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Assay Detail

CHEMBL886329

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

Binding
Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells
23
Total Activities
23
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 Intermediate

Target

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

Publication

Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.
Balavoine F, Malabre P, Alleaume T, Rey A, Cherfils V, Jeanneton O, Seigneurin-Venin S, Revah F.
Bioorg Med Chem Lett (2007) 17 : 3754 -3759
PubMed 17448659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.59 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213255 1 7.60
CHEMBL178707 1 7.42
CHEMBL246588 1 7.09
CHEMBL246790 1 7.00
CHEMBL246794 1 6.79
CHEMBL392403 1 6.75
CHEMBL440229 1 6.66
CHEMBL395699 1 6.58
CHEMBL247566 1 6.47
CHEMBL247764 1 6.45
CHEMBL246992 1 6.44
CHEMBL394310 1 6.38
CHEMBL248266 1 6.15
CHEMBL394311 1 6.00
CHEMBL246590 1 5.96
CHEMBL248267 1 5.69
CHEMBL397064 1 -
CHEMBL246741 1 -
CHEMBL392402 1 -
CHEMBL429293 1 -
CHEMBL428049 1 -
CHEMBL248462 1 -
CHEMBL392214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213255 Ki = 25.0 nM 7.60
CHEMBL178707 Ki = 38.0 nM 7.42
CHEMBL246588 Ki = 82.0 nM 7.09
CHEMBL246790 Ki = 101.0 nM 7.00
CHEMBL246794 Ki = 164.0 nM 6.79
CHEMBL392403 Ki = 176.0 nM 6.75
CHEMBL440229 Ki = 220.0 nM 6.66
CHEMBL395699 Ki = 260.0 nM 6.58
CHEMBL247566 Ki = 341.0 nM 6.47
CHEMBL247764 Ki = 357.0 nM 6.45
CHEMBL246992 Ki = 365.0 nM 6.44
CHEMBL394310 Ki = 415.0 nM 6.38
CHEMBL248266 Ki = 707.0 nM 6.15
CHEMBL394311 Ki = 1000.0 nM 6.00
CHEMBL246590 Ki = 1090.0 nM 5.96
CHEMBL248267 Ki = 2060.0 nM 5.69
CHEMBL397064 Ki > 5000.0 nM -
CHEMBL246741 Ki > 5000.0 nM -
CHEMBL392402 Ki > 5000.0 nM -
CHEMBL429293 Ki > 5000.0 nM -
CHEMBL428049 Ki > 5000.0 nM -
CHEMBL248462 Ki > 5000.0 nM -
CHEMBL392214 Ki > 5000.0 nM -