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Assay Detail

CHEMBL4146935

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

Binding
Displacement of [3H]-NMU-8 from human NMUR1 expressed in HEK293 cell membranes after 3 hrs by microscintillation counting
ChEMBL ↗
42
Total Activities
42
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 1 (CHEMBL1075178) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of potent and proteolytically stable human neuromedin U receptor agonists.
De Prins A, Martin C, Van Wanseele Y, Skov LJ, Tömböly C, Tourwé D, Caveliers V, Van Eeckhaut A, Holst B, Rosenkilde MM, Smolders I, Ballet S.
Eur J Med Chem (2018) 144 : 887 -897
PubMed 29329072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.94 10.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4174679 — — 1 10.43
CHEMBL4165538 — — 1 10.07
CHEMBL4177021 — — 1 9.82
CHEMBL4169726 — — 1 9.54
CHEMBL4160825 — — 1 9.51
CHEMBL4175546 — — 1 9.49
CHEMBL4172552 — — 1 9.47
CHEMBL4164922 — — 1 9.44
CHEMBL4165337 — — 1 9.39
CHEMBL4175953 — — 1 9.29
CHEMBL3356083 — — 1 9.11
CHEMBL4161902 — — 1 9.06
CHEMBL4164026 — — 1 9.01
CHEMBL4168753 — — 1 8.92
CHEMBL4167677 — — 1 8.80
CHEMBL4162868 — — 1 8.41
CHEMBL4169169 — — 1 8.07
CHEMBL4169739 — — 1 7.95
CHEMBL4176945 — — 1 7.61
CHEMBL4168351 — — 1 7.55
CHEMBL4176206 — — 1 7.52
CHEMBL4169433 — — 1 7.33
CHEMBL4166325 — — 1 7.26
CHEMBL4169824 — — 1 7.20
CHEMBL4172829 — — 1 7.18
CHEMBL4161501 — — 1 7.16
CHEMBL4171697 — — 1 7.08
CHEMBL4159176 — — 1 7.00
CHEMBL4173583 — — 1 6.79
CHEMBL4161095 — — 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4174679 — IC50 = 0.037 nM 10.43
CHEMBL4165538 — IC50 = 0.086 nM 10.07
CHEMBL4177021 — IC50 = 0.15 nM 9.82
CHEMBL4169726 — IC50 = 0.29 nM 9.54
CHEMBL4160825 — IC50 = 0.31 nM 9.51
CHEMBL4175546 — IC50 = 0.32 nM 9.49
CHEMBL4172552 — IC50 = 0.34 nM 9.47
CHEMBL4164922 — IC50 = 0.36 nM 9.44
CHEMBL4165337 — IC50 = 0.41 nM 9.39
CHEMBL4175953 — IC50 = 0.51 nM 9.29
CHEMBL3356083 — IC50 = 0.78 nM 9.11
CHEMBL4161902 — IC50 = 0.88 nM 9.06
CHEMBL4164026 — IC50 = 0.97 nM 9.01
CHEMBL4168753 — IC50 = 1.2 nM 8.92
CHEMBL4167677 — IC50 = 1.6 nM 8.80
CHEMBL4162868 — IC50 = 3.9 nM 8.41
CHEMBL4169169 — IC50 = 8.6 nM 8.07
CHEMBL4169739 — IC50 = 11.2 nM 7.95
CHEMBL4176945 — IC50 = 24.3 nM 7.61
CHEMBL4168351 — IC50 = 27.9 nM 7.55
CHEMBL4176206 — IC50 = 30.2 nM 7.52
CHEMBL4169433 — IC50 = 46.3 nM 7.33
CHEMBL4166325 — IC50 = 54.4 nM 7.26
CHEMBL4169824 — IC50 = 62.9 nM 7.20
CHEMBL4172829 — IC50 = 66.2 nM 7.18
CHEMBL4161501 — IC50 = 68.6 nM 7.16
CHEMBL4171697 — IC50 = 83.1 nM 7.08
CHEMBL4159176 — IC50 = 100.1 nM 7.00
CHEMBL4173583 — IC50 = 162.3 nM 6.79
CHEMBL4161095 — IC50 = 173.8 nM 6.76
CHEMBL4168961 — IC50 = 775.5 nM 6.11
CHEMBL4161037 — IC50 = 844.4 nM 6.07
CHEMBL4164680 — IC50 = 1167.0 nM 5.93
CHEMBL4164449 — IC50 = 3755.0 nM 5.42
CHEMBL3315335 — IC50 = 4286.0 nM 5.37
CHEMBL4176146 — IC50 = 18320.0 nM 4.74
CHEMBL4175315 — IC50 - — -
CHEMBL3356082 — IC50 - — -
CHEMBL4166161 — IC50 - — -
CHEMBL4172327 — IC50 - — -
CHEMBL4172768 — IC50 - — -
CHEMBL4176785 — IC50 - — -