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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 (2013) |
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 (2013) |
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 (2013) |
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 (2013) |
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 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]