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Assay Detail

CHEMBL716183

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Functional
Evaluated for partial agonistic activity at cloned mammalian Melanocortin 4 receptor
1
Total Activities
1
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 4 (CHEMBL259)
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
Kd 1 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428801 1 9.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428801 Kd = 0.1995 nM 9.70