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Assay Detail

CHEMBL1107083

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

Binding
Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting
22
Total Activities
22
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

Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.
Hu Y, Ho MK, Chan KH, New DC, Wong YH.
Bioorg Med Chem Lett (2010) 20 : 2582 -2585
PubMed 20227878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 8.04 10.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1091998 1 10.49
CHEMBL1091160 1 10.33
CHEMBL45 MELATONIN 4.0 1 9.37
CHEMBL50398 1 9.12
CHEMBL1091561 1 8.80
CHEMBL1091716 1 8.79
CHEMBL1091894 1 8.67
CHEMBL297947 1 8.15
CHEMBL1092047 1 7.90
CHEMBL1091895 1 7.87
CHEMBL1092400 1 7.58
CHEMBL1092839 1 7.55
CHEMBL1092062 1 7.33
CHEMBL1092647 1 7.16
CHEMBL1091896 1 7.14
CHEMBL1091997 1 6.99
CHEMBL1093457 1 6.98
CHEMBL1092911 1 6.92
CHEMBL1088826 1 5.64
CHEMBL1088825 1 -
CHEMBL1092646 1 -
CHEMBL1091161 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1091998 Ki = 0.0326 nM 10.49
CHEMBL1091160 Ki = 0.04705 nM 10.33
CHEMBL45 MELATONIN Ki = 0.429 nM 9.37
CHEMBL50398 Ki = 0.751 nM 9.12
CHEMBL1091561 Ki = 1.59 nM 8.80
CHEMBL1091716 Ki = 1.61 nM 8.79
CHEMBL1091894 Ki = 2.12 nM 8.67
CHEMBL297947 Ki = 7.07 nM 8.15
CHEMBL1092047 Ki = 12.6 nM 7.90
CHEMBL1091895 Ki = 13.4 nM 7.87
CHEMBL1092400 Ki = 26.1 nM 7.58
CHEMBL1092839 Ki = 27.9 nM 7.55
CHEMBL1092062 Ki = 46.2 nM 7.33
CHEMBL1092647 Ki = 69.3 nM 7.16
CHEMBL1091896 Ki = 72.2 nM 7.14
CHEMBL1091997 Ki = 102.0 nM 6.99
CHEMBL1093457 Ki = 105.0 nM 6.98
CHEMBL1092911 Ki = 121.0 nM 6.92
CHEMBL1088826 Ki = 2300.0 nM 5.64
CHEMBL1088825 Ki = 0.00103 nM -
CHEMBL1092646 Ki = 0.00069 nM -
CHEMBL1091161 Ki = 0.00055 nM -