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Assay Detail

CHEMBL3768199

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 HEK293 cells after 120 mins by radioligand competition assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of 2-arylfuro[3,2-b]pyridines: Effect of the C2-aryl group on melatoninergic activity.
Couhert A, Delagrange P, Caignard DH, Chartier A, Suzenet F, Guillaumet G.
Eur J Med Chem (2016) 109 : 268 -275
PubMed 26785296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.31 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765540 1 10.40
CHEMBL323332 1 9.82
CHEMBL3765401 1 9.70
CHEMBL3763503 1 9.70
CHEMBL1760944 1 9.62
CHEMBL45 MELATONIN 4.0 1 9.60
CHEMBL3763281 1 8.80
CHEMBL3764765 1 8.66
CHEMBL3765249 1 8.02
CHEMBL3764063 1 7.51
CHEMBL137969 1 7.40
CHEMBL3763537 1 7.17
CHEMBL3763247 1 7.14
CHEMBL3764421 1 6.92
CHEMBL3764879 1 6.70
CHEMBL2326199 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765540 Ki = 0.04 nM 10.40
CHEMBL323332 Ki = 0.15 nM 9.82
CHEMBL3765401 Ki = 0.2 nM 9.70
CHEMBL3763503 Ki = 0.2 nM 9.70
CHEMBL1760944 Ki = 0.24 nM 9.62
CHEMBL45 MELATONIN Ki = 0.25 nM 9.60
CHEMBL3763281 Ki = 1.6 nM 8.80
CHEMBL3764765 Ki = 2.2 nM 8.66
CHEMBL3765249 Ki = 9.5 nM 8.02
CHEMBL3764063 Ki = 31.0 nM 7.51
CHEMBL137969 Ki = 40.0 nM 7.40
CHEMBL3763537 Ki = 68.0 nM 7.17
CHEMBL3763247 Ki = 73.0 nM 7.14
CHEMBL3764421 Ki = 120.0 nM 6.92
CHEMBL3764879 Ki = 198.0 nM 6.70
CHEMBL2326199 Ki = 1350.0 nM 5.87