase TAO3 | Homo sapiens (human) | Kd | 1.7210 | 0.0002 | 2.7131 | 14.1960 | AID1425191 |
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 | 0.0130 | 0.0020 | 1.4122 | 8.3000 | AID1424958 |
Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0530 | 2.0622 | 5.7000 | AID1424964 |
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 | 56.0320 | 0.0022 | 2.4097 | 56.0320 | AID1424920 |
Interleukin-1 receptor-associated kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 3.4719 | 34.1450 | AID1425029 |
Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 30.0000 | 0.0023 | 1.7034 | 13.6380 | AID1425213 |
Cyclin-dependent kinase 12 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.8032 | 5.6350 | AID1424939 |
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 26 | Homo sapiens (human) | Kd | 30.0000 | 0.0074 | 1.7380 | 8.3000 | AID1425181 |
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 | 30.0000 | 0.0060 | 1.0226 | 4.4000 | AID1425090 |
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 | 30.0000 | 0.0009 | 1.7674 | 49.6010 | AID1425192 |
Septin-9 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 0.2430 | 0.6350 | AID1425165 |
Ribosomal protein S6 kinase alpha-6 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 2.4153 | 23.7620 | AID1425163 |
TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0047 | 1.3935 | 10.0000 | AID1425199 |
Serine/threonine-protein kinase TAO2 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.0176 | 12.9420 | AID1425190 |
Serine/threonine-protein kinase ICK | Homo sapiens (human) | Kd | 0.0530 | 0.0007 | 1.4717 | 9.3000 | AID1425021 |
RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.7646 | 6.2000 | AID1424912 |
Serine/threonine-protein kinase SIK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.5086 | 10.3180 | AID1425167 |
Mitogen-activated protein kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0024 | 1.3298 | 6.9000 | AID1425046 |
Thyroid hormone receptor-associated protein 3 | Homo sapiens (human) | Kd | 30.0000 | 2.7460 | 2.7460 | 2.7460 | AID1425198 |
Mitogen-activated protein kinase kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.9494 | 50.2140 | AID1425055 |
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 | 30.0000 | 0.0340 | 3.6252 | 50.0050 | AID1424934 |
Interleukin-1 receptor-associated kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.7137 | 25.5810 | AID1425028 |
Serine/threonine-protein kinase 24 | Homo sapiens (human) | Kd | 30.0000 | 0.0065 | 0.8920 | 4.0840 | AID1425180 |
Casein kinase I isoform gamma-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.3978 | 8.7000 | AID1424966 |
Mitogen-activated protein kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0390 | 2.3970 | 8.4000 | AID1425048 |
[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) |
---|---|---|---|---|---|---|---|
Cyclin-dependent kinase 4 | Homo sapiens (human) | INH | 6.7000 | 6.7000 | 6.7000 | 6.7000 | AID1239762 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | INH | 6.7000 | 6.7000 | 6.7000 | 6.7000 | AID1239762 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1608889 | Induction of apoptosis in human MDA-MB-231 cells at 40 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
AID1588682 | Inhibition of recombinant full length human GST-tagged DYRK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588728 | Inhibition of recombinant full length human His-tagged JNK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588841 | Inhibition of recombinant full length human GST-tagged p38alpha expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-15 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1909276 | Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 3 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 1.06%) | |||
AID1277161 | Inhibition of CDK9/Cyclin T1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
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. |
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. |
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. |
AID1588765 | Inhibition of recombinant full length human GST-tagged NEK4 expressed in baculovirus expression system at 0.1 uM using serine/threonine-17 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588671 | Inhibition of recombinant full length human His-tagged CAMK2beta expressed in baculovirus expression system at 0.1 uM using serine/threonine-17 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1425066 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative 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. |
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. |
AID1648274 | Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay | |||
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. |
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. |
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. |
AID1608876 | Antiproliferative activity against HUVEC cells assessed as reduction in cell viability at 40 nM measured upto 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588708 | Inhibition of recombinant full length human GST-tagged GRK6 expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588836 | Inhibition of recombinant full length human GST-tagged YES expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588661 | Inhibition of recombinant full length human GST-tagged CK1 gamma 1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-5 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588777 | Inhibition of recombinant human GST-tagged PI3Kgamma catalytic domain (468 to 1203 residues) expressed in insect expression system at 0.1 uM using PI Lipid Kinase as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1425132 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1551251 | Half life in human | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1513692 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G1 phase at 0.03 to 0.8 uM after 24 hrs by propidium iodide-staining based flow cytometry | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
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. |
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. |
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. |
AID1588743 | Inhibition of recombinant full length human His-tagged MEK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588787 | Inhibition of recombinant full length human GST-tagged PKD1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-17 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1551239 | Inhibition of wild-type human partial length HIPK1 (M146 to I555 residues) expressed in mammalian expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588644 | Inhibition of recombinant full length human GST-tagged CDK17/Cyclin Y (2 to end amino acids) expressed in insect expression system at 0.1 uM using serine/threonine-12 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588770 | Inhibition of recombinant full length human His-tagged PAK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-20 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1849057 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation of cells at G1 phase at 1.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 57.38%) | |||
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. |
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. |
AID1588668 | Inhibition of recombinant human His-tagged CSF1R catalytic domain (538 to 910 residues) expressed in Baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1239760 | Inhibition of human CDK1/cyclin B1 (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
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. |
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. |
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. |
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. |
AID1588674 | Inhibition of recombinant full length human full length GST-tagged CAMK4 expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-13 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1374357 | Inhibition of human ERG | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1737180 | Selectivity ratio of IC50 for inhibition of CDK9/cyclin T1 (unknown origin) to IC50 for inhibition of recombinant human full-length N-terminal GST-fused CDK4 (1 to 303 residues)/GST-tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression s | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1909295 | Antitumor activity against mouse EMT6 cells implanted in BALB/c mouse syngenic model assessed as tumor growth inhibition at 40 mg/kg, po qd and measured after 18 days relative to control | |||
AID1868058 | Inhibition of CDK6/Cyclin D (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. |
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. |
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. |
AID1608517 | Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1509690 | Half life in BALB/c mouse at 10 mg/kg, po measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
AID1653035 | Inhibition of CDK6 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. |
AID1509705 | Antitumor activity against human MCF7 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 50 mg/kg, po administered once daily for 19 days measured on 19th day | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1424509 | Inhibition of CDK6 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. |
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. |
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. |
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. |
AID1551228 | Protein binding in human plasma | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1737187 | Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
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. |
AID1653004 | Inhibition of CDK2 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. |
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. |
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. |
AID1588731 | Inhibition of recombinant full length human GST-tagged KHS1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588721 | Inhibition of recombinant human GST-tagged IRR (944 to 1297 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
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. |
AID1648277 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1588764 | Inhibition of recombinant full length human GST-tagged NEK1 catalytic domain (1 to 505 amino acids) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to contr | |||
AID1588827 | Inhibition of recombinant human GST-tagged TXK catalytic domain (260 to 527 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588811 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged SLK expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
AID1608515 | Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1382372 | Half life in rat liver microsomes at 1.11 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588749 | Inhibition of tracer 236 binding to full length human GST-tagged MKNK2 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
AID1588694 | Inhibition of recombinant human GST-tagged ERBB4 catalytic domain (708 to 993 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588646 | Inhibition of recombinant full length human His-tagged CDK2/Cyclin A expressed in baculovirus expression system at 0.1 uM using serine/threonine-12 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509673 | Metabolic stability in mouse liver microsomes assessed as intrinsic clearance rate per mg protein incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
AID1588726 | Inhibition of recombinant human GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588711 | Inhibition of recombinant human GST-tagged HIPK1 catalytic domain (158 to 555 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509669 | Metabolic stability in rat liver microsomes assessed as half life incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
AID1588715 | Inhibition of recombinant human His-tagged IGF1R catalytic domain (960 to 1397 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1317305 | Inhibition of CDK1/cyclin B (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1588660 | Inhibition of recombinant full length human His-tagged CK1 epsilon1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-11 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588796 | Inhibition of recombinant human GST-tagged RAF1 Y340D Y341D mutant catalytic domain (306 to 648 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to | |||
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. |
AID1588662 | Inhibition of recombinant full length human His-tagged CK1 gamma 2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-5 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
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. |
AID1588747 | Inhibition of recombinant full length human His-tagged MKK6 expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588627 | Inhibition of recombinant full length human His-tagged Aurora A expressed in baculovirus expression system at 0.1 uM using serine/threonine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1513679 | Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
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. |
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. |
AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
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. |
AID1588831 | Inhibition of recombinant human His-tagged TRKA catalytic domain (441 to 796 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588638 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged CAMKK2 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1648272 | Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay | |||
AID1588663 | Inhibition of recombinant full length human His-tagged CK2 alpha 1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-11 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1915588 | Inhibition of Cdk6 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1509686 | Volume of distribution at steady state in BALB/c mouse at 3 mg/kg, iv measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588586 | Efflux ratio in MDCK2 expressing mouse bcrp1 | |||
AID1277160 | Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) using (YSPTSPS)2KK peptide as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
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. |
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. |
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. |
AID1588695 | Inhibition of recombinant full length human GST-tagged FAK expressed in baculovirus expression system at 0.1 uM using tyrosine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551253 | Clearance in human | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588782 | Inhibition of recombinant full length human GST-tagged PKCdelta expressed in insect expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588775 | Inhibition of recombinant human His-tagged PDK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588849 | Inhibition of recombinant full length human GST-tagged PKG1 alpha expressed in baculovirus expression system at 0.1 uM using CREBtide as substrate 60 mins by Lanthascreen assay relative to control | |||
AID1588751 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged MLK2 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
AID1509666 | Antiproliferative activity against human PC3 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1909254 | Inhibition of recombinant N-terminal GST/His6-fusion tagged human CDK4/Cyclin D3 expressed in Sf9 insect cells using 5-FAM-IPTSPITTTYFFFKKK as substrate preincubated for 10 mins followed by substrate addition and incubated for 3 hrs in presence of ATP by | |||
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. |
AID1425050 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1648278 | Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
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. |
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. |
AID1382385 | AUClast in ICR mouse at 0.5 mg/kg, iv by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1588651 | Inhibition of recombinant full length human GST/His-tagged CDK5/p25 expressed in baculovirus expression system at 0.1 uM using serine/threonine-12 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588814 | Inhibition of tracer 236 binding to recombinant full length human His-tagged STK16 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
AID1588679 | Inhibition of recombinant human DNA-PK expressed in baculovirus expression system at 0.1 uM using serine/threonine-26 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509653 | Antiproliferative activity against human THP1 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588655 | Inhibition of recombinant full length human His-tagged CDK9/CyclinT1 expressed in baculovirus expression system at 0.1 uM using CDK7/9tide peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1513683 | Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1588771 | Inhibition of recombinant human GST-tagged PAK4 catalytic domain (295 to 591 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-20 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1824398 | Antiproliferative activity against human RPMI-8226 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1588732 | Inhibition of recombinant human His-tagged KIT (544 to 976 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588798 | Inhibition of recombinant human GST-tagged ROCK1 catalytic domain (1 to 535 amino acids) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509621 | Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588800 | Inhibition of recombinant full length human His-tagged RSK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382356 | Cell cycle arrest in human COLO205 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 64.4%) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1648275 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1824403 | Antiproliferative activity against human HEK293 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1648353 | Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c nu/nu mouse assessed as tumor growth inhibition at 45 mg/kg, po administered once daily for 3 weeks and measured at 3 days interval during compound dosing | |||
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. |
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. |
AID1608566 | Antitumor activity against human SiHa cells xenografted in NOD/SCID BALB/c mouse assessed as reduction in Ki67 expression at 40 mg/kg, po measured after 21 days by hematoxylin and eosin staining based immunohistochemistry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588703 | Inhibition of recombinant human GST-tagged FLT4 catalytic domain (800 to 1297 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588850 | Inhibition of recombinant full length human PRKAA1 expressed in baculovirus expression system at 0.1 uM using CREBtide as substrate 60 mins by Lanthascreen assay relative to control | |||
AID1382390 | Cmax in ICR mouse at 1 mg/kg, po via gavage by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
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. |
AID1653003 | Inhibition of CDK1 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. |
AID1551211 | Inhibition of CDK1 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1737228 | Inhibition of CDK1/cyclin B (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1239763 | Competitive inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1824412 | Induction of cell cycle arrest in human RPMI-8226 cells assessed as accumulation at G1 phase at 1 uM measured after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 41.96%) | |||
AID1588707 | Inhibition of recombinant full length human GST-tagged GRK5 expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588701 | Inhibition of recombinant human GST-tagged FLT1 catalytic domain (781 to 1338 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588838 | Inhibition of recombinant full length human GST-tagged ZIPK expressed in baculovirus expression system at 0.1 uM using serine/threonine-13 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588753 | Inhibition of recombinant full length human GST-tagged MSK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1382342 | Inhibition of human CDK4/cyclin D1 using ULight-substrate after 1 hr by LANCE assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1588696 | Inhibition of recombinant human His-tagged FGFR1 catalytic domain (308 to 731 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588851 | Inhibition of recombinant full length human GST-tagged ZAK expressed in baculovirus expression system at 0.1 uM using CREBtide as substrate 60 mins by Lanthascreen assay relative to control | |||
AID1588640 | Inhibition of tracer 236 binding to recombinant human GST/His-tagged CDK11/Cyclin C catalytic domain (CDK11: 1 to 502, Cyclin C: 1 to 283) expressed in insect cells expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to contr | |||
AID1588803 | Inhibition of recombinant human GST-tagged RET (658 to 1114 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588637 | Inhibition of tracer 236 binding to recombinant human GST-tagged CAMKK1 expressed in Escherichia coli expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588832 | Inhibition of recombinant human His-tagged TRKB catalytic domain (526 to 838 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1909278 | Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 3 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 98.04%) | |||
AID1588790 | Inhibition of recombinant human GST-tagged PLK3 catalytic domain (58 to 340 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1513680 | Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
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. |
AID1588619 | Inhibition of recombinant human GST-tagged ACVR1B catalytic domain (150 to 505 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588634 | Inhibition of recombinant full length human His-tagged BMX expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588783 | Inhibition of recombinant full length human GST-tagged PKCepsilon expressed in insect expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588705 | Inhibition of recombinant full length human His-tagged GRK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588801 | Inhibition of recombinant full length human His-tagged RSK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1382353 | Cell cycle arrest in human COLO205 cells assessed as accumulation at G2/M phase up to 10 uM after 24 hrs by propidium iodide staining based FACS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588647 | Inhibition of tracer 236 binding to recombinant human GST-tagged CDK2/CyclinA1 expressed by baculovirus in Sf9 insect cells expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
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. |
AID1648273 | Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay | |||
AID1588735 | Inhibition of recombinant human GST-tagged LTK (450 to 864 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509617 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588840 | Inhibition of recombinant human GST-tagged mTOR catalytic domain (1360 to 2549 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-11 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551254 | Clearance in rat | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588795 | Inhibition of recombinant full length human GST-tagged PRKX expressed in baculovirus expression system at 0.1 uM using serine/threonine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509655 | Antiproliferative activity against human SKHEP1 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
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. |
AID1588672 | Inhibition of recombinant full length human His-tagged CAMK1delta expressed in baculovirus expression system at 0.1 uM using serine/threonine-25 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
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. |
AID1509619 | Antiproliferative activity against human ZR-75-1 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588736 | Inhibition of recombinant full length human His-tagged LCK expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588805 | Inhibition of recombinant human GST-tagged ROS1 catalytic domain (1883 to 2347 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1824428 | Induction of apoptosis in human RPMI-8226 cells assessed as late apoptic cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 2.85%) | |||
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. |
AID1588706 | Inhibition of recombinant full length human GST-tagged GRK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588813 | Inhibition of recombinant full length human His-tagged SRPK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-18 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588665 | Inhibition of recombinant human GST-tagged CLK2 catalytic domain (137 to 498 residues) expressed in Baculovirus expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551245 | Metabolic stability in human microsomes assessed as parent compound remaining after 15 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
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. |
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. |
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. |
AID1588820 | Inhibition of recombinant human GST-tagged TAO2 catalytic domain (1 to 314 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588742 | Inhibition of recombinant full length human GST-tagged MARK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-25 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588673 | Inhibition of recombinant full length human His-tagged CAMK2alpha expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374359 | AUC in rat at 5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1513684 | Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1588845 | Inhibition of recombinant human GST-tagged p70S6K catalytic domain (1 to 421 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1509676 | Metabolic stability in monkey liver microsomes assessed as intrinsic clearance rate per mg protein incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588807 | Inhibition of recombinant human GST-tagged SGK1 catalytic domain (60 to 431 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374363 | Apparent volume of distribution in rat at 5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1588752 | Inhibition of recombinant human His-tagged MRCKalpha catalytic domain (1 to 473 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-13 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509667 | Metabolic stability in human liver microsomes assessed as half life incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
AID1551252 | Half life in rat | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1915550 | Inhibition of MSK1 (unknown origin) at 1 uM relative to control | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1509672 | Metabolic stability in human liver microsomes assessed as intrinsic clearance rate per mg protein incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1909275 | Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 3 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.58%) | |||
AID1588789 | Inhibition of recombinant full length human GST-tagged PLK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1915552 | Antiproliferative activity against breast cancer cell line (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1509664 | Antiproliferative activity against human BxPC3 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588810 | Inhibition of recombinant full length human GST-tagged SIK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-25 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1737182 | Inhibition of CDK9/cyclin T1 (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1588624 | Inhibition of recombinant full length human His-tagged ARK5 expressed in baculovirus expression system at 0.1 uM using CHKtide peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1588718 | Inhibition of recombinant full length human GST-tagged IKKepsilon expressed in baculovirus expression system at 0.1 uM using serine/threonine-11 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382345 | Selectivity ratio of IC50 for CDK1 (unknown origin) to IC50 for CDK4 (unknown origin) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1382389 | Bioavailability in ICR mouse at 0.5 mg/kg, iv by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1588778 | Inhibition of recombinant full length human His-tagged PIM1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608535 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation in G0/G1 phase at 40 nM incubated for 36 hrs by propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588809 | Inhibition of recombinant human GST-tagged SGK3 catalytic domain (87 to 496 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382346 | Antiproliferative activity against human MDA-MB-468 cells after 96 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588755 | Inhibition of recombinant full length human GST-tagged MST1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608891 | Induction of apoptosis in human SiHa cells at 40 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
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. |
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. |
AID1551250 | Metabolic stability in rat microsomes assessed as parent compound remaining after 45 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1551243 | Metabolic stability in human microsomes assessed as parent compound remaining after 5 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588733 | Inhibition of tracer 236 binding to recombinant human His-tagged LIMK1 catalytic domain (285 to 638 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588768 | Inhibition of tracer 178 binding to recombinant full length human GST-tagged NLK expressed by baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1509654 | Antiproliferative activity against human HepG2 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1824399 | Antiproliferative activity against human U-266 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
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. |
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. |
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. |
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. |
AID1588639 | Inhibition of recombinant full length human His-tagged CDK1/CyclinB expressed in baculovirus expression system at 0.1 uM using serine/threonine-18 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588652 | Inhibition of recombinant full length human GST-tagged CDK6/CyclinD1 expressed in baculovirus expression system at 0.1 uM using Rb peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1588734 | Inhibition of recombinant human GST-tagged LRRK2 catalytic domain (970 to 2527 amino acids) expressed in baculovirus expression system at 0.1 uM using ERM (LRRKtide) peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1588628 | Inhibition of recombinant full length human His-tagged Aurora B expressed in baculovirus expression system at 0.1 uM using serine/threonine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374364 | Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1402379 | Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assay | |||
AID1588750 | Inhibition of recombinant human GST-tagged MLK1 catalytic domain (1 to 500 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1509674 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance rate per mg protein incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588766 | Inhibition of recombinant full length human GST-tagged NEK6 expressed in insect expression system at 0.1 uM using serine/threonine-22 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588666 | Inhibition of recombinant full length human GST-tagged CLK3 expressed in Baculovirus expression system at 0.1 uM using serine/threonine-18 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588804 | Inhibition of recombinant human GST-tagged RON catalytic domain (983 to 1400 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382358 | Inhibition of CDK4 in human COLO205 cells assessed as reduction in Rb protein phosphorylation at Ser780 residue after 24 hrs by immunoblotting method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1509675 | Metabolic stability in dog liver microsomes assessed as intrinsic clearance rate per mg protein incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1551242 | Metabolic stability in rat microsomes assessed as parent compound remaining after 0 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588780 | Inhibition of recombinant human GST-tagged PKCalpha expressed in insect expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551237 | Inhibition of wild-type human partial length DYRK1A (H129 to S509 residues) expressed in mammalian expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
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. |
AID1588821 | Inhibition of recombinant full length human GST-tagged TBK1 expressed in insect expression system at 0.1 uM using serine/threonine-5 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509657 | Antiproliferative activity against human NCI-N87 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
AID1382364 | Inhibition of human CDK6/Cyclin-D3 | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1608884 | Antiproliferative activity against human MDA-MB-231 cells at 40 nM assessed as reduction in cell viability incubated for 48 hrs by EdU staining based laser scanning confocal microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1824416 | Induction of apoptosis in human RPMI-8226 cells assessed as late apoptic cells at 1 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 2.85%) | |||
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. |
AID1915551 | Antiproliferative activity against non-small cell lung cancer cell line (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1588830 | Inhibition of recombinant human GST-tagged TPL2 catalytic domain (30 to 397 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588737 | Inhibition of recombinant full length human LYN at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588779 | Inhibition of recombinant human His-tagged PKA catalytic domain (1 to 351 residues) expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1424508 | Inhibition of CDK4 (unknown origin) | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Structural insights of cyclin dependent kinases: Implications in design of selective inhibitors. |
AID1588740 | Inhibition of recombinant full length human His-tagged MAPKAPK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588700 | Inhibition of recombinant full length human His-tagged FGR expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1239761 | Inhibition of CDK4/6 in human COLO205 cells assessed as inhibition of Rb phosphorylation after 24 hrs by propidium iodide staining-based laser-scanning fluorescence microplate cytometric analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1509616 | Inhibition of recombinant human full length N-terminal GST-tagged CDK2 (1 to 298 residues)/cyclin A2 (1 to 432 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE u | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1824411 | Induction of cell cycle arrest in human RPMI-8226 cells assessed as accumulation at G2 phase at 0.5 uM measured after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 27.79%) | |||
AID1588631 | Inhibition of recombinant full length human GST-tagged BRAF expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382344 | Antiproliferative activity against human COLO205 cells after 96 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1509665 | Antiproliferative activity against human LNCAP cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
AID1588767 | Inhibition of recombinant human GST-tagged NEK9 catalytic domain (347 to 732 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588692 | Inhibition of recombinant human GST-tagged EPHB3 catalytic domain (623 to 907 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588621 | Inhibition of recombinant full length human His-tagged AKT1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-06 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588741 | Inhibition of recombinant full length human GST-tagged MARK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-21 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382376 | Intrinsic clearance in human liver microsomes at 1.11 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
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. |
AID1608892 | Induction of apoptosis in human HeLa cells at 40 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
AID1509651 | Antiproliferative activity against human U251 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588815 | Inhibition of tracer 236 binding to recombinant full length human His-tagged STK33 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1509709 | Antitumor activity against human COLO205 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 25 mg/kg, po administered once daily for 13 days relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1588709 | Inhibition of recombinant full length human GST-tagged GSK3alpha expressed in baculovirus expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1608900 | Antitumor activity against human SiHa cells xenografted in NOD/SCID BALB/c mouse assessed as tumor growth inhibition at 40 mg/kg, po administered for 21 days | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1608922 | Antiangiogenic activity against human SiHa cells xenografted in NOD/SCID BALB/c mouse assessed as reduction in CD31 expression at 40 mg/kg, po measured after 21 days by hematoxylin and eosin staining based immunohistochemistry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1551212 | Inhibition of CDK2 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588659 | Inhibition of recombinant full length human GST-tagged CK1delta expressed in baculovirus expression system at 0.1 uM using serine/threonine-11 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382354 | Cell cycle arrest in human COLO205 cells assessed as accumulation at G0/G1 phase at 0.01 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 64.4%) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588699 | Inhibition of recombinant full length human His-tagged FES (FPS) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608514 | Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588643 | Inhibition of tracer 236 binding to recombinant human GST-tagged CDK16/cyclin Y catalytic domain (CDK16: 108 to end, Cyclin Y: 2 to end) expressed by baculovirus in Sf9 insect cells expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
AID1509658 | Antiproliferative activity against human NCI-H1975 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588825 | Inhibition of recombinant full length human His-tagged TSSK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588625 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged ASK1 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1608541 | Induction of cell cycle arrest in human SiHa cells assessed as accumulation in G0/G1 phase at 80 nM incubated for 36 hrs by propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
AID1382359 | Inhibition of CDK4 in human COLO205 cells assessed as reduction in total Rb protein level at 0.1 to 10 uM after 24 hrs by immunoblotting method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
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. |
AID1824414 | Induction of apoptosis in human RPMI-8226 cells assessed as viable cells at 1 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 91.6%) | |||
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. |
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. |
AID1588781 | Inhibition of recombinant full length human GST-tagged PKCbeta1 expressed in insect expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
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. |
AID1374355 | Inhibition of recombinant human full length CDK6 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1588636 | Inhibition of recombinant full length human His-tagged BRK expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551247 | Metabolic stability in human microsomes assessed as parent compound remaining after 30 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1366693 | Antiproliferative activity against human COLO205 cells after 96 hrs by CCK-8 assay | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. |
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. |
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. |
AID1239762 | Inhibition of CDK4/6 in human COLO205 cells assessed as maximum cell cycle arrest at G1 phase after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer 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. |
AID1588758 | Inhibition of recombinant full length human GST-tagged MST4 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1849048 | Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
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. |
AID1588784 | Inhibition of recombinant full length human His-tagged PKCeta expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588788 | Inhibition of recombinant full length human His-tagged PLK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-16 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608881 | Inhibition of colony formation in human HeLa cells at 80 nM incubated for 5 days by crystal violet staining based light microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
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. |
AID1374354 | Inhibition of CDK4 (unknown origin) after 90 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1509659 | Antiproliferative activity against human NCI-H1993 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588629 | Inhibition of recombinant full length human GST-tagged AXL expressed in insect expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1374361 | MRT in rat at 5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
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. |
AID1588802 | Inhibition of recombinant full length human GST-tagged RSK3 expressed in insect expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588717 | Inhibition of recombinant full length human GST-tagged IKKbeta expressed in baculovirus expression system at 0.1 uM using serine/threonine-5 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588698 | Inhibition of recombinant human His-tagged FGFR4 catalytic domain (781 to 1338 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588676 | Inhibition of recombinant full length human GST-tagged DCAMKL2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-17 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588729 | Inhibition of recombinant full length human GST-tagged JNK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608893 | Induction of apoptosis in human SiHa cells assessed as decrease in Bcl2 expression at 80 nM incubated for 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1608879 | Inhibition of colony formation in human T47D cells at 40 nM incubated for 5 days by crystal violet staining based light microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588774 | Inhibition of recombinant human GST-tagged PDGFRalpha (550 to 1089 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1509684 | AUC (0 to t) in BALB/c mouse at 3 mg/kg, iv measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588797 | Inhibition of tracer 178 binding to recombinant human His-tagged RIPK2 catalytic domain (1 to 299 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1824413 | Induction of cell cycle arrest in human RPMI-8226 cells assessed as accumulation at G2 phase at 1 uM measured after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 27.79%) | |||
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. |
AID1509656 | Antiproliferative activity against human SNU5 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1737230 | Inhibition of CDK7/cyclin H (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1382384 | Cmax in ICR mouse at 0.5 mg/kg, iv by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1382355 | Cell cycle arrest in human COLO205 cells assessed as accumulation at G0/G1 phase at 0.1 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 64.4%) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588746 | Inhibition of recombinant human GST-tagged MELK catalytic domain (1 to 340 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-17 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509671 | Metabolic stability in monkey liver microsomes assessed as half life incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1737181 | Selectivity ratio of IC50 for inhibition of CDK2/cyclin A2 (unknown origin) to IC50 for inhibition of recombinant human full-length N-terminal GST-fused CDK4 (1 to 303 residues)/GST-tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression s | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
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. |
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. |
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. |
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. |
AID1915549 | Inhibition of IKKa (unknown origin) at 1 uM relative to control | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1317331 | Inhibition of recombinant full length human N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintilla | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
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. |
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. |
AID1588756 | Inhibition of recombinant full length human GST-tagged MST2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1317353 | Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1513682 | Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
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. |
AID1588587 | Efflux ratio in gMDCKI cells expressing human MDR1 | |||
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. |
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. |
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. |
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. |
AID1513681 | Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
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. |
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. |
AID1551215 | Inhibition of CDK6 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588664 | Inhibition of recombinant human GST-tagged CLK1 catalytic domain (129 to 484 residues) expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1915587 | Inhibition of Cdk4 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1588829 | Inhibition of recombinant human GST-tagged TIE2 (817 to 1101 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-5 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509689 | AUC (0 to t) in BALB/c mouse at 10 mg/kg, po measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
AID1588846 | Unbound brain to plasma ratio in Sprague-Dawley rat at 30 mg/kg, po after 48 hrs by LC-MS/MS analysis | |||
AID1551249 | Metabolic stability in human microsomes assessed as parent compound remaining after 45 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
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. |
AID1509683 | Cmax in BALB/c mouse at 3 mg/kg, iv measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1509620 | Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588722 | Inhibition of recombinant full length human GST-tagged ITK expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588713 | Inhibition of recombinant full length human GST-tagged HIPK4 expressed in baculovirus expression system at 0.1 uM using serine/threonine-18 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1239759 | Inhibition of human CDK4/cyclin D1 expressed in insect cells assessed as phosphorylation of CTRF after 50 mins by microplate scintillation counter | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
AID1909277 | Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 3 uM measured after 48 hrs by Annexin V-FITC/PI staining based flow cytometric analysis (Rvb = 0.32%) | |||
AID1588693 | Inhibition of recombinant human His-tagged ERBB2 catalytic domain (676 to 1255 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588826 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged TTK expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
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. |
AID1366701 | Antitumor activity against human COLO205 cells xenografted in nude BALB/c mouse assessed as tumor volume at 100 mg/kg, po administered once daily for 3 weeks measured twice per week relative to control | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. |
AID1737185 | Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1277156 | Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
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. |
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. |
AID1588702 | Inhibition of recombinant human His-tagged FLT3 catalytic domain (564 to 958 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1509687 | Clearance in BALB/c mouse at 3 mg/kg, iv measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588754 | Inhibition of recombinant full length human GST-tagged MSSK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-18 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1513743 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 0.03 to 0.8 uM after 24 hrs by propidium iodide-staining based flow cytometry | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
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. |
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. |
AID1732687 | Inhibition of CDK1/cyclin B1 (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors. |
AID1588670 | Inhibition of recombinant full length human His-tagged CAMK1 expressed in baculovirus expression system at 0.1 uM using ZIPtide peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
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. |
AID1588632 | Inhibition of recombinant full length human His-tagged BTK expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1382398 | Antitumor activity against human COLO205 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 25 mg/kg, po administered once daily for 21 days relative to control | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1551238 | Inhibition of wild-type human partial length PIM1 (A15 to K313 residues) expressed in bacterial expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
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. |
AID1382374 | Half life in mouse liver microsomes at 1.11 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
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. |
AID1824426 | Induction of apoptosis in human RPMI-8226 cells assessed as viable cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 91.6%) | |||
AID1588748 | Inhibition of recombinant full length human GST-tagged MKNK1 expressed in insect expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588739 | Inhibition of recombinant full length human His-tagged MAPKAPK2 expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1317332 | Inhibition of human CDK2/cyclin E | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1588653 | Inhibition of recombinant full length human His-tagged CDK7/CyclinH/MAT1 expressed in baculovirus expression system at 0.1 uM using CDK7/9tide peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
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. |
AID1588710 | Inhibition of recombinant full length human His-tagged GSK3beta expressed in baculovirus expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509615 | Inhibition of recombinant human full length N-terminal GST-tagged CDK6 (1 to 326 residues)/cyclin D3 (1 to 292 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE u | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
AID1588667 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged CLK4 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588681 | Inhibition of recombinant full length human GST-tagged DYRK1A expressed in baculovirus expression system at 0.1 uM using serine/threonine-18 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588611 | Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay | |||
AID1588626 | Inhibition of recombinant full length human His-tagged ABL1 expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
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. |
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. |
AID1588843 | Inhibition of recombinant full length human His-tagged p38delta expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1509668 | Metabolic stability in mouse liver microsomes assessed as half life incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1909315 | Inhibition of SHP2 (unknown origin) using DiFMUP as substrate at 10 uM incubated for 60 mins followed by substrate addition for 30 mins by microplate reader method | |||
AID1588635 | Inhibition of recombinant full length human GST-tagged BRSK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-21 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588712 | Inhibition of recombinant full length human GST-tagged HIPK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588822 | Inhibition of tracer 178 binding to recombinant full length human His-tagged TEC expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
AID1588786 | Inhibition of recombinant full length human PKCzeta expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588686 | Inhibition of recombinant full length human GST-tagged ERK2 expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382387 | Apparent volume of distribution in ICR mouse at 0.5 mg/kg, iv by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588687 | Inhibition of recombinant human GST-tagged EPHA1 (568 to 976 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608882 | Antiproliferative activity against human T47D cells assessed as reduction in cell viability at 40 nM incubated for 48 hrs by EdU staining based laser scanning confocal microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1509685 | Half life in BALB/c mouse at 3 mg/kg, iv measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
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. |
AID1608569 | Toxicity in NOD/SCID BALB/c mouse xenografted with human SiHa cells assessed as body weight at 40 mg/kg, po administered for 21 days | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
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. |
AID1382365 | Inhibition of human CDK9/Cyclin-T1 | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588725 | Inhibition of recombinant human GST-tagged JAK2 catalytic domain (809 to 1153+9 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE 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. |
AID1588793 | Inhibition of recombinant full length human GST-tagged PHKG1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1909273 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in S phase at 3 uM incubated for 48 hrs by RNase/propidium iodide staining based flow cytometry analysis (Rvb = 71.1%) | |||
AID1588791 | Inhibition of recombinant full length human His-tagged PRAK expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588612 | Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay | |||
AID1588824 | Inhibition of tracer 236 binding to recombinant human GST-tagged TNK2 catalytic domain (110 to 476 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
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. |
AID1382377 | Intrinsic clearance in mouse liver microsomes at 1.11 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588842 | Inhibition of recombinant full length human His-tagged p38beta expressed in baculovirus expression system at 0.1 uM using serine/threonine-15 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588812 | Inhibition of recombinant full length human GST-tagged SPHK1 expressed in baculovirus expression system at 0.1 uM using Sphingosine Lipid as substrate incubated for 60 mins by Adapta assay relative to control | |||
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. |
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. |
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. |
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. |
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. |
AID1509670 | Metabolic stability in dog liver microsomes assessed as half life incubated for 10 mins followed by NADPH addition and further incubated for 1 hr by LC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588828 | Inhibition of recombinant human GST-tagged TYK2 catalytic domain (833 to 1187 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1608564 | Induction of apoptosis in human T47D cells assessed as decrease in Bcl2 expression at 40 nM incubated for 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588724 | Inhibition of recombinant human GST-tagged JAK1 catalytic domain (866 to 1154 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588669 | Inhibition of recombinant full length human His-tagged CSK expressed in Escherichia coli expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588776 | Inhibition of recombinant full length human GST-tagged PI3Kalpha expressed in baculovirus expression system at 0.1 uM using PI Lipid Kinase as substrate incubated for 60 mins by Adapta assay relative to control | |||
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. |
AID1684534 | Antiproliferative activity against human MIA PaCa-2 cells assessed as inhibition of cell growth by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 33 | Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells. |
AID1608563 | Induction of apoptosis in human MDA-MB-231 cells assessed as decrease in Bcl2 expression at 40 nM incubated for 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1402372 | Unbound brain to plasma concentration ratio in mouse at 30 mg/kg, po | |||
AID1317308 | Inhibition of CDK9/cyclin T (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
AID1588689 | Inhibition of tracer 236 binding to recombinant human His-tagged EPHA7 (579 to 998 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
AID1608513 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
AID1509662 | Antiproliferative activity against human CFPAC-1 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588763 | Inhibition of recombinant human GST-tagged MUSK (519 to 869 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1382386 | Elimination half life in ICR mouse at 0.5 mg/kg, iv by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588760 | Inhibition of recombinant human GST-tagged MER (578 to 872 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588613 | Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay | |||
AID1588839 | Inhibition of recombinant full length human GST-tagged EEF2K expressed in Escherichia coli expression system at 0.1 uM using serine/threonine-24 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1277158 | Inhibition of CDK4/Cyclin D1 (unknown origin) using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
AID1588714 | Inhibition of recombinant full length human His-tagged HYL expressed in Escherichia coli expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588794 | Inhibition of recombinant full length human GST-tagged PHKG2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374353 | Inhibition of recombinant human full length CDK1/Cyclin D3 expressed in baculovirus infected Sf9 insect cells using histone H1 substrate after 90 mins by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1366691 | Inhibition of CDK4 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. |
AID1588675 | Inhibition of recombinant human GST-tagged DAPK1 catalytic domain (1 to 363 residues) expressed in baculovirus expression system at 0.1 uM using ZIPtide peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1551240 | Inhibition of wild-type human full length CAMK1A (M1 to L370 residues) expressed in bacterial expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588723 | Inhibition of recombinant human GST-tagged INSR (1011 to 1382 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374356 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by DAPI staining based assay | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1588808 | Inhibition of recombinant human GST-tagged SGK2 catalytic domain (54 to 427 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509618 | Antiproliferative activity against human T47D cells assessed as reduction in cell growth incubated for 4 to 6 days by cell titer-glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588642 | Inhibition of tracer 236 binding to recombinant human GST-tagged CDK14/cyclin Y catalytic domain (CDK14: full length, Cyclin Y: 2 to end) expressed by baculovirus in Sf9 insect cells expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
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. |
AID1588792 | Inhibition of recombinant full length human GST-tagged PRK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1732739 | Inhibition of human CDK4/cyclin D (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors. |
AID1588799 | Inhibition of recombinant human GST-tagged ROCK2 catalytic domain (1 to 552 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-13 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374360 | Half life in rat at 5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1588657 | Inhibition of recombinant full length human His-tagged CHK2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-07 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588704 | Inhibition of recombinant full length human GST-tagged FRK expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1909274 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in G2/M phase at 3 uM incubated for 48 hrs by RNase/propidium iodide staining based flow cytometry analysis (Rvb = 2.7%) | |||
AID1588759 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged MYLK expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588745 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged MEKK2 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
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. |
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. |
AID1588614 | Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay | |||
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. |
AID1588648 | Inhibition of tracer 236 binding to recombinant human GST-tagged CDK3/CyclinE1 expressed by baculovirus in Sf9 insect cells expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588762 | Inhibition of recombinant human GST-tagged MINK1 catalytic domain (1 to 320 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588720 | Inhibition of recombinant full length human His-tagged IRAK4 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1909255 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
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. |
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. |
AID1909258 | Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
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. |
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. |
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. |
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. |
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. |
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. |
AID1737179 | Cell cycle arrest in human COLO 205 cells assessed as accumulation at G0/G1 phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry relative to control | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1551241 | Metabolic stability in human microsomes assessed as parent compound remaining after 0 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1551227 | Tmax in human | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588819 | Inhibition of tracer 222 binding to recombinant human His-tagged TAK1-TAB1 catalytic domain (437 to 504 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1653034 | Inhibition of CDK4 (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Recent development of CDK inhibitors: An overview of CDK/inhibitor co-crystal structures. |
AID1588645 | Inhibition of recombinant full length human GST-tagged CDK18/Cyclin Y (2 to end amino acids) expressed in insect expression system at 0.1 uM using serine/threonine-12 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588622 | Inhibition of recombinant full length human His-tagged AKT2 expressed in baculovirus expression system at 0.1 uM using serine/threonine-06 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608883 | Antiproliferative activity against human SiHa cells assessed as reduction in cell viability at 80 nM incubated for 48 hrs by EdU staining based laser scanning confocal microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1402563 | Antiproliferative activity against human U87MG cells after 72 hrs by DAPI staining based assay | |||
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. |
AID1849071 | Induction of cell cycle arrest in human T47D cells assessed as accumulation of cells at G2 phase at 1.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 16.57%) | |||
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. |
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. |
AID1588658 | Inhibition of recombinant full length human GST-tagged CK1alpha1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-11 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1824402 | Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1382388 | Clearance in ICR mouse at 0.5 mg/kg, iv by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1509663 | Antiproliferative activity against human PANC1 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1608878 | Inhibition of colony formation in human MDA-MB-231 cells at 40 nM incubated for 5 days by crystal violet staining based light microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1824427 | Induction of apoptosis in human RPMI-8226 cells assessed as early apoptic cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 3.38%) | |||
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. |
AID1608877 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability at 80 nM incubated for 48 hrs by EdU staining based laser scanning confocal microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588656 | Inhibition of recombinant full length human His-tagged CHK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-19 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509708 | Antitumor activity against human MCF7 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 50 mg/kg, po administered once daily for 19 days relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1824429 | Induction of apoptosis in human RPMI-8226 cells assessed as necrotic cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 2.21%) | |||
AID1588730 | Inhibition of recombinant human His-tagged KDR (789 to 1356 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1588744 | Inhibition of recombinant full length human GST-tagged MEK3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
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. |
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. |
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. |
AID1551213 | Inhibition of CDK4 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588818 | Inhibition of recombinant full length human GST-tagged SYK expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551244 | Metabolic stability in rat microsomes assessed as parent compound remaining after 5 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1737184 | Inhibition of human full-length N-terminal GST tagged CDK6 (1 to 326 residues)/GST-tagged cyclinD3 (1 to 292 residues) expressed in baculovirus expression system using ULight-elF4E-binding protein 1 peptide as substrate measured after 30 mins by LANCE ass | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1509652 | Antiproliferative activity against human K562 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588685 | Inhibition of recombinant human GST-tagged EGFR T790M/L858R mutant (668 to 1210: T790M/L858R residues)expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588837 | Inhibition of recombinant full length human His-tagged ZAP70 expressed in baculovirus expression system at 0.1 uM using tyrosine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588610 | Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay | |||
AID1824401 | Antiproliferative activity against human HL-60 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
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. |
AID1366692 | Inhibition of CDK1 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. |
AID1588633 | Inhibition of recombinant full length human His-tagged BLK expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1382373 | Half life in human liver microsomes at 1.11 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1737183 | Inhibition of recombinant human full-length N-terminal GST-fused CDK4 (1 to 303 residues)/GST-tagged CyclinD3 (1 to 292 residues) expressed in baculovirus expression system using ULight-elF4E-binding protein 1 peptide as substrate measured after 30 mins b | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
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. |
AID1909256 | Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
AID1648276 | Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | |||
AID1608538 | Induction of cell cycle arrest in human T47D cells assessed as accumulation in G0/G1 phase at 40 nM incubated for 36 hrs by propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588772 | Inhibition of recombinant full length human His-tagged PAK6 expressed in baculovirus expression system at 0.1 uM using serine/threonine-20 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588848 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged MYLK3 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1608894 | Induction of apoptosis in human HeLa cells assessed as decrease in Bcl2 expression at 80 nM incubated for 48 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588691 | Inhibition of recombinant human GST-tagged EPHB1 catalytic domain (613 to 881 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1876328 | Antiviral activity against SARS-CoV-2 inoculated in african green monkey Vero E6 cells expressing ACE2 assessed as reduction of cytopathic effect measured after 72 hrs by CellTitre-Glo based plate reader method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
AID1588727 | Inhibition of recombinant full length human His-tagged JNK1alpha1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1876254 | Cytotoxicity against african green monkey Vero cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
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. |
AID1588816 | Inhibition of recombinant full length human His-tagged SRC expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1551217 | Inhibition of CDK9 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
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. |
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. |
AID1374362 | Apparent clearance in rat at 5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1588683 | Inhibition of recombinant full length human GST-tagged DYRK4 expressed in baculovirus expression system at 0.1 uM using serine/threonine-9 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
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. |
AID1909272 | Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in G0/G1 phase at 3 uM incubated for 48 hrs by RNase/propidium iodide staining based flow cytometry analysis (Rvb = 26.2%) | |||
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. |
AID1588680 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged DRAK1 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1513678 | Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
AID1588678 | Inhibition of tracer 236 binding to recombinant full length human GST-tagged DMPK expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588833 | Inhibition of tracer 178 binding to recombinant full length human GST-tagged WEE1 expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1509706 | Antitumor activity against human COLO205 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 25 mg/kg, po administered once daily for 13 days relative to control | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588769 | Inhibition of recombinant full length human GST-tagged PAK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-19 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1608880 | Inhibition of colony formation in human SiHa cells at 80 nM incubated for 5 days by crystal violet staining based light microscopy | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
AID1876253 | Antiviral activity against SARS-CoV-2 infected in african green monkey Vero cells incubated for 72 hrs by celltitre-glo luminescent assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinase Inhibitors as Underexplored Antiviral Agents. |
AID1849050 | Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
AID1732740 | Inhibition of human CDK2/cyclin E (unknown origin) using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors. |
AID1509660 | Antiproliferative activity against human NCI-H358 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
AID1588761 | Inhibition of recombinant human His-tagged MET (956 to 1390 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-6 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1824415 | Induction of apoptosis in human RPMI-8226 cells assessed as early apoptic cells at 1 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 3.38%) | |||
AID1849061 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation of cells at G2 phase at 1.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 29.66%) | |||
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. |
AID1737186 | Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition measured after 4 to 6 days by celltiter-glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
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. |
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. |
AID1588697 | Inhibition of recombinant human His-tagged FGFR3 catalytic domain (399 to 806 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1824400 | Antiproliferative activity against human K562 cells assessed as growth inhibition measured after 72 hrs by CCK8 assay | |||
AID1509650 | Antiproliferative activity against human U87MG cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1737229 | Inhibition of CDK2/cyclin A2 (unknown origin) | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors. |
AID1509614 | Inhibition of recombinant human full length N-terminal GST-tagged CDK4 (1 to 303 residues)/cyclin D3 (1 to 292 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE u | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
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. |
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. |
AID1608511 | Inhibition of recombinant full length human CDK4/Cyclin D3 using Rb-fragmen as substrate at 1 uM incubated for 40 mins by [gamma-33P]-ATP based radiometric assay relative to control | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588834 | Inhibition of tracer 1710 binding to recombinant human His-tagged WNK2 catalytic domain (166 to 489 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
AID1588785 | Inhibition of recombinant full length human His-tagged PKCtheta expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588688 | Inhibition of tracer 236 binding to recombinant human His-tagged EPHA3 (569 to 976 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588684 | Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-4 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588623 | Inhibition of tracer 236 binding to recombinant human GST-tagged ALK2 catalytic domain (145 to 509 residues) expressed in baculovirus at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588844 | Inhibition of recombinant full length human His-tagged p38gamma expressed in baculovirus expression system at 0.1 uM using serine/threonine-3 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588823 | Inhibition of tracer 178 binding to recombinant human GST-tagged TGFBR1 catalytic domain (200 to 503 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
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. |
AID1588690 | Inhibition of recombinant human GST-tagged EPHA8 catalytic domain (565 to 1005 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588738 | Inhibition of recombinant human GST-tagged MAP4K4 catalytic domain (1 to 328 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509688 | Cmax in BALB/c mouse at 10 mg/kg, po measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588630 | Inhibition of tracer 178 binding to recombinant human GST-tagged BMPR1A catalytic domain (187 to 532 amino acids) expressed insect cell expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
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. |
AID1876332 | Antiviral activity against SARS-CoV-2 inoculated in african green monkey Vero E6 cells expressing ACE2 assessed as reduction of cytopathic effect measured after 72 hrs by CellTitre-Glo based plate reader method relative to control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
AID1588806 | Inhibition of recombinant human GST-tagged RSE catalytic domain (451 to 890 residues) expressed in baculovirus expression system at 0.1 uM using tyrosine-2 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1509661 | Antiproliferative activity against human H441 cells | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1588649 | Inhibition of recombinant full length human GST-tagged CDK4/Cyclin D1 expressed in baculovirus expression system at 0.1 uM using Rb peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1277159 | Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
AID1509691 | Oral bioavailability in BALB/c mouse at 10 mg/kg measured upto 1440 mins by UPLC-MS/MS analysis | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer. |
AID1551216 | Inhibition of CDK7 (unknown origin) | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1382343 | Inhibition of human CDK1/Cyclin-B using ULight-substrate after 1 hr by LANCE assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1824417 | Induction of apoptosis in human RPMI-8226 cells assessed as necrotic cells at 1 uM measured after 24 hrs by Annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 2.21%) | |||
AID1849068 | Induction of cell cycle arrest in human T47D cells assessed as accumulation of cells at G1 phase at 1.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 69.55 %) | |||
AID1588641 | Inhibition of tracer 236 binding to human GST/His-tagged CDK13/Cyclin K at 0.1 uM | |||
AID1608516 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
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. |
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. |
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. |
AID1551246 | Metabolic stability in rat microsomes assessed as parent compound remaining after 15 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588773 | Inhibition of recombinant human GST-tagged PASK catalytic domain (879 to 1323 residues) expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1374365 | Inhibition of recombinant human N-terminal GST-tagged CDK4 (M1 to A326 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells using Rb protein (773 to 928 residues) as substrate in presence of [33P]-ATP by scintillation counting method | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1849047 | Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | |||
AID1824410 | Induction of cell cycle arrest in human RPMI-8226 cells assessed as accumulation at G1 phase at 0.5 uM measured after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 41.96%) | |||
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. |
AID1551248 | Metabolic stability in rat microsomes assessed as parent compound remaining after 30 mins | 2019 | European journal of medicinal chemistry, Jun-15, Volume: 172 | Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. |
AID1588654 | Inhibition of tracer 236 binding to recombinant full length human His-tagged CDK8/cyclin C expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
AID1366690 | Inhibition of CDK6 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors. |
AID1382375 | Intrinsic clearance in rat liver microsomes at 1.11 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588835 | Inhibition of recombinant full length human GST-tagged YSK1 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1317329 | Inhibition of recombinant human N-terminal GST-tagged CDK4 (4 to 303 residues)/cyclin D1 (4 to 295 residues) expressed in sf9 cells using C-terminal retinoblastoma fragment as substrate after 90 mins by [gamma-33P]ATP based microbeta scintillation countin | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1608890 | Induction of apoptosis in human T47D cells at 40 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1239764 | Competitive inhibition of CDK6/cyclin D3 (unknown origin) assessed as phosphorylation of CTRF after 50 mins by Michaelis-Menten plot analysis in presence of ATP | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. |
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. |
AID1382391 | AUClast in ICR mouse at 1 mg/kg, po via gavage by HPLC analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy. |
AID1588716 | Inhibition of recombinant full length human His-tagged IKKalpha expressed in baculovirus expression system at 0.1 uM incubated for 60 mins by Adapta assay relative to control | |||
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. |
AID1374358 | Cmax in rat at 5 mg/kg | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity |
AID1608544 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation in G0/G1 phase at 80 nM incubated for 36 hrs by propidium iodide staining based flow cytometry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis. |
AID1588817 | Inhibition of recombinant full length human GST-tagged SRM expressed in baculovirus expression system at 0.1 uM using tyrosine-1 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
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. |
AID1588677 | Inhibition of tracer 178 binding to recombinant human GST-tagged DDR1 catalytic domain (440 to 876 residues) expressed in baculovirus expression system at 0.1 uM measured after 60 mins by Lanthascreen assay relative to control | |||
AID1588719 | Inhibition of recombinant human GST-tagged IRAK1 catalytic domain (194 to 712 residues) expressed in baculovirus expression system at 0.1 uM using Histone H3 (1-20) peptide as substrate incubated for 60 mins by Adapta assay relative to control | |||
AID1588620 | Inhibition of tracer 178 binding to recombinant human GST-tagged ACVR2B catalytic domain (185 to 488 residues) expressed in baculovirus at 0.1 uM measured after 60 mins by Lanthascreen assay | |||
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. |
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. |
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. |
AID1588757 | Inhibition of recombinant full length human GST-tagged MST3 expressed in baculovirus expression system at 0.1 uM using serine/threonine-7 peptide as substrate incubated for 60 mins by Z'-LYTE assay relative to control | |||
AID1588615 | Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay | |||
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. |
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. |
AID1868085 | Inhibition of CDK4/cyclin D (unknown origin) | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. |
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. |
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. |
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. |
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. |
AID1345601 | Human cyclin dependent kinase 4 (CDK4 subfamily) | 2014 | Investigational new drugs, Oct, Volume: 32, Issue:5 | Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. |
AID1345613 | Human cyclin dependent kinase 6 (CDK4 subfamily) | 2014 | Investigational new drugs, Oct, Volume: 32, Issue:5 | Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 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. |
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. |
AID1804171 | DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\ | 2020 | Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7 | Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs. |
[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 | 0 (0.00) | 29.6817 |
2010's | 117 (33.52) | 24.3611 |
2020's | 232 (66.48) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (87.49) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 43 (12.22%) | 5.53% |
Reviews | 77 (21.88%) | 6.00% |
Case Studies | 20 (5.68%) | 4.05% |
Observational | 8 (2.27%) | 0.25% |
Other | 204 (57.95%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |