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Assay Detail

CHEMBL712439

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

Binding
Binding affinity towards melatonin receptor was determined using 2-[125I]iodomelatonin as radioligand in chick brain membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gallus gallus
Tissue Brain
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Melatonin receptor (CHEMBL2095154)
Type PROTEIN FAMILY
Organism Gallus gallus

Publication

Mapping the melatonin receptor. 2. synthesis and biological activity of indole derived melatonin analogues with restricted conformations of the C-3 amidoethane side chain
Garratt PJ, Vonhoff S, Rowe SJ, Sugden D
Bioorg Med Chem Lett (1994) 4 : 1559 -1564
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.00 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290895 1 9.42
CHEMBL45 MELATONIN 4.0 1 9.23
CHEMBL38728 1 9.01
CHEMBL441966 1 8.84
CHEMBL288225 1 8.70
CHEMBL38520 1 8.08
CHEMBL287988 1 7.52
CHEMBL287776 1 7.39
CHEMBL288198 1 7.09
CHEMBL417343 1 6.99
CHEMBL289549 1 6.69
CHEMBL287944 1 6.67
CHEMBL41105 1 6.66
CHEMBL290903 1 6.64
CHEMBL33700 1 6.59
CHEMBL38587 1 6.57
CHEMBL41148 1 6.36
CHEMBL290271 1 6.25
CHEMBL288206 1 6.24
CHEMBL291120 1 6.13
CHEMBL41744 1 6.12
CHEMBL38720 1 5.97
CHEMBL288746 1 5.35
CHEMBL289370 1 5.33
CHEMBL41973 1 5.27
CHEMBL41581 1 -
CHEMBL38962 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290895 Ki = 0.378 nM 9.42
CHEMBL45 MELATONIN Ki = 0.59 nM 9.23
CHEMBL38728 Ki = 0.97 nM 9.01
CHEMBL441966 Ki = 1.44 nM 8.84
CHEMBL288225 Ki = 1.98 nM 8.70
CHEMBL38520 Ki = 8.3 nM 8.08
CHEMBL287988 Ki = 30.0 nM 7.52
CHEMBL287776 Ki = 41.0 nM 7.39
CHEMBL288198 Ki = 82.0 nM 7.09
CHEMBL417343 Ki = 102.0 nM 6.99
CHEMBL289549 Ki = 204.0 nM 6.69
CHEMBL287944 Ki = 215.0 nM 6.67
CHEMBL41105 Ki = 219.0 nM 6.66
CHEMBL290903 Ki = 227.0 nM 6.64
CHEMBL33700 Ki = 254.0 nM 6.59
CHEMBL38587 Ki = 271.0 nM 6.57
CHEMBL41148 Ki = 436.0 nM 6.36
CHEMBL290271 Ki = 560.0 nM 6.25
CHEMBL288206 Ki = 570.0 nM 6.24
CHEMBL291120 Ki = 740.0 nM 6.13
CHEMBL41744 Ki = 766.0 nM 6.12
CHEMBL38720 Ki = 1060.0 nM 5.97
CHEMBL288746 Ki = 4460.0 nM 5.35
CHEMBL289370 Ki = 4630.0 nM 5.33
CHEMBL41973 Ki = 5350.0 nM 5.27
CHEMBL41581 Ki > 10000.0 nM -
CHEMBL38962 Ki > 10000.0 nM -