ChEMBL ligand: CHEMBL226838 (SB-505124)
activin A receptor type 1B/Activin receptor type-1B in Human [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] There should be some charts here, you may need to enable JavaScript!
transforming growth factor beta receptor 1 in Human [GtoPdb: 1788] [UniProtKB: P36897] transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Mouse [ChEMBL: CHEMBL2021750] [GtoPdb: 1788] [UniProtKB: Q64729] There should be some charts here, you may need to enable JavaScript!
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] 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
activin A receptor type 1B/Activin receptor type-1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5310] [GtoPdb: 1787] [UniProtKB: P36896]
ChEMBL	Inhibition of ALK4 (unknown origin) by radioisotopic assay	B	7.15	pIC50	70	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL	Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay	B	6.18	pIC50	668	nM	IC50	Bioorg Med Chem Lett (2015) 25: 5228-5231 [PMID:26483198]
ChEMBL	Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay	B	6.23	pIC50	594	nM	IC50	Bioorg Med Chem (2011) 19: 2633-2640 [PMID:21435890]
ChEMBL	Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay	B	6.23	pIC50	594	nM	IC50	Eur J Med Chem (2012) 57: 74-84 [PMID:23047226]
ChEMBL	Inhibition of recombinant human p38-alpha expressed in Escherichia coli using ATF2 as substrate by radioisotope-based assay	B	6.23	pIC50	590	nM	IC50	Bioorg Med Chem (2014) 22: 2724-2732 [PMID:24704197]
ChEMBL	Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by radioisotopic assay	B	6.23	pIC50	590	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL	Inhibition of RIPK2 (unknown origin) by radioisotopic assay	B	6.16	pIC50	685	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]
transforming growth factor beta receptor 1 in Human [GtoPdb: 1788] [UniProtKB: P36897]
GtoPdb	Assay used purified human TGFβR1 kinase domain produced in Sf9 insect cells.	-	7.27	pIC50	54	nM	IC50	Eur J Med Chem (2011) 46: 3917-25 [PMID:21696866]
transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2021750] [GtoPdb: 1788] [UniProtKB: Q64729]
ChEMBL	Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	B	7.12	pIC50	76.6	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL	Antagonistic activity at TGFBR1	F	1.33	pIC50	-1.33	-	logIC50	Bioorg Med Chem Lett (2010) 20: 1918-1923 [PMID:20176484]
ChEMBL	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	B	6.77	pIC50	169	nM	IC50	Bioorg Med Chem (2010) 18: 4459-4467 [PMID:20472445]
ChEMBL	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay	B	7.26	pIC50	54.4	nM	IC50	Eur J Med Chem (2012) 57: 74-84 [PMID:23047226]
ChEMBL	Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay	B	7.27	pIC50	54	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]
ChEMBL	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells	B	7.27	pIC50	54	nM	IC50	Bioorg Med Chem (2011) 19: 2633-2640 [PMID:21435890]
ChEMBL	Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay	B	7.27	pIC50	54	nM	IC50	Bioorg Med Chem (2014) 22: 2724-2732 [PMID:24704197]
GtoPdb	Assay used purified human TGFβR1 kinase domain produced in Sf9 insect cells.	-	7.27	pIC50	54	nM	IC50	Eur J Med Chem (2011) 46: 3917-25 [PMID:21696866]
ChEMBL	Inhibition of GST-tagged ALK5 kinase domain (unknown origin) using GST-tagged SMAD3 as substrate in presence of [33P] gammaATP by liquid scintillation counter method	B	7.33	pIC50	47	nM	IC50	Bioorg Med Chem Lett (2019) 29: 2070-2075 [PMID:31303386]
ChEMBL	Inhibition of ALK5 assessed as inhibition of immobilized Smad3 phosphorylation	B	7.33	pIC50	47	nM	IC50	Bioorg Med Chem Lett (2009) 19: 4868-4872 [PMID:19616940]
ChEMBL	Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay	B	7.36	pIC50	43.8	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]
ChEMBL	Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay	B	7.46	pIC50	34.9	nM	IC50	Bioorg Med Chem Lett (2015) 25: 5228-5231 [PMID:26483198]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL	Inhibition of VEGFR2 (unknown origin) by radioisotopic assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2014) 57: 4213-4238 [PMID:24786585]

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]