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Assay Detail

CHEMBL714368

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Binding
pA2 value for human Melanocortin-4 receptor
10
Total Activities
10
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 4 (CHEMBL259)
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
Kd 10 8.43 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161313 1 9.80
CHEMBL1161322 1 9.30
CHEMBL2096742 1 9.10
CHEMBL1161323 1 8.90
CHEMBL2372588 1 8.60
CHEMBL1161318 1 8.40
CHEMBL2372589 1 8.00
CHEMBL1161316 1 8.00
CHEMBL1161321 1 7.70
CHEMBL1161320 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161313 Kd = 0.1585 nM 9.80
CHEMBL1161322 Kd = 0.5012 nM 9.30
CHEMBL2096742 Kd = 0.7943 nM 9.10
CHEMBL1161323 Kd = 1.259 nM 8.90
CHEMBL2372588 Kd = 2.512 nM 8.60
CHEMBL1161318 Kd = 3.981 nM 8.40
CHEMBL2372589 Kd = 10.0 nM 8.00
CHEMBL1161316 Kd = 10.0 nM 8.00
CHEMBL1161321 Kd = 19.95 nM 7.70
CHEMBL1161320 Kd = 316.23 nM 6.50