ChEMBL ligand: CHEMBL3702836
ribosomal protein S6 kinase A3/Ribosomal protein S6 kinase alpha 3 in Human [ChEMBL: CHEMBL2345] [GtoPdb: 1528] [UniProtKB: P51812] There should be some charts here, you may need to enable JavaScript!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
erb-b2 receptor tyrosine kinase 4 in Human [GtoPdb: 1799] [UniProtKB: Q15303] There should be some charts here, you may need to enable JavaScript!
BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451] There should be some charts here, you may need to enable JavaScript!
BMX non-receptor tyrosine kinase in Human [GtoPdb: 1942] [UniProtKB: P51813] There should be some charts here, you may need to enable JavaScript!
tec protein tyrosine kinase in Human [GtoPdb: 2238] [UniProtKB: P42680] There should be some charts here, you may need to enable JavaScript!
TXK tyrosine kinase in Human [GtoPdb: 2268] [UniProtKB: P42681] There should be some charts here, you may need to enable JavaScript!

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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]