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Assay Detail

CHEMBL837198

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Functional
Inhibition of Melanin-concentrating hormone (MCH) mediated [Ca2+] release in IMR-32 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type IMR-32
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Melanin-concentrating hormone receptor (CHEMBL2111437)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Souers AJ, Gao J, Wodka D, Judd AS, Mulhern MM, Napier JJ, Brune ME, Bush EN, Brodjian SJ, Dayton BD, Shapiro R, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR.
Bioorg Med Chem Lett (2005) 15 : 2752 -2757
PubMed 15911251 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.31 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179501 1 7.96
CHEMBL426292 1 6.98
CHEMBL196599 1 6.83
CHEMBL197054 1 6.77
CHEMBL195319 1 6.75
CHEMBL197210 1 6.56
CHEMBL364071 1 6.29
CHEMBL196839 1 6.20
CHEMBL195914 1 6.18
CHEMBL196388 1 6.12
CHEMBL424836 1 6.05
CHEMBL425013 1 5.95
CHEMBL196115 1 5.93
CHEMBL193583 1 5.74
CHEMBL197571 1 5.54
CHEMBL372570 1 5.15
CHEMBL196991 1 -
CHEMBL425744 1 -
CHEMBL383798 1 -
CHEMBL196390 1 -
CHEMBL196332 1 -
CHEMBL196781 1 -
CHEMBL370839 1 -
CHEMBL364936 1 -
CHEMBL195896 1 -
CHEMBL372291 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179501 IC50 = 11.0 nM 7.96
CHEMBL426292 IC50 = 104.0 nM 6.98
CHEMBL196599 IC50 = 147.0 nM 6.83
CHEMBL197054 IC50 = 171.0 nM 6.77
CHEMBL195319 IC50 = 178.0 nM 6.75
CHEMBL197210 IC50 = 275.0 nM 6.56
CHEMBL364071 IC50 = 516.0 nM 6.29
CHEMBL196839 IC50 = 626.0 nM 6.20
CHEMBL195914 IC50 = 654.0 nM 6.18
CHEMBL196388 IC50 = 751.0 nM 6.12
CHEMBL424836 IC50 = 894.0 nM 6.05
CHEMBL425013 IC50 = 1120.0 nM 5.95
CHEMBL196115 IC50 = 1177.0 nM 5.93
CHEMBL193583 IC50 = 1810.0 nM 5.74
CHEMBL197571 IC50 = 2880.0 nM 5.54
CHEMBL372570 IC50 = 7140.0 nM 5.15
CHEMBL196991 IC50 > 10000.0 nM -
CHEMBL425744 IC50 > 10000.0 nM -
CHEMBL383798 IC50 > 10000.0 nM -
CHEMBL196390 IC50 > 10000.0 nM -
CHEMBL196332 IC50 > 10000.0 nM -
CHEMBL196781 IC50 > 10000.0 nM -
CHEMBL370839 IC50 > 10000.0 nM -
CHEMBL364936 IC50 > 10000.0 nM -
CHEMBL195896 IC50 > 10000.0 nM -
CHEMBL372291 IC50 > 10000.0 nM -