Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4834840

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

Functional
Agonist activity at human MT1 receptor expressed in CHO cells assessed as increase in forskolin induced cAMP production incubated at 37 degreeC by HitHunter-cAMP assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melatonin receptor type 1A (CHEMBL1945)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of <b>ACH-000143</b>: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats.
Ferreira MA, Azevedo H, Mascarello A, Segretti ND, Russo E, Russo V, Guimarães CRW.
J Med Chem (2021) 64 : 1904 -1929
PubMed 33626870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 10.15 10.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852096 1 10.46
CHEMBL4848885 1 10.44
CHEMBL4852440 1 10.43
CHEMBL4859677 1 10.40
CHEMBL4854625 1 10.38
CHEMBL4873903 1 10.38
CHEMBL4859295 1 10.20
CHEMBL4854836 1 9.63
CHEMBL4846505 1 9.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852096 EC50 = 0.035 nM 10.46
CHEMBL4848885 EC50 = 0.036 nM 10.44
CHEMBL4852440 EC50 = 0.037 nM 10.43
CHEMBL4859677 EC50 = 0.04 nM 10.40
CHEMBL4854625 EC50 = 0.042 nM 10.38
CHEMBL4873903 EC50 = 0.042 nM 10.38
CHEMBL4859295 EC50 = 0.063 nM 10.20
CHEMBL4854836 EC50 = 0.233 nM 9.63
CHEMBL4846505 EC50 = 0.937 nM 9.03