[3H]valsartan [Ligand Id: 593] 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 | - | - | 9 | pIC50 | 1 | nM | IC50 | Fundam Clin Pharmacol (2000) 14: 577-585 [PMID:11206708] |
| 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 (2013) |
| 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 | - | - | 9 | pIC50 | 1 | nM | IC50 | Fundam Clin Pharmacol (2000) 14: 577-585 [PMID:11206708] |
| 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 (2013) |
| 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) |
| AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Fundam Clin Pharmacol (2000) 14: 577-585 [PMID:11206708] |
| 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 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]
