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Assay Detail

CHEMBL3372984

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

Binding
Inhibition of GST-tagged human Wee1
22
Total Activities
22
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

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
Ki 22 8.18 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355531 1 8.92
CHEMBL3355528 1 8.80
CHEMBL3355535 1 8.70
CHEMBL3355518 1 8.64
CHEMBL3355532 1 8.27
CHEMBL3355522 1 8.26
CHEMBL3355525 1 8.21
CHEMBL3355524 1 8.18
CHEMBL3355530 1 8.13
CHEMBL3355523 1 8.08
CHEMBL3355529 1 8.07
CHEMBL3355519 1 7.68
CHEMBL3355527 1 7.58
CHEMBL3355521 1 7.06
CHEMBL3355526 1 -
CHEMBL3355533 1 -
CHEMBL3355534 1 -
CHEMBL3355520 1 -
CHEMBL3355536 1 -
CHEMBL3355537 1 -
CHEMBL3355538 1 -
CHEMBL3355539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355531 Ki = 1.2 nM 8.92
CHEMBL3355528 Ki = 1.6 nM 8.80
CHEMBL3355535 Ki = 2.0 nM 8.70
CHEMBL3355518 Ki = 2.3 nM 8.64
CHEMBL3355532 Ki = 5.4 nM 8.27
CHEMBL3355522 Ki = 5.5 nM 8.26
CHEMBL3355525 Ki = 6.2 nM 8.21
CHEMBL3355524 Ki = 6.6 nM 8.18
CHEMBL3355530 Ki = 7.4 nM 8.13
CHEMBL3355523 Ki = 8.3 nM 8.08
CHEMBL3355529 Ki = 8.6 nM 8.07
CHEMBL3355519 Ki = 21.0 nM 7.68
CHEMBL3355527 Ki = 26.0 nM 7.58
CHEMBL3355521 Ki = 87.0 nM 7.06
CHEMBL3355526 Ki > 3140.0 nM -
CHEMBL3355533 Ki < 1.0 nM -
CHEMBL3355534 Ki < 1.0 nM -
CHEMBL3355520 Ki > 3140.0 nM -
CHEMBL3355536 Ki < 1.0 nM -
CHEMBL3355537 Ki < 1.0 nM -
CHEMBL3355538 Ki < 1.0 nM -
CHEMBL3355539 Ki < 1.0 nM -