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Assay Detail

CHEMBL714926

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

Binding
Binding affinity against melatonin receptor in the quail optica tecta using 2-[125] iodomelatonin as labelled ligand
16
Total Activities
16
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
Ki 16 7.84 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15060 1 10.77
CHEMBL33415 1 10.44
CHEMBL61991 1 9.41
CHEMBL61380 1 9.32
CHEMBL45 MELATONIN 4.0 1 9.21
CHEMBL34730 1 9.00
CHEMBL60832 1 8.57
CHEMBL60719 1 8.10
CHEMBL292108 1 7.70
CHEMBL60033 1 7.20
CHEMBL61418 1 6.48
CHEMBL64517 1 6.44
CHEMBL60001 1 6.09
CHEMBL58015 1 5.92
CHEMBL14701 1 5.72
CHEMBL61505 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15060 Ki = 0.017 nM 10.77
CHEMBL33415 Ki = 0.036 nM 10.44
CHEMBL61991 Ki = 0.39 nM 9.41
CHEMBL61380 Ki = 0.48 nM 9.32
CHEMBL45 MELATONIN Ki = 0.61 nM 9.21
CHEMBL34730 Ki = 0.99 nM 9.00
CHEMBL60832 Ki = 2.7 nM 8.57
CHEMBL60719 Ki = 8.0 nM 8.10
CHEMBL292108 Ki = 20.0 nM 7.70
CHEMBL60033 Ki = 63.0 nM 7.20
CHEMBL61418 Ki = 330.0 nM 6.48
CHEMBL64517 Ki = 360.0 nM 6.44
CHEMBL60001 Ki = 820.0 nM 6.09
CHEMBL58015 Ki = 1200.0 nM 5.92
CHEMBL14701 Ki = 1900.0 nM 5.72
CHEMBL61505 Ki = 9100.0 nM 5.04