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Assay Detail

CHEMBL839970

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

Binding
Binding affinity at melanocortin-5 receptor stably transfected in HEK 293 cells using [125I]NDP-MSH as radiolabeled
8
Total Activities
8
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 5 (CHEMBL4608)
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 8 6.31 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195110 1 6.80
CHEMBL363576 1 6.52
CHEMBL195308 1 6.46
CHEMBL194987 1 6.46
CHEMBL436122 1 6.25
CHEMBL192464 1 6.17
CHEMBL195071 1 6.14
CHEMBL195734 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195110 Ki = 160.0 nM 6.80
CHEMBL363576 Ki = 300.0 nM 6.52
CHEMBL195308 Ki = 350.0 nM 6.46
CHEMBL194987 Ki = 350.0 nM 6.46
CHEMBL436122 Ki = 560.0 nM 6.25
CHEMBL192464 Ki = 680.0 nM 6.17
CHEMBL195071 Ki = 730.0 nM 6.14
CHEMBL195734 Ki = 2300.0 nM 5.64