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ChEMBL ligand: CHEMBL408403 (5-l-isoleucineangiotensin ii, Angiotensin ii, Angiotensin ii human, Angiotensin ii (human type), Asp-arg-val-tyr-ile-his-pro-phe, Delivert, LJPC-501) |
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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 | 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 [125-I]-[Sar1, Ile8] from recombinant human AT2R transfected in human HEK293 cells incubated for 2 hrs by liquid scintillation counter analysis | B | 9.21 | pIC50 | 0.62 | nM | IC50 | Bioorg Med Chem Lett (2021) 43: 128086-128086 [PMID:33965531] |
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] |
ChEMBL | Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay | B | 8.17 | pEC50 | 6.8 | nM | EC50 | US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null) |
ChEMBL | Agonist activity at rat AT1aR expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay | F | 8.89 | pEC50 | 1.3 | nM | EC50 | US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null) |
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 [125-I]-[Sar1, Ile8] from recombinant human AT1R transfected in human HEK293 cells incubated for 2 hrs by liquid scintillation counter analysis | B | 7.99 | pIC50 | 10.2 | nM | IC50 | Bioorg Med Chem Lett (2021) 43: 128086-128086 [PMID:33965531] |
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 AT1R expressed in HEK293 cells incubated for 60 mins by luminescence based beta-arrestin recruitment assay | B | 8.01 | pEC50 | 9.7 | nM | EC50 | US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null) |
ChEMBL | Agonist activity at human AT1R expressed in HEK293 cells incubated for 30 mins by IP1 accumulation assay | F | 8.59 | pEC50 | 2.6 | nM | EC50 | US-8486885-B2. beta-arrestin effectors and compositions and methods of use thereof (null) |
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 | F | 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 | F | 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 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]