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Assay Detail

CHEMBL713797

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Binding
In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.
Arasasingham PN, Fotsch C, Ouyang X, Norman MH, Kelly MG, Stark KL, Karbon B, Hale C, Baumgartner JW, Zambrano M, Cheetham J, Tamayo NA.
J Med Chem (2003) 46 : 9 -11
PubMed 12502354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.35 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441342 1 6.82
CHEMBL12487 1 6.79
CHEMBL12480 1 6.75
CHEMBL12783 1 6.73
CHEMBL12457 1 6.71
CHEMBL12811 1 6.66
CHEMBL416890 1 6.60
CHEMBL12310 1 6.33
CHEMBL12369 1 6.22
CHEMBL275299 1 6.22
CHEMBL12120 1 5.82
CHEMBL12370 1 5.49
CHEMBL12615 1 5.42
CHEMBL12187 1 -
CHEMBL12402 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441342 IC50 = 150.0 nM 6.82
CHEMBL12487 IC50 = 164.0 nM 6.79
CHEMBL12480 IC50 = 178.0 nM 6.75
CHEMBL12783 IC50 = 188.0 nM 6.73
CHEMBL12457 IC50 = 193.0 nM 6.71
CHEMBL12811 IC50 = 217.0 nM 6.66
CHEMBL416890 IC50 = 249.0 nM 6.60
CHEMBL12310 IC50 = 469.0 nM 6.33
CHEMBL12369 IC50 = 597.0 nM 6.22
CHEMBL275299 IC50 = 598.0 nM 6.22
CHEMBL12120 IC50 = 1500.0 nM 5.82
CHEMBL12370 IC50 = 3226.0 nM 5.49
CHEMBL12615 IC50 = 3829.0 nM 5.42
CHEMBL12187 IC50 > 10000.0 nM -
CHEMBL12402 IC50 > 10000.0 nM -