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Assay Detail

CHEMBL3269751

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

Binding
Displacement of [125I]2-iodomelatonin from human MT1 receptor expressed in CHO cells
7
Total Activities
7
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 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 7 8.48 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334079 1 9.20
CHEMBL14453 1 8.51
CHEMBL3260984 1 8.47
CHEMBL3260985 1 8.41
CHEMBL429392 1 8.41
CHEMBL1097525 1 8.28
CHEMBL3260986 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334079 Ki = 0.63 nM 9.20
CHEMBL14453 Ki = 3.1 nM 8.51
CHEMBL3260984 Ki = 3.4 nM 8.47
CHEMBL3260985 Ki = 3.9 nM 8.41
CHEMBL429392 Ki = 3.9 nM 8.41
CHEMBL1097525 Ki = 5.2 nM 8.28
CHEMBL3260986 Ki = 7.9 nM 8.10