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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 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]