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Assay Detail

CHEMBL714922

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

Binding
Inhibitory activity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin as radiolabeled ligand
19
Total Activities
19
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

Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
Spadoni G, Balsamini C, Diamantini G, Di Giacomo B, Tarzia G, Mor M, Plazzi PV, Rivara S, Lucini V, Nonno R, Pannacci M, Fraschini F, Stankov BM.
J Med Chem (1997) 40 : 1990 -2002
PubMed 9207940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.42 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15060 1 10.21
CHEMBL33415 1 9.89
CHEMBL61991 1 8.85
CHEMBL61380 1 8.77
CHEMBL45 MELATONIN 4.0 1 8.66
CHEMBL34730 1 8.44
CHEMBL60832 1 8.00
CHEMBL60719 1 7.54
CHEMBL292108 1 7.14
CHEMBL60033 1 6.64
CHEMBL61418 1 5.92
CHEMBL64517 1 5.89
CHEMBL60001 1 5.52
CHEMBL58015 1 5.37
CHEMBL61505 1 4.48
CHEMBL60946 1 -
CHEMBL64368 1 -
CHEMBL61216 1 -
CHEMBL302883 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15060 IC50 = 0.062 nM 10.21
CHEMBL33415 IC50 = 0.13 nM 9.89
CHEMBL61991 IC50 = 1.4 nM 8.85
CHEMBL61380 IC50 = 1.7 nM 8.77
CHEMBL45 MELATONIN IC50 = 2.2 nM 8.66
CHEMBL34730 IC50 = 3.6 nM 8.44
CHEMBL60832 IC50 = 9.9 nM 8.00
CHEMBL60719 IC50 = 29.0 nM 7.54
CHEMBL292108 IC50 = 73.0 nM 7.14
CHEMBL60033 IC50 = 230.0 nM 6.64
CHEMBL61418 IC50 = 1200.0 nM 5.92
CHEMBL64517 IC50 = 1300.0 nM 5.89
CHEMBL60001 IC50 = 3000.0 nM 5.52
CHEMBL58015 IC50 = 4300.0 nM 5.37
CHEMBL61505 IC50 = 33000.0 nM 4.48
CHEMBL60946 IC50 > 10000.0 nM -
CHEMBL64368 IC50 > 10000.0 nM -
CHEMBL61216 IC50 > 10000.0 nM -
CHEMBL302883 IC50 > 10000.0 nM -