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Assay Detail

CHEMBL832326

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

Binding
Concentration required to inhibit binding of [125I]MCH radioligand to human melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes
57
Total Activities
55
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

Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 1.
Souers AJ, Wodka D, Gao J, Lewis JC, Vasudevan A, Gentles R, Brodjian S, Dayton B, Ogiela CA, Fry D, Hernandez LE, Marsh KC, Collins CA, Kym PR.
Bioorg Med Chem Lett (2004) 14 : 4873 -4877
PubMed 15341942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.57 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183159 3 7.70
CHEMBL362713 1 7.50
CHEMBL362720 1 7.44
CHEMBL186770 1 7.28
CHEMBL184520 1 7.22
CHEMBL364377 1 7.05
CHEMBL187702 1 6.98
CHEMBL363311 1 6.94
CHEMBL361288 1 6.88
CHEMBL184394 1 6.86
CHEMBL186750 1 6.86
CHEMBL186818 1 6.76
CHEMBL365459 1 6.72
CHEMBL364104 1 6.70
CHEMBL185095 1 6.70
CHEMBL187859 1 6.51
CHEMBL184446 1 6.51
CHEMBL185096 1 6.49
CHEMBL184573 1 6.46
CHEMBL185235 1 6.44
CHEMBL184980 1 6.37
CHEMBL365254 1 6.36
CHEMBL186949 1 6.31
CHEMBL186481 1 6.24
CHEMBL363011 1 6.22
CHEMBL184476 1 6.21
CHEMBL183932 1 6.19
CHEMBL187165 1 6.14
CHEMBL186659 1 6.10
CHEMBL187295 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183159 IC50 = 20.0 nM 7.70
CHEMBL362713 IC50 = 32.0 nM 7.50
CHEMBL362720 IC50 = 36.0 nM 7.44
CHEMBL183159 IC50 = 41.0 nM 7.39
CHEMBL186770 IC50 = 53.0 nM 7.28
CHEMBL184520 IC50 = 60.0 nM 7.22
CHEMBL364377 IC50 = 90.0 nM 7.05
CHEMBL187702 IC50 = 105.0 nM 6.98
CHEMBL363311 IC50 = 115.0 nM 6.94
CHEMBL361288 IC50 = 132.0 nM 6.88
CHEMBL184394 IC50 = 137.0 nM 6.86
CHEMBL186750 IC50 = 137.0 nM 6.86
CHEMBL186818 IC50 = 174.0 nM 6.76
CHEMBL365459 IC50 = 191.0 nM 6.72
CHEMBL185095 IC50 = 199.0 nM 6.70
CHEMBL364104 IC50 = 201.0 nM 6.70
CHEMBL187859 IC50 = 306.0 nM 6.51
CHEMBL184446 IC50 = 310.0 nM 6.51
CHEMBL185096 IC50 = 326.0 nM 6.49
CHEMBL184573 IC50 = 349.0 nM 6.46
CHEMBL185235 IC50 = 361.0 nM 6.44
CHEMBL184980 IC50 = 432.0 nM 6.37
CHEMBL365254 IC50 = 437.0 nM 6.36
CHEMBL186949 IC50 = 492.0 nM 6.31
CHEMBL183159 IC50 = 550.0 nM 6.26
CHEMBL186481 IC50 = 580.0 nM 6.24
CHEMBL363011 IC50 = 606.0 nM 6.22
CHEMBL184476 IC50 = 614.0 nM 6.21
CHEMBL183932 IC50 = 640.0 nM 6.19
CHEMBL187165 IC50 = 722.0 nM 6.14
CHEMBL186659 IC50 = 789.0 nM 6.10
CHEMBL184102 IC50 = 808.0 nM 6.09
CHEMBL187295 IC50 = 818.0 nM 6.09
CHEMBL183739 IC50 = 823.0 nM 6.08
CHEMBL184001 IC50 = 1070.0 nM 5.97
CHEMBL427153 IC50 = 1100.0 nM 5.96
CHEMBL77072 IC50 = 1590.0 nM 5.80
CHEMBL186547 IC50 = 1640.0 nM 5.79
CHEMBL363222 IC50 > 2000.0 nM -
CHEMBL186771 IC50 > 2000.0 nM -
CHEMBL183532 IC50 > 2000.0 nM -
CHEMBL185065 IC50 > 2000.0 nM -
CHEMBL363120 IC50 > 2000.0 nM -
CHEMBL366307 IC50 > 2000.0 nM -
CHEMBL426971 IC50 > 2000.0 nM -
CHEMBL185187 IC50 > 2000.0 nM -
CHEMBL181798 IC50 > 2000.0 nM -
CHEMBL119647 IC50 > 2000.0 nM -
CHEMBL366041 IC50 > 2000.0 nM -
CHEMBL184086 IC50 > 2000.0 nM -