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Assay Detail

CHEMBL1016924

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Binding
Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Ribosyldihydronicotinamide dehydrogenase [quinone] (CHEMBL3959)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel quantitative structure-activity relationship method to predict the affinities of MT3 melatonin binding site.
Du H, Wang J, Zhang X, Hu Z.
Eur J Med Chem (2008) 43 : 2861 -2869
PubMed 18400335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.90 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300056 1 10.05
CHEMBL300728 1 9.89
CHEMBL52559 1 9.70
CHEMBL511675 1 9.52
CHEMBL53622 1 9.51
CHEMBL300195 1 8.92
CHEMBL33700 1 8.55
CHEMBL457126 1 8.52
CHEMBL465378 1 8.11
CHEMBL457992 1 8.04
CHEMBL457541 1 7.96
CHEMBL493424 1 7.96
CHEMBL455339 1 7.92
CHEMBL495399 1 7.85
CHEMBL457539 1 7.85
CHEMBL446329 1 7.80
CHEMBL456727 1 7.74
CHEMBL494566 1 7.74
CHEMBL458209 1 7.68
CHEMBL521826 1 7.64
CHEMBL456691 1 7.62
CHEMBL443636 1 7.55
CHEMBL34348 1 7.54
CHEMBL457763 1 7.49
CHEMBL456646 1 7.43
CHEMBL443429 1 7.38
CHEMBL37703 1 7.36
CHEMBL457764 1 7.29
CHEMBL467573 1 7.28
CHEMBL457540 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300056 IC50 = 0.08913 nM 10.05
CHEMBL300728 IC50 = 0.1288 nM 9.89
CHEMBL52559 IC50 = 0.1995 nM 9.70
CHEMBL511675 IC50 = 0.302 nM 9.52
CHEMBL53622 IC50 = 0.309 nM 9.51
CHEMBL300195 IC50 = 1.202 nM 8.92
CHEMBL33700 IC50 = 2.818 nM 8.55
CHEMBL457126 IC50 = 3.02 nM 8.52
CHEMBL465378 IC50 = 7.762 nM 8.11
CHEMBL457992 IC50 = 9.12 nM 8.04
CHEMBL493424 IC50 = 10.96 nM 7.96
CHEMBL457541 IC50 = 10.96 nM 7.96
CHEMBL455339 IC50 = 12.02 nM 7.92
CHEMBL495399 IC50 = 14.13 nM 7.85
CHEMBL457539 IC50 = 14.13 nM 7.85
CHEMBL446329 IC50 = 15.85 nM 7.80
CHEMBL456727 IC50 = 18.2 nM 7.74
CHEMBL494566 IC50 = 18.2 nM 7.74
CHEMBL458209 IC50 = 20.89 nM 7.68
CHEMBL521826 IC50 = 22.91 nM 7.64
CHEMBL456691 IC50 = 23.99 nM 7.62
CHEMBL443636 IC50 = 28.18 nM 7.55
CHEMBL34348 IC50 = 28.84 nM 7.54
CHEMBL457763 IC50 = 32.36 nM 7.49
CHEMBL456646 IC50 = 37.15 nM 7.43
CHEMBL443429 IC50 = 41.69 nM 7.38
CHEMBL37703 IC50 = 43.65 nM 7.36
CHEMBL457764 IC50 = 51.29 nM 7.29
CHEMBL467573 IC50 = 52.48 nM 7.28
CHEMBL457540 IC50 = 53.7 nM 7.27
CHEMBL521827 IC50 = 56.23 nM 7.25
CHEMBL504585 IC50 = 57.54 nM 7.24
CHEMBL511361 IC50 = 61.66 nM 7.21
CHEMBL457533 IC50 = 61.66 nM 7.21
CHEMBL45 MELATONIN IC50 = 64.57 nM 7.19
CHEMBL323332 IC50 = 64.57 nM 7.19
CHEMBL451333 IC50 = 67.61 nM 7.17
CHEMBL505118 IC50 = 67.61 nM 7.17
CHEMBL111674 IC50 = 70.79 nM 7.15