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Assay Detail

CHEMBL917734

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

Functional
Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a potent and selective melanocortin-4 receptor antagonist--design, synthesis, and characterization.
Chen C, Pontillo J, Fleck BA, Gao Y, Wen J, Tran JA, Tucci FC, Marinkovic D, Foster AC, Saunders J.
J Med Chem (2004) 47 : 6821 -6830
PubMed 15615531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.42 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360716 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360716 EC50 = 3.8 nM 8.42