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Assay Detail

CHEMBL5512926

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Binding
Binding affinity to human MT1 receptor assessed as inhibition constant
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The location, physiology, pathology of hippocampus Melatonin MT<sub>2</sub> receptor and MT<sub>2</sub>-selective modulators.
Feng Y, Jiang X, Liu W, Lu H.
Eur J Med Chem (2023) 262 : 115888 -115888
PubMed 37866336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.84 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774529 1 10.96
CHEMBL5566857 1 9.05
CHEMBL274842 1 8.74
CHEMBL9997 1 8.36
CHEMBL10009 1 8.35
CHEMBL10099 1 8.35
CHEMBL5557851 1 7.96
CHEMBL3612464 1 7.77
CHEMBL5555481 1 7.72
CHEMBL3612471 1 7.54
CHEMBL5558348 1 7.26
CHEMBL274438 1 7.18
CHEMBL5542464 1 7.00
CHEMBL33185 1 5.89
CHEMBL5555823 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774529 Ki = 0.011 nM 10.96
CHEMBL5566857 Ki = 0.9 nM 9.05
CHEMBL274842 Ki = 1.82 nM 8.74
CHEMBL9997 Ki = 4.37 nM 8.36
CHEMBL10009 Ki = 4.47 nM 8.35
CHEMBL10099 Ki = 4.47 nM 8.35
CHEMBL5557851 Ki = 11.0 nM 7.96
CHEMBL3612464 Ki = 17.0 nM 7.77
CHEMBL5555481 Ki = 19.0 nM 7.72
CHEMBL3612471 Ki = 29.0 nM 7.54
CHEMBL5558348 Ki = 55.0 nM 7.26
CHEMBL274438 Ki = 66.1 nM 7.18
CHEMBL5542464 Ki = 99.0 nM 7.00
CHEMBL33185 Ki = 1290.0 nM 5.89
CHEMBL5555823 Ki = 2980.0 nM 5.53