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ChEMBL ligand: CHEMBL7550 (L-158809) |
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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 | Compound was tested for in vitro for AII receptor antagonistic activity in bovine adrenal cortex. | F | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1709-1714 |
Angiotensin II type 1a (AT-1a) receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3948] [UniProtKB: P34976] | ||||||||
ChEMBL | Inhibition of Angiotensin II receptor type 1 in rabbit aorta binding assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 189-194 |
ChEMBL | In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII. | F | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (1993) 36: 4239-4249 [PMID:8277506] |
ChEMBL | Displacement of [1251][Sar1,IIe8]AII from rabbit aorta Angiotensin II receptor, type 1 | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (1993) 36: 3738-3742 [PMID:8246245] |
ChEMBL | In vitro antagonist activity against angiotensin II receptor type 1 in rabbit aorta using [125I]-Sar, Ile AII. | F | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (1993) 36: 4230-4238 [PMID:8277505] |
ChEMBL | In vitro binding affinity towards Angiotensin II type 1-AT1 receptor determined as its ability to displace 125I-Sarl,Ile8-AII from the receptor expressed in rabbit aorta membrane. | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1693-1696 |
ChEMBL | Binding affinity evaluated by its ability to displace the specific binding ligand 125I-SAR1, Ile8-AII from Angiotensin II receptor, type 1 in rabbit aorta membrane | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 207-212 |
ChEMBL | Inhibitory activity was evaluated against Angiotensin II receptor, type 1 in rabbit aorta | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1996) 39: 625-656 [PMID:8576904] |
ChEMBL | Inhibition of Angiotensin II receptor, type 1 | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1993) 36: 2051-2058 [PMID:8340909] |
ChEMBL | Binding affinity to angiotensin AT1 receptor in rabbit aortic rings | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem (2010) 18: 8418-8456 [PMID:21071232] |
ChEMBL | In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1994) 37: 4068-4072 [PMID:7990105] |
ChEMBL | Displacement of the specific binding ligand [125I]Sar1,Ile8-AII from Angiotensin II receptor, type 1 in rabbit aorta membrane. | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 41-44 |
ChEMBL | In vitro binding affinity determined by its ability to displace the specific binding ligand [125I]-Sar1, Ile8-AII from Angiotensin II receptor, type 1 in rabbit aorta membranes | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 17-22 |
ChEMBL | Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1 | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1993) 36: 591-609 [PMID:8496939] |
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052] | ||||||||
ChEMBL | Binding affinity to angiotensin AT2 receptor | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2010) 18: 8418-8456 [PMID:21071232] |
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351] | ||||||||
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] |
ChEMBL | In vitro binding affinity towards Angiotensin II receptor, type 2 determined as its ability to displace 125I-Sarl,Ile8-AII from the receptor expressed in rat midbrain membrane. | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1693-1696 |
ChEMBL | In vitro antagonist activity against angiotensin II receptor type 2 in rat midbrain using [125I]-Sar,Ile AII. | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1993) 36: 4230-4238 [PMID:8277505] |
ChEMBL | In vitro antagonist activity against angiotensin II type 2 (AT2) receptor in rat midbrain using [125I]- Sar, Ile AII. | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1993) 36: 4239-4249 [PMID:8277506] |
ChEMBL | In vitro binding affinity determined by its ability to displace the specific binding ligand [125I]-Sar1, Ile8-AII from AT2 receptor in rat midbrain membranes | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 17-22 |
ChEMBL | Displacement of [1251][Sar1,IIe8]AII from rat midbrain angiotensin II (AT2) receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1993) 36: 3738-3742 [PMID:8246245] |
ChEMBL | Inhibition of rat midbrain angiotensin II type 2 receptor | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 189-194 |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
ChEMBL | Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay | B | 4.7 | pEC50 | >20000 | nM | EC50 | J Med Chem (2011) 54: 4219-4233 [PMID:21557540] |
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095] | ||||||||
GtoPdb | - | - | 9.18 | pKd | 0.66 | nM | Kd | Mol Pharmacol (1992) 42: 1077-82 [PMID:1480133] |
ChEMBL | Binding affinity against angiotensin II receptor from rat liver | B | 9.35 | pKi | 0.45 | nM | Ki | J Med Chem (1993) 36: 2676-2688 [PMID:8410980] |
ChEMBL | Displacement of [125I]Sar1,Ile8-Ang2 from AT1 receptor in Wistar rat hepatic membrane | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2008) 51: 2137-2146 [PMID:18318468] |
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
ChEMBL | Displacement of [125I]Tyr4-Sar1,Ile8-Angiotensin II from human Angiotensin 1 receptor after 60 mins by scintillation counting | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2011) 54: 4219-4233 [PMID:21557540] |
ChEMBL | Antagonist activity at angiotensin 1 receptor | F | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
AT1 receptor in Rat [GtoPdb: 34] [UniProtKB: P29089, P25095] | ||||||||
GtoPdb | - | - | 9.18 | pKd | 0.66 | nM | Kd | Mol Pharmacol (1992) 42: 1077-82 [PMID:1480133] |
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089] | ||||||||
GtoPdb | - | - | 9.18 | pKd | 0.66 | nM | Kd | Mol Pharmacol (1992) 42: 1077-82 [PMID:1480133] |
ChEMBL | Binding affinity for rat angiotensin II receptor, type 1 | B | 9.4 | pIC50 | 0.4 | 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]