TRV027 [Ligand Id: 6902] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4297447 (Sar-val-tyr-ile-his-pro-d-ala-oh, Trv027, TRV 027, TRV-027, TRV027, Trv-120027, Trv120027)
  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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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
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 7.72 pKd 19 nM Kd J Pharmacol Exp Ther (2010) 335: 572-9 [PMID:20801892]
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
ChEMBL Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay F 5 pEC50 >10000 nM EC50 US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null)
ChEMBL Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay B 7.8 pEC50 16 nM EC50 US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null)
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 7.72 pKd 19 nM Kd J Pharmacol Exp Ther (2010) 335: 572-9 [PMID:20801892]
ChEMBL Agonist activity at human AT1R expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay F 5 pEC50 >10000 nM EC50 US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null)
ChEMBL Agonist activity at human AT1R expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay B 7.77 pEC50 17 nM EC50 US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null)

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]