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Assay Detail

CHEMBL828893

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

Binding
Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH
29
Total Activities
29
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

Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Tran JA, Pontillo J, Arellano M, White NS, Fleck BA, Marinkovic D, Tucci FC, Lanier M, Nelson J, Saunders J, Foster AC, Chen C.
Bioorg Med Chem Lett (2005) 15 : 833 -837
PubMed 15664867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.31 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183799 1 8.32
CHEMBL182277 1 8.20
CHEMBL360716 1 8.19
CHEMBL368023 1 8.00
CHEMBL366706 1 7.96
CHEMBL368022 1 7.66
CHEMBL362850 1 7.62
CHEMBL183831 1 7.52
CHEMBL361210 1 7.48
CHEMBL182823 1 7.47
CHEMBL183610 1 7.44
CHEMBL180545 1 7.39
CHEMBL179889 1 7.33
CHEMBL361985 1 7.31
CHEMBL2113020 1 7.28
CHEMBL369104 1 7.28
CHEMBL181788 1 7.25
CHEMBL2113023 1 7.11
CHEMBL362841 1 7.06
CHEMBL2113019 1 7.05
CHEMBL183114 1 6.96
CHEMBL366708 1 6.96
CHEMBL180304 1 6.92
CHEMBL183134 1 6.92
CHEMBL182900 1 6.85
CHEMBL369348 1 6.80
CHEMBL2113022 1 6.62
CHEMBL360296 1 6.57
CHEMBL181277 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183799 Ki = 4.8 nM 8.32
CHEMBL182277 Ki = 6.3 nM 8.20
CHEMBL360716 Ki = 6.4 nM 8.19
CHEMBL368023 Ki = 10.0 nM 8.00
CHEMBL366706 Ki = 11.0 nM 7.96
CHEMBL368022 Ki = 22.0 nM 7.66
CHEMBL362850 Ki = 24.0 nM 7.62
CHEMBL183831 Ki = 30.0 nM 7.52
CHEMBL361210 Ki = 33.0 nM 7.48
CHEMBL182823 Ki = 34.0 nM 7.47
CHEMBL183610 Ki = 36.0 nM 7.44
CHEMBL180545 Ki = 41.0 nM 7.39
CHEMBL179889 Ki = 47.0 nM 7.33
CHEMBL361985 Ki = 49.0 nM 7.31
CHEMBL2113020 Ki = 53.0 nM 7.28
CHEMBL369104 Ki = 52.0 nM 7.28
CHEMBL181788 Ki = 56.0 nM 7.25
CHEMBL2113023 Ki = 78.0 nM 7.11
CHEMBL362841 Ki = 87.0 nM 7.06
CHEMBL2113019 Ki = 89.0 nM 7.05
CHEMBL183114 Ki = 110.0 nM 6.96
CHEMBL366708 Ki = 110.0 nM 6.96
CHEMBL180304 Ki = 120.0 nM 6.92
CHEMBL183134 Ki = 120.0 nM 6.92
CHEMBL182900 Ki = 140.0 nM 6.85
CHEMBL369348 Ki = 160.0 nM 6.80
CHEMBL2113022 Ki = 240.0 nM 6.62
CHEMBL360296 Ki = 270.0 nM 6.57
CHEMBL181277 Ki = 370.0 nM 6.43