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Assay Detail

CHEMBL4835798

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

Functional
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay
20
Total Activities
20
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 3 (CHEMBL4774)
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 20 6.47 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.44
CHEMBL438402 1 9.25
CHEMBL264190 1 7.51
CHEMBL4868636 1 6.68
CHEMBL4848322 1 6.66
CHEMBL4863206 1 6.62
CHEMBL342954 1 6.58
CHEMBL4864094 1 6.51
CHEMBL4862172 1 6.46
CHEMBL4868223 1 6.44
CHEMBL4878201 1 6.44
CHEMBL4846261 1 6.43
CHEMBL4872932 1 6.38
CHEMBL4877442 1 5.70
CHEMBL4878558 1 5.55
CHEMBL4856877 1 5.43
CHEMBL4869531 1 5.40
CHEMBL4877232 1 5.37
CHEMBL4866532 1 5.28
CHEMBL4869669 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441738 AFAMELANOTIDE EC50 = 0.36 nM 9.44
CHEMBL438402 EC50 = 0.56 nM 9.25
CHEMBL264190 EC50 = 31.0 nM 7.51
CHEMBL4868636 EC50 = 210.0 nM 6.68
CHEMBL4848322 EC50 = 220.0 nM 6.66
CHEMBL4863206 EC50 = 240.0 nM 6.62
CHEMBL342954 EC50 = 260.0 nM 6.58
CHEMBL4864094 EC50 = 310.0 nM 6.51
CHEMBL4862172 EC50 = 350.0 nM 6.46
CHEMBL4868223 EC50 = 360.0 nM 6.44
CHEMBL4878201 EC50 = 360.0 nM 6.44
CHEMBL4846261 EC50 = 370.0 nM 6.43
CHEMBL4872932 EC50 = 420.0 nM 6.38
CHEMBL4877442 EC50 = 2000.0 nM 5.70
CHEMBL4878558 EC50 = 2800.0 nM 5.55
CHEMBL4856877 EC50 = 3700.0 nM 5.43
CHEMBL4869531 EC50 = 4000.0 nM 5.40
CHEMBL4877232 EC50 = 4300.0 nM 5.37
CHEMBL4866532 EC50 = 5200.0 nM 5.28
CHEMBL4869669 EC50 = 6200.0 nM 5.21