compound 26 [PMID: 21733693] [Ligand Id: 8783] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1808264
  • activin A receptor type 2B/Activin receptor type-2B in Human [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705]
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  • nuclear receptor coactivator 1/Nuclear receptor coactivator 1 in Human [ChEMBL: CHEMBL1615387] [GtoPdb: 2693] [UniProtKB: Q15788]
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  • erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
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  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
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  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
activin A receptor type 2B/Activin receptor type-2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5466] [GtoPdb: 1792] [UniProtKB: Q13705]
ChEMBL Inhibition of ACTR-2B B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
nuclear receptor coactivator 1/Nuclear receptor coactivator 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615387] [GtoPdb: 2693] [UniProtKB: Q15788]
GtoPdb - - 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-40 [PMID:21733693]
ChEMBL Inhibition of Src1 B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
ChEMBL Inhibition of ErbB4 B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL Inhibition of B-Raf V600E mutant (unknown origin) using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay B 8.42 pIC50 3.8 nM IC50 Medchemcomm (2017) 8: 1835-1844 [PMID:30108894]
ChEMBL Inhibition of B-Raf V600E mutant B 8.42 pIC50 3.8 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
ChEMBL Inhibition of B-Raf V600E mutant (unknown origin) using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay B 8.42 pIC50 3.8 nM IC50 Medchemcomm (2017) 8: 1835-1844 [PMID:30108894]
ChEMBL Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as reduction of ERK phosphorylation after 1 hr B 7.64 pEC50 23 nM EC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Inhibition of ALK5 B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of Btk B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of Lck B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of Lyn B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2011) 21: 4436-4440 [PMID:21733693]

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]