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ChEMBL ligand: CHEMBL907 (E-3174) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]