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Assay Detail

CHEMBL854908

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

Binding
Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Iyengar RR, Lynch JK, Mulhern MM, Judd AS, Freeman JC, Gao J, Souers AJ, Zhao G, Wodka D, Doug Falls H, Brodjian S, Dayton BD, Reilly RM, Swanson S, Su Z, Martin RL, Leitza ST, Houseman KA, Diaz G, Collins CA, Sham HL, Kym PR.
Bioorg Med Chem Lett (2007) 17 : 874 -878
PubMed 17234405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.53 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386281 1 9.00
CHEMBL266725 1 8.52
CHEMBL214021 1 8.52
CHEMBL216104 1 8.40
CHEMBL274168 1 8.30
CHEMBL216554 1 8.15
CHEMBL216482 1 8.15
CHEMBL216524 1 8.00
CHEMBL217233 1 7.72
CHEMBL216180 1 7.42
CHEMBL217435 1 7.37
CHEMBL269352 1 7.33
CHEMBL384043 1 7.02
CHEMBL384844 1 6.78
CHEMBL215457 1 5.90
CHEMBL216680 1 5.77
CHEMBL216323 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386281 IC50 = 1.0 nM 9.00
CHEMBL266725 IC50 = 3.0 nM 8.52
CHEMBL214021 IC50 = 3.0 nM 8.52
CHEMBL216104 IC50 = 4.0 nM 8.40
CHEMBL274168 IC50 = 5.0 nM 8.30
CHEMBL216554 IC50 = 7.0 nM 8.15
CHEMBL216482 IC50 = 7.0 nM 8.15
CHEMBL216524 IC50 = 10.0 nM 8.00
CHEMBL217233 IC50 = 19.0 nM 7.72
CHEMBL216180 IC50 = 38.0 nM 7.42
CHEMBL217435 IC50 = 43.0 nM 7.37
CHEMBL269352 IC50 = 47.0 nM 7.33
CHEMBL384043 IC50 = 95.0 nM 7.02
CHEMBL384844 IC50 = 166.0 nM 6.78
CHEMBL215457 IC50 = 1267.0 nM 5.90
CHEMBL216680 IC50 = 1700.0 nM 5.77
CHEMBL216323 IC50 = 2010.0 nM 5.70