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Assay Detail

CHEMBL4835801

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

Functional
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 4 (CHEMBL3719)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
Doering SR, Freeman K, Debevec G, Geer P, Santos RG, Lavoi TM, Giulianotti MA, Pinilla C, Appel JR, Houghten RA, Ericson MD, Haskell-Luevano C.
J Med Chem (2021) 64 : 5577 -5592
PubMed 33886285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.81 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL342954 1 9.05
CHEMBL438402 1 8.80
CHEMBL264190 1 8.26
CHEMBL4868636 1 6.57
CHEMBL4868223 1 6.24
CHEMBL4863206 1 6.19
CHEMBL4871577 1 5.88
CHEMBL4877537 1 5.17
CHEMBL4878922 1 5.09
CHEMBL441738 AFAMELANOTIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL342954 EC50 = 0.9 nM 9.05
CHEMBL438402 EC50 = 1.6 nM 8.80
CHEMBL264190 EC50 = 5.5 nM 8.26
CHEMBL4868636 EC50 = 270.0 nM 6.57
CHEMBL4868223 EC50 = 580.0 nM 6.24
CHEMBL4863206 EC50 = 650.0 nM 6.19
CHEMBL4871577 EC50 = 1330.0 nM 5.88
CHEMBL4877537 EC50 = 6700.0 nM 5.17
CHEMBL4878922 EC50 = 8200.0 nM 5.09
CHEMBL441738 AFAMELANOTIDE EC50 = 0.12 nM -