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Assay Detail

CHEMBL2351682

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
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
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Urotensin-2 receptor (CHEMBL3764)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.
Taylor SJ, Soleymanzadeh F, Muegge I, Akiba I, Taki N, Ueda S, Mainolfi E, Eldrup AB.
Bioorg Med Chem Lett (2013) 23 : 2177 -2180
PubMed 23453841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.41 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567303 PALOSURAN 2.0 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567303 PALOSURAN IC50 = 39.0 nM 7.41