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Assay Detail

CHEMBL3762917

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

Functional
Intrinsic activity at human MT2 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
14
Total Activities
14
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

Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.
Landagaray E, Ettaoussi M, Duroux R, Boutin JA, Caignard DH, Delagrange P, Melnyk P, Berthelot P, Yous S.
Eur J Med Chem (2016) 109 : 360 -370
PubMed 26820449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.63 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10878 AGOMELATINE 4.0 1 9.74
CHEMBL3759802 1 9.15
CHEMBL3758717 1 9.01
CHEMBL3758679 1 9.01
CHEMBL3759084 1 8.96
CHEMBL3758225 1 8.85
CHEMBL3759606 1 8.49
CHEMBL3759160 1 8.47
CHEMBL3759859 1 8.24
CHEMBL3760044 1 8.21
CHEMBL3759816 1 8.06
CHEMBL3759054 1 8.06
CHEMBL3759080 1 8.00
CHEMBL3758720 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10878 AGOMELATINE EC50 = 0.18 nM 9.74
CHEMBL3759802 EC50 = 0.7 nM 9.15
CHEMBL3758717 EC50 = 0.98 nM 9.01
CHEMBL3758679 EC50 = 0.98 nM 9.01
CHEMBL3759084 EC50 = 1.1 nM 8.96
CHEMBL3758225 EC50 = 1.4 nM 8.85
CHEMBL3759606 EC50 = 3.2 nM 8.49
CHEMBL3759160 EC50 = 3.4 nM 8.47
CHEMBL3759859 EC50 = 5.8 nM 8.24
CHEMBL3760044 EC50 = 6.2 nM 8.21
CHEMBL3759816 EC50 = 8.8 nM 8.06
CHEMBL3759054 EC50 = 8.8 nM 8.06
CHEMBL3759080 EC50 = 10.0 nM 8.00
CHEMBL3758720 EC50 > 10000.0 nM -