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Assay Detail

CHEMBL4149974

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

Binding
Displacement of [3H]-NMU-8 from human NMUR2 expressed in HEK293 cells after 3 hrs by topcount micro scintillation counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuromedin-U receptor 2 (CHEMBL1075144)
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
IC50 13 7.14 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356083 1 8.77
CHEMBL4169726 1 8.70
CHEMBL4159554 1 7.73
CHEMBL4167803 1 7.54
CHEMBL4164957 1 7.54
CHEMBL4162351 1 7.39
CHEMBL4173224 1 7.14
CHEMBL4161479 1 6.93
CHEMBL4162728 1 6.52
CHEMBL4175581 1 6.49
CHEMBL4164987 1 6.33
CHEMBL4171236 1 6.22
CHEMBL4170275 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356083 IC50 = 1.7 nM 8.77
CHEMBL4169726 IC50 = 2.0 nM 8.70
CHEMBL4159554 IC50 = 18.8 nM 7.73
CHEMBL4167803 IC50 = 29.1 nM 7.54
CHEMBL4164957 IC50 = 28.8 nM 7.54
CHEMBL4162351 IC50 = 40.4 nM 7.39
CHEMBL4173224 IC50 = 72.4 nM 7.14
CHEMBL4161479 IC50 = 116.5 nM 6.93
CHEMBL4162728 IC50 = 301.9 nM 6.52
CHEMBL4175581 IC50 = 327.5 nM 6.49
CHEMBL4164987 IC50 = 465.5 nM 6.33
CHEMBL4171236 IC50 = 598.9 nM 6.22
CHEMBL4170275 IC50 = 2869.0 nM 5.54