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Assay Detail

CHEMBL5113217

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

Functional
Agonist activity at human MT1 receptor transfected in HEK293T cells co-transfected with tet-inducible luciferase reporter plasmid, pCDNA3.1(+)-CMV-betaArrestin2-tev plasmid and TANGO plasmid assessed as tango arrestin recruitment incubated for 24 hrs by TANGO-GPCR assay based luminescence plate reader analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.
Li TZ, Hu J, Sun JJ, Huang XY, Geng CA, Liu SB, Zhang XM, Chen JJ.
RSC Med Chem (2022) 13 : 1212 -1224
PubMed 36325395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 4.68 4.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15060 1 4.78
CHEMBL5186032 1 4.68
CHEMBL10878 AGOMELATINE 4.0 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15060 EC50 = 16500.0 nM 4.78
CHEMBL5186032 EC50 = 21000.0 nM 4.68
CHEMBL10878 AGOMELATINE EC50 = 26500.0 nM 4.58