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Assay Detail

CHEMBL714927

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

Binding
Binding affinity for Melatonin receptor using 2-[125I]iodomelatonin as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Coturnix
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Melatonin receptor (CHEMBL2094268)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study.
Mor M, Rivara S, Silva C, Bordi F, Plazzi PV, Spadoni G, Diamantini G, Balsamini C, Tarzia G, Fraschini F, Lucini V, Nonno R, Stankov BM.
J Med Chem (1998) 41 : 3831 -3844
PubMed 9748358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.34 9.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127337 1 9.75
CHEMBL45 MELATONIN 4.0 1 9.21
CHEMBL123900 1 8.53
CHEMBL127134 1 8.24
CHEMBL33700 1 8.17
CHEMBL33800 1 8.05
CHEMBL288562 1 7.52
CHEMBL284521 1 7.14
CHEMBL285477 1 6.92
CHEMBL284158 1 6.75
CHEMBL286814 1 6.72
CHEMBL34327 1 6.54
CHEMBL126809 1 6.54
CHEMBL33869 1 6.42
CHEMBL30930 1 6.21
CHEMBL283600 1 6.19
CHEMBL33099 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127337 Ki = 0.176 nM 9.75
CHEMBL45 MELATONIN Ki = 0.61 nM 9.21
CHEMBL123900 Ki = 2.98 nM 8.53
CHEMBL127134 Ki = 5.75 nM 8.24
CHEMBL33700 Ki = 6.72 nM 8.17
CHEMBL33800 Ki = 8.91 nM 8.05
CHEMBL288562 Ki = 30.0 nM 7.52
CHEMBL284521 Ki = 72.8 nM 7.14
CHEMBL285477 Ki = 121.0 nM 6.92
CHEMBL284158 Ki = 180.0 nM 6.75
CHEMBL286814 Ki = 190.0 nM 6.72
CHEMBL34327 Ki = 287.0 nM 6.54
CHEMBL126809 Ki = 289.0 nM 6.54
CHEMBL33869 Ki = 380.0 nM 6.42
CHEMBL30930 Ki = 617.0 nM 6.21
CHEMBL283600 Ki = 647.0 nM 6.19
CHEMBL33099 Ki = 1180.0 nM 5.93