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Assay Detail

CHEMBL987966

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

Functional
Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
12
Total Activities
12
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 1B (CHEMBL1946)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of 3-phenylnaphthalenic derivatives as new selective MT(2) melatoninergic ligands.
Poissonnier-Durieux S, Ettaoussi M, Pérès B, Boutin JA, Audinot V, Bennejean C, Delagrange P, Caignard DH, Renard P, Berthelot P, Lesieur D, Yous S.
Bioorg Med Chem (2008) 16 : 8339 -8348
PubMed 18778943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 9.12 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10878 AGOMELATINE 4.0 1 10.00
CHEMBL45 MELATONIN 4.0 1 9.31
CHEMBL477835 1 9.30
CHEMBL476341 1 9.22
CHEMBL518113 1 9.15
CHEMBL476131 1 9.12
CHEMBL490595 1 9.00
CHEMBL491604 1 8.89
CHEMBL490188 1 8.89
CHEMBL478217 1 8.82
CHEMBL453138 1 8.62
CHEMBL477834 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10878 AGOMELATINE EC50 = 0.1 nM 10.00
CHEMBL45 MELATONIN EC50 = 0.49 nM 9.31
CHEMBL477835 EC50 = 0.5 nM 9.30
CHEMBL476341 EC50 = 0.6 nM 9.22
CHEMBL518113 EC50 = 0.7 nM 9.15
CHEMBL476131 EC50 = 0.76 nM 9.12
CHEMBL490595 EC50 = 1.0 nM 9.00
CHEMBL491604 EC50 = 1.3 nM 8.89
CHEMBL490188 EC50 = 1.3 nM 8.89
CHEMBL478217 EC50 = 1.5 nM 8.82
CHEMBL453138 EC50 = 2.4 nM 8.62
CHEMBL477834 EC50 - -