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Assay Detail

CHEMBL716360

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

Functional
Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melanocortin receptor 3 (CHEMBL4644)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of gamma-MSH analogues at the human melanocortin MC3, MC4, and MC5 receptors. Discovery of highly selective hMC3R, hMC4R, and hMC5R analogues.
Balse-Srinivasan P, Grieco P, Cai M, Trivedi D, Hruby VJ.
J Med Chem (2003) 46 : 4965 -4973
PubMed 14584947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 7.23 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438030 1 8.80
CHEMBL437050 1 8.43
CHEMBL439128 1 8.38
CHEMBL2370967 1 7.92
CHEMBL438235 1 7.72
CHEMBL410168 1 7.44
CHEMBL263878 1 7.41
CHEMBL2370965 1 6.82
CHEMBL427629 1 6.68
CHEMBL409636 1 6.62
CHEMBL409049 1 6.40
CHEMBL2370968 1 5.77
CHEMBL2370963 1 5.62
CHEMBL443590 1 -
CHEMBL441760 1 -
CHEMBL2370964 1 -
CHEMBL411564 1 -
CHEMBL2370966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438030 EC50 = 1.6 nM 8.80
CHEMBL437050 EC50 = 3.7 nM 8.43
CHEMBL439128 EC50 = 4.2 nM 8.38
CHEMBL2370967 EC50 = 12.0 nM 7.92
CHEMBL438235 EC50 = 19.0 nM 7.72
CHEMBL410168 EC50 = 36.0 nM 7.44
CHEMBL263878 EC50 = 39.0 nM 7.41
CHEMBL2370965 EC50 = 150.0 nM 6.82
CHEMBL427629 EC50 = 210.0 nM 6.68
CHEMBL409636 EC50 = 240.0 nM 6.62
CHEMBL409049 EC50 = 400.0 nM 6.40
CHEMBL2370968 EC50 = 1700.0 nM 5.77
CHEMBL2370963 EC50 = 2400.0 nM 5.62
CHEMBL443590 EC50 > 10000.0 nM -
CHEMBL441760 EC50 > 10000.0 nM -
CHEMBL2370964 EC50 > 10000.0 nM -
CHEMBL411564 EC50 > 10000.0 nM -
CHEMBL2370966 EC50 > 10000.0 nM -