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Assay Detail

CHEMBL826381

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

Binding
Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-5 receptor
7
Total Activities
7
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

Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor.
Pontillo J, Tran JA, Arellano M, Fleck BA, Huntley R, Marinkovic D, Lanier M, Nelson J, Parker J, Saunders J, Tucci FC, Jiang W, Chen CW, White NS, Foster AC, Chen C.
Bioorg Med Chem Lett (2004) 14 : 4417 -4423
PubMed 15357964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.23 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366706 1 6.62
CHEMBL365278 1 6.58
CHEMBL360716 1 6.57
CHEMBL185035 1 6.23
CHEMBL339053 1 6.07
CHEMBL340355 1 5.92
CHEMBL183434 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366706 Ki = 240.0 nM 6.62
CHEMBL365278 Ki = 260.0 nM 6.58
CHEMBL360716 Ki = 270.0 nM 6.57
CHEMBL185035 Ki = 590.0 nM 6.23
CHEMBL339053 Ki = 860.0 nM 6.07
CHEMBL340355 Ki = 1200.0 nM 5.92
CHEMBL183434 Ki = 2300.0 nM 5.64