angiotensin II [Ligand Id: 2504] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL408403 (Angiotensin ii (human type), Angiotensin Ii, LJPC-501)
  • Angiotensin II type 1a (AT-1a) receptor in Bovine [ChEMBL: CHEMBL3374] [UniProtKB: P25104]
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  • AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
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  • AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
  • 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]
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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 Dissociation constant for [125 I] Ang binding to type 1 Angiotensin II receptor of bovine adrenocortical membranes B 8.24 pKd 5.75 nM Kd J. Med. Chem. (1997) 40: 3271-3279 [PMID:9379447]
AT2 receptor/Angiotensin II type 2 (AT-2) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4607] [GtoPdb: 35] [UniProtKB: P50052]
GtoPdb - - 10.2 pKd - - - Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Biochem. Biophys. Res. Commun. (1989) 163: 284-91 [PMID:2775266];
Curr. Opin. Nephrol. Hypertens. (1994) 3: 112-22 [PMID:7850406]
ChEMBL Displacement of [125I]-Ang II from pig uterus myometrium angiotensin II type 2 (AT2) receptor B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2004) 47: 6009-6019 [PMID:15537355]
ChEMBL Displacement of [125I]Ang2 from AT2 receptor in pig uterus myometrium B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2006) 49: 6133-6137 [PMID:17004728]
ChEMBL Displacement of [125I]Ang2 from AT2 receptor in pig uterus myometrial membrane B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2007) 50: 1711-1715 [PMID:17358051]
ChEMBL Displacement of [125I]-Ang II from angiotensin II receptor type 2 in pig uterus myometrium B 9.64 pKi 0.23 nM Ki J. Med. Chem. (2005) 48: 4009-4024 [PMID:15943474]
ChEMBL Binding affinity for Angiotensin II receptor type 2 using [125I]- Ang II in pig uterus myometrium B 9.64 pKi 0.23 nM Ki J. Med. Chem. (2004) 47: 859-870 [PMID:14761188]
ChEMBL Binding affinity for angiotensin II receptor, type 2 in pig uterus myometrium using [125I]-Ang II as radioligand, in pH 7.4 Tris-HCl buffer for 1.5 hr at 25 degree C B 9.7 pKi 0.2 nM Ki J. Med. Chem. (2005) 48: 6620-6631 [PMID:16220978]
ChEMBL Binding affinity to type-2 angiotensin-2 receptor (unknown origin) B 9.7 pKi 0.2 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 1355-1359 [PMID:26810314]
ChEMBL In vitro binding affinity at angiotensin II (type 2) receptor in rabbit uterus. B 8.6 pIC50 2.5 nM IC50 J. Med. Chem. (1993) 36: 1902-1913 [PMID:8515427]
ChEMBL Displacement of [125I]CGP 42112A from human recombinant AT2 receptor expressed in HEK293 cells measured after 4 hrs by scintillation counting method B 10.1 pIC50 0.08 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 9.3 pIC50 - - - Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Br. J. Pharmacol. (1999) 126: 1057-65 [PMID:10193788]
AT1 receptor/Type-1A angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL329] [GtoPdb: 34] [UniProtKB: P25095]
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 Binding affinity was determined against Angiotensin II receptor, type 1 B 8.7 pKd 2 nM Kd J. Med. Chem. (1996) 39: 2738-2744 [PMID:8709104]
ChEMBL Displacement of [125I][Sar1,Ile8]Ang2 from wild-type human AT1 receptor expressed in CHO cells by gamma counting B 9.05 pKi 0.9 nM Ki J. Med. Chem. (2010) 53: 2063-2075 [PMID:20146480]
ChEMBL Displacement of [125I][Sar1,Ile8]Ang2 from human AT1 receptor N111G constitutively active mutant expressed in CHO cells by gamma counting B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2010) 53: 2063-2075 [PMID:20146480]
ChEMBL Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting B 9.62 pKi 0.24 nM Ki J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
ChEMBL Displacement of [3H]-Angiotensin 2 from human placental AT1 receptor expressed in African green monkey COS7 cell membranes after 90 mins by gamma counting B 9.8 pKi 0.16 nM Ki J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
ChEMBL Displacement of [3H]-Asp-{Nomega-[N-(4-propanoylaminobutyl)aminocarbonyl]}Arg-ValTyr-Ile-His-Pro-Phe-OH Tris(hydrotrifluoroacetate) from human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ after 2 hrs by liquid scintillation counting B 9.14 pIC50 0.72 nM IC50 J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
GtoPdb - - 9.3 pIC50 - - - Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Br. J. Pharmacol. (1999) 126: 1057-65 [PMID:10193788]
ChEMBL Agonist activity at human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ assessed as induction of intracellular Ca2+ mobilization by bioluminescence assay B 9.28 pEC50 0.52 nM EC50 J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
ChEMBL Agonist activity at human AT1 receptor transfected in CHO cells co-expressing Galpha16-mtAEQ assessed as induction of intracellular Ca2+ mobilization by bioluminescence assay B 9.31 pEC50 0.49 nM EC50 J. Med. Chem. (2016) 59: 1925-1945 [PMID:26824643]
AT1 receptor in Human [GtoPdb: 34] [UniProtKB: P30556]
GtoPdb - - 9.3 pIC50 - - - Heterogeneity of angiotensin receptor subtypes.. Medicinal Chemistry of the Renin-Angiotensin System. (1994);
Br. J. Pharmacol. (1999) 126: 1057-65 [PMID:10193788]
AT1 receptor/Type-1B angiotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL263] [GtoPdb: 34] [UniProtKB: P29089]
ChEMBL Binding affinity for angiotensin II receptor, type 1 in rat liver membrane using [125I]-Ang II as radioligand, in pH 7.4 Tris-HCl buffer for 2 hr at 25 degree C B 9.02 pKi 0.95 nM Ki J. Med. Chem. (2005) 48: 6620-6631 [PMID:16220978]
ChEMBL In vitro binding affinity at rat liver Angiotensin II receptor, type 1 was determined based on displacement of [125I]-Ang II B 9.51 pKi 0.31 nM Ki J. Med. Chem. (2002) 45: 1767-1777 [PMID:11960488]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]