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Assay Detail

CHEMBL3424975

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

Binding
Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocyte-stimulating hormone receptor (CHEMBL4077)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
Doering SR, Todorovic A, Haskell-Luevano C.
ACS Med Chem Lett (2015) 6 : 123 -127
PubMed 25699138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 6.27 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN 1 9.66
CHEMBL3422426 1 9.17
CHEMBL264190 1 7.15
CHEMBL3422427 1 5.70
CHEMBL3422430 1 5.57
CHEMBL3422432 1 5.26
CHEMBL3422433 1 5.24
CHEMBL3422431 1 5.19
CHEMBL3422429 1 5.08
CHEMBL3422428 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 0.22 nM 9.66
CHEMBL3422426 EC50 = 0.67 nM 9.17
CHEMBL264190 EC50 = 71.0 nM 7.15
CHEMBL3422427 EC50 = 2000.0 nM 5.70
CHEMBL3422430 EC50 = 2700.0 nM 5.57
CHEMBL3422432 EC50 = 5500.0 nM 5.26
CHEMBL3422433 EC50 = 5800.0 nM 5.24
CHEMBL3422431 EC50 = 6500.0 nM 5.19
CHEMBL3422429 EC50 = 8300.0 nM 5.08
CHEMBL3422428 EC50 = 20700.0 nM 4.68