[3H]L158809 [Ligand Id: 3939] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7550 (L-158809)
  • 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 Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Rat [ChEMBL: CHEMBL257] [GtoPdb: 35] [UniProtKB: P35351]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • AT1 receptor/Type-1A angiotensin II receptor in Rat [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
  • AT1 receptor in Rat [GtoPdb: 34] [UniProtKB: P29089P25095]
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  • 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 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: P29089P25095]
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]