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Assay Detail

CHEMBL1914127

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

Binding
Inhibition of bovine recombinant PI3K p110delta expressed in Sf21 insect cells using phosphatidylinositol as substrate after 1 hr by phosphoimaging
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
Rewcastle GW, Gamage SA, Flanagan JU, Frederick R, Denny WA, Baguley BC, Kestell P, Singh R, Kendall JD, Marshall ES, Lill CL, Lee WJ, Kolekar S, Buchanan CM, Jamieson SM, Shepherd PR.
J Med Chem (2011) 54 : 7105 -7126
PubMed 21882832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.60 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1910998 1 9.57
CHEMBL1911122 1 9.57
CHEMBL1911114 1 9.52
CHEMBL1911117 1 9.42
CHEMBL1911118 1 9.28
CHEMBL586702 ZSTK-474 2.0 1 9.15
CHEMBL1911005 1 9.07
CHEMBL1911115 1 8.74
CHEMBL1910999 1 8.41
CHEMBL1911000 1 8.26
CHEMBL1911119 1 8.17
CHEMBL1911002 1 8.13
CHEMBL1911121 1 8.00
CHEMBL1911008 1 7.92
CHEMBL1911116 1 7.90
CHEMBL1911124 1 7.89
CHEMBL1910990 1 7.89
CHEMBL1911125 1 7.85
CHEMBL1911123 1 7.75
CHEMBL1910994 1 7.46
CHEMBL1910989 1 7.46
CHEMBL1911014 1 7.41
CHEMBL1910993 1 7.39
CHEMBL1910995 1 7.27
CHEMBL1911009 1 7.19
CHEMBL1911013 1 7.18
CHEMBL1911006 1 7.17
CHEMBL1910991 1 7.16
CHEMBL1910997 1 7.12
CHEMBL1909655 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1910998 IC50 = 0.27 nM 9.57
CHEMBL1911122 IC50 = 0.27 nM 9.57
CHEMBL1911114 IC50 = 0.3 nM 9.52
CHEMBL1911117 IC50 = 0.38 nM 9.42
CHEMBL1911118 IC50 = 0.52 nM 9.28
CHEMBL586702 ZSTK-474 IC50 = 0.7 nM 9.15
CHEMBL1911005 IC50 = 0.85 nM 9.07
CHEMBL1911115 IC50 = 1.8 nM 8.74
CHEMBL1910999 IC50 = 3.9 nM 8.41
CHEMBL1911000 IC50 = 5.5 nM 8.26
CHEMBL1911119 IC50 = 6.8 nM 8.17
CHEMBL1911002 IC50 = 7.4 nM 8.13
CHEMBL1911121 IC50 = 10.0 nM 8.00
CHEMBL1911008 IC50 = 12.0 nM 7.92
CHEMBL1911116 IC50 = 12.5 nM 7.90
CHEMBL1911124 IC50 = 13.0 nM 7.89
CHEMBL1910990 IC50 = 13.0 nM 7.89
CHEMBL1911125 IC50 = 14.0 nM 7.85
CHEMBL1911123 IC50 = 18.0 nM 7.75
CHEMBL1910994 IC50 = 35.0 nM 7.46
CHEMBL1910989 IC50 = 35.0 nM 7.46
CHEMBL1911014 IC50 = 39.0 nM 7.41
CHEMBL1910993 IC50 = 41.0 nM 7.39
CHEMBL1910995 IC50 = 54.0 nM 7.27
CHEMBL1911009 IC50 = 65.0 nM 7.19
CHEMBL1911013 IC50 = 66.0 nM 7.18
CHEMBL1911006 IC50 = 67.0 nM 7.17
CHEMBL1910991 IC50 = 70.0 nM 7.16
CHEMBL1910997 IC50 = 76.0 nM 7.12
CHEMBL1909655 IC50 = 95.0 nM 7.02
CHEMBL1910988 IC50 = 142.0 nM 6.85
CHEMBL1911001 IC50 = 156.0 nM 6.81
CHEMBL1911004 IC50 = 158.0 nM 6.80
CHEMBL1911015 IC50 = 258.0 nM 6.59
CHEMBL1910996 IC50 = 270.0 nM 6.57
CHEMBL1911003 IC50 = 430.0 nM 6.37
CHEMBL1911007 IC50 = 539.0 nM 6.27
CHEMBL1911011 IC50 = 1000.0 nM 6.00
CHEMBL1911010 IC50 = 1000.0 nM 6.00
CHEMBL1911120 IC50 = 1600.0 nM 5.80
CHEMBL1910992 IC50 = 5470.0 nM 5.26
CHEMBL1911012 IC50 > 1000.0 nM -