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

CHEMBL4149975

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

Functional
Agonist activity at human NMUR1 expressed in HEK293 cells assessed as IP3 accumulation after 60 mins in presence of myo-[2-3H(N)]inositol by scintillation proximity assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuromedin-U receptor 1 (CHEMBL1075178)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists.
De Prins A, Martin C, Van Wanseele Y, Tömböly C, Tourwé D, Caveliers V, Holst B, Van Eeckhaut A, Rosenkilde MM, Smolders I, Ballet S.
ACS Med Chem Lett (2018) 9 : 496 -501
PubMed 29795766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 7.40 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4169726 1 9.29
CHEMBL4162728 1 8.54
CHEMBL4170275 1 8.43
CHEMBL4159554 1 7.96
CHEMBL4164987 1 7.72
CHEMBL4162351 1 7.54
CHEMBL3356083 1 7.41
CHEMBL4173224 1 7.27
CHEMBL4167803 1 7.24
CHEMBL4161479 1 6.81
CHEMBL4175581 1 6.07
CHEMBL4171236 1 5.99
CHEMBL4164957 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4169726 EC50 = 0.51 nM 9.29
CHEMBL4162728 EC50 = 2.9 nM 8.54
CHEMBL4170275 EC50 = 3.7 nM 8.43
CHEMBL4159554 EC50 = 10.9 nM 7.96
CHEMBL4164987 EC50 = 18.9 nM 7.72
CHEMBL4162351 EC50 = 28.5 nM 7.54
CHEMBL3356083 EC50 = 38.9 nM 7.41
CHEMBL4173224 EC50 = 53.3 nM 7.27
CHEMBL4167803 EC50 = 57.2 nM 7.24
CHEMBL4161479 EC50 = 155.7 nM 6.81
CHEMBL4175581 EC50 = 843.0 nM 6.07
CHEMBL4171236 EC50 = 1028.0 nM 5.99
CHEMBL4164957 EC50 = 1314.0 nM 5.88