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 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]
