Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1000364

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

Binding
Inhibition of Cdc2/cyclin B assessed as inhibition of histone H1 phosphorylation in human HT29 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 1/cyclin B1 (CHEMBL1907602)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.
Smaill JB, Baker EN, Booth RJ, Bridges AJ, Dickson JM, Dobrusin EM, Ivanovic I, Kraker AJ, Lee HH, Lunney EA, Ortwine DF, Palmer BD, Quin J, Squire CJ, Thompson AM, Denny WA.
Eur J Med Chem (2008) 43 : 1276 -1296
PubMed 17869387 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.00 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411662 1 6.19
CHEMBL508541 1 6.15
CHEMBL462011 1 5.89
CHEMBL529669 1 5.77
CHEMBL472542 1 -
CHEMBL511280 1 -
CHEMBL517744 1 -
CHEMBL460940 1 -
CHEMBL512342 1 -
CHEMBL511992 1 -
CHEMBL471329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411662 IC50 = 650.0 nM 6.19
CHEMBL508541 IC50 = 710.0 nM 6.15
CHEMBL462011 IC50 = 1300.0 nM 5.89
CHEMBL529669 IC50 = 1700.0 nM 5.77
CHEMBL472542 IC50 > 3400.0 nM -
CHEMBL511280 IC50 > 3400.0 nM -
CHEMBL517744 IC50 > 3400.0 nM -
CHEMBL460940 IC50 > 3400.0 nM -
CHEMBL512342 IC50 > 3400.0 nM -
CHEMBL511992 IC50 > 3400.0 nM -
CHEMBL471329 IC50 > 3400.0 nM -