SB-436811 [Ligand Id: 2164] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL366221 (SB-436811) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Urotensin II receptor in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4845] [UniProtKB: Q8HYC3] | ||||||||
| ChEMBL | Binding affinity for monkey urotensin-2 receptor | B | 6.6 | pKi | 251.19 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3229-3232 [PMID:15936190] |
| UT receptor/Urotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3764] [GtoPdb: 365] [UniProtKB: Q9UKP6] | ||||||||
| ChEMBL | Agonist activity at human urotensin 2 expressed in CHO cells by FLIPR | F | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2010) 53: 2695-2708 [PMID:20043680] |
| ChEMBL | Displacement of [I125]hU2 from human recombinant urotensin 2 receptor expressed in HEK293 cells | B | 6.7 | pKi | 200 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3950-3954 [PMID:18573659] |
| ChEMBL | Binding affinity to human urotensin 2 receptor | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2010) 53: 2695-2708 [PMID:20043680] |
| ChEMBL | Binding affinity using [125I]hU-II radioligand binding assay in HEK293 cell membranes expressing human Urotensin 2 receptor | B | 6.7 | pKi | 199.53 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3229-3232 [PMID:15936190] |
| ChEMBL | Antagonist activity at human recombinant urotensin 2 receptor expressed in HEK293 cells assessed as inhibition of urotensin 2-induced calcium mobilization by FLIPR assay | F | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3950-3954 [PMID:18573659] |
| ChEMBL | Inhibition of hU-II-mediated [Ca2+]i mobilization in HEK293 cells expressing human recombinant Urotensin 2 receptor in FLIPR assay | B | 6.8 | pIC50 | 158.49 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3229-3232 [PMID:15936190] |
| UT receptor/Urotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4921] [GtoPdb: 365] [UniProtKB: P49684] | ||||||||
| ChEMBL | Binding affinity for rat urotensin-2 receptor | B | 5.5 | pKi | 3162.28 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3229-3232 [PMID:15936190] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Bioorg Med Chem Lett (2005) 15: 3229-32 [PMID:15936190] |
| ChEMBL | Displacement of [125I]U2 from rat urotensin 2 receptor expressed in CHO cells | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2010) 53: 2695-2708 [PMID:20043680] |
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]
