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Assay Detail

CHEMBL1000360

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

Binding
Inhibition of human Wee1 assessed as polyornithine-tyrosine copolymer phosphorylation
64
Total Activities
64
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 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 64 7.29 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL472542 1 8.22
CHEMBL471163 1 8.15
CHEMBL515352 1 8.15
CHEMBL471157 1 8.10
CHEMBL411662 1 8.05
CHEMBL472208 1 8.05
CHEMBL459889 1 8.05
CHEMBL379975 1 7.96
CHEMBL460940 1 7.92
CHEMBL511992 1 7.89
CHEMBL461116 1 7.85
CHEMBL511280 1 7.82
CHEMBL471329 1 7.80
CHEMBL472209 1 7.72
CHEMBL512012 1 7.68
CHEMBL512342 1 7.68
CHEMBL462170 1 7.64
CHEMBL520904 1 7.64
CHEMBL513079 1 7.62
CHEMBL471156 1 7.60
CHEMBL488054 1 7.57
CHEMBL213593 1 7.55
CHEMBL512341 1 7.52
CHEMBL487891 1 7.52
CHEMBL520240 1 7.48
CHEMBL462011 1 7.46
CHEMBL511991 1 7.35
CHEMBL486665 1 7.27
CHEMBL209388 1 7.24
CHEMBL516488 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL472542 IC50 = 6.0 nM 8.22
CHEMBL471163 IC50 = 7.0 nM 8.15
CHEMBL515352 IC50 = 7.0 nM 8.15
CHEMBL471157 IC50 = 8.0 nM 8.10
CHEMBL411662 IC50 = 9.0 nM 8.05
CHEMBL472208 IC50 = 9.0 nM 8.05
CHEMBL459889 IC50 = 9.0 nM 8.05
CHEMBL379975 IC50 = 11.0 nM 7.96
CHEMBL460940 IC50 = 12.0 nM 7.92
CHEMBL511992 IC50 = 13.0 nM 7.89
CHEMBL461116 IC50 = 14.0 nM 7.85
CHEMBL511280 IC50 = 15.0 nM 7.82
CHEMBL471329 IC50 = 16.0 nM 7.80
CHEMBL472209 IC50 = 19.0 nM 7.72
CHEMBL512342 IC50 = 21.0 nM 7.68
CHEMBL512012 IC50 = 21.0 nM 7.68
CHEMBL462170 IC50 = 23.0 nM 7.64
CHEMBL520904 IC50 = 23.0 nM 7.64
CHEMBL513079 IC50 = 24.0 nM 7.62
CHEMBL471156 IC50 = 25.0 nM 7.60
CHEMBL488054 IC50 = 27.0 nM 7.57
CHEMBL213593 IC50 = 28.0 nM 7.55
CHEMBL512341 IC50 = 30.0 nM 7.52
CHEMBL487891 IC50 = 30.0 nM 7.52
CHEMBL520240 IC50 = 33.0 nM 7.48
CHEMBL462011 IC50 = 35.0 nM 7.46
CHEMBL511991 IC50 = 45.0 nM 7.35
CHEMBL486665 IC50 = 54.0 nM 7.27
CHEMBL209388 IC50 = 57.0 nM 7.24
CHEMBL516488 IC50 = 57.0 nM 7.24
CHEMBL517744 IC50 = 58.0 nM 7.24
CHEMBL452829 IC50 = 59.0 nM 7.23
CHEMBL215900 IC50 = 59.0 nM 7.23
CHEMBL452078 IC50 = 62.0 nM 7.21
CHEMBL486828 IC50 = 64.0 nM 7.19
CHEMBL529669 IC50 = 64.0 nM 7.19
CHEMBL461134 IC50 = 67.0 nM 7.17
CHEMBL508541 IC50 = 69.0 nM 7.16
CHEMBL486661 IC50 = 71.0 nM 7.15
CHEMBL460079 IC50 = 74.0 nM 7.13
CHEMBL508412 IC50 = 82.0 nM 7.09
CHEMBL529897 IC50 = 92.0 nM 7.04
CHEMBL452079 IC50 = 93.0 nM 7.03
CHEMBL486868 IC50 = 96.0 nM 7.02
CHEMBL214253 IC50 = 97.0 nM 7.01
CHEMBL454908 IC50 = 100.0 nM 7.00
CHEMBL452336 IC50 = 110.0 nM 6.96
CHEMBL519238 IC50 = 110.0 nM 6.96
CHEMBL520071 IC50 = 110.0 nM 6.96
CHEMBL508294 IC50 = 120.0 nM 6.92