palosuran [Ligand Id: 3516] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL567303 (Palosuran, ACT-058362)
  • UT receptor/Urotensin II receptor in Human [ChEMBL: CHEMBL3764] [GtoPdb: 365] [UniProtKB: Q9UKP6]
  • UT receptor/Urotensin II receptor in Rat [ChEMBL: CHEMBL4921] [GtoPdb: 365] [UniProtKB: P49684]
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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]
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: CHEMBL4921] [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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]