PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9884685 |
| CHEMBL ID | 573339 |
| CHEBI ID | 90524 |
| SCHEMBL ID | 258242 |
| MeSH ID | M0513765 |
| Synonym |
|---|
| HY-10115 |
| 3-(4-morpholin-4-ylpyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol |
| 3-(4-morpholin-4-ylpyrido[3 ,2 :4,5]furo[3,2-d]pyrimidin-2-yl)phenol |
| 3-[4-(4-morpholinyl)-2-pyrido[2,3]furo[2,4-b]pyrimidinyl]phenol |
| mtor inhibitor, pi103 |
| 3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2,4,6,10,12-hexaen-4-yl]phenol |
| cid_9884685 |
| pyridofuropyrimidine derivative, 2 |
| bdbm25045 |
| 3-(4-morpholinopyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol |
| pi-103 , |
| 3-(4-(4-morpholinyl)pyrido[3?,2?:4,5]furo[3,2-d]pyrimidin-2- yl)phenol |
| HMS3229C15 |
| chebi:90524 , |
| CHEMBL573339 |
| 3-(4-morpholin-4-ylpyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol |
| x6k , |
| KINOME_3597 |
| NCGC00187906-03 |
| NCGC00187906-01 |
| pi103 |
| pi 103 |
| 3-(4-morpholinopyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl)phenol |
| CCG-101301 |
| 3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(13),2,4,6,9,11-hexaen-4-yl]phenol |
| HMS3244F11 |
| HMS3244E12 |
| HMS3244E11 |
| 371935-74-9 |
| BCPP000107 |
| NCGC00187906-02 |
| CS-0127 |
| S1038 |
| pik 103 |
| gtpl5701 |
| BRD-K67868012-003-01-5 |
| compound 2 [pmid: 17601739] |
| SCHEMBL258242 |
| MLS006010988 |
| smr002530603 |
| pik-103 |
| phenol, 3-(4-(4-morpholinyl)pyrido(3',2':4,5)furo(3,2-d)pyrimidin-2-yl)- |
| unii-yqx02f616f |
| yqx02f616f , |
| 2X6K |
| phenol, 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]- |
| 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol |
| AC-31514 |
| AKOS024462563 |
| HMS3650M10 |
| 4L23 |
| 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl] |
| mfcd11983145 |
| 3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol |
| DTXSID40190676 |
| EX-A039 |
| HMS3654E09 |
| TUVCWJQQGGETHL-UHFFFAOYSA-N |
| 3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl]phenol |
| SW218117-2 |
| 3-(6-morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl)phenol |
| FT-0712341 |
| pi 103 hydrobromide |
| BCP19373 |
| 371935-74-9 (free base) |
| Q27088379 |
| AS-16221 |
| sr-01000946304 |
| SR-01000946304-1 |
| pi-103 hydrobromide |
| BCP01923 |
| AMY23717 |
| HMS3295E19 |
| nsc759676 |
| nsc-759676 |
| NCGC00187906-15 |
| pi 3-k inhibitor v |
| nsc-776996 |
| pi-103 hcl |
| nsc776996 |
PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha, p110beta, and p110delta.
| Excerpt | Reference | Relevance |
|---|---|---|
| "PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (2 nmol/L), p110beta (3 nmol/L), p110delta (3 nmol/L), and p110gamma (15 nmol/L)." | ( Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. Ahmad, Z; Alix, S; Bjerke, LM; Clarke, PA; de Haven Brandon, A; Di-Stefano, F; Eccles, S; Gowan, S; Guillard, S; Hayakawa, M; Hayes, A; Henley, A; Kaizawa, H; Kelland, L; Koizumi, T; Nutley, B; Ohishi, T; Parker, P; Patel, S; Patterson, L; Raynaud, FI; Saghir, N; Valenti, M; Waterfield, M; Workman, P, 2007) | 1.06 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "On treatment with PI103 or Ku-0063794, only the PIK3CA mutant cells displayed increased resistance in LG conditions." | ( Increased drug resistance is associated with reduced glucose levels and an enhanced glycolysis phenotype. Beloueche-Babari, M; Bhattacharya, B; Kamal Mustapa, N; Koh, KX; Loh, J; Low, SH; Soh, C; Soong, R, 2014) | 0.73 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Our results suggest that PI-103 in combination with DNR may be a potent and less toxic therapy for targeting LSCs and deserve further preclinical and clinical studies in the treatment of AML." | ( PI-103 sensitizes acute myeloid leukemia stem cells to daunorubicin-induced cytotoxicity. Chen, Y; Ding, Q; Gu, R; Liang, J; Zhang, X, 2013) | 0.39 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " p110alpha inhibitors blocked phosphorylation of both protein kinase B/Akt and S6 in all cell lines examined, effectively decreased cellular proliferation, and produced additive cytotoxic effects in combination with radiation therapy." | ( Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Chen, JS; Donker, M; Entin-Meer, M; Haas-Kogan, D; Knight, ZA; Shokat, KM; Stokoe, D; Weiss, W; Yang, X; Zhou, LJ, 2008) | 0.35 |
| " Therefore, we hypothesized the improved anticancer efficacy of QUE in combination with isoenzyme inhibitors-rottlerin (ROT-PKCδ inhibitor), G0 6983 (PKCα inhibitor), and PI-103 (p110α-class I PI3K inhibitor) in MCF-7 and RAW 264." | ( Improved synergistic anticancer efficacy of quercetin in combination with PI-103, rottlerin, and G0 6983 against MCF-7 and RAW 264.7 cells. Maurya, AK; Vinayak, M, 2019) | 0.51 |
| " Herein, we utilized near-infrared dye IR820 nanobubbles (NBs) combined with a dual PI3K/mTOR inhibitor PI-103 for the SDT treatment of hepatocellular carcinoma (HCC) in vitro." | ( Synergistic Anticancer Strategy of Sonodynamic Therapy Combined with PI-103 Against Hepatocellular Carcinoma. Cheng, W; Han, X; Jing, H; Tan, H; Yang, H, 2021) | 0.62 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Preclinical effects of the novel orally bioavailable HSP90 inhibitor NVP-HSP990 on the viability, apoptosis and client protein levels of MM cells (established cell lines and clinical specimens) were tested alone and in combination with other drugs." | ( Preclinical activity of the novel orally bioavailable HSP90 inhibitor NVP-HSP990 against multiple myeloma cells. Bargou, RC; Bumm, T; Chatterjee, M; Einsele, H; Gao, Z; Grella, E; Iskandarov, K; Jensen, MR; Stühmer, T, 2012) | 0.38 |
| "Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule." | ( Highly predictive and interpretable models for PAMPA permeability. Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017) | 0.46 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| " To improve the bioavailability of PI-103, we designed and synthesized a PI-103 bioisostere, PI-103BE (9) in which the phenolic hydroxyl group of PI-103 was replaced by a boronate, a structural modification known to enhance bioavailability of molecules containing phenolic hydroxyl moieties." | ( Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. Guo, S; He, L; Luo, L; Wang, G; Zhang, C; Zhang, Q; Zheng, S; Zhong, Q, 2020) | 0.56 |
| Role | Description |
|---|---|
| EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | An inhibitor of phosphatidylinositol 3-kinase, EC 2.7.1.137, a family of related enzymes capable of phosphorylating the 3 position hydroxy group of the inositol ring of a phosphatidylinositol. |
| mTOR inhibitor | A protein kinase inhibitor of the mammalian target of rapamycin (mTOR), a protein that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis and transcription. mTOR inhibitors are used to prevent transplant rejection and in treatment of cancer. |
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| morpholines | Any compound containing morpholine as part of its structure. |
| phenols | Organic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring. |
| organic heterotricyclic compound | An organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms. |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| aromatic amine | An amino compound in which the amino group is linked directly to an aromatic system. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fumarate hydratase | Homo sapiens (human) | Potency | 2.7041 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| PPM1D protein | Homo sapiens (human) | Potency | 0.2082 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.4041 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| polyprotein | Zika virus | Potency | 2.7041 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| Interferon beta | Homo sapiens (human) | Potency | 0.2082 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4 | Navigating the kinome. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
| AID720479 | Millipore: Percentage of residual kinase activity of PRKCG at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1568316 | Inhibition of recombinant human full length N-terminal GST-tagged PI3Kalpha (1 to 1068 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 1 hr by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID720124 | Millipore: Percentage of residual kinase activity of EPHA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1464027 | Inhibition of human DNA-PK catalytic subunit using DNA and [EPPLSQEAFADLWKK] peptide substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20 | Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation. |
| AID1294639 | Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide substrate incubated for 1 hr by TR-FRET assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720294 | Millipore: Percentage of residual kinase activity of TGFBR1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1481071 | Inhibition of human BTK using KVEKIGEGTYGVVYK as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720396 | Millipore: Percentage of residual kinase activity of TSSK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435184 | Binding constant for PTK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435159 | Binding constant for EPHB3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720358 | Millipore: Percentage of residual kinase activity of MYLK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435529 | Binding constant for LATS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1277988 | Inhibition of PI3K-gamma (unknown origin) after 40 mins by ADP-Glo luminescent kinase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1560707 | Inhibition of recombinant human full-length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system using PIP2 as substrate measured after 1 hr by kinase-glo assay | |||
| AID683674 | Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID1427280 | Selectivity index, ratio of IC50 for human fibroblasts to IC50 for human RL cells | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435350 | Percentage ERK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720135 | Millipore: Percentage of residual kinase activity of EPHA8 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720227 | Millipore: Percentage of residual kinase activity of PIM3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720244 | Millipore: Percentage of residual kinase activity of MST1R at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720306 | Millipore: Percentage of residual kinase activity of IRAK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435553 | Binding constant for PRKCD kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720474 | Millipore: Percentage of residual kinase activity of PRKCB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1434322 | Cytotoxicity against human FR2 cells assessed as growth inhibition at 10 uM measured after 48 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID1434327 | Cytotoxicity against human FR2 cells measured after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID435123 | Percentage NEK7 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720130 | Millipore: Percentage of residual kinase activity of EPHA4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435905 | Binding constant for full-length CSNK1G3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720159 | Millipore: Percentage of residual kinase activity of FES at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720235 | Millipore: Percentage of residual kinase activity of PTK2B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224775 | Delta TM value showing the stabilisation of ERK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720152 | Millipore: Percentage of residual kinase activity of FGFR2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720418 | Millipore: Percentage of residual kinase activity of YES1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720415 | Millipore: Percentage of residual kinase activity of WNK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720047 | Millipore: Percentage of residual kinase activity of BLK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720158 | Millipore: Percentage of residual kinase activity of FER at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720036 | Millipore: Percentage of residual kinase activity of AURKA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720407 | Millipore: Percentage of residual kinase activity of TXK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720201 | Millipore: Percentage of residual kinase activity of PRKCH at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436036 | Percentage Lck activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720443 | Millipore: Percentage of residual kinase activity of NLK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1605951 | Inhibition of human PI3Kgamma assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID435554 | Binding constant for PRKD3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435430 | Binding constant for INSRR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1893420 | Inhibition of PI3Kbeta (unknown origin) in presence of [33P]-ATP incubated for 2 hrs by hotspot kinase assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer. |
| AID1857288 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | |||
| AID435688 | Binding constant for full-length PCTK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435166 | Binding constant for full-length JNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720464 | Millipore: Percentage of residual kinase activity of PRKACA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224785 | Delta TM value showing the stabilisation of PDK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID719920 | Inhibition of PI3Kbeta in presence of 10 uM ATP | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID720248 | Millipore: Percentage of residual kinase activity of TYRO3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427272 | Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID436076 | Percentage DYRK1A activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID507031 | Cell cycle arrest in human U87 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720167 | Millipore: Percentage of residual kinase activity of FLT4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID683668 | Inhibition of PI3K p110gamma by fluorescence based immunoassay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID720272 | Millipore: Percentage of residual kinase activity of SIK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720171 | Millipore: Percentage of residual kinase activity of FYN at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435854 | Percentage IKK-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1427320 | Cell cycle arrest in human HaCaT cells harboring wild-type p53 assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 52.3%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720300 | Millipore: Percentage of residual kinase activity of IKBKB at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435788 | Binding constant for CLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1724539 | Inhibition of C-MET (unknown origin) at 1 uM relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID435328 | Binding constant for YES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435909 | Binding constant for full-length LKB1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720241 | Millipore: Percentage of residual kinase activity of ROCK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1481074 | Inhibition of human JAK3 using GEEEEYFELVKKKK as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID683669 | Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID720027 | Millipore: Percentage of residual kinase activity of NUAK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720392 | Millipore: Percentage of residual kinase activity of TLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720258 | Millipore: Percentage of residual kinase activity of MAPK14 at 1uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224750 | Delta TM value showing the stabilisation of CAMK1G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435283 | Binding constant for DAPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID599957 | Binding affinity to human KIT incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720280 | Millipore: Percentage of residual kinase activity of PLK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720087 | Millipore: Percentage of residual kinase activity of CSNK2A2 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720302 | Millipore: Percentage of residual kinase activity of INSR at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720394 | Millipore: Percentage of residual kinase activity of TSSK1B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435318 | Binding constant for PAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1442193 | Inhibition of human PI3K p120gamma at 10 uM using phosphatidylinositol 4,5-bisphosphate as substrate after 30 mins by HTRF assay relative to control | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
| AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720068 | Millipore: Percentage of residual kinase activity of CDK6 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720451 | Millipore: Percentage of residual kinase activity of PAK7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435738 | Percentage p38delta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1175452 | Inhibition of mTOR kinase (unknown origin) at 10 uM after 1 hr by TR-FRET assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors. |
| AID720220 | Millipore: Percentage of residual kinase activity of PHKG2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720381 | Millipore: Percentage of residual kinase activity of MET at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1605955 | Inhibition of human PI3Kgamma assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1224764 | Delta TM value showing the stabilisation of CK1G1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435276 | Binding constant for BMPR1A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720278 | Millipore: Percentage of residual kinase activity of STK33 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435933 | Binding constant for PKN2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID683666 | Inhibition of human recombinant CDK5/P25 using myelin basic protein substrate | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID1702054 | Inhibition of human PI3Kdelta incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720053 | Millipore: Percentage of residual kinase activity of BRSK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435728 | Percentage JNK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720196 | Millipore: Percentage of residual kinase activity of HCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720105 | Millipore: Percentage of residual kinase activity of CAMK1D at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720056 | Millipore: Percentage of residual kinase activity of CDK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435941 | Binding constant for ZAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1427310 | Cell cycle arrest in human Caco2 cells assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 52.4%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720410 | Millipore: Percentage of residual kinase activity of ULK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435278 | Binding constant for full-length CDK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID507064 | Induction of apoptosis in mouse BA/F3 cells harboring Bcr/Abl gene at 2.5 uM after 36 hrs by FITC-conjugated annexin V staining-based FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720099 | Millipore: Percentage of residual kinase activity of CAMK2G at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435881 | Percentage ROCK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435412 | Binding constant for MAP3K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435516 | Binding constant for ADCK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435280 | Binding constant for CSF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1467667 | Cytotoxicity against human triple negative MDA-MB-468 cells assessed as cell viability at 10 uM after 48 hrs by CellTiter-Glo 2D assay relative to control | |||
| AID1624206 | Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1327482 | Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide as substrate after 1 hr in presence of ATP by lance ultra assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor. |
| AID435441 | Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720416 | Millipore: Percentage of residual kinase activity of WNK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720118 | Millipore: Percentage of residual kinase activity of STK17A at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720059 | Millipore: Percentage of residual kinase activity of CDK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435198 | Binding constant for TIE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID719918 | Inhibition of PI3Kdelta in presence of 10 uM ATP | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID1177101 | Inhibition of human PI3KCalpha by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1758209 | Inhibition of human PI3Kalpha using ATP as substrate at 25 uM incubated for 60 mins by ADP-glo based luminescence assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Ring closure strategy leads to potent RIPK3 inhibitors. |
| AID720041 | Millipore: Percentage of residual kinase activity of AXL at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720179 | Millipore: Percentage of residual kinase activity of GRK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1427302 | Cell cycle arrest in human PC3 cells harboring p53 mutant assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 40.8%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1605952 | Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID720233 | Millipore: Percentage of residual kinase activity of PRKX at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1434319 | Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition at 10 uM measured after 48 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID720287 | Millipore: Percentage of residual kinase activity of TAOK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435282 | Binding constant for full-length CSNK1G2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720079 | Millipore: Percentage of residual kinase activity of CSNK1G2 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435311 | Binding constant for HCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720384 | Millipore: Percentage of residual kinase activity of MUSK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1605957 | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 h | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID720290 | Millipore: Percentage of residual kinase activity of TAOK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435146 | Binding constant for ABL1(H396P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720108 | Millipore: Percentage of residual kinase activity of DAPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427269 | Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427277 | Selectivity index, ratio of IC50 for human fibroblasts to IC50 for human PC3 cells | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720019 | Millipore: Percentage of residual kinase activity of ALK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1628741 | Inhibition of PI3K p110alpha/p85 (unknown origin) using PIP2/ATP as substrate after 1 hr by kinase glo luminescent assay | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors. |
| AID435374 | Percentage PLK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720417 | Millipore: Percentage of residual kinase activity of WNK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1560706 | Inhibition of recombinant human full-length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system at 1 nM using PIP2 as substrate measured after 1 hr by kinase-glo assay relative to control | |||
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720457 | Millipore: Percentage of residual kinase activity of PASK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435431 | Binding constant for MAP4K1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435402 | Binding constant for EGFR(G719S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720202 | Millipore: Percentage of residual kinase activity of PRKCQ at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720437 | Millipore: Percentage of residual kinase activity of RPS6KB1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1263102 | Inhibition of PI3Kbeta (unknown origin) after 1 hr by ADP-Glo Luminescent assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID720034 | Millipore: Percentage of residual kinase activity of ABL2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720351 | Millipore: Percentage of residual kinase activity of MELK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507050 | Inhibition of Bcr/Abl-mediated tyrosine phosphorylation in human K562 cells at 0.08 to 20 uM after 120 mins by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1224780 | Delta TM value showing the stabilisation of OSR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1481068 | Inhibition of human AKT1 using KGSGSGRPRTSSFAEG as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1765909 | Inhibition of PI3Kalpha (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID720149 | Millipore: Percentage of residual kinase activity of FGFR1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID599959 | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| AID435803 | Binding constant for full-length LIMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1467657 | Competitive inhibition of human PI3K p110alpha/p85alpha using PIP2 as substrate preincubated for 10 mins followed by ATP addition measured after 30 mins by HTRF assay | |||
| AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720117 | Millipore: Percentage of residual kinase activity of STK17A at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720469 | Millipore: Percentage of residual kinase activity of AKT2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1765921 | Antiproliferative activity against human A549 cells | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID436023 | Binding constant for MERTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1857281 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate incubated for 2 hrs in presence of ATP by Kinase Glo luminescence assay | |||
| AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435197 | Binding constant for TEC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720081 | Millipore: Percentage of residual kinase activity of CSNK1G3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720194 | Millipore: Percentage of residual kinase activity of HCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1481087 | Inhibition of PI3Kalpha (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID1663884 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, po measured after 0.5 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720217 | Millipore: Percentage of residual kinase activity of PKN2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720411 | Millipore: Percentage of residual kinase activity of ULK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720448 | Millipore: Percentage of residual kinase activity of PAK4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720098 | Millipore: Percentage of residual kinase activity of CAMK2B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1702072 | Inhibition of human PI3Kbeta incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435315 | Percentage MARK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435820 | Percentage PKCalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1189532 | Inhibition of rapamycin-sensitive mTORC1 (unknown origin) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. |
| AID1442195 | Inhibition of human PI3K p110alpha/p85alpha using phosphatidylinositol 4,5-bisphosphate as substrate after 30 mins by HTRF assay | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720210 | Millipore: Percentage of residual kinase activity of PRKG1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720471 | Millipore: Percentage of residual kinase activity of AKT3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720020 | Millipore: Percentage of residual kinase activity of ALK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720188 | Millipore: Percentage of residual kinase activity of HIPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720092 | Millipore: Percentage of residual kinase activity of CLK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720035 | Millipore: Percentage of residual kinase activity of AURKA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1724535 | Inhibition of EGFR T790M mutant (unknown origin) using FAM-labelled peptide as substrate at 1 uM incubated for 10 mins in presence of ATP by Kinase Glo luminescence assay relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427298 | Cell cycle arrest in human MDA-MB-231 cells harboring p53 mutant assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 42.2%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702080 | Inhibition of human DNA-PK | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720413 | Millipore: Percentage of residual kinase activity of VRK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224789 | Delta TM value showing the stabilisation of PLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720089 | Millipore: Percentage of residual kinase activity of CLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435819 | Percentage PKBbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720237 | Millipore: Percentage of residual kinase activity of RIPK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720408 | Millipore: Percentage of residual kinase activity of ULK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1481073 | Inhibition of human FAK/PTK2 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID720450 | Millipore: Percentage of residual kinase activity of PAK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720346 | Millipore: Percentage of residual kinase activity of MARK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435789 | Binding constant for full-length CSNK2A2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720238 | Millipore: Percentage of residual kinase activity of ROCK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720218 | Millipore: Percentage of residual kinase activity of FRK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720376 | Millipore: Percentage of residual kinase activity of STK24 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720472 | Millipore: Percentage of residual kinase activity of PRKCA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435787 | Binding constant for CLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224770 | Delta TM value showing the stabilisation of JAK1~B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435937 | Binding constant for TESK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1663883 | AUC in ovariectomized nu/nu mouse at 10 mg/kg, ip measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID1663879 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, ip measured after 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435779 | Binding constant for ALK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435723 | Percentage GSK3-beta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720228 | Millipore: Percentage of residual kinase activity of PLK1 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 20 mM DTT | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436014 | Binding constant for full-length DYRK1B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1605956 | Inhibition of human PI3Kdelta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID435541 | Percentage PKA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720442 | Millipore: Percentage of residual kinase activity of NLK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720267 | Millipore: Percentage of residual kinase activity of SGK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1280675 | Inhibition of human recombinant PI3K alpha by scintillation proximity radiometric assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435657 | Binding constant for full-length IKK-epsilon | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435181 | Binding constant for full-length p38-alpha | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720236 | Millipore: Percentage of residual kinase activity of RIPK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663870 | Stability of compound in cell culture medium assessed as fraction of parent compound remaining measured after 0.5 hr | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435238 | Percentage JNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720112 | Millipore: Percentage of residual kinase activity of DCLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720140 | Millipore: Percentage of residual kinase activity of EPHB2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720382 | Millipore: Percentage of residual kinase activity of MKNK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663882 | Half life in ovariectomized nu/nu mouse at 10 mg/kg, ip measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224765 | Delta TM value showing the stabilisation of CK1G2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720180 | Millipore: Percentage of residual kinase activity of GRK7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507046 | Antiangiogenic activity against HUVEC after 24 hrs by calcein AM staining-based fluorescent microscopy | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1724543 | Inhibition of EGFR T790M/L858R mutant (unknown origin) using FAM-labelled peptide as substrate incubated for 10 mins in presence of ATP by Kinase Glo luminescence assay | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1724538 | Inhibition of mTOR (unknown origin) at 1 uM relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID435518 | Binding constant for AURKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435793 | Binding constant for EPHA1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720037 | Millipore: Percentage of residual kinase activity of AURKB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1177094 | Inhibition of human PI3KC2alpha by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID435373 | Percentage PKCzeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720476 | Millipore: Percentage of residual kinase activity of PRKCB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435317 | Percentage PIM1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1224806 | Delta TM value showing the stabilisation of VRK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1857289 | Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | |||
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1177095 | Inhibition of human PI3KC2beta by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720335 | Millipore: Percentage of residual kinase activity of LCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427340 | Cell cycle arrest in human HaCaT cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720288 | Millipore: Percentage of residual kinase activity of TAOK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224782 | Delta TM value showing the stabilisation of PAK5 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605940 | Inhibition of recombinant full length human C-terminal His-tagged HDAC3 (1 to 428 residues) expressed in baculovirus infected insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720261 | Millipore: Percentage of residual kinase activity of MAPK11 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427299 | Cell cycle arrest in human HCT116 cells harboring wild-type p53 assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.3 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1663863 | Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720462 | Millipore: Percentage of residual kinase activity of PDPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435434 | Binding constant for RET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720033 | Millipore: Percentage of residual kinase activity of ABL2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435522 | Binding constant for CDK11 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1198179 | Inhibition of mTOR kinase (unknown origin) using ULight-4E-BP1 as substrate after 1 hr by TR-FRET assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720313 | Millipore: Percentage of residual kinase activity of ITK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720219 | Millipore: Percentage of residual kinase activity of FRK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435415 | Binding constant for MYLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720281 | Millipore: Percentage of residual kinase activity of PLK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436008 | Binding constant for full-length BTK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720193 | Millipore: Percentage of residual kinase activity of HCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435987 | Percentage PRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1224749 | Delta TM value showing the stabilisation of CAMK1D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1189526 | Inhibition of DNA-PK (unknown origin) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. |
| AID720296 | Millipore: Percentage of residual kinase activity of IGF1R at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720269 | Millipore: Percentage of residual kinase activity of SGK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224797 | Delta TM value showing the stabilisation of MPSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435521 | Binding constant for CAMKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1263095 | Inhibition of mTOR (unknown origin) using ULight-4E-BP1 peptide as substrate after 1 hr by lance ultra assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720406 | Millipore: Percentage of residual kinase activity of TXK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720430 | Millipore: Percentage of residual kinase activity of EEF2K at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435833 | Binding constant for full-length TNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427304 | Cell cycle arrest in human NCI-H727 cells harboring p53 mutant assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 40.3%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1663873 | Stability of compound in cell culture medium assessed as fraction of parent compound remaining measured after 8 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID1765922 | Antiproliferative activity against human HL-60 cells | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID715638 | Inhibition of PI3Kgamma by HTRF assay in presence of ATP | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines. |
| AID436046 | Binding constant for PRKD2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720065 | Millipore: Percentage of residual kinase activity of CDK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427264 | Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720423 | Millipore: Percentage of residual kinase activity of DAPK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435155 | Binding constant for full-length DLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435797 | Binding constant for ERBB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224804 | Delta TM value showing the stabilisation of VRK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435830 | Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720230 | Millipore: Percentage of residual kinase activity of PLK3 at 1uM relative to control. Control inhibitor: Wortmannin at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720206 | Millipore: Percentage of residual kinase activity of PRKD1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720114 | Millipore: Percentage of residual kinase activity of DDR2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605945 | Inhibition of recombinant C-terminal His-fusion tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in insect cells using fluorogenic peptide p53 residues 379-382 (RHK(Ac)K(Ac)AMC) as substrate measured after 1 to 2 hrs by | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435561 | Binding constant for SRMS kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720136 | Millipore: Percentage of residual kinase activity of EPHA8 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507063 | Induction of apoptosis in human K562 cells harboring Bcr/Abl T315I mutant gene at 5 uM after 72 hrs by FITC-conjugated annexin V staining-based FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID719921 | Inhibition of PI3Kalpha in presence of 10 uM ATP | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720078 | Millipore: Percentage of residual kinase activity of CSNK1G1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1724541 | Inhibition of wild type EGFR (unknown origin) using FAM-labelled peptide as substrate incubated for 10 mins in presence of ATP by Kinase Glo luminescence assay | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435706 | Percentage BRSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720160 | Millipore: Percentage of residual kinase activity of FES at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436004 | Binding constant for ACVR2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435525 | Binding constant for EGFR(L858R) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720338 | Millipore: Percentage of residual kinase activity of MAPK3 at 1uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720449 | Millipore: Percentage of residual kinase activity of PAK4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427335 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase by Hoechst staining based fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720123 | Millipore: Percentage of residual kinase activity of EPHA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435320 | Binding constant for PRKCE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720319 | Millipore: Percentage of residual kinase activity of MAPK8 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ? -mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427314 | Cell cycle arrest in human HCT116 cells harboring wild-type p53 assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 68.4%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435566 | Selectivity for PIK3CA as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436017 | Binding constant for ERK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720292 | Millipore: Percentage of residual kinase activity of TBK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435199 | Binding constant for TLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436054 | Binding constant for TLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435661 | Binding constant for full-length MKNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436009 | Binding constant for full-length CAMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224751 | Delta TM value showing the stabilisation of CAMK2A produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720021 | Millipore: Percentage of residual kinase activity of ACVR1B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224795 | Delta TM value showing the stabilisation of SLK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435530 | Binding constant for MAP3K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435417 | Percentage PAK4 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720305 | Millipore: Percentage of residual kinase activity of INSR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720185 | Millipore: Percentage of residual kinase activity of HIPK1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720055 | Millipore: Percentage of residual kinase activity of CDK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1294640 | Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate incubated for 60 mins by Kinase-Glo luminescent kinase assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors. |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720336 | Millipore: Percentage of residual kinase activity of LYN at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720360 | Millipore: Percentage of residual kinase activity of MAP3K9 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663864 | Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435783 | Binding constant for full-length BRSK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435995 | Percentage SRPK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435902 | Binding constant for BRAF(V600E) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720323 | Millipore: Percentage of residual kinase activity of MAPK10 at 10uM relative to control. Control inhibitor: JAK Inhibitor I at 30.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720125 | Millipore: Percentage of residual kinase activity of EPHA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1467664 | Half life in CD-1 mouse liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | |||
| AID715639 | Inhibition of PI3Kdelta by HTRF assay in presence of ATP | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines. |
| AID1605950 | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID435501 | Percentage SmMLCK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720438 | Millipore: Percentage of residual kinase activity of NEK6 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435674 | Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1175453 | Inhibition of mTOR kinase (unknown origin) after 1 hr by TR-FRET assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors. |
| AID1725752 | Inhibition of human PI3K p110alpha/p85alpha using PIP2 as substrate incubated for 10 mins followed by ATP addition and measured after 30 mins in presence of 10 uM ATP by HTRF assay | |||
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720214 | Millipore: Percentage of residual kinase activity of MAPKAPK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720091 | Millipore: Percentage of residual kinase activity of CLK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435911 | Binding constant for MEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720203 | Millipore: Percentage of residual kinase activity of PRKCQ at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663876 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, ip measured after 1 hr by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720322 | Millipore: Percentage of residual kinase activity of MAPK10 at 1uM relative to control. Control inhibitor: JAK Inhibitor I at 30.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224768 | Delta TM value showing the stabilisation of DMPK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720301 | Millipore: Percentage of residual kinase activity of IKBKB at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720318 | Millipore: Percentage of residual kinase activity of MAPK8 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ? -mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224752 | Delta TM value showing the stabilisation of CAMK2B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720483 | Millipore: Percentage of residual kinase activity of PRKCE at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720207 | Millipore: Percentage of residual kinase activity of PRKD1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720409 | Millipore: Percentage of residual kinase activity of ULK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507039 | Antiproliferative activity against human TT cells after 13 days by fluorescence assay | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720042 | Millipore: Percentage of residual kinase activity of AXL at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720166 | Millipore: Percentage of residual kinase activity of FLT3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224803 | Delta TM value showing the stabilisation of PBK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435756 | Percentage Src activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1663877 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, ip measured after 3 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435801 | Binding constant for full-length GSK3A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720434 | Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720052 | Millipore: Percentage of residual kinase activity of BRSK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224790 | Delta TM value showing the stabilisation of PLK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1663862 | Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720357 | Millipore: Percentage of residual kinase activity of MAP2K7 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720277 | Millipore: Percentage of residual kinase activity of SRPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435289 | Binding constant for ERK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720058 | Millipore: Percentage of residual kinase activity of CDK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435666 | Binding constant for full-length NEK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435795 | Binding constant for EPHA4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224760 | Delta TM value showing the stabilisation of CHEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435432 | Binding constant for MLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720383 | Millipore: Percentage of residual kinase activity of MKNK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663868 | Stability of compound in cell culture medium assessed as compound hydrolysis measured after 8 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720192 | Millipore: Percentage of residual kinase activity of GSG2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435912 | Binding constant for MRCKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720234 | Millipore: Percentage of residual kinase activity of PTK2B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435648 | Binding constant for CAMKK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720173 | Millipore: Percentage of residual kinase activity of GCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435300 | Percentage PAK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720374 | Millipore: Percentage of residual kinase activity of STK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720461 | Millipore: Percentage of residual kinase activity of PDGFRB at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435288 | Binding constant for EPHB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720144 | Millipore: Percentage of residual kinase activity of EPHB4 at 10uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1605960 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1125 residues) expressed in baculovirus infected insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence as | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID720184 | Millipore: Percentage of residual kinase activity of GSK3B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1725763 | Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability at 10 uM after 48 hrs by celltiter-glo 2D luminescent assay relative to control | |||
| AID435285 | Binding constant for DMPK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435526 | Binding constant for FGFR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224802 | Delta TM value showing the stabilisation of TNIK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427270 | Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435655 | Binding constant for ERK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435689 | Binding constant for full-length PFTK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224757 | Delta TM value showing the stabilisation of CDK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720077 | Millipore: Percentage of residual kinase activity of CSNK1G1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720095 | Millipore: Percentage of residual kinase activity of CAMK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507030 | Antiproliferative activity against human LN229 cells harboring mutations in PI(3)K pathway components at 0.04 to 10 uM after 72 hrs by fluorescence assay | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1065013 | Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design. |
| AID1198181 | Cytotoxicity against human H460 cells after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435865 | Percentage MKK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1857282 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase Glo luminescence assay | |||
| AID720455 | Millipore: Percentage of residual kinase activity of MARK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720428 | Millipore: Percentage of residual kinase activity of SRC at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720051 | Millipore: Percentage of residual kinase activity of BRSK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1725761 | Cytotoxicity against human primary fibroblasts assessed as cell viability at 10 uM after 48 hrs by celltiter-glo 2D luminescent assay relative to control | |||
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435681 | Percentage MAPKAPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID436071 | Percentage CHK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720082 | Millipore: Percentage of residual kinase activity of CSNK1G3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427265 | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720286 | Millipore: Percentage of residual kinase activity of TAOK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663891 | Half life in ovariectomized nu/nu mouse at 10 mg/kg, po measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID1327481 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by kinase-glo luminescence assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor. |
| AID720252 | Millipore: Percentage of residual kinase activity of RPS6KA3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720063 | Millipore: Percentage of residual kinase activity of CDK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720477 | Millipore: Percentage of residual kinase activity of PRKCB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1357599 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate after 1 hr by Kinase-Glo luminescent kinase assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Phthalimide conjugations for the degradation of oncogenic PI3K. |
| AID720104 | Millipore: Percentage of residual kinase activity of CAMK4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 40 mM HEPES pH 7.4, 5 mM CaCl2, 30 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427330 | Cell cycle arrest in human Caco2 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1663861 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 4 days by coulter counter method | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1765920 | Antiproliferative activity against human HepG2 cells | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID720064 | Millipore: Percentage of residual kinase activity of CDK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435156 | Binding constant for EGFR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702071 | Inhibition of human PI3Kalpha incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID1663866 | Stability of compound in cell culture medium assessed as compound hydrolysis measured after 1 hr | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720445 | Millipore: Percentage of residual kinase activity of PAK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720154 | Millipore: Percentage of residual kinase activity of FGFR3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224794 | Delta TM value showing the stabilisation of RSK2b produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224776 | Delta TM value showing the stabilisation of ERK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435784 | Binding constant for CAMK2G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436019 | Binding constant for FRK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720143 | Millipore: Percentage of residual kinase activity of EPHB4 at 1uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1467658 | Competitive inhibition of human mTOR using 4EBP1 as substrate in presence of [33gammaP]-ATP after 120 mins by filter binding method | |||
| AID720424 | Millipore: Percentage of residual kinase activity of RAF1 at 1uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720246 | Millipore: Percentage of residual kinase activity of ROS1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720482 | Millipore: Percentage of residual kinase activity of PRKCE at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720165 | Millipore: Percentage of residual kinase activity of FLT3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720102 | Millipore: Percentage of residual kinase activity of CAMK2D at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224748 | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1857285 | Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | |||
| AID1481078 | Inhibition of human MEK1 using ERK2 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID720380 | Millipore: Percentage of residual kinase activity of MET at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720157 | Millipore: Percentage of residual kinase activity of FER at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720363 | Millipore: Percentage of residual kinase activity of CDC42BPA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720308 | Millipore: Percentage of residual kinase activity of IRAK4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720403 | Millipore: Percentage of residual kinase activity of NTRK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435667 | Binding constant for full-length NLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720186 | Millipore: Percentage of residual kinase activity of HIPK1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436050 | Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436052 | Binding constant for full-length SNF1LK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID683671 | Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID1198182 | Cytotoxicity against human PC3 cells after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors. |
| AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435883 | Percentage SGK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435778 | Binding constant for full-length ADCK4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1427274 | Selectivity index, ratio of IC50 for human fibroblasts to IC50 for human Caco2 cells | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435223 | Percentage CSK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435656 | Binding constant for FGFR4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435250 | Percentage MSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720435 | Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: Rapamycin at 10.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20, 10 uM FKBP12 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663886 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, po measured after 3 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1467663 | Aqueous solubility of the compound at pH 7.4 at 200 uM after 90 mins by UV-spectrophotometric method | |||
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1280678 | Inhibition of human recombinant PI3K gamma by scintillation proximity radiometric assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720253 | Millipore: Percentage of residual kinase activity of RPS6KA3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1442192 | Inhibition of human PI3K p110beta/p85alpha at 10 uM using phosphatidylinositol 4,5-bisphosphate as substrate after 30 mins by HTRF assay relative to control | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
| AID436034 | Binding constant for PRKCH kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720191 | Millipore: Percentage of residual kinase activity of GSG2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427295 | Cell cycle arrest in human Caco2 cells assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 3.6 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720373 | Millipore: Percentage of residual kinase activity of STK4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435176 | Percentage PIM2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720285 | Millipore: Percentage of residual kinase activity of MAP3K7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720304 | Millipore: Percentage of residual kinase activity of INSR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720350 | Millipore: Percentage of residual kinase activity of MELK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436051 | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID325751 | Inhibition of p33cdk2/cyclin E | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID683675 | Antiproliferative activity against human Skin fibroblasts incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID1427267 | Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435454 | Percentage CaMKKalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435207 | Inhibition of CHK1-S345 phosphorylation in MMS treated HEK293 cells at 0.5uM | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1280674 | Inhibition of mTOR (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID1605943 | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1125 residues) expressed in baculovirus infected insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1198178 | Inhibition of PI3K-alpha kinase (unknown origin) using ULight-4E-BP1 as substrate at 10 uM after 60 mins by luminescence assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors. |
| AID1605942 | Inhibition of recombinant human C-terminal His-fusion tagged HDAC5 (657 to 1123 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1481085 | Inhibition of human YES/YES1 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID1224801 | Delta TM value showing the stabilisation of MST1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1434325 | Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID720209 | Millipore: Percentage of residual kinase activity of PRKD2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720399 | Millipore: Percentage of residual kinase activity of TEC at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1605949 | Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID435322 | Binding constant for PRKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1857280 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase Glo luminescence assay | |||
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435901 | Binding constant for BRAF kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435704 | Percentage Aurora B activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1724542 | Inhibition of EGFR T790M mutant (unknown origin) using FAM-labelled peptide as substrate incubated for 10 mins fin presence of ATP by Kinase Glo luminescence assay | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID720386 | Millipore: Percentage of residual kinase activity of NEK11 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435233 | Percentage HIPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720177 | Millipore: Percentage of residual kinase activity of GRK6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720275 | Millipore: Percentage of residual kinase activity of SRPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720070 | Millipore: Percentage of residual kinase activity of CDK7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435804 | Binding constant for LYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1300800 | Inhibition of PI3Kalpha (unknown origin) after 10 mins by Kinase-Glo Luminescent Assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
| AID720083 | Millipore: Percentage of residual kinase activity of CSNK1D at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720162 | Millipore: Percentage of residual kinase activity of FGR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720425 | Millipore: Percentage of residual kinase activity of RAF1 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1306914 | Inhibition of PI3Kalpha (unknown origin) using PI substrate incubated for 60 mins by kinase-glo luminescence assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety. |
| AID720421 | Millipore: Percentage of residual kinase activity of ZAP70 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1481070 | Inhibition of human ABL1 using EAIYAAPFAKKK as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID720298 | Millipore: Percentage of residual kinase activity of CHUK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427309 | Cell cycle arrest in human Caco2 cells assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 3.6 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720090 | Millipore: Percentage of residual kinase activity of CLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224777 | Delta TM value showing the stabilisation of MST4(1) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224807 | Delta TM value showing the stabilisation of YSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID629401 | Inhibition of PI3Kalpha | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. |
| AID720334 | Millipore: Percentage of residual kinase activity of LCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435807 | Binding constant for MARK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720040 | Millipore: Percentage of residual kinase activity of AURKC at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720147 | Millipore: Percentage of residual kinase activity of PTK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720200 | Millipore: Percentage of residual kinase activity of PRKCH at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224754 | Delta TM value showing the stabilisation of CAMK2G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID507069 | Cell cycle arrest in mouse BA/F3 cells harboring Bcr/Abl T315I mutant gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID638927 | Antiproliferative activity against human ECV304 cells | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720045 | Millipore: Percentage of residual kinase activity of BTK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720293 | Millipore: Percentage of residual kinase activity of TBK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427317 | Cell cycle arrest in human NCI-H727 cells harboring p53 mutant assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 1.1 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720262 | Millipore: Percentage of residual kinase activity of MAPK12 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720454 | Millipore: Percentage of residual kinase activity of MARK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720050 | Millipore: Percentage of residual kinase activity of BMX at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702078 | Inhibition of human PI3K2alpha incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID720368 | Millipore: Percentage of residual kinase activity of RPS6KA4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720440 | Millipore: Percentage of residual kinase activity of NEK7 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435782 | Binding constant for BRSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1481082 | Inhibition of human PKCg using histone H1 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID435560 | Binding constant for SNF1LK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605953 | Inhibition of human PI3Kalpha assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to contro | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID720341 | Millipore: Percentage of residual kinase activity of MAPK1 at 10uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435842 | Percentage Aurora C activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720273 | Millipore: Percentage of residual kinase activity of SIK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720097 | Millipore: Percentage of residual kinase activity of CAMK2B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720148 | Millipore: Percentage of residual kinase activity of PTK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224759 | Delta TM value showing the stabilisation of CDKL1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1434324 | Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435665 | Binding constant for NEK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720229 | Millipore: Percentage of residual kinase activity of PLK1 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 20 mM DTT | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720426 | Millipore: Percentage of residual kinase activity of KIT at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435279 | Binding constant for full-length CDK9 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1065015 | Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design. |
| AID435938 | Binding constant for TGFBR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435169 | Binding constant for full-length MEK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720307 | Millipore: Percentage of residual kinase activity of IRAK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1189533 | Inhibition of rapamycin-insensitive mTORC2 (unknown origin) | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring. |
| AID720259 | Millipore: Percentage of residual kinase activity of MAPK14 at 10uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435444 | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1663869 | Stability of compound in cell culture medium assessed as compound hydrolysis measured after 24 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435545 | Binding constant for NEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605958 | Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay relative t | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720274 | Millipore: Percentage of residual kinase activity of SRPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435256 | Percentage p38-gamma MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427279 | Selectivity index, ratio of IC50 for human fibroblasts to IC50 for human HaCaT cells | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1857279 | Inhibition of N-terminal FLAG-tagged recombinant human mTOR (1362 to end residue) using ULight-4EBP1 peptide as substrate incubated for 30 mins in presence of ATP by Lance ultra assay | |||
| AID1427293 | Cell cycle arrest in human HuH7 cells assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.2 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435291 | Binding constant for FGFR3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1263106 | Inhibition of PI3Kdelta (unknown origin) after 1 hr by ADP-Glo Luminescent assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID435433 | Binding constant for full-length MST1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720352 | Millipore: Percentage of residual kinase activity of MINK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720199 | Millipore: Percentage of residual kinase activity of PRKCZ at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720084 | Millipore: Percentage of residual kinase activity of CSNK1D at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720120 | Millipore: Percentage of residual kinase activity of DYRK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435552 | Binding constant for PIK3CA(E545K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720398 | Millipore: Percentage of residual kinase activity of TEC at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224778 | Delta TM value showing the stabilisation of NEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720072 | Millipore: Percentage of residual kinase activity of CDK9 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435621 | Percentage p38alpha MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID436024 | Binding constant for MRCKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720279 | Millipore: Percentage of residual kinase activity of STK33 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224786 | Delta TM value showing the stabilisation of PIM1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1568315 | Inhibition of recombinant human full length N-terminal GST-tagged PI3Kdelta (1 to 1044 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID720339 | Millipore: Percentage of residual kinase activity of MAPK3 at 10uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720484 | Millipore: Percentage of residual kinase activity of PRKCZ at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720321 | Millipore: Percentage of residual kinase activity of MAPK9 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720441 | Millipore: Percentage of residual kinase activity of NEK7 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720303 | Millipore: Percentage of residual kinase activity of INSR at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435898 | Binding constant for ACVR1B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605939 | Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1741415 | Inhibition of mTOR (unknown origin) using ULight-4E-BP1 as substrate measured after 45 mins in presence of ATP by LANCE Ultra assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. |
| AID1758208 | Inhibition of mTOR (unknown origin) using ATP as substrate after 60 mins by Lance ultra assay | 2021 | European journal of medicinal chemistry, May-05, Volume: 217 | Ring closure strategy leads to potent RIPK3 inhibitors. |
| AID1702099 | Inhibition of human PI4kbeta incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435834 | Binding constant for YANK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720049 | Millipore: Percentage of residual kinase activity of BMX at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1278052 | Inhibition of mTOR kinase (unknown origin) assessed as suppression of ULight-4E-BP1 substrate phosphorylation incubated for 1 hr by lance ultra assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
| AID1605938 | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in baculovirus infected Sf21 insect cells using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by flu | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1624202 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720212 | Millipore: Percentage of residual kinase activity of PRKG1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720226 | Millipore: Percentage of residual kinase activity of PIM3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID325614 | Inhibition of Cdk5/p25 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720266 | Millipore: Percentage of residual kinase activity of SGK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436086 | Percentage HIPK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID638909 | Inhibition of PI3Kalpha by luminescent kinase assay | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1306912 | Inhibition of mTOR (unknown origin) using ULight4E-BP1 peptide as substrate incubated for 1 hr by TR-FRET assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety. |
| AID720395 | Millipore: Percentage of residual kinase activity of TSSK1B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720170 | Millipore: Percentage of residual kinase activity of CSF1R at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720379 | Millipore: Percentage of residual kinase activity of MERTK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435931 | Binding constant for PIM1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720128 | Millipore: Percentage of residual kinase activity of EPHA3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720215 | Millipore: Percentage of residual kinase activity of MAPKAPK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427301 | Cell cycle arrest in human PC3 cells harboring p53 mutant assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.5 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1263104 | Inhibition of PI3Kgamma (unknown origin) after 1 hr by ADP-Glo Luminescent assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID1434321 | Cytotoxicity against human HepG2 cells assessed as growth inhibition at 10 uM measured after 48 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID1427315 | Cell cycle arrest in human PC3 cells harboring p53 mutant assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.5 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1224799 | Delta TM value showing the stabilisation of NDR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720419 | Millipore: Percentage of residual kinase activity of YES1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID507051 | Inhibition of Bcr/Abl-mediated tyrosine phosphorylation in mouse BA/F3 cells at 0.08 to 20 uM after 120 mins by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720067 | Millipore: Percentage of residual kinase activity of CDK6 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720071 | Millipore: Percentage of residual kinase activity of CDK9 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435734 | Percentage NEK6 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1277986 | Inhibition of PI3K-delta (unknown origin) using PIP2 as substrate incubated for 1 hr by Kinase-Glo luminescent kinase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
| AID720369 | Millipore: Percentage of residual kinase activity of RPS6KA4 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435558 | Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435791 | Binding constant for EGFR(E746-A750del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID683672 | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID720317 | Millipore: Percentage of residual kinase activity of JAK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720332 | Millipore: Percentage of residual kinase activity of LCK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435363 | Percentage MELK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720061 | Millipore: Percentage of residual kinase activity of CDK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720122 | Millipore: Percentage of residual kinase activity of EGFR at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720371 | Millipore: Percentage of residual kinase activity of SRPK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720039 | Millipore: Percentage of residual kinase activity of AURKC at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435183 | Binding constant for PLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720043 | Millipore: Percentage of residual kinase activity of PTK6 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720216 | Millipore: Percentage of residual kinase activity of PKN2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435658 | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720094 | Millipore: Percentage of residual kinase activity of CSK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435427 | Percentage PKBalpha activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720378 | Millipore: Percentage of residual kinase activity of MERTK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720342 | Millipore: Percentage of residual kinase activity of MAPKAPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435669 | Percentage PDK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1624199 | Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436083 | Percentage ERK8 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435461 | Percentage CK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720205 | Millipore: Percentage of residual kinase activity of PRKCI at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1857290 | Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | |||
| AID683680 | Antiproliferative activity against human NCI-H727 cells assessed as cell diminution incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID720453 | Millipore: Percentage of residual kinase activity of PAK6 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720327 | Millipore: Percentage of residual kinase activity of LIMK1 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720316 | Millipore: Percentage of residual kinase activity of JAK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224783 | Delta TM value showing the stabilisation of PAK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720340 | Millipore: Percentage of residual kinase activity of MAPK1 at 1uM relative to control. Control inhibitor: ERK Inhibitor II at 30.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720260 | Millipore: Percentage of residual kinase activity of MAPK11 at 1uM relative to control. Control inhibitor: SB203580 at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720291 | Millipore: Percentage of residual kinase activity of TAOK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224763 | Delta TM value showing the stabilisation of CLK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435935 | Binding constant for RIPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1624200 | Antiproliferative activity against human HuH7 cells at 0.1 to 25 uM after 48 hrs by Hoechst 33342 staining-based assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID1765918 | Antiproliferative activity against human U-87 MG cells | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID1224769 | Delta TM value showing the stabilisation of GSK3B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1427311 | Cell cycle arrest in human MDA-MB-231 cells harboring p53 mutant assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.1 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720225 | Millipore: Percentage of residual kinase activity of PIM2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720245 | Millipore: Percentage of residual kinase activity of MST1R at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1765908 | Inhibition of PI3Kdelta (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID720391 | Millipore: Percentage of residual kinase activity of NEK3 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1568305 | Inhibition of recombinant human full length N-terminal DYKDDDDK-tagged PI3Kgamma (1 to 1102 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435517 | Binding constant for AKT2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1427266 | Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720265 | Millipore: Percentage of residual kinase activity of MAPK13 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435396 | Binding constant for CHEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435693 | Binding constant for TGFBR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720073 | Millipore: Percentage of residual kinase activity of CHEK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720221 | Millipore: Percentage of residual kinase activity of PHKG2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435903 | Binding constant for CDK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720333 | Millipore: Percentage of residual kinase activity of LCK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435404 | Binding constant for EPHB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1605941 | Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720310 | Millipore: Percentage of residual kinase activity of INSRR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID683676 | Antiproliferative activity against human HuH7 cells assessed as cell diminution incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID435690 | Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720232 | Millipore: Percentage of residual kinase activity of PRKX at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1624207 | Antiproliferative activity against human PC3 cells at 0.1 to 25 uM after 48 hrs by Hoechst 33342 staining-based assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID1663871 | Stability of compound in cell culture medium assessed as fraction of parent compound remaining measured after 1 hr | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720168 | Millipore: Percentage of residual kinase activity of FLT4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID683665 | Inhibition of rat recombinant GST-tagged DYRK1A expressed in Escherichia coli using myelin basic protein substrate | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID1427281 | Selectivity index, ratio of IC50 for human fibroblasts to IC50 for human MCF7 cells | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720388 | Millipore: Percentage of residual kinase activity of NEK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1481076 | Inhibition of human LCK using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID720100 | Millipore: Percentage of residual kinase activity of CAMK2G at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720069 | Millipore: Percentage of residual kinase activity of CDK7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720427 | Millipore: Percentage of residual kinase activity of KIT at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1434326 | Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID507053 | Inhibition of Bcr/Abl T315I mutant-mediated tyrosine phosphorylation in mouse BA/F3 cells at 0.08 to 20 uM after 120 mins by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1427337 | Cell cycle arrest in human PC3 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1224753 | Delta TM value showing the stabilisation of CAMK2D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720270 | Millipore: Percentage of residual kinase activity of SGK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435292 | Binding constant for ITK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID638930 | Antiproliferative activity against human HT-29 cells | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1442191 | Inhibition of human PI3K p110alpha/p85alpha at 10 uM using phosphatidylinositol 4,5-bisphosphate as substrate after 30 mins by HTRF assay relative to control | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
| AID720106 | Millipore: Percentage of residual kinase activity of CAMK1D at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720026 | Millipore: Percentage of residual kinase activity of PRKAA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720312 | Millipore: Percentage of residual kinase activity of ITK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435564 | Binding constant for TRKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435524 | Binding constant for full-length CSNK1D | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663875 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, ip measured after 0.5 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720161 | Millipore: Percentage of residual kinase activity of FGR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1434318 | Cytotoxicity against human MCF7 cells assessed as growth inhibition at 10 uM measured after 48 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID720080 | Millipore: Percentage of residual kinase activity of CSNK1G2 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1327485 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by kinase-glo luminescence assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor. |
| AID715641 | Inhibition of PI3Kalpha by HTRF assay in presence of ATP | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines. |
| AID435727 | Percentage JNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720458 | Millipore: Percentage of residual kinase activity of PDGFRA at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1467668 | Cytotoxicity against human MCF7 cells assessed as cell viability at 10 uM after 48 hrs by CellTiter-Glo 2D assay relative to control | |||
| AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID507038 | Inhibition of S6K autophosphorylation in human TT cells at 0.04 to 10 uM after 2 hrs by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1177098 | Inhibition of human class 3 PI3K by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID720146 | Millipore: Percentage of residual kinase activity of ERBB4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224771 | Delta TM value showing the stabilisation of MEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1224756 | Delta TM value showing the stabilisation of CAMKK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436072 | Percentage CK1delta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1568304 | Inhibition of recombinant human full length N-terminal GST-tagged PI3Kbeta (1 to 1070 residues)/PIK3R1 (1 to 724 residues) expressed in baculovirus expression system using PIP2 as substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720254 | Millipore: Percentage of residual kinase activity of RPS6KA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720348 | Millipore: Percentage of residual kinase activity of MAP2K1 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 50 mM Tris pH 7.5, 0.2 mM EGTA, 0.1% ?-mercaptoethanol, 0.01% Brij-35 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720088 | Millipore: Percentage of residual kinase activity of CSNK2A2 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435718 | Percentage EF2K activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1427276 | Selectivity index, ratio of IC50 for human fibroblasts to IC50 for human HCT116 cells | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720271 | Millipore: Percentage of residual kinase activity of SGK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1587173 | Inhibition of His-tagged recombinant human PI3K p110delta/p85alpha using lipid substrate incubated for 2 hrs by ADP-Glo assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. |
| AID1175451 | Inhibition of PI3K-alpha (unknown origin) using l-alpha-phosphatidylinositol as substrate after 60 mins by luminescence assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24 | Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436025 | Binding constant for NDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1893421 | Inhibition of PI3Kdelta (unknown origin) in presence of [33P]-ATP incubated for 2 hrs by hotspot kinase assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720367 | Millipore: Percentage of residual kinase activity of RPS6KA5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720030 | Millipore: Percentage of residual kinase activity of MAP3K5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1725754 | Kinetic aqueous solubility of compound in 2% DMSO/Phosphate buffer saline incubated for 90 mins under shaking condition by | |||
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720172 | Millipore: Percentage of residual kinase activity of FYN at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435153 | Binding constant for full-length DAPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720251 | Millipore: Percentage of residual kinase activity of RPS6KA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1198177 | Inhibition of mTOR kinase (unknown origin) using ULight-4E-BP1 as substrate at 10 uM after 1 hr by TR-FRET assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors. |
| AID435202 | Binding constant for TRKC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720057 | Millipore: Percentage of residual kinase activity of CDK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435907 | Binding constant for EGFR(L861Q) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1605954 | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation by measuring displacement of biotin-labelled PIP3 from complex at 1 uM using PIP2 as substrate measured after 30 mins in presence of ATP by HTRF assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID720256 | Millipore: Percentage of residual kinase activity of RPS6KA6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427263 | Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427296 | Cell cycle arrest in human Caco2 cells assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 52.4%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436069 | Percentage CHK1 activity remaining in the presence of 25uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720249 | Millipore: Percentage of residual kinase activity of TYRO3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720432 | Millipore: Percentage of residual kinase activity of MTOR at 1uM relative to control. Control inhibitor: PI-103 at 30.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427308 | Cell cycle arrest in human HuH7 cells assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 44%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720060 | Millipore: Percentage of residual kinase activity of CDK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435319 | Binding constant for PKN1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435515 | Binding constant for ABL1(Q252H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436005 | Binding constant for ANKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720025 | Millipore: Percentage of residual kinase activity of PRKAA2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435194 | Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720189 | Millipore: Percentage of residual kinase activity of HIPK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720107 | Millipore: Percentage of residual kinase activity of DAPK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435896 | Binding constant for AAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224755 | Delta TM value showing the stabilisation of CAMK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435160 | Binding constant for FER kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1442196 | Inhibition of human N-terminal FLAG-tagged mTOR (1362-end residues) in presence of [gamma33P]ATP after 40 mins | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
| AID720224 | Millipore: Percentage of residual kinase activity of PIM2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1893422 | Inhibition of PI3Kgamma (unknown origin) in presence of [33P]-ATP incubated for 2 hrs by hotspot kinase assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer. |
| AID720297 | Millipore: Percentage of residual kinase activity of IGF1R at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM Na3VO4, 5 mM Na-?-glycerophosphate | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663865 | Stability of compound in cell culture medium assessed as compound hydrolysis measured after 0.5 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720197 | Millipore: Percentage of residual kinase activity of IGF1R at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1568314 | Inhibition of recombinant human N-terminal FLAG-tagged mTOR (1362 to end residues) using Ulight-4E-BP1 as substrate incubated for 30 mins by fluorescence assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors. |
| AID720115 | Millipore: Percentage of residual kinase activity of DMPK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720481 | Millipore: Percentage of residual kinase activity of PRKCD at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663872 | Stability of compound in cell culture medium assessed as fraction of parent compound remaining measured after 3 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720190 | Millipore: Percentage of residual kinase activity of HIPK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720311 | Millipore: Percentage of residual kinase activity of INSRR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720263 | Millipore: Percentage of residual kinase activity of MAPK12 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605944 | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1224773 | Delta TM value showing the stabilisation of ASK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720414 | Millipore: Percentage of residual kinase activity of WNK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435519 | Binding constant for AURKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720361 | Millipore: Percentage of residual kinase activity of MAP3K9 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663890 | Tmax in ovariectomized nu/nu mouse at 10 mg/kg, po measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435523 | Binding constant for CIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435411 | Binding constant for KIT(D816V) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720393 | Millipore: Percentage of residual kinase activity of TLK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435193 | Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435182 | Binding constant for full-length PKAC-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1624211 | Antiproliferative activity against human HaCaT cells at 0.1 to 25 uM after 48 hrs by Hoechst 33342 staining-based assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720116 | Millipore: Percentage of residual kinase activity of DMPK at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720362 | Millipore: Percentage of residual kinase activity of CDC42BPA at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507052 | Inhibition of Bcr/Abl T315I mutant-mediated tyrosine phosphorylation in human K562 cells at 0.08 to 20 uM after 120 mins by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435339 | Percentage CaMKKbeta activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720028 | Millipore: Percentage of residual kinase activity of NUAK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1481077 | Inhibition of human LYN using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID1434320 | Cytotoxicity against human A549 cells assessed as growth inhibition at 10 uM measured after 48 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID1605948 | Inhibition of human recombinant N-terminal Streptavidin2-tagged HDAC11 (1 to 347 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1702079 | Inhibition of PI3K2beta (unknown origin) incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720150 | Millipore: Percentage of residual kinase activity of FGFR1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435514 | Binding constant for ABL1(M351T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720282 | Millipore: Percentage of residual kinase activity of SYK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720459 | Millipore: Percentage of residual kinase activity of PDGFRA at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720242 | Millipore: Percentage of residual kinase activity of RET at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720029 | Millipore: Percentage of residual kinase activity of MAP3K5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1512658 | Inhibition of recombinant mTORC2 (unknown origin) expressed in Escherichia coli after 15 mins in presence of gamma-[32]P-ATP by high-throughput screening assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy. |
| AID435407 | Binding constant for FLT3(D835Y) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720420 | Millipore: Percentage of residual kinase activity of ZAP70 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435979 | Percentage MST2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435906 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720329 | Millipore: Percentage of residual kinase activity of STK11 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1198180 | Inhibition of PI3K-alpha kinase (unknown origin) using ULight-4E-BP1 as substrate after 60 mins by luminescence assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435190 | Binding constant for full-length PIP5K1A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720046 | Millipore: Percentage of residual kinase activity of BTK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720325 | Millipore: Percentage of residual kinase activity of KDR at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435806 | Binding constant for MAPKAPK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720038 | Millipore: Percentage of residual kinase activity of AURKB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 50 mM NaCl, 0.1% v/v Triton-X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435165 | Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID507037 | Inhibition of Ret autophosphorylation in human TT cells at 0.04 to 10 uM after 2 hrs by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436010 | Binding constant for full-length CDK5 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1280676 | Inhibition of human recombinant PI3K beta by scintillation proximity radiometric assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID507033 | Cell cycle arrest in human SEG1 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720347 | Millipore: Percentage of residual kinase activity of MARK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507062 | Induction of apoptosis in human K562 cells harboring Bcr/Abl gene at 2.5 uM after 36 hrs by FITC-conjugated annexin V staining-based FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224796 | Delta TM value showing the stabilisation of LOK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1481084 | Inhibition of human TYK2 using KKSRGDYMTMQIG as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID507068 | Cell cycle arrest in mouse BA/F3 cells harboring Bcr/Abl gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1725755 | Half life in CD1 mouse liver microsomes at 1 uM incubated for 60 mins under shaking condition by LC-MS/MS analysis | |||
| AID720422 | Millipore: Percentage of residual kinase activity of DAPK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720096 | Millipore: Percentage of residual kinase activity of CAMK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436015 | Binding constant for EPHA6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720211 | Millipore: Percentage of residual kinase activity of PRKG1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720076 | Millipore: Percentage of residual kinase activity of CHEK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1702081 | Inhibition of human PIK3C3 incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID715640 | Inhibition of PI3Kbeta by HTRF assay in presence of ATP | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis, DNA-PK inhibition, anti-platelet activity studies of 2-(N-substituted-3-aminopyridine)-substituted-1,3-benzoxazines and DNA-PK and PI3K inhibition, homology modelling studies of 2-morpholino-(7,8-di and 8-substituted)-1,3-benzoxazines. |
| AID1427268 | Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720377 | Millipore: Percentage of residual kinase activity of STK24 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435613 | Percentage MNK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435847 | Percentage DYRK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1512657 | Inhibition of mTORC1 (unknown origin) expressed in HEK293T cells after 15 mins in presence of gamma-[32]P-ATP by high-throughput screening assay | 2018 | Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11 | Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy. |
| AID1224791 | Delta TM value showing the stabilisation of PRKACA produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1280673 | Inhibition of PI3K delta (unknown origin) using PIP2 as substrate after 1 hr by kinase-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1724537 | Inhibition of PI3K (unknown origin) at 1 uM relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435294 | Binding constant for full-length LIMK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1781085 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate in presence of ATP measured after 60 mins by ADP-Glo assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Bioisosteric replacements of the indole moiety for the development of a potent and selective PI3Kδ inhibitor: Design, synthesis and biological evaluation. |
| AID1724534 | Inhibition of wild type EGFR (unknown origin) using FAM-labelled peptide as substrate at 1 uM incubated for 10 mins in presence of ATP by Kinase Glo luminescence assay relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID720337 | Millipore: Percentage of residual kinase activity of LYN at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507067 | Cell cycle arrest in human K562 cells harboring Bcr/Abl T315I mutant gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720155 | Millipore: Percentage of residual kinase activity of FGFR4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720328 | Millipore: Percentage of residual kinase activity of STK11 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.1% v/v Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720349 | Millipore: Percentage of residual kinase activity of MAP2K1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 50 mM Tris pH 7.5, 0.2 mM EGTA, 0.1% ?-mercaptoethanol, 0.01% Brij-35 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435260 | Percentage RSK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1624205 | Antiproliferative activity against human HCT116 cells at 0.1 to 25 uM after 48 hrs by Hoechst 33342 staining-based assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID720324 | Millipore: Percentage of residual kinase activity of KDR at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435832 | Binding constant for SLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224788 | Delta TM value showing the stabilisation of PIM3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435162 | Binding constant for FLT3(N841I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720466 | Millipore: Percentage of residual kinase activity of AKT1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720164 | Millipore: Percentage of residual kinase activity of FLT1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720364 | Millipore: Percentage of residual kinase activity of CDC42BPB at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605962 | Inhibition of HDAC10 (unknown origin) at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay relative to control | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224798 | Delta TM value showing the stabilisation of DRAK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435647 | Binding constant for CAMK2D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720467 | Millipore: Percentage of residual kinase activity of AKT1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1280677 | Inhibition of human recombinant PI3K delta by scintillation proximity radiometric assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID720103 | Millipore: Percentage of residual kinase activity of CAMK4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 40 mM HEPES pH 7.4, 5 mM CaCl2, 30 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435393 | Binding constant for CAMK1D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435650 | Binding constant for full-length CSNK1E | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720359 | Millipore: Percentage of residual kinase activity of MYLK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1481081 | Inhibition of human PKCa using histone H1 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID1765923 | Antiproliferative activity against human MCF7 cells | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID436049 | Binding constant for PTK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435649 | Binding constant for CDC2L2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720330 | Millipore: Percentage of residual kinase activity of STK10 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720048 | Millipore: Percentage of residual kinase activity of BLK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720276 | Millipore: Percentage of residual kinase activity of SRPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663889 | Cmax in ovariectomized nu/nu mouse at 10 mg/kg, po measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720257 | Millipore: Percentage of residual kinase activity of RPS6KA6 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 30 mM NaCl | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1624203 | Antiproliferative activity against human MDA-MB-231 cells at 0.1 to 25 uM after 48 hrs by Hoechst 33342 staining-based assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID720085 | Millipore: Percentage of residual kinase activity of CSNK2A1 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435281 | Binding constant for full-length CSNK1A1L | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435324 | Binding constant for full-length RIOK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1893419 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate in presence of ATP measured after 1 hr by ADP-Glo assay | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of Novel Phosphoinositide-3-Kinase α Inhibitors with High Selectivity, Excellent Bioavailability, and Long-Acting Efficacy for Gastric Cancer. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720480 | Millipore: Percentage of residual kinase activity of PRKCD at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720354 | Millipore: Percentage of residual kinase activity of MAP2K6 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4, 1 mg/mL BSA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1481088 | Inhibition of PI3Kbeta (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID1481086 | Inhibition of human ZAP70 using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID435151 | Binding constant for CAMK1G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436012 | Binding constant for full-length CSNK2A1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID719919 | Inhibition of PI3Kgamma in presence of 10 uM ATP | 2012 | Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20 | PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. |
| AID720195 | Millipore: Percentage of residual kinase activity of HCK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720093 | Millipore: Percentage of residual kinase activity of CSK at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435147 | Binding constant for ACVR2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720284 | Millipore: Percentage of residual kinase activity of MAP3K7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720264 | Millipore: Percentage of residual kinase activity of MAPK13 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 25 mM Tris pH 7.5, 0.02 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435414 | Binding constant for MLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720131 | Millipore: Percentage of residual kinase activity of EPHA5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID683670 | Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1571681 | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate after 2 hrs by ADP-Glo assay | 2019 | MedChemComm, Mar-01, Volume: 10, Issue:3 | Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720452 | Millipore: Percentage of residual kinase activity of PAK6 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1702077 | Inhibition of human mTOR | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435692 | Binding constant for STK16 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435397 | Binding constant for CSNK1G1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1624210 | Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID1224762 | Delta TM value showing the stabilisation of CLK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720044 | Millipore: Percentage of residual kinase activity of PTK6 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435394 | Binding constant for CAMK2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720133 | Millipore: Percentage of residual kinase activity of EPHA7 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720239 | Millipore: Percentage of residual kinase activity of ROCK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720436 | Millipore: Percentage of residual kinase activity of RPS6KB1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663874 | Stability of compound in cell culture medium assessed as fraction of parent compound remaining measured after 24 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1765911 | Inhibition of PI3Kgamma (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID1277985 | Inhibition of PI3K-alpha (unknown origin) using PIP2 as substrate incubated for 1 hr by Kinase-Glo luminescent kinase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
| AID435215 | Percentage AMPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID683681 | Antiproliferative activity against human Skin fibroblasts assessed as cell diminution incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID435195 | Binding constant for SRC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1427305 | Cell cycle arrest in human HaCaT cells harboring wild-type p53 assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.6 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1663859 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435443 | Binding constant for TXK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435676 | Binding constant for LCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720390 | Millipore: Percentage of residual kinase activity of NEK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720187 | Millipore: Percentage of residual kinase activity of HIPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720023 | Millipore: Percentage of residual kinase activity of PRKAA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1277987 | Inhibition of PI3K-beta (unknown origin) after 40 mins by ADP-Glo luminescent kinase assay | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. |
| AID435551 | Binding constant for full-length p38-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720156 | Millipore: Percentage of residual kinase activity of FGFR4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435910 | Binding constant for MAP4K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720243 | Millipore: Percentage of residual kinase activity of RET at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507034 | Inhibition of v-Src phosphorylation expressed in mouse NIH/3T3 cells at 0.08 to 20 uM by Western blot analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1857287 | Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | |||
| AID720365 | Millipore: Percentage of residual kinase activity of CDC42BPB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1177104 | Inhibition of human DNA-PK by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID435531 | Binding constant for MKNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427297 | Cell cycle arrest in human MDA-MB-231 cells harboring p53 mutant assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.1 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1224758 | Delta TM value showing the stabilisation of CDK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435148 | Binding constant for AMPK-alpha1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224787 | Delta TM value showing the stabilisation of PIM2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435563 | Binding constant for TNIK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720402 | Millipore: Percentage of residual kinase activity of NTRK1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720132 | Millipore: Percentage of residual kinase activity of EPHA5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435822 | Binding constant for MEK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720343 | Millipore: Percentage of residual kinase activity of MAPKAPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435546 | Binding constant for PRKG1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720356 | Millipore: Percentage of residual kinase activity of MAP2K7 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435653 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720182 | Millipore: Percentage of residual kinase activity of GSK3A at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720138 | Millipore: Percentage of residual kinase activity of EPHB1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720295 | Millipore: Percentage of residual kinase activity of TGFBR1 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 1 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435167 | Binding constant for KIT(V559D) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436037 | Percentage MAPKAPK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720017 | Millipore: Percentage of residual kinase activity of TNK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435449 | Inhibition of CHK2-T68 phosphorylation in MMS treated HEK293 cells at 0.5uM | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720387 | Millipore: Percentage of residual kinase activity of NEK11 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1442194 | Inhibition of human PI3K p110delta/p85alpha at 10 uM using phosphatidylinositol 4,5-bisphosphate as substrate after 30 mins by HTRF assay relative to control | 2017 | European journal of medicinal chemistry, Mar-31, Volume: 129 | Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors. |
| AID720456 | Millipore: Percentage of residual kinase activity of PASK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1065012 | Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design. |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435228 | Percentage ERK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1702076 | Inhibition of human PI3Kgamma incubated for 1 hr by ADP-Glo kinase assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID435329 | Binding constant for YSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1481083 | Inhibition of human SYK using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720142 | Millipore: Percentage of residual kinase activity of EPHB3 at 10uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1224792 | Delta TM value showing the stabilisation of RIOK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720223 | Millipore: Percentage of residual kinase activity of PIM1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435370 | Percentage p38beta MAPK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720075 | Millipore: Percentage of residual kinase activity of CHEK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1624198 | Antiproliferative activity against human Caco2 cells at 0.1 to 25 uM after 48 hrs by Hoechst 33342 staining-based assay relative to control | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224774 | Delta TM value showing the stabilisation of p38beta produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1427271 | Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435539 | Percentage PHK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720289 | Millipore: Percentage of residual kinase activity of TAOK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720163 | Millipore: Percentage of residual kinase activity of FLT1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720412 | Millipore: Percentage of residual kinase activity of VRK2 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435275 | Binding constant for BIKE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720111 | Millipore: Percentage of residual kinase activity of DCLK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663888 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, po measured after 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435652 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435814 | Percentage PIM3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID1725764 | Antiproliferative activity against human MCF7 cells assessed as cell viability at 10 uM after 48 hrs by celltiter-glo 2D luminescent assay relative to control | |||
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435675 | Binding constant for KIT(V559D,T670I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720463 | Millipore: Percentage of residual kinase activity of PDPK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720478 | Millipore: Percentage of residual kinase activity of PRKCG at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427316 | Cell cycle arrest in human PC3 cells harboring p53 mutant assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 40.8%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720268 | Millipore: Percentage of residual kinase activity of SGK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663881 | Tmax in ovariectomized nu/nu mouse at 10 mg/kg, ip measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID507032 | Cell cycle arrest in human LN229 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720299 | Millipore: Percentage of residual kinase activity of CHUK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1624201 | Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID590158 | Inhibition of PI3Kalpha at 20 uM after 1 hr by luminescence assay | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors. |
| AID1280671 | Inhibition of PI3K beta (unknown origin) after 1 hr by ADP-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID507065 | Induction of apoptosis in mouse BA/F3 harboring Bcr/Abl T315I mutant gene at 5 uM after 72 hrs by FITC-conjugated annexin V staining-based FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID720439 | Millipore: Percentage of residual kinase activity of NEK6 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435277 | Binding constant for full-length CDK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435429 | Binding constant for FLT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720405 | Millipore: Percentage of residual kinase activity of NTRK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224800 | Delta TM value showing the stabilisation of MST4 (2) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720447 | Millipore: Percentage of residual kinase activity of PAK3 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663878 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, ip measured after 8 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID1663880 | Cmax in ovariectomized nu/nu mouse at 10 mg/kg, ip measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720355 | Millipore: Percentage of residual kinase activity of MAP2K6 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol, 0.1 mM Na3VO4, 1 mg/mL BSA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1327483 | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by ADP-glo based luminescence assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor. |
| AID720127 | Millipore: Percentage of residual kinase activity of EPHA3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435831 | Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435939 | Binding constant for TIE2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1427294 | Cell cycle arrest in human HuH7 cells assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 44%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1224767 | Delta TM value showing the stabilisation of DAPK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435897 | Binding constant for ABL1(T315I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID638928 | Antiproliferative activity against human Bel7404 cells | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID720222 | Millipore: Percentage of residual kinase activity of PIM1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1741414 | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-Glo reagent based assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors. |
| AID720331 | Millipore: Percentage of residual kinase activity of STK10 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427312 | Cell cycle arrest in human MDA-MB-231 cells harboring p53 mutant assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 42.2%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1434323 | Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Green synthesis and anticancer potential of chalcone linked-1,2,3-triazoles. |
| AID1224805 | Delta TM value showing the stabilisation of VRK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1663885 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, po measured after 1 hr by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720134 | Millipore: Percentage of residual kinase activity of EPHA7 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720137 | Millipore: Percentage of residual kinase activity of EPHB1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720444 | Millipore: Percentage of residual kinase activity of PAK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427306 | Cell cycle arrest in human HaCaT cells harboring wild-type p53 assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 52.3%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID1663860 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 4 days by coulter counter method | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720344 | Millipore: Percentage of residual kinase activity of MAPKAPK3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720119 | Millipore: Percentage of residual kinase activity of DYRK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663892 | AUC (0 to 24 hrs) in ovariectomized nu/nu mouse at 10 mg/kg, po measured upto 24 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID720181 | Millipore: Percentage of residual kinase activity of GSK3A at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436048 | Binding constant for full-length PTK2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720176 | Millipore: Percentage of residual kinase activity of GRK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427313 | Cell cycle arrest in human HCT116 cells harboring wild-type p53 assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.3 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720024 | Millipore: Percentage of residual kinase activity of PRKAA1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 200 uM AMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720086 | Millipore: Percentage of residual kinase activity of CSNK2A1 at 10uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 20 mM HEPES pH 7.6, 0.15 M NaCl, 0.1 mM EDTA, 5 mM DTT, 0.1% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1263100 | Inhibition of PI3Kalpha (unknown origin) after 1 hr by Kinase-Glo Luminescent assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24 | Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation. |
| AID720018 | Millipore: Percentage of residual kinase activity of TNK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224766 | Delta TM value showing the stabilisation of CK1G3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720320 | Millipore: Percentage of residual kinase activity of MAPK9 at 1uM relative to control. Control inhibitor: Jnk Inhibitor II at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435792 | Binding constant for EGFR(S752-I759del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720129 | Millipore: Percentage of residual kinase activity of EPHA4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720429 | Millipore: Percentage of residual kinase activity of SRC at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427318 | Cell cycle arrest in human NCI-H727 cells harboring p53 mutant assessed as accumulation at S phase at 25 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 40.3%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435378 | Percentage S6K1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720174 | Millipore: Percentage of residual kinase activity of GCK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 200 mM NaCl, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435827 | Binding constant for PDGFRA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720375 | Millipore: Percentage of residual kinase activity of STK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1765910 | Inhibition of PI3Kbeta (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1481080 | Inhibition of human PKACA using LCGRTGRRNSI as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID436013 | Binding constant for DMPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435418 | Percentage PAK5 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID435691 | Binding constant for SgK085 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID507029 | Antiproliferative activity against human U87 cells harboring mutations in PI(3)K pathway components at 0.04 to 10 uM after 72 hrs by fluorescence assay | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1224772 | Delta TM value showing the stabilisation of MAP2K6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427300 | Cell cycle arrest in human HCT116 cells harboring wild-type p53 assessed as accumulation at S phase at 10 uM measured after 48 hrs by Hoechst/BrdU staining based fluorescence assay (Rvb = 68.4%) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID507066 | Cell cycle arrest in human K562 cells harboring Bcr/Abl gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID435296 | Binding constant for MARK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1724536 | Inhibition of EGFR T790M/L858R mutant (unknown origin) using FAM-labelled peptide as substrate at 1 uM incubated for 10 mins in presence of ATP by Kinase Glo luminescence assay relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID720178 | Millipore: Percentage of residual kinase activity of GRK6 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720231 | Millipore: Percentage of residual kinase activity of PLK3 at 10uM relative to control. Control inhibitor: Wortmannin at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720431 | Millipore: Percentage of residual kinase activity of EEF2K at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1605947 | Inhibition of HDAC10 (unknown origin) using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1224779 | Delta TM value showing the stabilisation of NEK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720074 | Millipore: Percentage of residual kinase activity of CHEK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224781 | Delta TM value showing the stabilisation of PAK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720141 | Millipore: Percentage of residual kinase activity of EPHB3 at 1uM relative to control. Control inhibitor: PP2 at 30.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720433 | Millipore: Percentage of residual kinase activity of MTOR at 10uM relative to control. Control inhibitor: PI-103 at 30.0uM. Buffer: 50 mM HEPES pH 7.5, 1 mM EGTA, 0.01% Tween 20 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720345 | Millipore: Percentage of residual kinase activity of MAPKAPK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Na-?-glycerophosphate pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1467666 | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability at 10 uM after 48 hrs by CellTiter-Glo 2D assay relative to control | |||
| AID435867 | Percentage NEK2a activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720032 | Millipore: Percentage of residual kinase activity of ABL1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720404 | Millipore: Percentage of residual kinase activity of NTRK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435821 | Binding constant for GAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435406 | Binding constant for FLT3(D835H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435321 | Binding constant for PRKCQ kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435557 | Binding constant for RIPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720460 | Millipore: Percentage of residual kinase activity of PDGFRB at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435701 | Inhibition of PKB-S473 phosphorylation in IGF-1 treated HEK293 cells at 0.5uM | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720401 | Millipore: Percentage of residual kinase activity of TEK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1294641 | Inhibition of c-Met kinase (unknown origin) using FAM-labelled peptide substrate incubated for 10 mins by mobility shift assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720151 | Millipore: Percentage of residual kinase activity of FGFR2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720389 | Millipore: Percentage of residual kinase activity of NEK2 at 10uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720139 | Millipore: Percentage of residual kinase activity of EPHB2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435527 | Binding constant for FGFR3(G697C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720109 | Millipore: Percentage of residual kinase activity of DAPK2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435338 | Percentage CaMK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID638931 | Cell cycle arrest in human Rh30 cells assessed as increase in G1 cell population at 1 to 10 uM by flow cytometric analysis | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1224784 | Delta TM value showing the stabilisation of PCTK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720066 | Millipore: Percentage of residual kinase activity of CDK5 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435731 | Percentage MNK2 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720309 | Millipore: Percentage of residual kinase activity of IRAK4 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720204 | Millipore: Percentage of residual kinase activity of PRKCI at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720315 | Millipore: Percentage of residual kinase activity of JAK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1624204 | Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID720031 | Millipore: Percentage of residual kinase activity of ABL1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436022 | Binding constant for full-length MEK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720110 | Millipore: Percentage of residual kinase activity of DAPK2 at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435962 | Percentage CDK2-cyclinA activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1427307 | Cell cycle arrest in human HuH7 cells assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.2 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720121 | Millipore: Percentage of residual kinase activity of EGFR at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1467665 | Cytotoxicity against human primary skin fibroblast cells assessed as cell viability at 10 uM after 48 hrs by CellTiter-Glo 2D assay relative to control | |||
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720247 | Millipore: Percentage of residual kinase activity of ROS1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435533 | Binding constant for NEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720446 | Millipore: Percentage of residual kinase activity of PAK3 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720145 | Millipore: Percentage of residual kinase activity of ERBB4 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 2.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720208 | Millipore: Percentage of residual kinase activity of PRKD2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1663867 | Stability of compound in cell culture medium assessed as compound hydrolysis measured after 3 hrs | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID1857286 | Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay | |||
| AID720022 | Millipore: Percentage of residual kinase activity of ACVR1B at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720470 | Millipore: Percentage of residual kinase activity of AKT3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436006 | Binding constant for full-length AURKC | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435287 | Binding constant for EPHA8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1224761 | Delta TM value showing the stabilisation of CLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720250 | Millipore: Percentage of residual kinase activity of RPS6KA1 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1765919 | Antiproliferative activity against human HeLa cells | 2021 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 48 | Discovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720198 | Millipore: Percentage of residual kinase activity of IGF1R at 10uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435900 | Binding constant for AKT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435562 | Binding constant for STK36 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720370 | Millipore: Percentage of residual kinase activity of SRPK3 at 1uM relative to control. Control inhibitor: Phosphoric acid* at 0.3uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435325 | Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720283 | Millipore: Percentage of residual kinase activity of SYK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% ?-mercaptoethanol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720465 | Millipore: Percentage of residual kinase activity of PRKACA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1624212 | Antiproliferative activity against human fibroblast cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID720062 | Millipore: Percentage of residual kinase activity of CDK3 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720353 | Millipore: Percentage of residual kinase activity of MINK1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1725762 | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability at 10 uM after 48 hrs by celltiter-glo 2D luminescent assay relative to control | |||
| AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720385 | Millipore: Percentage of residual kinase activity of MUSK at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435925 | Binding constant for PCTK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720366 | Millipore: Percentage of residual kinase activity of RPS6KA5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720255 | Millipore: Percentage of residual kinase activity of RPS6KA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435829 | Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720101 | Millipore: Percentage of residual kinase activity of CAMK2D at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM CaCl2, 16 ug/mL calmodulin | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435904 | Binding constant for full-length CSK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720113 | Millipore: Percentage of residual kinase activity of DDR2 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID507035 | Inhibition of v-Src expressed in mouse NIH/3T3 cells assessed as restoration of actin stress fiber at 2.5 uM after 24 hrs by FITC-conjugated DAPI staining | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID435790 | Binding constant for DRAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720372 | Millipore: Percentage of residual kinase activity of STK4 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1481075 | Inhibition of human JNK1 using ATF2 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID435189 | Binding constant for full-length PDPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1605959 | Inhibition of recombinant full length human C-terminal His-tagged HDAC3 (1 to 428 residues) expressed in baculovirus infected insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHKK(Ac)AMC) as substrate measured after 1 to 2 hrs by fluo | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1427303 | Cell cycle arrest in human NCI-H727 cells harboring p53 mutant assessed as mitotic index at 10 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 1.1 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435440 | Binding constant for PIM2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435798 | Binding constant for FGR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1177096 | Inhibition of human PI3KC2gamma by non-radiometric ADP-Glo assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1 | Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435747 | Percentage PRAK activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID720213 | Millipore: Percentage of residual kinase activity of PRKG1 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 10 uM cGMP | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1724540 | Inhibition of KDR (unknown origin) at 1 uM relative to control | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19 | Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. |
| AID1481072 | Inhibition of human CDK4/cyclinD1 using RB-CTF as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720183 | Millipore: Percentage of residual kinase activity of GSK3B at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720314 | Millipore: Percentage of residual kinase activity of JAK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID720473 | Millipore: Percentage of residual kinase activity of PRKCA at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720468 | Millipore: Percentage of residual kinase activity of AKT2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1327484 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate after 1 hr in presence of ATP by ADP-glo based luminescence assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor. |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1388807 | Inhibition of recombinant human N-terminal GST-tagged PI3Kalpha expressed in baculovirus expression system using PIP2 as substrate measured after 1 hr by Kinase-GLo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors. |
| AID1857283 | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate incubated for 2 hrs in presence of ATP by Kinase Glo luminescence assay | |||
| AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720175 | Millipore: Percentage of residual kinase activity of GRK5 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435677 | Binding constant for LOK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1605961 | Inhibition of recombinant C-terminal His-fusion tagged and N-terminal Streptavidin2-tagged human HDAC8 (1 to 377 residues) expressed in insect cells at 10 uM using fluorogenic peptide p53 residues 379-382 (RHK(Ac)K(Ac)AMC) as substrate measured after 1 to | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1300801 | Inhibition of mTOR (unknown origin) by lance ultra assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors. |
| AID435154 | Binding constant for DDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720400 | Millipore: Percentage of residual kinase activity of TEK at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA, 0.5 mM MnCl2 | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1605946 | Inhibition of HDAC9 (unknown origin) using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay | 2020 | Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8 | Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors. |
| AID1224793 | Delta TM value showing the stabilisation of RSK2a produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51 | A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID720475 | Millipore: Percentage of residual kinase activity of PRKCB at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 20 mM HEPES pH 7.4, 0.03% Triton X-100, 0.1 mM CaCl2, 0.1 mg/mL phosphatidylserine, 10 ug/mL diacylglycerol | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435225 | Percentage DYRK3 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1280670 | Inhibition of PI3K alpha (unknown origin) using PIP2 as substrate after 1 hr by kinase-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID720153 | Millipore: Percentage of residual kinase activity of FGFR3 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435152 | Binding constant for CAMK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720397 | Millipore: Percentage of residual kinase activity of TSSK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1481079 | Inhibition of human mTOR/FRAP1 using 4EBP1 as substrate in presence of [gamma-32P]ATP | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer. |
| AID683667 | Inhibition of PI3K p110alpha/p85alpha by fluorescence based immunoassay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID720126 | Millipore: Percentage of residual kinase activity of EPHA2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID638929 | Antiproliferative activity against human MCF7 cells | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID435290 | Binding constant for FGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720240 | Millipore: Percentage of residual kinase activity of ROCK2 at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 50 mM Tris pH 7.5, 0.1 mM EGTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID435493 | Percentage PKD1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1663887 | Drug concentration in ovariectomized nu/nu mouse plasma at 10 mg/kg, po measured after 8 hrs by UHPLC-MS analysis | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. |
| AID435375 | Percentage RSK1 activity remaining in the presence of 1uM inhibitor | 2007 | The Biochemical journal, Dec-15, Volume: 408, Issue:3 | The selectivity of protein kinase inhibitors: a further update. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID720169 | Millipore: Percentage of residual kinase activity of CSF1R at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID1427319 | Cell cycle arrest in human HaCaT cells harboring wild-type p53 assessed as mitotic index at 25 uM measured after 48 hrs by Hoechst staining based fluorescence assay (Rvb = 2.6 No_unit) | 2017 | Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6 | Mechanisms of action and structure-activity relationships of cytotoxic flavokawain derivatives. |
| AID720054 | Millipore: Percentage of residual kinase activity of BRSK2 at 10uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID683673 | Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis and biological evaluation of new 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles as PI3Kα inhibitors. |
| AID1280672 | Inhibition of PI3K gamma (unknown origin) after 1 hr by ADP-Glo luminescent assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents. |
| AID435399 | Binding constant for DCAMKL3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID1624208 | Antiproliferative activity against human NCI-H727 cells after 48 hrs by Hoechst 33342 staining-based assay | 2019 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 29, Issue:5 | Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents. |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1065014 | Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Crystal Structures of PI3Kα Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design. |
| AID436020 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID435645 | Binding constant for ACVRL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1 | A quantitative analysis of kinase inhibitor selectivity. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1725753 | Inhibition of human mTOR using 4EBP1 as substrate after 120 mins by [gamma-33P]-ATP assay | |||
| AID720326 | Millipore: Percentage of residual kinase activity of LIMK1 at 1uM relative to control. Control inhibitor: Staurosporine at 100.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA | 2013 | The Biochemical journal, Apr-15, Volume: 451, Issue:2 | A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| 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. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| AID1345749 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha (Phosphatidylinositol kinases) | 2009 | Molecular cancer therapeutics, Jul, Volume: 8, Issue:7 | Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. |
| AID1346204 | Human DNA-dependent protein kinase catalytic subunit (Other PIKK family kinases) | 2009 | Molecular cancer therapeutics, Jul, Volume: 8, Issue:7 | Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. |
| AID1345778 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases) | 2009 | Molecular cancer therapeutics, Jul, Volume: 8, Issue:7 | Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. |
| AID1345726 | Human mechanistic target of rapamycin kinase (FRAP subfamily) | 2009 | Molecular cancer therapeutics, Jul, Volume: 8, Issue:7 | Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. |
| AID1345748 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases) | 2009 | Molecular cancer therapeutics, Jul, Volume: 8, Issue:7 | Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. |
| AID1345786 | Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma (Phosphatidylinositol kinases) | 2009 | Molecular cancer therapeutics, Jul, Volume: 8, Issue:7 | Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. |
| AID1345764 | Human phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta (Phosphatidylinositol kinases) | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. |
| AID1798508 | Scintillation Proximity Assay from Article 10.1016/j.bmc.2007.05.070: \\Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.\\ | 2007 | Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17 | Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. |
| AID1799846 | Radiometric Filtration Assay from Article 10.1021/bi100673c: \\Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.\\ | 2010 | Biochemistry, Oct-05, Volume: 49, Issue:39 | Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. |
| AID1799847 | TR-FRET Assay from Article 10.1021/bi100673c: \\Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.\\ | 2010 | Biochemistry, Oct-05, Volume: 49, Issue:39 | Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2010 | Science (New York, N.Y.), Mar-26, Volume: 327, Issue:5973 | Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34. |
| [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 | 27 (14.92) | 29.6817 |
| 2010's | 129 (71.27) | 24.3611 |
| 2020's | 25 (13.81) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (32.88) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 4 (2.21%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 177 (97.79%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||