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Assay Detail

CHEMBL4388516

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

Binding
Inhibition of WEE1 in human NCI-H1299 cells assessed as reduction in Cdc2 phosphorylation at Tyr15 residue measured after 6 hrs by ELISA
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H1299
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Wee1-like protein kinase (CHEMBL5491)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of biaryl heterocycles as inhibitors of Wee1 kinase.
Mastracchio A, Lai C, Torrent M, Bromberg K, Buchanan FG, Ferguson D, Bontcheva V, Johnson EF, Lasko L, Maag D, Shoemaker AR, Penning TD.
Bioorg Med Chem Lett (2019) 29 : 1481 -1486
PubMed 31014911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.16 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4441166 1 7.96
CHEMBL4447769 1 7.75
CHEMBL4554796 1 7.72
CHEMBL4444364 1 7.68
CHEMBL4551299 1 7.66
CHEMBL4529353 1 7.60
CHEMBL4526423 1 7.55
CHEMBL4470852 1 7.54
CHEMBL4454675 1 7.51
CHEMBL3355539 1 7.22
CHEMBL4443172 1 7.10
CHEMBL4544916 1 6.61
CHEMBL4469678 1 6.49
CHEMBL4450036 1 5.54
CHEMBL4562919 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4441166 EC50 = 11.0 nM 7.96
CHEMBL4447769 EC50 = 18.0 nM 7.75
CHEMBL4554796 EC50 = 19.0 nM 7.72
CHEMBL4444364 EC50 = 21.0 nM 7.68
CHEMBL4551299 EC50 = 22.0 nM 7.66
CHEMBL4529353 EC50 = 25.0 nM 7.60
CHEMBL4526423 EC50 = 28.0 nM 7.55
CHEMBL4470852 EC50 = 29.0 nM 7.54
CHEMBL4454675 EC50 = 31.0 nM 7.51
CHEMBL3355539 EC50 = 60.0 nM 7.22
CHEMBL4443172 EC50 = 79.0 nM 7.10
CHEMBL4544916 EC50 = 246.0 nM 6.61
CHEMBL4469678 EC50 = 324.0 nM 6.49
CHEMBL4450036 EC50 = 2850.0 nM 5.54
CHEMBL4562919 EC50 = 4020.0 nM 5.40