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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]