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Assay Detail

CHEMBL4047454

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

Functional
Agonist activity at human NMUR2 expressed in CHO cells assessed as increase in intracellular calcium influx after 180 secs by Fluo 4-AM dye based FLIPR assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuromedin-U receptor 2 (CHEMBL1075144)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A potent neuromedin U receptor 2-selective alkylated peptide.
Nishizawa N, Kanematsu-Yamaki Y, Funata M, Nagai H, Shimizu A, Fujita H, Sakamoto J, Takekawa S, Asami T.
Bioorg Med Chem Lett (2017) 27 : 4626 -4629
PubMed 28935264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 8.53 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4074121 1 9.70
CHEMBL3356083 1 9.37
CHEMBL4061906 1 9.10
CHEMBL4083670 1 8.82
CHEMBL4060830 1 8.74
CHEMBL4092080 1 8.72
CHEMBL4081819 1 8.70
CHEMBL4097408 1 8.52
CHEMBL4088810 1 8.48
CHEMBL4073508 1 8.46
CHEMBL4103826 1 8.44
CHEMBL4080881 1 8.42
CHEMBL4079565 1 8.38
CHEMBL4105113 1 8.24
CHEMBL4094147 1 8.21
CHEMBL4070228 1 8.14
CHEMBL4087316 1 8.08
CHEMBL4067577 1 8.03
CHEMBL4076016 1 8.03
CHEMBL4071009 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4074121 EC50 = 0.2 nM 9.70
CHEMBL3356083 EC50 = 0.43 nM 9.37
CHEMBL4061906 EC50 = 0.8 nM 9.10
CHEMBL4083670 EC50 = 1.5 nM 8.82
CHEMBL4060830 EC50 = 1.8 nM 8.74
CHEMBL4092080 EC50 = 1.9 nM 8.72
CHEMBL4081819 EC50 = 2.0 nM 8.70
CHEMBL4097408 EC50 = 3.0 nM 8.52
CHEMBL4088810 EC50 = 3.3 nM 8.48
CHEMBL4073508 EC50 = 3.5 nM 8.46
CHEMBL4103826 EC50 = 3.6 nM 8.44
CHEMBL4080881 EC50 = 3.8 nM 8.42
CHEMBL4079565 EC50 = 4.2 nM 8.38
CHEMBL4105113 EC50 = 5.8 nM 8.24
CHEMBL4094147 EC50 = 6.2 nM 8.21
CHEMBL4070228 EC50 = 7.3 nM 8.14
CHEMBL4087316 EC50 = 8.4 nM 8.08
CHEMBL4067577 EC50 = 9.3 nM 8.03
CHEMBL4076016 EC50 = 9.4 nM 8.03
CHEMBL4071009 EC50 = 11.0 nM 7.96