TRV023 [Ligand Id: 11943] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4438122 |
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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 | Receptor binding | - | 8.64 | pKi | - | - | - | Cell (2019) 176: 468-478.e11 [PMID:30639099] |
| GtoPdb | β-arrestin recruitment assay | - | 5.68 | pEC50 | 2100 | nM | EC50 | US8486885B2. β-arrestin effectors and compositions and methods of use thereof (2013) |
| 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 60 mins by luminescence based beta-arrestin recruitment assay | B | 7.41 | pEC50 | 39 | 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 30 mins by IP1 accumulation assay | F | 7.96 | pEC50 | 11 | 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 | Receptor binding | - | 8.64 | pKi | - | - | - | Cell (2019) 176: 468-478.e11 [PMID:30639099] |
| 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) |
| GtoPdb | β-arrestin recruitment assay | - | 5.68 | pEC50 | 2100 | nM | EC50 | US8486885B2. β-arrestin effectors and compositions and methods of use thereof (2013) |
| ChEMBL | Agonist activity at human AT1 receptor assessed as increase in beta-arrestin recruitment by chemiluminescent assay | B | 7.36 | pEC50 | 44 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at human AT1R expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay | B | 7.36 | pEC50 | 44 | 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]
