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Assay Detail

CHEMBL874168

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Binding
inhibitory concentration against Melatonin receptor
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
IC50 17 6.75 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127337 1 9.18
CHEMBL45 MELATONIN 4.0 1 8.66
CHEMBL123900 1 7.89
CHEMBL127134 1 7.63
CHEMBL33700 1 7.59
CHEMBL33800 1 7.47
CHEMBL288562 1 6.90
CHEMBL284521 1 6.53
CHEMBL285477 1 6.31
CHEMBL284158 1 6.14
CHEMBL286814 1 6.11
CHEMBL126809 1 5.99
CHEMBL34327 1 5.96
CHEMBL33869 1 5.83
CHEMBL30930 1 5.61
CHEMBL283600 1 5.58
CHEMBL33099 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127337 IC50 = 0.654 nM 9.18
CHEMBL45 MELATONIN IC50 = 2.2 nM 8.66
CHEMBL123900 IC50 = 12.8 nM 7.89
CHEMBL127134 IC50 = 23.3 nM 7.63
CHEMBL33700 IC50 = 25.5 nM 7.59
CHEMBL33800 IC50 = 33.6 nM 7.47
CHEMBL288562 IC50 = 126.0 nM 6.90
CHEMBL284521 IC50 = 295.0 nM 6.53
CHEMBL285477 IC50 = 491.0 nM 6.31
CHEMBL284158 IC50 = 719.0 nM 6.14
CHEMBL286814 IC50 = 772.0 nM 6.11
CHEMBL126809 IC50 = 1020.0 nM 5.99
CHEMBL34327 IC50 = 1090.0 nM 5.96
CHEMBL33869 IC50 = 1470.0 nM 5.83
CHEMBL30930 IC50 = 2460.0 nM 5.61
CHEMBL283600 IC50 = 2620.0 nM 5.58
CHEMBL33099 IC50 = 4800.0 nM 5.32