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Assay Detail

CHEMBL2034663

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

Binding
Inhibition of CDC7 in human MDA-MB-231T cells assessed as inhibition of MCM2 phosphorylation at Ser53 after 4 hrs
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cell division cycle 7-related protein kinase (CHEMBL5443)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of XL413, a potent and selective CDC7 inhibitor.
Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M, Galan A, Holst CR, Huang P, Kane B, Kim MH, Li J, Markby D, Mohan M, Noson K, Plonowski A, Richards SJ, Robertson S, Shaw K, Stott G, Stout TJ, Young J, Yu P, Zaharia CA, Zhang W, Zhou P, Nuss JM, Xu W, Kearney PC.
Bioorg Med Chem Lett (2012) 22 : 3727 -3731
PubMed 22560567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.22 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2030393 1 7.12
CHEMBL2030400 1 7.09
CHEMBL2030402 1 6.93
CHEMBL2030404 1 6.78
CHEMBL2030405 1 6.54
CHEMBL2030389 1 6.45
CHEMBL2030390 1 6.44
CHEMBL2030399 1 6.36
CHEMBL2030401 1 6.25
CHEMBL2030387 1 6.20
CHEMBL2030398 1 6.10
CHEMBL2030397 1 6.06
CHEMBL2030403 1 5.86
CHEMBL2030396 1 5.84
CHEMBL2030376 1 5.83
CHEMBL2030386 1 5.74
CHEMBL2030395 1 5.63
CHEMBL2030392 1 5.60
CHEMBL2030394 1 5.34
CHEMBL2030391 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2030393 IC50 = 75.0 nM 7.12
CHEMBL2030400 IC50 = 82.0 nM 7.09
CHEMBL2030402 IC50 = 118.0 nM 6.93
CHEMBL2030404 IC50 = 167.0 nM 6.78
CHEMBL2030405 IC50 = 292.0 nM 6.54
CHEMBL2030389 IC50 = 353.0 nM 6.45
CHEMBL2030390 IC50 = 362.0 nM 6.44
CHEMBL2030399 IC50 = 440.0 nM 6.36
CHEMBL2030401 IC50 = 566.0 nM 6.25
CHEMBL2030387 IC50 = 625.0 nM 6.20
CHEMBL2030398 IC50 = 802.0 nM 6.10
CHEMBL2030397 IC50 = 874.0 nM 6.06
CHEMBL2030403 IC50 = 1374.0 nM 5.86
CHEMBL2030396 IC50 = 1434.0 nM 5.84
CHEMBL2030376 IC50 = 1471.0 nM 5.83
CHEMBL2030386 IC50 = 1805.0 nM 5.74
CHEMBL2030395 IC50 = 2356.0 nM 5.63
CHEMBL2030392 IC50 = 2536.0 nM 5.60
CHEMBL2030394 IC50 = 4592.0 nM 5.34
CHEMBL2030391 IC50 > 40000.0 nM -