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Assay Detail

CHEMBL839716

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

Binding
Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice.
Pontillo J, Tran JA, Markison S, Joppa M, Fleck BA, Marinkovic D, Arellano M, Tucci FC, Lanier M, Nelson J, Saunders J, Hoare SR, Foster AC, Chen C.
Bioorg Med Chem Lett (2005) 15 : 2541 -2546
PubMed 15863313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.85 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194990 1 8.89
CHEMBL363190 1 8.85
CHEMBL195110 1 8.82
CHEMBL363576 1 8.77
CHEMBL365597 1 8.74
CHEMBL194987 1 8.70
CHEMBL364463 1 8.70
CHEMBL191701 1 8.68
CHEMBL195071 1 8.62
CHEMBL191857 1 8.62
CHEMBL192090 1 8.55
CHEMBL195308 1 8.54
CHEMBL363641 1 8.51
CHEMBL436122 1 8.49
CHEMBL192464 1 8.35
CHEMBL194393 1 8.34
CHEMBL373099 1 8.30
CHEMBL195734 1 8.30
CHEMBL362985 1 8.10
CHEMBL195414 1 7.85
CHEMBL186074 1 7.82
CHEMBL192153 1 7.80
CHEMBL191831 1 7.75
CHEMBL191645 1 7.75
CHEMBL186083 1 7.68
CHEMBL364913 1 7.64
CHEMBL193061 1 7.64
CHEMBL435933 1 7.51
CHEMBL365940 1 7.03
CHEMBL40711 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194990 Ki = 1.3 nM 8.89
CHEMBL363190 Ki = 1.4 nM 8.85
CHEMBL195110 Ki = 1.5 nM 8.82
CHEMBL363576 Ki = 1.7 nM 8.77
CHEMBL365597 Ki = 1.8 nM 8.74
CHEMBL194987 Ki = 2.0 nM 8.70
CHEMBL364463 Ki = 2.0 nM 8.70
CHEMBL191701 Ki = 2.1 nM 8.68
CHEMBL195071 Ki = 2.4 nM 8.62
CHEMBL191857 Ki = 2.4 nM 8.62
CHEMBL192090 Ki = 2.8 nM 8.55
CHEMBL195308 Ki = 2.9 nM 8.54
CHEMBL363641 Ki = 3.1 nM 8.51
CHEMBL436122 Ki = 3.2 nM 8.49
CHEMBL192464 Ki = 4.5 nM 8.35
CHEMBL194393 Ki = 4.6 nM 8.34
CHEMBL373099 Ki = 5.0 nM 8.30
CHEMBL195734 Ki = 5.0 nM 8.30
CHEMBL362985 Ki = 7.9 nM 8.10
CHEMBL195414 Ki = 14.0 nM 7.85
CHEMBL186074 Ki = 15.0 nM 7.82
CHEMBL192153 Ki = 16.0 nM 7.80
CHEMBL191831 Ki = 18.0 nM 7.75
CHEMBL191645 Ki = 18.0 nM 7.75
CHEMBL186083 Ki = 21.0 nM 7.68
CHEMBL364913 Ki = 23.0 nM 7.64
CHEMBL193061 Ki = 23.0 nM 7.64
CHEMBL435933 Ki = 31.0 nM 7.51
CHEMBL365940 Ki = 94.0 nM 7.03
CHEMBL40711 Ki = 160.0 nM 6.80
CHEMBL366171 Ki = 420.0 nM 6.38
CHEMBL363561 Ki = 1100.0 nM 5.96
CHEMBL193786 Ki = 2300.0 nM 5.64
CHEMBL195172 Ki = 3600.0 nM 5.44
CHEMBL370926 Ki = 5700.0 nM 5.24
CHEMBL194819 Ki > 10000.0 nM -