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Assay Detail

CHEMBL839715

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

Binding
Binding affinity for melanocortin-3 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand
17
Total Activities
17
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 3 (CHEMBL4644)
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 17 6.12 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195308 1 6.41
CHEMBL363190 1 6.35
CHEMBL194987 1 6.25
CHEMBL195071 1 6.24
CHEMBL194990 1 6.24
CHEMBL365597 1 6.19
CHEMBL195110 1 6.17
CHEMBL436122 1 6.10
CHEMBL363576 1 6.10
CHEMBL194393 1 6.10
CHEMBL373099 1 6.09
CHEMBL192090 1 6.08
CHEMBL191701 1 6.07
CHEMBL364463 1 6.02
CHEMBL191857 1 6.00
CHEMBL192464 1 5.89
CHEMBL363641 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195308 Ki = 390.0 nM 6.41
CHEMBL363190 Ki = 450.0 nM 6.35
CHEMBL194987 Ki = 560.0 nM 6.25
CHEMBL195071 Ki = 570.0 nM 6.24
CHEMBL194990 Ki = 580.0 nM 6.24
CHEMBL365597 Ki = 640.0 nM 6.19
CHEMBL195110 Ki = 670.0 nM 6.17
CHEMBL436122 Ki = 790.0 nM 6.10
CHEMBL363576 Ki = 790.0 nM 6.10
CHEMBL194393 Ki = 800.0 nM 6.10
CHEMBL373099 Ki = 810.0 nM 6.09
CHEMBL192090 Ki = 830.0 nM 6.08
CHEMBL191701 Ki = 860.0 nM 6.07
CHEMBL364463 Ki = 950.0 nM 6.02
CHEMBL191857 Ki = 1000.0 nM 6.00
CHEMBL192464 Ki = 1300.0 nM 5.89
CHEMBL363641 Ki = 1600.0 nM 5.80