olodanrigan [Ligand Id: 8374] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL34124 (Ema401, EMA-401, EMA401, Olodanrigan, PD-126055)
  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
  • AT2 receptor in Rat [GtoPdb: 35] [UniProtKB: P35351]
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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
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
ChEMBL Binding affinity to type-2 angiotensin-2 receptor (unknown origin) B 7.4 pKi 39.5 nM Ki Bioorg Med Chem Lett (2016) 26: 1355-1359 [PMID:26810314]
ChEMBL Inhibition of human AT2 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2020) 63: 1978-1995 [PMID:32030982]
ChEMBL Inhibitory activity was evaluated against Angiotensin II receptor, type 2 B 9.22 pIC50 0.6 nM IC50 J Med Chem (1996) 39: 625-656 [PMID:8576904]
ChEMBL In vitro binding affinity of compound was measured against angiotensin II (AT2) receptor B 9.24 pIC50 0.58 nM IC50 Bioorg Med Chem Lett (1994) 4: 1479-1484
GtoPdb - - 9.3 pIC50 - - IC50 Lancet (2014) 383: 1637-47 [PMID:24507377];
Pain Med (2013) 14: 692-705 [PMID:23489258];
Lancet (2014) 383: 1613-4 [PMID:24507378]
AT2 receptor in Rat [GtoPdb: 35] [UniProtKB: P35351]
GtoPdb - - 7.53 pIC50 29.5 nM IC50 Pain Med (2013) 14: 692-705 [PMID:23489258]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Inhibition of human AT1 receptor B 7.41 pIC50 39 nM IC50 J Med Chem (2020) 63: 1978-1995 [PMID:32030982]

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]