palosuran [Ligand Id: 3516] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL567303 (ACT-058362) |
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| DB | Assay description | Assay Type | Standard value | Standard activity | Original value | Original units | Original activity | Reference |
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| UT receptor/Urotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: 10927] [GtoPdb: 365] [UniProtKB: Q9UKP6] | ||||||||
| ChEMBL | Displacement of [125I]urotensin 2 from urotensin 2 receptor in human RMS13 cells by scintillation proximity assay | B | 7.39 | pKi | 41 | nM | Ki | J. Med. Chem. (2009) 52: 7432-7445 [PMID:19731961] |
| 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 | 6.49 | pIC50 | 320 | nM | IC50 | J. Med. Chem. (2009) 52: 7432-7445 [PMID:19731961] |
| GtoPdb | - | - | 7.1 | pIC50 | - | - | IC50 | J. Pharmacol. Exp. Ther. (2004) 311: 204-12 [PMID:15146030] |
| ChEMBL | Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization incubated 10 mins prior to urotensin2 stimulation measured after 10 mins by fluorometric analysis | B | 7.41 | pIC50 | 39 | nM | IC50 | Bioorg. Med. Chem. Lett. (2013) 23: 2177-2180 [PMID:23453841] |
| ChEMBL | Displacement of [125I]-U2 from recombinant human urotensin2 receptor expressed in human U2OS cells after 30 mins by gamma counting analysis | B | 8.3 | pIC50 | <5 | nM | IC50 | Bioorg. Med. Chem. Lett. (2013) 23: 2177-2180 [PMID:23453841] |
| UT receptor/Urotensin II receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: 10928] [GtoPdb: 365] [UniProtKB: P49684] | ||||||||
| 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 | 4.12 | pIC50 | >75000 | nM | IC50 | J. Med. Chem. (2009) 52: 7432-7445 [PMID:19731961] |
ChEMBL data shown on this page come from version 23:
A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]
