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Assay Detail

CHEMBL713030

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Binding
Binding affinity against human Melanocortin 5 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melanocortin receptor 5 (CHEMBL4608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.
Grieco P, Lavecchia A, Cai M, Trivedi D, Weinberg D, MacNeil T, Van der Ploeg LH, Hruby VJ.
J Med Chem (2002) 45 : 5287 -5294
PubMed 12431055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.72 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161313 1 10.57
CHEMBL2096742 1 10.05
CHEMBL1161323 1 9.96
CHEMBL1161320 1 8.39
CHEMBL1161318 1 8.34
CHEMBL1161321 1 7.92
CHEMBL415333 1 7.80
CHEMBL1161316 1 7.80
CHEMBL2372588 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161313 IC50 = 0.027 nM 10.57
CHEMBL2096742 IC50 = 0.09 nM 10.05
CHEMBL1161323 IC50 = 0.11 nM 9.96
CHEMBL1161320 IC50 = 4.1 nM 8.39
CHEMBL1161318 IC50 = 4.6 nM 8.34
CHEMBL1161321 IC50 = 12.0 nM 7.92
CHEMBL415333 IC50 = 16.0 nM 7.80
CHEMBL1161316 IC50 = 16.0 nM 7.80
CHEMBL2372588 IC50 = 21.0 nM 7.68