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Assay Detail

CHEMBL878682

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

Functional
Inhibition of 2-[125I]iodomelatonin stimulated calcium dependent dopamine release from the rabbit retina.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Melatonin receptor (CHEMBL2094268)
Type PROTEIN FAMILY
Organism Homo sapiens

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
IC50 18 8.98 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421013 1 11.00
CHEMBL45 MELATONIN 4.0 1 10.77
CHEMBL34730 1 10.40
CHEMBL95920 1 10.20
CHEMBL99377 1 9.32
CHEMBL330385 1 9.00
CHEMBL99376 1 8.92
CHEMBL95266 1 8.89
CHEMBL53015 1 8.85
CHEMBL316854 1 8.80
CHEMBL95364 1 8.60
CHEMBL52801 1 8.52
CHEMBL95366 1 8.19
CHEMBL95851 1 8.10
CHEMBL421569 1 8.09
CHEMBL99778 1 7.66
CHEMBL322193 1 7.28
CHEMBL289233 IODOMELATONIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421013 IC50 = 0.01 nM 11.00
CHEMBL45 MELATONIN IC50 = 0.017 nM 10.77
CHEMBL34730 IC50 = 0.04 nM 10.40
CHEMBL95920 IC50 = 0.063 nM 10.20
CHEMBL99377 IC50 = 0.48 nM 9.32
CHEMBL330385 IC50 = 1.0 nM 9.00
CHEMBL99376 IC50 = 1.2 nM 8.92
CHEMBL95266 IC50 = 1.3 nM 8.89
CHEMBL53015 IC50 = 1.4 nM 8.85
CHEMBL316854 IC50 = 1.6 nM 8.80
CHEMBL95364 IC50 = 2.5 nM 8.60
CHEMBL52801 IC50 = 3.0 nM 8.52
CHEMBL95366 IC50 = 6.5 nM 8.19
CHEMBL95851 IC50 = 7.9 nM 8.10
CHEMBL421569 IC50 = 8.1 nM 8.09
CHEMBL99778 IC50 = 22.0 nM 7.66
CHEMBL322193 IC50 = 52.0 nM 7.28
CHEMBL289233 IODOMELATONIN IC50 = 0.005 nM -