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Assay Detail

CHEMBL854904

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

Binding
Inhibition of 125I-MCH binding to human MCH-R1 expressed in CHO cell membranes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.
Guo T, Gu H, Hobbs DW, Busler DE, Rokosz LL.
Bioorg Med Chem Lett (2007) 17 : 1718 -1721
PubMed 17251014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.17 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361215 1 9.01
CHEMBL205285 1 8.57
CHEMBL216820 1 8.40
CHEMBL217574 1 8.22
CHEMBL384701 1 8.07
CHEMBL191393 1 8.05
CHEMBL385011 1 7.96
CHEMBL216460 1 7.21
CHEMBL216286 1 7.04
CHEMBL216267 1 7.02
CHEMBL386487 1 6.80
CHEMBL216209 1 6.75
CHEMBL217182 1 6.72
CHEMBL426339 1 6.58
CHEMBL216066 1 6.47
CHEMBL217430 1 6.42
CHEMBL217114 1 5.89
CHEMBL217618 1 5.52
CHEMBL217080 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361215 Ki = 0.98 nM 9.01
CHEMBL205285 Ki = 2.7 nM 8.57
CHEMBL216820 Ki = 4.0 nM 8.40
CHEMBL217574 Ki = 6.0 nM 8.22
CHEMBL384701 Ki = 8.5 nM 8.07
CHEMBL191393 Ki = 8.9 nM 8.05
CHEMBL385011 Ki = 11.0 nM 7.96
CHEMBL216460 Ki = 61.0 nM 7.21
CHEMBL216286 Ki = 92.0 nM 7.04
CHEMBL216267 Ki = 96.0 nM 7.02
CHEMBL386487 Ki = 160.0 nM 6.80
CHEMBL216209 Ki = 180.0 nM 6.75
CHEMBL217182 Ki = 190.0 nM 6.72
CHEMBL426339 Ki = 260.0 nM 6.58
CHEMBL216066 Ki = 340.0 nM 6.47
CHEMBL217430 Ki = 380.0 nM 6.42
CHEMBL217114 Ki = 1300.0 nM 5.89
CHEMBL217618 Ki = 3000.0 nM 5.52
CHEMBL217080 Ki = 3000.0 nM 5.52