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Assay Detail

CHEMBL3762919

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

Binding
Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cell membranes after 120 mins
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 20 8.62 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3759802 1 10.05
CHEMBL10878 AGOMELATINE 4.0 1 9.68
CHEMBL323332 1 9.47
CHEMBL3758717 1 9.40
CHEMBL45 MELATONIN 4.0 1 9.28
CHEMBL3758679 1 9.22
CHEMBL3758225 1 9.15
CHEMBL3759084 1 9.15
CHEMBL3759372 1 9.10
CHEMBL3758720 1 8.77
CHEMBL3759160 1 8.68
CHEMBL3759080 1 8.38
CHEMBL3759677 1 8.15
CHEMBL3759859 1 7.96
CHEMBL3759606 1 7.88
CHEMBL3759816 1 7.82
CHEMBL3759054 1 7.62
CHEMBL3759180 1 7.34
CHEMBL3760044 1 6.65
CHEMBL3759661 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3759802 Ki = 0.09 nM 10.05
CHEMBL10878 AGOMELATINE Ki = 0.21 nM 9.68
CHEMBL323332 Ki = 0.34 nM 9.47
CHEMBL3758717 Ki = 0.4 nM 9.40
CHEMBL45 MELATONIN Ki = 0.52 nM 9.28
CHEMBL3758679 Ki = 0.6 nM 9.22
CHEMBL3758225 Ki = 0.7 nM 9.15
CHEMBL3759084 Ki = 0.7 nM 9.15
CHEMBL3759372 Ki = 0.8 nM 9.10
CHEMBL3758720 Ki = 1.7 nM 8.77
CHEMBL3759160 Ki = 2.1 nM 8.68
CHEMBL3759080 Ki = 4.2 nM 8.38
CHEMBL3759677 Ki = 7.0 nM 8.15
CHEMBL3759859 Ki = 11.0 nM 7.96
CHEMBL3759606 Ki = 13.3 nM 7.88
CHEMBL3759816 Ki = 15.0 nM 7.82
CHEMBL3759054 Ki = 24.0 nM 7.62
CHEMBL3759180 Ki = 46.0 nM 7.34
CHEMBL3760044 Ki = 226.0 nM 6.65
CHEMBL3759661 Ki - -