BMS pyrazole inhibitor 7f [Ligand Id: 7030] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL468927
  • coactivator associated arginine methyltransferase 1/Histone-arginine methyltransferase CARM1 in Human [ChEMBL: CHEMBL5406] [GtoPdb: 1255] [UniProtKB: Q86X55]
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  • protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
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  • protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coactivator associated arginine methyltransferase 1/Histone-arginine methyltransferase CARM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5406] [GtoPdb: 1255] [UniProtKB: Q86X55]
ChEMBL Inhibition of CARM1 assessed as blockade of histone H3 methylation B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2009) 19: 2924-2927 [PMID:19419866]
GtoPdb - - 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2009) 19: 2924-7 [PMID:19419866]
ChEMBL Inhibition of human CARM1 assessed as inhibition of histone3 methylation B 10.4 pIC50 0.04 nM IC50 Bioorg Med Chem Lett (2009) 19: 5063-5066 [PMID:19632837]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Inhibition of human PXR B 4.6 pEC50 >25000 nM EC50 Bioorg Med Chem Lett (2009) 19: 2924-2927 [PMID:19419866]
protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873]
ChEMBL Inhibition of PRMT1 by methylation assay B 4.6 pIC50 >25000 nM IC50 Bioorg Med Chem Lett (2009) 19: 2924-2927 [PMID:19419866]
protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
ChEMBL Inhibition of PRMT3 by methylation assay B 4.6 pIC50 >25000 nM IC50 Bioorg Med Chem Lett (2009) 19: 2924-2927 [PMID:19419866]

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]