ML221 [Ligand Id: 6282] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2158347
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414]
ChEMBL Antagonist activity at APJ receptor expressed in CHOK1 cells assessed as inhibition of apelin13-induced beta-arrestin recruitment after 90 mins by luminescence assay F 5.76 pIC50 1750 nM IC50 Bioorg Med Chem Lett (2012) 22: 6656-6660 [PMID:23010269]
ChEMBL Antagonist activity at APJ receptor assessed as inhibition of apelin13-induced cAMP accumulation F 6.15 pIC50 700 nM IC50 Bioorg Med Chem Lett (2012) 22: 6656-6660 [PMID:23010269]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Inhibition of AT1 receptor B 4.1 pIC50 >79000 nM IC50 Bioorg Med Chem Lett (2012) 22: 6656-6660 [PMID:23010269]

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]