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Assay Detail

CHEMBL710993

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

Binding
Binding affinity to compete for 2-[125I]iodomelatonin binding to chicken retinal membranes
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Retina
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Melatonin receptor (CHEMBL2095154)
Type PROTEIN FAMILY
Organism Gallus gallus

Publication

2-Amido-8-methoxytetralins: a series of nonindolic melatonin-like agents.
Copinga S, Tepper PG, Grol CJ, Horn AS, Dubocovich ML.
J Med Chem (1993) 36 : 2891 -2898
PubMed 8411005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.48 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289233 IODOMELATONIN 1 9.89
CHEMBL421013 1 9.64
CHEMBL34622 1 9.57
CHEMBL34730 1 9.47
CHEMBL45 MELATONIN 4.0 1 9.24
CHEMBL288084 1 9.14
CHEMBL99376 1 8.44
CHEMBL95920 1 8.43
CHEMBL99377 1 8.13
CHEMBL330385 1 7.35
CHEMBL53015 1 7.33
CHEMBL95266 1 7.02
CHEMBL316854 1 6.92
CHEMBL95364 1 6.85
CHEMBL421569 1 6.84
CHEMBL95851 1 6.51
CHEMBL52801 1 6.38
CHEMBL53722 1 6.24
CHEMBL322193 1 6.18
CHEMBL299966 1 6.13
CHEMBL50943 1 6.10
CHEMBL95366 1 5.71
CHEMBL99778 1 4.64
CHEMBL535852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289233 IODOMELATONIN Ki = 0.13 nM 9.89
CHEMBL421013 Ki = 0.23 nM 9.64
CHEMBL34622 Ki = 0.27 nM 9.57
CHEMBL34730 Ki = 0.34 nM 9.47
CHEMBL45 MELATONIN Ki = 0.57 nM 9.24
CHEMBL288084 Ki = 0.73 nM 9.14
CHEMBL99376 Ki = 3.6 nM 8.44
CHEMBL95920 Ki = 3.75 nM 8.43
CHEMBL99377 Ki = 7.4 nM 8.13
CHEMBL330385 Ki = 44.4 nM 7.35
CHEMBL53015 Ki = 46.3 nM 7.33
CHEMBL95266 Ki = 95.1 nM 7.02
CHEMBL316854 Ki = 121.0 nM 6.92
CHEMBL95364 Ki = 141.0 nM 6.85
CHEMBL421569 Ki = 145.0 nM 6.84
CHEMBL95851 Ki = 312.0 nM 6.51
CHEMBL52801 Ki = 420.0 nM 6.38
CHEMBL53722 Ki = 581.0 nM 6.24
CHEMBL322193 Ki = 665.0 nM 6.18
CHEMBL299966 Ki = 748.0 nM 6.13
CHEMBL50943 Ki = 789.0 nM 6.10
CHEMBL95366 Ki = 1950.0 nM 5.71
CHEMBL99778 Ki = 23100.0 nM 4.64
CHEMBL535852 Ki > 100000.0 nM -