Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL716356

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

Functional
Evaluated for agonist activity at cloned Melanocortin 3 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 3 (CHEMBL4644)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
Hruby VJ, Lu D, Sharma SD, Castrucci AL, Kesterson RA, al-Obeidi FA, Hadley ME, Cone RD.
J Med Chem (1995) 38 : 3454 -3461
PubMed 7658432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 9.41 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413212 1 10.20
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.88
CHEMBL428615 1 9.72
CHEMBL214332 INTERMEDINE 2.0 1 9.18
CHEMBL428801 1 8.95
CHEMBL266417 1 8.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413212 EC50 = 0.063 nM 10.20
CHEMBL441738 AFAMELANOTIDE EC50 = 0.132 nM 9.88
CHEMBL428615 EC50 = 0.191 nM 9.72
CHEMBL214332 INTERMEDINE EC50 = 0.669 nM 9.18
CHEMBL428801 EC50 = 1.134 nM 8.95
CHEMBL266417 EC50 = 2.813 nM 8.55