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Assay Detail

CHEMBL894445

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

Functional
Antagonist activity at rat MCH1 receptor expressed in HEK293 cells by FLIPR calcium mobility assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Melanin-concentrating hormone receptor 1 (CHEMBL1075228)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR.
J Med Chem (2007) 50 : 3883 -3890
PubMed 17668922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.13 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL394569 1 7.14
CHEMBL245231 1 6.96
CHEMBL242004 1 6.64
CHEMBL389128 1 6.50
CHEMBL245010 1 6.46
CHEMBL242003 1 6.44
CHEMBL243794 1 6.24
CHEMBL389129 1 6.15
CHEMBL245229 1 6.14
CHEMBL244004 1 5.89
CHEMBL245008 1 5.85
CHEMBL244578 1 5.70
CHEMBL395789 1 5.62
CHEMBL244791 1 5.58
CHEMBL395788 1 5.57
CHEMBL244790 1 5.27
CHEMBL244003 1 -
CHEMBL244163 1 -
CHEMBL390212 1 -
CHEMBL244576 1 -
CHEMBL244374 1 -
CHEMBL244373 1 -
CHEMBL244372 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL394569 IC50 = 72.0 nM 7.14
CHEMBL245231 IC50 = 110.0 nM 6.96
CHEMBL242004 IC50 = 230.0 nM 6.64
CHEMBL389128 IC50 = 320.0 nM 6.50
CHEMBL245010 IC50 = 350.0 nM 6.46
CHEMBL242003 IC50 = 360.0 nM 6.44
CHEMBL243794 IC50 = 570.0 nM 6.24
CHEMBL389129 IC50 = 710.0 nM 6.15
CHEMBL245229 IC50 = 720.0 nM 6.14
CHEMBL244004 IC50 = 1300.0 nM 5.89
CHEMBL245008 IC50 = 1400.0 nM 5.85
CHEMBL244578 IC50 = 2000.0 nM 5.70
CHEMBL395789 IC50 = 2400.0 nM 5.62
CHEMBL244791 IC50 = 2600.0 nM 5.58
CHEMBL395788 IC50 = 2700.0 nM 5.57
CHEMBL244790 IC50 = 5400.0 nM 5.27
CHEMBL244003 IC50 > 10000.0 nM -
CHEMBL244163 IC50 - -
CHEMBL390212 IC50 - -
CHEMBL244576 IC50 - -
CHEMBL244374 IC50 - -
CHEMBL244373 IC50 - -
CHEMBL244372 IC50 - -