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Assay Detail

CHEMBL4013732

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

ADMET
Agonist activity at human NMUR1 expressed in CHO cells assessed as induction of Ca2+ flux measured for 180 secs by Fluo 4-AM dye-based FLIPR assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
Kanematsu-Yamaki Y, Nishizawa N, Kaisho T, Nagai H, Mochida T, Asakawa T, Inooka H, Dote K, Fujita H, Matsumiya K, Hirabayashi H, Sakamoto J, Ohtaki T, Takekawa S, Asami T.
J Med Chem (2017) 60 : 6089 -6097
PubMed 28657315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 8.45 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098010 1 9.51
CHEMBL4068681 1 9.49
CHEMBL4088263 1 9.39
CHEMBL3356083 1 9.27
CHEMBL4059530 1 9.14
CHEMBL4073946 1 9.11
CHEMBL4095998 1 9.02
CHEMBL4079986 1 9.00
CHEMBL4063830 1 8.89
CHEMBL4087867 1 8.72
CHEMBL4061507 1 8.66
CHEMBL4099780 1 8.57
CHEMBL4089636 1 8.57
CHEMBL4091611 1 8.11
CHEMBL4097355 1 8.09
CHEMBL4081760 1 8.04
CHEMBL4063341 1 8.02
CHEMBL4090300 1 7.77
CHEMBL4060571 1 7.41
CHEMBL4100718 1 7.38
CHEMBL4070175 1 7.09
CHEMBL4092033 1 6.70
CHEMBL4091208 1 -
CHEMBL4069256 1 -
CHEMBL4071218 1 -
CHEMBL4060027 1 -
CHEMBL4082455 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098010 EC50 = 0.31 nM 9.51
CHEMBL4068681 EC50 = 0.32 nM 9.49
CHEMBL4088263 EC50 = 0.41 nM 9.39
CHEMBL3356083 EC50 = 0.54 nM 9.27
CHEMBL4059530 EC50 = 0.73 nM 9.14
CHEMBL4073946 EC50 = 0.77 nM 9.11
CHEMBL4095998 EC50 = 0.96 nM 9.02
CHEMBL4079986 EC50 = 1.0 nM 9.00
CHEMBL4063830 EC50 = 1.3 nM 8.89
CHEMBL4087867 EC50 = 1.9 nM 8.72
CHEMBL4061507 EC50 = 2.2 nM 8.66
CHEMBL4099780 EC50 = 2.7 nM 8.57
CHEMBL4089636 EC50 = 2.7 nM 8.57
CHEMBL4091611 EC50 = 7.8 nM 8.11
CHEMBL4097355 EC50 = 8.1 nM 8.09
CHEMBL4081760 EC50 = 9.2 nM 8.04
CHEMBL4063341 EC50 = 9.5 nM 8.02
CHEMBL4090300 EC50 = 17.0 nM 7.77
CHEMBL4060571 EC50 = 39.0 nM 7.41
CHEMBL4100718 EC50 = 42.0 nM 7.38
CHEMBL4070175 EC50 = 81.0 nM 7.09
CHEMBL4092033 EC50 = 200.0 nM 6.70
CHEMBL4091208 EC50 > 1000.0 nM -
CHEMBL4069256 EC50 > 1000.0 nM -
CHEMBL4071218 EC50 > 1000.0 nM -
CHEMBL4060027 EC50 > 1000.0 nM -
CHEMBL4082455 EC50 > 1000.0 nM -