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Assay Detail

CHEMBL828790

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

Binding
Inhibition of human melanin concentrating hormone receptor 1
25
Total Activities
25
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

Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.
Palani A, Shapiro S, McBriar MD, Clader JW, Greenlee WJ, Spar B, Kowalski TJ, Farley C, Cook J, van Heek M, Weig B, O'neill K, Graziano M, Hawes B.
J Med Chem (2005) 48 : 4746 -4749
PubMed 16033253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.88 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL364162 1 8.80
CHEMBL191393 1 8.74
CHEMBL363044 1 8.72
CHEMBL364871 1 8.59
CHEMBL189147 1 8.48
CHEMBL191409 1 8.40
CHEMBL190780 1 8.25
CHEMBL187721 1 8.24
CHEMBL189611 1 8.22
CHEMBL190401 1 8.22
CHEMBL191078 1 8.15
CHEMBL191079 1 8.15
CHEMBL187931 1 8.14
CHEMBL187996 1 8.09
CHEMBL433596 1 8.05
CHEMBL189029 1 7.96
CHEMBL433591 1 7.90
CHEMBL191390 1 7.72
CHEMBL190219 1 7.70
CHEMBL187719 1 7.01
CHEMBL371809 1 6.86
CHEMBL187942 1 6.78
CHEMBL363459 1 6.71
CHEMBL188088 1 6.63
CHEMBL186156 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL364162 Ki = 1.6 nM 8.80
CHEMBL191393 Ki = 1.8 nM 8.74
CHEMBL363044 Ki = 1.9 nM 8.72
CHEMBL364871 Ki = 2.6 nM 8.59
CHEMBL189147 Ki = 3.3 nM 8.48
CHEMBL191409 Ki = 4.0 nM 8.40
CHEMBL190780 Ki = 5.6 nM 8.25
CHEMBL187721 Ki = 5.8 nM 8.24
CHEMBL189611 Ki = 6.0 nM 8.22
CHEMBL190401 Ki = 6.0 nM 8.22
CHEMBL191078 Ki = 7.1 nM 8.15
CHEMBL191079 Ki = 7.1 nM 8.15
CHEMBL187931 Ki = 7.3 nM 8.14
CHEMBL187996 Ki = 8.2 nM 8.09
CHEMBL433596 Ki = 8.9 nM 8.05
CHEMBL189029 Ki = 11.0 nM 7.96
CHEMBL433591 Ki = 12.5 nM 7.90
CHEMBL191390 Ki = 19.0 nM 7.72
CHEMBL190219 Ki = 20.0 nM 7.70
CHEMBL187719 Ki = 98.0 nM 7.01
CHEMBL371809 Ki = 139.0 nM 6.86
CHEMBL187942 Ki = 166.0 nM 6.78
CHEMBL363459 Ki = 197.0 nM 6.71
CHEMBL188088 Ki = 233.0 nM 6.63
CHEMBL186156 Ki = 374.0 nM 6.43