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 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]