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Assay Detail

CHEMBL3372986

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

Binding
Inhibition of human Weel1 in human NCI-H1299 cells assessed as phosphorylation of Cdk1 after overnight incubation by ELISA PD assay
20
Total Activities
20
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

Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.
Tong Y, Torrent M, Florjancic AS, Bromberg KD, Buchanan FG, Ferguson DC, Johnson EF, Lasko LM, Maag D, Merta PJ, Olson AM, Osterling DJ, Soni N, Shoemaker AR, Penning TD.
ACS Med Chem Lett (2015) 6 : 58 -62
PubMed 25589931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.25 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355536 1 7.57
CHEMBL3355537 1 7.54
CHEMBL3355539 1 7.22
CHEMBL3355534 1 7.06
CHEMBL3355533 1 7.01
CHEMBL3355531 1 7.00
CHEMBL3355535 1 6.77
CHEMBL3355528 1 6.66
CHEMBL3355518 1 6.43
CHEMBL3355532 1 6.21
CHEMBL3355524 1 5.96
CHEMBL3355525 1 5.82
CHEMBL3355529 1 5.64
CHEMBL3355530 1 5.57
CHEMBL3355523 1 5.51
CHEMBL3355522 1 5.42
CHEMBL3355527 1 5.22
CHEMBL3355519 1 5.17
CHEMBL3355521 1 5.00
CHEMBL3355538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355536 EC50 = 27.0 nM 7.57
CHEMBL3355537 EC50 = 29.0 nM 7.54
CHEMBL3355539 EC50 = 60.0 nM 7.22
CHEMBL3355534 EC50 = 87.0 nM 7.06
CHEMBL3355533 EC50 = 98.0 nM 7.01
CHEMBL3355531 EC50 = 100.0 nM 7.00
CHEMBL3355535 EC50 = 170.0 nM 6.77
CHEMBL3355528 EC50 = 220.0 nM 6.66
CHEMBL3355518 EC50 = 370.0 nM 6.43
CHEMBL3355532 EC50 = 620.0 nM 6.21
CHEMBL3355524 EC50 = 1100.0 nM 5.96
CHEMBL3355525 EC50 = 1500.0 nM 5.82
CHEMBL3355529 EC50 = 2300.0 nM 5.64
CHEMBL3355530 EC50 = 2700.0 nM 5.57
CHEMBL3355523 EC50 = 3100.0 nM 5.51
CHEMBL3355522 EC50 = 3800.0 nM 5.42
CHEMBL3355527 EC50 = 6000.0 nM 5.22
CHEMBL3355519 EC50 = 6800.0 nM 5.17
CHEMBL3355521 EC50 = 10000.0 nM 5.00
CHEMBL3355538 EC50 < 13.0 nM -