compound 9 [PMID: 26006010] [Ligand Id: 9761] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3702836
  • ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • erb-b2 receptor tyrosine kinase 4 in Human [GtoPdb: 1799] [UniProtKB: Q15303]
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  • BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
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  • BMX non-receptor tyrosine kinase in Human [GtoPdb: 1942] [UniProtKB: P51813]
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  • tec protein tyrosine kinase in Human [GtoPdb: 2238] [UniProtKB: P42680]
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  • TXK tyrosine kinase in Human [GtoPdb: 2268] [UniProtKB: P42681]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812]
ChEMBL Binding affinity to RPS6KA3 (unknown origin) B 9.27 pKd 0.54 nM Kd Eur J Med Chem (2018) 151: 315-326 [PMID:29631132]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Caliper-Based Kinase Assay: A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of the present disclosure. Serial dilutions of test compounds were incubated with human recombinant Btk (0.5 nM), ATP (16 μM) and a phosphoacceptor peptide substrate FAM-GEEPLYWSFPAKKK-NH2 (1 μM) at room temperature for 3 h. The reaction was then terminated with EDTA, final concentration 20 mM and the phosphorylated reaction product was quantified on a Caliper Desktop Profiler (Caliper LabChip 3000). B 8.68 pIC50 2.1 nM IC50 US-8940744-B2. Pyrazolopyrimidine compounds as kinase inhibitors (2015)
ChEMBL Caliper-Based Kinase Assay: A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of the present disclosure. Serial dilutions of test compounds were incubated with human recombinant Btk (0.5 nM), ATP (16 μM) and a phosphoacceptor peptide substrate FAM-GEEPLYWSFPAKKK-NH2 (1 μM) at room temperature for 3 h. The reaction was then terminated with EDTA, final concentration 20 mM and the phosphorylated reaction product was quantified on a Caliper Desktop Profiler (Caliper LabChip 3000). B 8.68 pIC50 2.1 nM IC50 US-9266895-B2. Substituted pyrazolo[3,4-d]pyrimidines as kinase inhibitors (2016)
GtoPdb - - 8.72 pIC50 1.9 nM IC50 Nat. Chem. Biol. (2015) 11: 525-31 [PMID:26006010]
ChEMBL Inhibition of BTK (unknown origin) B 8.72 pIC50 1.9 nM IC50 Eur J Med Chem (2018) 151: 315-326 [PMID:29631132]
erb-b2 receptor tyrosine kinase 4 in Human [GtoPdb: 1799] [UniProtKB: Q15303]
GtoPdb - - 7.19 pIC50 65 nM IC50 Nat. Chem. Biol. (2015) 11: 525-31 [PMID:26006010]
BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451]
GtoPdb - - 7.17 pIC50 68 nM IC50 Nat. Chem. Biol. (2015) 11: 525-31 [PMID:26006010]
BMX non-receptor tyrosine kinase in Human [GtoPdb: 1942] [UniProtKB: P51813]
GtoPdb - - 8.12 pIC50 7.6 nM IC50 Nat. Chem. Biol. (2015) 11: 525-31 [PMID:26006010]
tec protein tyrosine kinase in Human [GtoPdb: 2238] [UniProtKB: P42680]
GtoPdb - - 8.47 pIC50 3.4 nM IC50 Nat. Chem. Biol. (2015) 11: 525-31 [PMID:26006010]
TXK tyrosine kinase in Human [GtoPdb: 2268] [UniProtKB: P42681]
GtoPdb - - 7.39 pIC50 41 nM IC50 Nat. Chem. Biol. (2015) 11: 525-31 [PMID:26006010]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]