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 (2013)
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 (2013)
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 (2013)
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 (2013)

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]