valsartan [Ligand Id: 3937] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1069 (CGP 48933, CGP-48933, Diovan, Exforge, NSC-758927, Prexxartan, Valsartan) |
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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 | Displacement of Europium-labeled angiotensin-2 from human AT2 receptor expressed in CHOK1 cell membranes after 120 mins by DELFIA | B | 5 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2019) 10: 86-91 [PMID:30655952] |
| BLT2 receptor/Leukotriene B4 receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1] | ||||||||
| ChEMBL | Agonist activity at human BLT2 overexpressed in CHO-K1 cells assessed as accumulation of inositol monophosphate measured after 90 mins by HTRF assay | F | 4.8 | pEC50 | 16000 | nM | EC50 | ACS Med Chem Lett (2021) 12: 1261-1266 [PMID:34413955] |
| Platelet glycoprotein VI (GPVI) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308912] [UniProtKB: Q9HCN6] | ||||||||
| ChEMBL | Binding affinity to recombinant GP6 (unknown origin) at protein to compound ratio of 1 : 1 to 1 : 10 by 2D 15N-1H TROSY-HSQC NMR spectroscopy | B | 4 | pKd | 100000 | nM | Kd | J Med Chem (2020) 63: 12213-12242 [PMID:32463237] |
| AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| GtoPdb | - | - | 8.61 | pIC50 | 2.43 | nM | IC50 | Regul Pept (1995) 59: 303-11 [PMID:8577935] |
| AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095] | ||||||||
| ChEMBL | Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membrane | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2008) 51: 2137-2146 [PMID:18318468] |
| ChEMBL | Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay | B | 5 | pEC50 | >10000 | 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] | ||||||||
| ChEMBL | Inhibition constant against Angiotensin II receptor, type 1 was determined | B | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (2003) 46: 2261-2270 [PMID:12773029] |
| ChEMBL | Displacement of [125I-Sar1-Ile8]-Ang2 from human angiotensin 2 receptor type 1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis | B | 8.52 | pKi | 3 | nM | Ki | Eur J Med Chem (2018) 145: 273-290 [PMID:29329002] |
| ChEMBL | Displacement of [125-I]-[Sar1, AngII from AT1R (unknown origin) expressed in Escherichia coli BL 21 (DE3) incubated for 2 hrs by radioimmunoassay | B | 8.13 | pIC50 | 7.4 | nM | IC50 | J Med Chem (2021) 64: 4196-4205 [PMID:33784102] |
| ChEMBL | Tested for inhibition of Angiotensin II receptor, type 1 in the absence of bovine serum albumin (BSA) | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 29-34 |
| GtoPdb | - | - | 8.61 | pIC50 | 2.43 | nM | IC50 | Regul Pept (1995) 59: 303-11 [PMID:8577935] |
| ChEMBL | Agonist activity at human AT1R expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay | B | 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 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) |
| AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| GtoPdb | - | - | 8.61 | pIC50 | 2.43 | nM | IC50 | Regul Pept (1995) 59: 303-11 [PMID:8577935] |
| AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089] | ||||||||
| ChEMBL | Binding affinity for rat angiotensin II receptor, type 1 | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2004) 47: 2574-2586 [PMID:15115399] |
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]
