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Assay Detail

CHEMBL4734042

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

Binding
Inhibition of recombinant human CDC7/Dbf4 expressed in baculovirus infected Sf9 insect cells assessed as inhibition of fluorescein labelled substrate phosphorylation in presence of ATP measured after 60 mins by TR-FRET assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis.
Rojas-Prats E,Martinez-Gonzalez L,Gonzalo-Consuegra C,Liachko NF,Perez C,Ramírez D,Kraemer BC,Martin-Requero Á,Perez DI,Gil C,de Lago E,Martinez A
Eur J Med Chem (2021) 210 : 112968 -112968
PubMed 33139113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.45 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4747601 1 7.10
CHEMBL4083753 1 7.05
CHEMBL4094018 1 6.89
CHEMBL4798875 1 6.89
CHEMBL4791355 1 6.85
CHEMBL4754930 1 6.85
CHEMBL4778242 1 6.85
CHEMBL342925 1 6.77
CHEMBL1402653 1 6.75
CHEMBL4786570 1 6.72
CHEMBL4753615 1 6.72
CHEMBL4788849 1 6.72
CHEMBL397434 1 6.70
CHEMBL4740308 1 6.64
CHEMBL4748528 1 6.62
CHEMBL4776786 1 6.60
CHEMBL4776788 1 6.57
CHEMBL4744159 1 6.54
CHEMBL4756665 1 6.52
CHEMBL4745322 1 6.52
CHEMBL4747259 1 6.52
CHEMBL4787888 1 6.50
CHEMBL4787327 1 6.47
CHEMBL4746008 1 6.44
CHEMBL4758430 1 6.44
CHEMBL4747973 1 6.41
CHEMBL4752489 1 6.41
CHEMBL1600876 1 6.36
CHEMBL4795521 1 6.33
CHEMBL4752064 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4747601 IC50 = 80.0 nM 7.10
CHEMBL4083753 IC50 = 90.0 nM 7.05
CHEMBL4094018 IC50 = 130.0 nM 6.89
CHEMBL4798875 IC50 = 130.0 nM 6.89
CHEMBL4791355 IC50 = 140.0 nM 6.85
CHEMBL4754930 IC50 = 140.0 nM 6.85
CHEMBL4778242 IC50 = 140.0 nM 6.85
CHEMBL342925 IC50 = 170.0 nM 6.77
CHEMBL1402653 IC50 = 180.0 nM 6.75
CHEMBL4753615 IC50 = 190.0 nM 6.72
CHEMBL4788849 IC50 = 190.0 nM 6.72
CHEMBL4786570 IC50 = 190.0 nM 6.72
CHEMBL397434 IC50 = 200.0 nM 6.70
CHEMBL4740308 IC50 = 230.0 nM 6.64
CHEMBL4748528 IC50 = 240.0 nM 6.62
CHEMBL4776786 IC50 = 250.0 nM 6.60
CHEMBL4776788 IC50 = 270.0 nM 6.57
CHEMBL4744159 IC50 = 290.0 nM 6.54
CHEMBL4756665 IC50 = 300.0 nM 6.52
CHEMBL4747259 IC50 = 300.0 nM 6.52
CHEMBL4745322 IC50 = 300.0 nM 6.52
CHEMBL4787888 IC50 = 320.0 nM 6.50
CHEMBL4787327 IC50 = 340.0 nM 6.47
CHEMBL4746008 IC50 = 360.0 nM 6.44
CHEMBL4758430 IC50 = 360.0 nM 6.44
CHEMBL4747973 IC50 = 390.0 nM 6.41
CHEMBL4752489 IC50 = 390.0 nM 6.41
CHEMBL1600876 IC50 = 440.0 nM 6.36
CHEMBL4795521 IC50 = 470.0 nM 6.33
CHEMBL4752064 IC50 = 580.0 nM 6.24
CHEMBL4789025 IC50 = 910.0 nM 6.04
CHEMBL4760791 IC50 = 1380.0 nM 5.86
CHEMBL4750945 IC50 = 1720.0 nM 5.76
CHEMBL4781617 IC50 = 2120.0 nM 5.67
CHEMBL1870315 IC50 = 3060.0 nM 5.51
CHEMBL1336029 IC50 = 3110.0 nM 5.51
CHEMBL1532238 IC50 = 4150.0 nM 5.38