SB-706375 [Ligand Id: 2165] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL522770 (SB-706375) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| UT receptor/Urotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3764] [GtoPdb: 365] [UniProtKB: Q9UKP6] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | Br J Pharmacol (2005) 145: 620-35 [PMID:15852036] |
| ChEMBL | Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2009) 52: 7432-7445 [PMID:19731961] |
| ChEMBL | Binding affinity to urotensin-2 receptor | B | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (2009) 52: 2923-2932 [PMID:19374402] |
| ChEMBL | Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay | F | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 2177-2180 [PMID:23453841] |
| ChEMBL | Antagonist activity at urotensin 2 receptor in human RMS13 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay | F | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2009) 52: 7432-7445 [PMID:19731961] |
| ChEMBL | Displacement of [125I]-U2 from human recombinant urotensin2 receptor expressed in human Chem-2 cells after 4 hrs by scintillation proximity assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 2177-2180 [PMID:23453841] |
| UT receptor in Mouse [GtoPdb: 365] [UniProtKB: Q8VIH9] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Br J Pharmacol (2005) 145: 620-35 [PMID:15852036] |
| UT receptor/Urotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4921] [GtoPdb: 365] [UniProtKB: P49684] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Br J Pharmacol (2005) 145: 620-35 [PMID:15852036] |
| ChEMBL | Antagonist activity at rat urotensin 2 receptor expressed in CHOK1 cells assessed as inhibition of urotensin 2-induced intracellular calcium mobilization after 1 hr by FLIPR assay | F | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2009) 52: 7432-7445 [PMID:19731961] |
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]
