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 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]
