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Assay Detail

CHEMBL949042

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Binding
Inhibition of human Wee1
24
Total Activities
24
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

Wee1-like protein kinase (CHEMBL5491)
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 24 7.48 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411662 1 8.05
CHEMBL272267 1 7.82
CHEMBL271715 1 7.82
CHEMBL401776 1 7.75
CHEMBL258067 1 7.72
CHEMBL404335 1 7.70
CHEMBL270021 1 7.62
CHEMBL255565 1 7.62
CHEMBL256480 1 7.58
CHEMBL272479 1 7.58
CHEMBL438566 1 7.52
CHEMBL270866 1 7.48
CHEMBL255416 1 7.47
CHEMBL271071 1 7.46
CHEMBL271084 1 7.44
CHEMBL403679 1 7.43
CHEMBL402093 1 7.34
CHEMBL401746 1 7.31
CHEMBL272946 1 7.30
CHEMBL410261 1 7.24
CHEMBL272351 1 7.24
CHEMBL255427 1 7.12
CHEMBL214253 1 7.01
CHEMBL257857 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411662 IC50 = 9.0 nM 8.05
CHEMBL272267 IC50 = 15.0 nM 7.82
CHEMBL271715 IC50 = 15.0 nM 7.82
CHEMBL401776 IC50 = 18.0 nM 7.75
CHEMBL258067 IC50 = 19.0 nM 7.72
CHEMBL404335 IC50 = 20.0 nM 7.70
CHEMBL270021 IC50 = 24.0 nM 7.62
CHEMBL255565 IC50 = 24.0 nM 7.62
CHEMBL256480 IC50 = 26.0 nM 7.58
CHEMBL272479 IC50 = 26.0 nM 7.58
CHEMBL438566 IC50 = 30.0 nM 7.52
CHEMBL270866 IC50 = 33.0 nM 7.48
CHEMBL255416 IC50 = 34.0 nM 7.47
CHEMBL271071 IC50 = 35.0 nM 7.46
CHEMBL271084 IC50 = 36.0 nM 7.44
CHEMBL403679 IC50 = 37.0 nM 7.43
CHEMBL402093 IC50 = 46.0 nM 7.34
CHEMBL401746 IC50 = 49.0 nM 7.31
CHEMBL272946 IC50 = 50.0 nM 7.30
CHEMBL410261 IC50 = 58.0 nM 7.24
CHEMBL272351 IC50 = 57.0 nM 7.24
CHEMBL255427 IC50 = 75.0 nM 7.12
CHEMBL214253 IC50 = 97.0 nM 7.01
CHEMBL257857 IC50 = 160.0 nM 6.80