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Assay Detail

CHEMBL949046

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

Binding
Inhibition of human Cdc2 kinase PY15 phosphorylation in HT29 cells by Western blot
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 1 (CHEMBL308)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases.
Smaill JB, Lee HH, Palmer BD, Thompson AM, Squire CJ, Baker EN, Booth RJ, Kraker A, Hook K, Denny WA.
Bioorg Med Chem Lett (2008) 18 : 929 -933
PubMed 18191399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.97 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410261 1 8.00
CHEMBL270021 1 7.52
CHEMBL255427 1 7.52
CHEMBL272946 1 6.70
CHEMBL411662 1 6.60
CHEMBL271715 1 6.60
CHEMBL401776 1 6.60
CHEMBL403679 1 6.60
CHEMBL401746 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410261 IC50 = 10.0 nM 8.00
CHEMBL270021 IC50 = 30.0 nM 7.52
CHEMBL255427 IC50 = 30.0 nM 7.52
CHEMBL272946 IC50 = 200.0 nM 6.70
CHEMBL411662 IC50 = 250.0 nM 6.60
CHEMBL271715 IC50 = 250.0 nM 6.60
CHEMBL401776 IC50 = 250.0 nM 6.60
CHEMBL403679 IC50 = 250.0 nM 6.60
CHEMBL401746 IC50 = 250.0 nM 6.60