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Assay Detail

CHEMBL714710

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

Binding
Binding affinity against ovine pars tuberalis melatonin receptor using 2-[125I]- melatonin radioligand binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melatonin receptor (CHEMBL2094268)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and biological activity of conformationally restricted tricyclic analogs of the hormone melatonin
Leclerc V, Depreux P, Lesieur D, Caignard D, Renard P, Delagrange P, Guardiola-Lemaitre B, Morgan P
Bioorg Med Chem Lett (1996) 6 : 1071 -1076
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.76 10.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45 MELATONIN 4.0 1 10.04
CHEMBL10878 AGOMELATINE 4.0 1 10.00
CHEMBL11356 1 9.86
CHEMBL274358 1 9.67
CHEMBL11404 1 9.11
CHEMBL11328 1 8.21
CHEMBL11416 1 7.86
CHEMBL11148 1 7.21
CHEMBL10816 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45 MELATONIN Ki = 0.0915 nM 10.04
CHEMBL10878 AGOMELATINE Ki = 0.1 nM 10.00
CHEMBL11356 Ki = 0.137 nM 9.86
CHEMBL274358 Ki = 0.216 nM 9.67
CHEMBL11404 Ki = 0.78 nM 9.11
CHEMBL11328 Ki = 6.17 nM 8.21
CHEMBL11416 Ki = 13.9 nM 7.86
CHEMBL11148 Ki = 62.2 nM 7.21
CHEMBL10816 Ki = 130.0 nM 6.89