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Assay Detail

CHEMBL716490

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

Functional
effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocyte-stimulating hormone receptor (CHEMBL3795)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
Haskell-Luevano C, Hendrata S, North C, Sawyer TK, Hadley ME, Hruby VJ, Dickinson C, Gantz I.
J Med Chem (1997) 40 : 2133 -2139
PubMed 9216831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.98 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.72
CHEMBL263948 1 9.72
CHEMBL264190 1 6.64
CHEMBL302703 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.19 nM 9.72
CHEMBL263948 EC50 = 0.19 nM 9.72
CHEMBL264190 EC50 = 228.0 nM 6.64
CHEMBL302703 EC50 = 1428.0 nM 5.84