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Assay Detail

CHEMBL714923

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

Functional
Inhibitory activity against melatonin receptor of quail optica tecta with 200 pM 2-[125] iodomelatonin as gamma-S (10e-4 M)
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 4 6.95 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61991 1 8.52
CHEMBL45 MELATONIN 4.0 1 7.82
CHEMBL292108 1 6.40
CHEMBL61418 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61991 IC50 = 2.99 nM 8.52
CHEMBL45 MELATONIN IC50 = 15.2 nM 7.82
CHEMBL292108 IC50 = 396.0 nM 6.40
CHEMBL61418 IC50 = 8970.0 nM 5.05