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Assay Detail

CHEMBL5530358

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

Functional
Partial agonist activity at C-terminal HA-tagged human MC1-R stably expressed in HEK293 cells co-expressing GScAMP22P cAMP reporter assessed as inhibition of alpha-MSH induced cAMP production by cell based luminescence assay
ChEMBL ↗
69
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design.
Gimenez LE, Martin C, Yu J, Hollanders C, Hernandez CC, Wu Y, Yao D, Han GW, Dahir NS, Wu L, Van der Poorten O, Lamouroux A, Mannes M, Zhao S, Tourwé D, Stevens RC, Cone RD, Ballet S.
J Med Chem (2024) 67 : 2690 -2711
PubMed 38345933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 7.62 10.11
pIC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5574804 — — 2 10.11
CHEMBL5557625 — — 2 9.92
CHEMBL5566308 — — 2 9.70
CHEMBL3422426 — — 2 9.70
CHEMBL5572502 — — 2 9.61
CHEMBL5568902 — — 2 9.31
CHEMBL5592759 — — 2 8.82
CHEMBL5570494 — — 2 8.77
CHEMBL5571320 — — 2 8.60
CHEMBL5562859 — — 2 8.29
CHEMBL5583794 — — 2 8.00
CHEMBL5570854 — — 2 7.98
CHEMBL5575814 — — 2 7.92
CHEMBL5542612 — — 2 7.87
CHEMBL5589988 — — 2 7.81
CHEMBL5571514 — — 2 7.65
CHEMBL5579693 — — 2 7.27
CHEMBL5575572 — — 2 7.16
CHEMBL5590202 — — 2 7.13
CHEMBL5575805 — — 2 7.11
CHEMBL5542650 — — 2 7.05
CHEMBL5542391 — — 2 7.04
CHEMBL5573419 — — 2 6.80
CHEMBL5572575 — — 2 6.76
CHEMBL5566348 — — 2 6.69
CHEMBL5572691 — — 2 6.67
CHEMBL5549790 — — 2 6.53
CHEMBL5575530 — — 2 6.44
CHEMBL5572145 — — 2 6.41
CHEMBL5575419 — — 2 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5574804 — IC50 = 0.07762 nM 10.11
CHEMBL5574804 — IC50 = 0.08 nM 10.10
CHEMBL5557625 — IC50 = 0.12 nM 9.92
CHEMBL5557625 — IC50 = 0.123 nM 9.91
CHEMBL3422426 — IC50 = 0.2 nM 9.70
CHEMBL5566308 — IC50 = 0.2 nM 9.70
CHEMBL3422426 — IC50 = 0.1995 nM 9.70
CHEMBL5566308 — IC50 = 0.1995 nM 9.70
CHEMBL5572502 — IC50 = 0.2455 nM 9.61
CHEMBL5572502 — IC50 = 0.25 nM 9.60
CHEMBL5568902 — IC50 = 0.49 nM 9.31
CHEMBL5568902 — IC50 = 0.4898 nM 9.31
CHEMBL5592759 — IC50 = 1.514 nM 8.82
CHEMBL5592759 — IC50 = 1.53 nM 8.81
CHEMBL5570494 — IC50 = 1.698 nM 8.77
CHEMBL5570494 — IC50 = 1.71 nM 8.77
CHEMBL5571320 — IC50 = 2.512 nM 8.60
CHEMBL5571320 — IC50 = 2.53 nM 8.60
CHEMBL5562859 — IC50 = 5.09 nM 8.29
CHEMBL5562859 — IC50 = 5.129 nM 8.29
CHEMBL5583794 — IC50 = 10.0 nM 8.00
CHEMBL5583794 — IC50 = 10.1 nM 8.00
CHEMBL5570854 — IC50 = 10.47 nM 7.98
CHEMBL5570854 — IC50 = 10.5 nM 7.98
CHEMBL5575814 — IC50 = 12.0 nM 7.92
CHEMBL5575814 — IC50 = 12.02 nM 7.92
CHEMBL5542612 — IC50 = 13.5 nM 7.87
CHEMBL5542612 — IC50 = 13.49 nM 7.87
CHEMBL5589988 — IC50 = 15.4 nM 7.81
CHEMBL5589988 — IC50 = 15.49 nM 7.81
CHEMBL5571514 — IC50 = 22.5 nM 7.65
CHEMBL5571514 — IC50 = 22.39 nM 7.65
CHEMBL5579693 — IC50 = 53.7 nM 7.27
CHEMBL5579693 — IC50 = 53.6 nM 7.27
CHEMBL5575572 — IC50 = 68.9 nM 7.16
CHEMBL5575572 — IC50 = 69.18 nM 7.16
CHEMBL5590202 — IC50 = 74.13 nM 7.13
CHEMBL5590202 — IC50 = 75.0 nM 7.12
CHEMBL5575805 — IC50 = 77.62 nM 7.11
CHEMBL5575805 — IC50 = 77.4 nM 7.11
CHEMBL5542650 — IC50 = 89.13 nM 7.05
CHEMBL5542650 — IC50 = 90.0 nM 7.05
CHEMBL5542391 — IC50 = 91.2 nM 7.04
CHEMBL5542391 — IC50 = 92.0 nM 7.04
CHEMBL5573419 — IC50 = 158.49 nM 6.80
CHEMBL5573419 — IC50 = 158.0 nM 6.80
CHEMBL5572575 — IC50 = 175.0 nM 6.76
CHEMBL5572575 — IC50 = 173.78 nM 6.76
CHEMBL5566348 — IC50 = 204.17 nM 6.69
CHEMBL5566348 — IC50 = 204.0 nM 6.69