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Assay Detail

CHEMBL829373

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Binding
Inhibition of checkpoint kinase Wee1
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.
Palmer BD, Smaill JB, Rewcastle GW, Dobrusin EM, Kraker A, Moore CW, Steinkampf RW, Denny WA.
Bioorg Med Chem Lett (2005) 15 : 1931 -1935
PubMed 15780636 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.07 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113070 — — 1 7.50
CHEMBL181314 — — 1 7.40
CHEMBL366922 — — 1 7.40
CHEMBL178510 — — 1 7.16
CHEMBL181233 — — 1 7.13
CHEMBL540206 — — 1 7.10
CHEMBL181285 — — 1 7.07
CHEMBL435732 — — 1 7.05
CHEMBL362862 — — 1 7.02
CHEMBL178758 — — 1 6.92
CHEMBL179065 — — 1 6.91
CHEMBL361347 — — 1 6.85
CHEMBL362692 — — 1 6.85
CHEMBL181423 — — 1 6.82
CHEMBL49120 PD-0166285 1.0 1 6.78
CHEMBL433559 — — 1 6.72
CHEMBL179898 — — 1 6.66
CHEMBL369296 — — 1 6.60
CHEMBL180316 — — 1 6.58
CHEMBL362402 — — 1 6.39
CHEMBL360799 — — 1 6.39
CHEMBL180821 — — 1 6.27
CHEMBL181017 — — 1 6.26
CHEMBL369732 — — 1 6.24
CHEMBL181095 — — 1 6.00
CHEMBL359898 — — 1 6.00
CHEMBL178439 — — 1 6.00
CHEMBL180794 — — 1 5.92
CHEMBL434907 — — 1 5.82
CHEMBL180810 — — 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113070 — IC50 = 32.0 nM 7.50
CHEMBL181314 — IC50 = 40.0 nM 7.40
CHEMBL366922 — IC50 = 40.0 nM 7.40
CHEMBL178510 — IC50 = 69.0 nM 7.16
CHEMBL181233 — IC50 = 74.0 nM 7.13
CHEMBL540206 — IC50 = 80.0 nM 7.10
CHEMBL181285 — IC50 = 86.0 nM 7.07
CHEMBL435732 — IC50 = 90.0 nM 7.05
CHEMBL362862 — IC50 = 95.0 nM 7.02
CHEMBL178758 — IC50 = 120.0 nM 6.92
CHEMBL179065 — IC50 = 124.0 nM 6.91
CHEMBL361347 — IC50 = 140.0 nM 6.85
CHEMBL362692 — IC50 = 142.0 nM 6.85
CHEMBL181423 — IC50 = 150.0 nM 6.82
CHEMBL49120 PD-0166285 IC50 = 165.0 nM 6.78
CHEMBL433559 — IC50 = 190.0 nM 6.72
CHEMBL179898 — IC50 = 220.0 nM 6.66
CHEMBL369296 — IC50 = 250.0 nM 6.60
CHEMBL180316 — IC50 = 260.0 nM 6.58
CHEMBL362402 — IC50 = 410.0 nM 6.39
CHEMBL360799 — IC50 = 410.0 nM 6.39
CHEMBL180821 — IC50 = 540.0 nM 6.27
CHEMBL181017 — IC50 = 550.0 nM 6.26
CHEMBL369732 — IC50 = 580.0 nM 6.24
CHEMBL178439 — IC50 = 1000.0 nM 6.00
CHEMBL359898 — IC50 = 990.0 nM 6.00
CHEMBL181095 — IC50 = 990.0 nM 6.00
CHEMBL180794 — IC50 = 1200.0 nM 5.92
CHEMBL434907 — IC50 = 1500.0 nM 5.82
CHEMBL180810 — IC50 = 1900.0 nM 5.72
CHEMBL181733 — IC50 = 2400.0 nM 5.62
CHEMBL181476 — IC50 = 2600.0 nM 5.58
CHEMBL301612 — IC50 = 2600.0 nM 5.58
CHEMBL182044 — IC50 = 3200.0 nM 5.50
CHEMBL181282 — IC50 = 3400.0 nM 5.47
CHEMBL180035 — IC50 = 3500.0 nM 5.46
CHEMBL178122 — IC50 = 3600.0 nM 5.44
CHEMBL181982 — IC50 = 3700.0 nM 5.43
CHEMBL180149 — IC50 = 4500.0 nM 5.35
CHEMBL179806 — IC50 = 8600.0 nM 5.07
CHEMBL362005 — IC50 = 8600.0 nM 5.07
CHEMBL425873 — IC50 = 9700.0 nM 5.01
CHEMBL180290 — IC50 = 11000.0 nM 4.96
CHEMBL360544 — IC50 = 27000.0 nM 4.57
CHEMBL181822 — IC50 = 31000.0 nM 4.51
CHEMBL359824 — IC50 = 33000.0 nM 4.48
CHEMBL181871 — IC50 = 41000.0 nM 4.39
CHEMBL360689 — IC50 = 50000.0 nM 4.30
CHEMBL359732 — IC50 > 50000.0 nM -
CHEMBL180673 — IC50 > 50000.0 nM -