valsartan [Ligand Id: 3937] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1069 (CGP-48933, Exforge, Valsartan, Prexxartan, CGP 48933, Diovan)
  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
  • This target only has 1 pki data point
  • 5
1 CHEMBL1069_lig_chart_1 Angiotensin II type 2 (AT-2) receptor Human
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  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
  • This target only has 0 pki data point
  • 0
2 CHEMBL1069_lig_chart_2 AT1 receptor HumanRat
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
  • 6.93
3 CHEMBL1069_lig_chart_3 Type-1 angiotensin II receptor Human
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  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor/Type-1B angiotensin II receptor in Rat [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1069_lig_chart_4 AT1 receptor HumanRat
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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]
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 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]