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Assay Detail

CHEMBL3268962

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

Binding
Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
Zlotos DP, Jockers R, Cecon E, Rivara S, Witt-Enderby PA.
J Med Chem (2014) 57 : 3161 -3185
PubMed 24228714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.66 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289233 IODOMELATONIN 1 10.17
CHEMBL3260979 1 8.87
CHEMBL34730 1 7.94
CHEMBL339105 1 7.49
CHEMBL3260983 1 7.04
CHEMBL286615 LUZINDOLE 1 6.80
CHEMBL124699 1 6.68
CHEMBL285718 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289233 IODOMELATONIN Ki = 0.068 nM 10.17
CHEMBL3260979 Ki = 1.34 nM 8.87
CHEMBL34730 Ki = 11.4 nM 7.94
CHEMBL339105 Ki = 32.7 nM 7.49
CHEMBL3260983 Ki = 90.4 nM 7.04
CHEMBL286615 LUZINDOLE Ki = 158.0 nM 6.80
CHEMBL124699 Ki = 207.0 nM 6.68
CHEMBL285718 Ki = 501.0 nM 6.30