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Assay Detail

CHEMBL4775170

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Functional
Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay
ChEMBL ↗
42
Total Activities
21
Compounds Tested
1
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

Melanocortin receptor 3 (CHEMBL4644) ↗
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
IC50 42 6.56 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4779301 — — 2 7.37
CHEMBL4794168 — — 2 7.36
CHEMBL4792986 — — 2 7.32
CHEMBL4798971 — — 2 7.12
CHEMBL4777048 — — 2 7.11
CHEMBL4794121 — — 2 7.09
CHEMBL3422426 — — 2 7.08
CHEMBL4799891 — — 2 6.98
CHEMBL4778074 — — 2 6.69
CHEMBL4788071 — — 2 6.57
CHEMBL4797266 — — 2 6.53
CHEMBL4784635 — — 2 6.49
CHEMBL4794990 — — 2 6.46
CHEMBL4787322 — — 2 6.43
CHEMBL4799036 — — 2 6.26
CHEMBL4793821 — — 2 6.23
CHEMBL4800268 — — 2 6.12
CHEMBL4782808 — — 2 6.01
CHEMBL4793346 — — 2 6.00
CHEMBL4796506 — — 2 5.39
CHEMBL4776915 — — 2 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4779301 — IC50 = 43.0 nM 7.37
CHEMBL4779301 — IC50 = 43.65 nM 7.36
CHEMBL4794168 — IC50 = 43.65 nM 7.36
CHEMBL4794168 — IC50 = 44.0 nM 7.36
CHEMBL4792986 — IC50 = 48.0 nM 7.32
CHEMBL4792986 — IC50 = 47.86 nM 7.32
CHEMBL4798971 — IC50 = 76.0 nM 7.12
CHEMBL4798971 — IC50 = 75.86 nM 7.12
CHEMBL4777048 — IC50 = 78.0 nM 7.11
CHEMBL4777048 — IC50 = 77.62 nM 7.11
CHEMBL4794121 — IC50 = 81.0 nM 7.09
CHEMBL4794121 — IC50 = 81.28 nM 7.09
CHEMBL3422426 — IC50 = 83.0 nM 7.08
CHEMBL3422426 — IC50 = 83.18 nM 7.08
CHEMBL4799891 — IC50 = 104.71 nM 6.98
CHEMBL4799891 — IC50 = 105.0 nM 6.98
CHEMBL4778074 — IC50 = 204.17 nM 6.69
CHEMBL4778074 — IC50 = 206.0 nM 6.69
CHEMBL4788071 — IC50 = 271.0 nM 6.57
CHEMBL4788071 — IC50 = 269.15 nM 6.57
CHEMBL4797266 — IC50 = 298.0 nM 6.53
CHEMBL4797266 — IC50 = 295.12 nM 6.53
CHEMBL4784635 — IC50 = 323.59 nM 6.49
CHEMBL4784635 — IC50 = 322.0 nM 6.49
CHEMBL4794990 — IC50 = 345.0 nM 6.46
CHEMBL4794990 — IC50 = 346.74 nM 6.46
CHEMBL4787322 — IC50 = 371.54 nM 6.43
CHEMBL4787322 — IC50 = 374.0 nM 6.43
CHEMBL4799036 — IC50 = 545.0 nM 6.26
CHEMBL4799036 — IC50 = 549.54 nM 6.26
CHEMBL4793821 — IC50 = 586.0 nM 6.23
CHEMBL4793821 — IC50 = 588.84 nM 6.23
CHEMBL4800268 — IC50 = 751.0 nM 6.12
CHEMBL4800268 — IC50 = 758.58 nM 6.12
CHEMBL4782808 — IC50 = 977.24 nM 6.01
CHEMBL4793346 — IC50 = 1000.0 nM 6.00
CHEMBL4793346 — IC50 = 1012.0 nM 6.00
CHEMBL4782808 — IC50 = 1349.0 nM 5.87
CHEMBL4796506 — IC50 = 4055.0 nM 5.39
CHEMBL4796506 — IC50 = 4073.8 nM 5.39
CHEMBL4776915 — IC50 = 5128.61 nM 5.29
CHEMBL4776915 — IC50 = 5140.0 nM 5.29