Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3366482

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

Binding
Agonist activity at UT receptor in rat aorta assessed as contraction
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Urotensin-2 receptor (CHEMBL4921)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor.
Carotenuto A, Auriemma L, Merlino F, Yousif AM, Marasco D, Limatola A, Campiglia P, Gomez-Monterrey I, Santicioli P, Meini S, Maggi CA, Novellino E, Grieco P.
J Med Chem (2014) 57 : 5965 -5974
PubMed 24992374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 8.85 10.90
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3315148 1 10.90
CHEMBL3315144 1 10.71
CHEMBL3315139 1 9.40
CHEMBL3315152 1 9.20
CHEMBL3315140 1 9.14
CHEMBL3315146 1 9.09
CHEMBL3315150 1 8.97
CHEMBL3315147 1 8.57
CHEMBL593662 UROTENSIN-II 1 8.50
CHEMBL218994 1 8.44
CHEMBL3315141 1 8.42
CHEMBL3315142 1 8.30
CHEMBL3315149 1 7.89
CHEMBL3315143 1 7.74
CHEMBL3315145 1 7.47
CHEMBL223905 URANTIDE 1 -
CHEMBL3315151 1 -
CHEMBL3315153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3315148 EC50 = 0.01259 nM 10.90
CHEMBL3315144 EC50 = 0.0195 nM 10.71
CHEMBL3315139 EC50 = 0.3981 nM 9.40
CHEMBL3315152 EC50 = 0.631 nM 9.20
CHEMBL3315140 EC50 = 0.7244 nM 9.14
CHEMBL3315146 EC50 = 0.8128 nM 9.09
CHEMBL3315150 EC50 = 1.072 nM 8.97
CHEMBL3315147 EC50 = 2.692 nM 8.57
CHEMBL593662 UROTENSIN-II EC50 = 3.162 nM 8.50
CHEMBL218994 EC50 = 3.631 nM 8.44
CHEMBL3315141 EC50 = 3.802 nM 8.42
CHEMBL3315142 EC50 = 5.012 nM 8.30
CHEMBL3315149 EC50 = 12.88 nM 7.89
CHEMBL3315143 EC50 = 18.2 nM 7.74
CHEMBL3315145 EC50 = 33.88 nM 7.47
CHEMBL223905 URANTIDE pEC50 - -
CHEMBL3315151 pEC50 - -
CHEMBL3315153 pEC50 - -