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Assay Detail

CHEMBL853090

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

Binding
Inhibition of human MCH1 receptor by SPA assay
39
Total Activities
39
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

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

Publication

6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists: structure-activity exploration of eastern and western parts.
Ulven T, Little PB, Receveur JM, Frimurer TM, Rist O, Nørregaard PK, Högberg T.
Bioorg Med Chem Lett (2006) 16 : 1070 -1075
PubMed 16289819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.10 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205111 1 8.30
CHEMBL425407 1 8.28
CHEMBL204428 1 8.21
CHEMBL204952 1 8.02
CHEMBL436320 1 7.92
CHEMBL203558 1 7.89
CHEMBL203586 1 7.82
CHEMBL203699 1 7.80
CHEMBL379886 1 7.75
CHEMBL379693 1 7.75
CHEMBL204801 1 7.75
CHEMBL189118 1 7.72
CHEMBL2113218 1 7.70
CHEMBL202095 1 7.70
CHEMBL382161 1 7.66
CHEMBL184084 1 7.54
CHEMBL204082 1 7.40
CHEMBL204968 1 7.40
CHEMBL442794 1 7.38
CHEMBL202563 1 7.32
CHEMBL202854 1 7.20
CHEMBL205115 1 7.08
CHEMBL203161 1 7.06
CHEMBL204912 1 6.98
CHEMBL203804 1 6.90
CHEMBL382126 1 6.79
CHEMBL203549 1 6.68
CHEMBL204798 1 6.57
CHEMBL203544 1 6.37
CHEMBL204168 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205111 IC50 = 5.0 nM 8.30
CHEMBL425407 IC50 = 5.3 nM 8.28
CHEMBL204428 IC50 = 6.2 nM 8.21
CHEMBL204952 IC50 = 9.6 nM 8.02
CHEMBL436320 IC50 = 12.0 nM 7.92
CHEMBL203558 IC50 = 13.0 nM 7.89
CHEMBL203586 IC50 = 15.0 nM 7.82
CHEMBL203699 IC50 = 16.0 nM 7.80
CHEMBL379886 IC50 = 18.0 nM 7.75
CHEMBL379693 IC50 = 18.0 nM 7.75
CHEMBL204801 IC50 = 18.0 nM 7.75
CHEMBL189118 IC50 = 19.0 nM 7.72
CHEMBL2113218 IC50 = 20.0 nM 7.70
CHEMBL202095 IC50 = 20.0 nM 7.70
CHEMBL382161 IC50 = 22.0 nM 7.66
CHEMBL184084 IC50 = 29.0 nM 7.54
CHEMBL204082 IC50 = 40.0 nM 7.40
CHEMBL204968 IC50 = 40.0 nM 7.40
CHEMBL442794 IC50 = 42.0 nM 7.38
CHEMBL202563 IC50 = 48.0 nM 7.32
CHEMBL202854 IC50 = 63.0 nM 7.20
CHEMBL205115 IC50 = 83.0 nM 7.08
CHEMBL203161 IC50 = 87.0 nM 7.06
CHEMBL204912 IC50 = 105.0 nM 6.98
CHEMBL203804 IC50 = 125.0 nM 6.90
CHEMBL382126 IC50 = 162.0 nM 6.79
CHEMBL203549 IC50 = 210.0 nM 6.68
CHEMBL204798 IC50 = 271.0 nM 6.57
CHEMBL203544 IC50 = 423.0 nM 6.37
CHEMBL204168 IC50 = 568.0 nM 6.25
CHEMBL205112 IC50 = 2100.0 nM 5.68
CHEMBL201813 IC50 = 2540.0 nM 5.59
CHEMBL381143 IC50 = 2760.0 nM 5.56
CHEMBL203929 IC50 = 3280.0 nM 5.48
CHEMBL203858 IC50 = 6970.0 nM 5.16
CHEMBL203917 IC50 = 9460.0 nM 5.02
CHEMBL203820 IC50 > 10000.0 nM -
CHEMBL426481 IC50 > 10000.0 nM -
CHEMBL203504 IC50 > 10000.0 nM -