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Assay Detail

CHEMBL714909

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Binding
Binding affinity against chicken brain melatonin receptors using 2-[125I]iodomelatonin as radioligand
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melatonin receptor (CHEMBL2095154)
Type PROTEIN FAMILY
Organism Gallus gallus

Publication

Three-dimensional quantitative structure-activity relationship of melatonin receptor ligands: a comparative molecular field analysis study.
Sicsic S, Serraz I, Andrieux J, Brémont B, Mathé-Allainmat M, Poncet A, Shen S, Langlois M.
J Med Chem (1997) 40 : 739 -748
PubMed 9057860 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 8.03 10.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290493 1 10.53
CHEMBL289233 IODOMELATONIN 1 10.49
CHEMBL291857 1 10.14
CHEMBL322269 1 9.92
CHEMBL111599 1 9.85
CHEMBL37771 1 9.74
CHEMBL428882 1 9.62
CHEMBL61626 1 9.41
CHEMBL10878 AGOMELATINE 4.0 1 9.27
CHEMBL62992 1 9.26
CHEMBL294517 1 9.17
CHEMBL45 MELATONIN 4.0 1 9.17
CHEMBL124462 1 8.97
CHEMBL305383 1 8.94
CHEMBL64142 1 8.86
CHEMBL138549 1 8.77
CHEMBL37549 1 8.60
CHEMBL109086 1 8.60
CHEMBL64471 1 8.57
CHEMBL126143 1 8.45
CHEMBL428342 1 8.23
CHEMBL12477 1 8.22
CHEMBL137949 1 8.17
CHEMBL109842 1 8.03
CHEMBL349435 1 7.92
CHEMBL417151 1 7.71
CHEMBL342162 1 7.66
CHEMBL109784 1 7.52
CHEMBL12795 1 7.46
CHEMBL62306 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290493 Ki = 0.02951 nM 10.53
CHEMBL289233 IODOMELATONIN Ki = 0.03236 nM 10.49
CHEMBL291857 Ki = 0.07244 nM 10.14
CHEMBL322269 Ki = 0.1202 nM 9.92
CHEMBL111599 Ki = 0.1413 nM 9.85
CHEMBL37771 Ki = 0.182 nM 9.74
CHEMBL428882 Ki = 0.2399 nM 9.62
CHEMBL61626 Ki = 0.389 nM 9.41
CHEMBL10878 AGOMELATINE Ki = 0.537 nM 9.27
CHEMBL62992 Ki = 0.5495 nM 9.26
CHEMBL294517 Ki = 0.6761 nM 9.17
CHEMBL45 MELATONIN Ki = 0.6761 nM 9.17
CHEMBL124462 Ki = 1.072 nM 8.97
CHEMBL305383 Ki = 1.148 nM 8.94
CHEMBL64142 Ki = 1.38 nM 8.86
CHEMBL138549 Ki = 1.698 nM 8.77
CHEMBL37549 Ki = 2.512 nM 8.60
CHEMBL109086 Ki = 2.512 nM 8.60
CHEMBL64471 Ki = 2.692 nM 8.57
CHEMBL126143 Ki = 3.548 nM 8.45
CHEMBL428342 Ki = 5.888 nM 8.23
CHEMBL12477 Ki = 6.026 nM 8.22
CHEMBL137949 Ki = 6.761 nM 8.17
CHEMBL109842 Ki = 9.333 nM 8.03
CHEMBL349435 Ki = 12.02 nM 7.92
CHEMBL417151 Ki = 19.5 nM 7.71
CHEMBL342162 Ki = 21.88 nM 7.66
CHEMBL109784 Ki = 30.2 nM 7.52
CHEMBL12795 Ki = 34.67 nM 7.46
CHEMBL62306 Ki = 41.69 nM 7.38
CHEMBL34349 Ki = 44.67 nM 7.35
CHEMBL162456 Ki = 56.23 nM 7.25
CHEMBL162914 Ki = 64.57 nM 7.19
CHEMBL63006 Ki = 70.79 nM 7.15
CHEMBL162154 Ki = 114.82 nM 6.94
CHEMBL124076 Ki = 158.49 nM 6.80
CHEMBL304685 Ki = 194.98 nM 6.71
CHEMBL53015 Ki = 204.17 nM 6.69
CHEMBL52801 Ki = 213.8 nM 6.67
CHEMBL104997 Ki = 213.8 nM 6.67
CHEMBL291378 Ki = 218.78 nM 6.66
CHEMBL165186 Ki = 229.09 nM 6.64
CHEMBL350753 Ki = 239.88 nM 6.62
CHEMBL53722 Ki = 251.19 nM 6.60
CHEMBL125081 Ki = 288.4 nM 6.54
CHEMBL62495 Ki = 323.59 nM 6.49
CHEMBL33171 NB-ACETYLTRYPTAMINE Ki = 489.78 nM 6.31
CHEMBL165685 Ki = 1905.46 nM 5.72