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 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]