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Assay Detail

CHEMBL4052191

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

Functional
Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocortin receptor 3 (CHEMBL4774)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.
Doering SR, Freeman KT, Schnell SM, Haslach EM, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Speth RC, Houghten RA, Haskell-Luevano C.
J Med Chem (2017) 60 : 4342 -4357
PubMed 28453292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 5.57 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068643 1 5.80
CHEMBL4089759 1 5.70
CHEMBL4084136 1 5.60
CHEMBL4080138 1 5.60
CHEMBL4068777 1 5.60
CHEMBL4099096 1 5.40
CHEMBL4105142 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068643 Kd = 1584.89 nM 5.80
CHEMBL4089759 Kd = 1995.26 nM 5.70
CHEMBL4084136 Kd = 2511.89 nM 5.60
CHEMBL4080138 Kd = 2511.89 nM 5.60
CHEMBL4068777 Kd = 2511.89 nM 5.60
CHEMBL4099096 Kd = 3981.07 nM 5.40
CHEMBL4105142 Kd = 5011.87 nM 5.30