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Assay Detail

CHEMBL1924587

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

Binding
Displacement of [125I]-MCH from MCHR1 after 2 hrs by beta scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanin-concentrating hormone receptor 1 (CHEMBL344)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Mihalic JT, Chen X, Fan P, Chen X, Fu Y, Liang L, Reed M, Tang L, Chen JL, Jaen J, Li L, Dai K.
Bioorg Med Chem Lett (2011) 21 : 7001 -7005
PubMed 22019296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.13 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1922270 1 9.30
CHEMBL1922269 1 9.05
CHEMBL1922262 1 8.52
CHEMBL1922271 1 8.36
CHEMBL1922268 1 8.15
CHEMBL1922265 1 7.40
CHEMBL1922267 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1922270 IC50 = 0.5 nM 9.30
CHEMBL1922269 IC50 = 0.9 nM 9.05
CHEMBL1922262 IC50 = 3.0 nM 8.52
CHEMBL1922271 IC50 = 4.4 nM 8.36
CHEMBL1922268 IC50 = 7.0 nM 8.15
CHEMBL1922265 IC50 = 40.0 nM 7.40
CHEMBL1922267 IC50 = 750.0 nM 6.12