EXP3174 [Ligand Id: 586] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL907 (E-3174)
  • Angiotensin II type 1a (AT-1a) receptor in Bovine [ChEMBL: CHEMBL3374] [UniProtKB: P25104]
  • Angiotensin II type 1a (AT-1a) receptor in Rabbit [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
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  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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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]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Angiotensin II type 1a (AT-1a) receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3374] [UniProtKB: P25104]
ChEMBL In vitro for inhibition of [125I]-angiotensin II (0.1 nM) binding to angiotensin II receptor type 1 in membrane fractions of bovine adrenal cortex B 7.66 pIC50 22 nM IC50 J Med Chem (1996) 39: 323-338 [PMID:8568823]
ChEMBL Inhibition of [125l]-All binding to bovine adrenal cortex B 7.66 pIC50 22 nM IC50 Bioorg Med Chem Lett (1994) 4: 177-182
Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976]
ChEMBL Antagonist activity at angiotensin AT1 receptor in rabbit aorta assessed as reduction of angiotensin 2-induced contractile response F 10.09 pKd 0.08 nM Kd Bioorg Med Chem (2010) 18: 8418-8456 [PMID:21071232]
ChEMBL In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA) F 7.43 pIC50 37 nM IC50 J Med Chem (1993) 36: 2558-2568 [PMID:8355255]
ChEMBL In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta B 8.22 pIC50 6 nM IC50 J Med Chem (1994) 37: 4068-4072 [PMID:7990105]
ChEMBL Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1 B 8.22 pIC50 6 nM IC50 J Med Chem (1993) 36: 591-609 [PMID:8496939]
ChEMBL In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA) F 8.22 pIC50 6 nM IC50 J Med Chem (1993) 36: 2558-2568 [PMID:8355255]
ChEMBL Evaluation of Angiotensin II antagonistic activity by displacement of [125I]-Sar Ile-AII at the rabbit aorta Angiotensin II receptor, type 1 F 8.55 pIC50 2.8 nM IC50 J Med Chem (1993) 36: 3595-3605 [PMID:8246227]
ChEMBL In vitro inhibitory activity against angiotensin II rabbit aorta AT1 receptor using radioligand [125I]-Sar Ile-AII B 8.55 pIC50 2.8 nM IC50 J Med Chem (1994) 37: 2808-2824 [PMID:8064808]
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351]
ChEMBL In vitro inhibitory activity against angiotensin II rat midbrain AT2 receptor using radioligand [125I]-Sar Ile-AII B 4.3 pIC50 >50000 nM IC50 J Med Chem (1994) 37: 2808-2824 [PMID:8064808]
ChEMBL In vitro binding affinity for angiotensin II AT2 receptor in rat midbrain B 4.3 pIC50 50000 nM IC50 J Med Chem (1994) 37: 4068-4072 [PMID:7990105]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Inhibition of ATR1 (unknown origin) B 8.7 pIC50 2 nM IC50 J Med Chem (2019) 62: 8915-8930 [PMID:31083946]
GtoPdb - - 9.49 pIC50 0.32 nM IC50 Br J Pharmacol (1999) 126: 1057-65 [PMID:10193788];
Pharmacol Rev (1993) 45: 205-51 [PMID:8372104]
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 9.49 pIC50 0.32 nM IC50 Br J Pharmacol (1999) 126: 1057-65 [PMID:10193788];
Pharmacol Rev (1993) 45: 205-51 [PMID:8372104]
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
ChEMBL In vitro antagonistic activity by displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta Angiotensin II receptor, type 1 F 7.43 pIC50 37 nM IC50 J Med Chem (1993) 36: 591-609 [PMID:8496939]
ChEMBL Concentration required to inhibit binding of radioligand [125I]AII to Angiotensin II receptor, type 1 in rat adrenal glomerulosa tissue B 7.96 pIC50 11 nM IC50 J Med Chem (1992) 35: 2658-2667 [PMID:1635064]
ChEMBL Binding affinity against AT1 receptor in the presence of 0.01% BSA B 8.74 pIC50 1.8 nM IC50 J Med Chem (1994) 37: 1632-1645 [PMID:8201597]

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]