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Assay Detail

CHEMBL4775180

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

Binding
Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins
ChEMBL ↗
34
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
Martin C,Gimenez LE,Williams SY,Jing Y,Wu Y,Hollanders C,Van der Poorten O,Gonzalez S,Van Holsbeeck K,Previti S,Lamouroux A,Zhao S,Tourwé D,Stevens RC,Cone RD,Ballet S
J Med Chem (2021) 64 : 357 -369
PubMed 33190475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 10.11 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4798971 — — 2 10.82
CHEMBL4794168 — — 2 10.80
CHEMBL4794121 — — 2 10.78
CHEMBL4777048 — — 2 10.71
CHEMBL4793821 — — 2 10.68
CHEMBL4788071 — — 2 10.68
CHEMBL4794990 — — 2 10.59
CHEMBL4791788 — — 2 10.56
CHEMBL3422426 — — 2 10.55
CHEMBL4800268 — — 2 10.46
CHEMBL4776915 — — 2 10.38
CHEMBL4791306 — — 2 9.34
CHEMBL430239 MELATONAN — 2 9.34
CHEMBL4795842 — — 2 9.26
CHEMBL4776340 — — 2 9.11
CHEMBL4784053 — — 2 9.04
CHEMBL4787753 — — 2 8.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4798971 — Ki = 0.015 nM 10.82
CHEMBL4798971 — Ki = 0.01514 nM 10.82
CHEMBL4794168 — Ki = 0.01585 nM 10.80
CHEMBL4794168 — Ki = 0.016 nM 10.80
CHEMBL4794121 — Ki = 0.0166 nM 10.78
CHEMBL4794121 — Ki = 0.017 nM 10.77
CHEMBL4777048 — Ki = 0.0195 nM 10.71
CHEMBL4777048 — Ki = 0.02 nM 10.70
CHEMBL4788071 — Ki = 0.021 nM 10.68
CHEMBL4793821 — Ki = 0.02089 nM 10.68
CHEMBL4793821 — Ki = 0.021 nM 10.68
CHEMBL4788071 — Ki = 0.02138 nM 10.67
CHEMBL4794990 — Ki = 0.026 nM 10.59
CHEMBL4794990 — Ki = 0.0257 nM 10.59
CHEMBL4791788 — Ki = 0.02754 nM 10.56
CHEMBL3422426 — Ki = 0.02818 nM 10.55
CHEMBL4791788 — Ki = 0.028 nM 10.55
CHEMBL3422426 — Ki = 0.029 nM 10.54
CHEMBL4800268 — Ki = 0.03467 nM 10.46
CHEMBL4800268 — Ki = 0.035 nM 10.46
CHEMBL4776915 — Ki = 0.042 nM 10.38
CHEMBL4776915 — Ki = 0.04169 nM 10.38
CHEMBL430239 MELATONAN Ki = 0.456 nM 9.34
CHEMBL4791306 — Ki = 0.459 nM 9.34
CHEMBL4791306 — Ki = 0.4571 nM 9.34
CHEMBL430239 MELATONAN Ki = 0.4571 nM 9.34
CHEMBL4795842 — Ki = 0.551 nM 9.26
CHEMBL4795842 — Ki = 0.5495 nM 9.26
CHEMBL4776340 — Ki = 0.769 nM 9.11
CHEMBL4776340 — Ki = 0.7762 nM 9.11
CHEMBL4784053 — Ki = 0.915 nM 9.04
CHEMBL4784053 — Ki = 0.912 nM 9.04
CHEMBL4787753 — Ki = 1.38 nM 8.86
CHEMBL4787753 — Ki = 1.38 nM 8.86