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Assay Detail

CHEMBL709896

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

Functional
Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

beta-alanine dipeptides as MC4R agonists.
Ruel R, Herpin TF, Iben L, Luo G, Martel A, Mason H, Mattson G, Poirier B, Ruediger EH, Shi D, Thibault C, Yu G, Antal Zimanyi I, Poindexter GS, Macor JE.
Bioorg Med Chem Lett (2003) 13 : 4341 -4344
PubMed 14643322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.44 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339053 1 8.44
CHEMBL341982 1 7.40
CHEMBL337571 1 7.16
CHEMBL337351 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339053 EC50 = 3.6 nM 8.44
CHEMBL341982 EC50 = 40.0 nM 7.40
CHEMBL337571 EC50 = 70.0 nM 7.16
CHEMBL337351 EC50 = 170.0 nM 6.77