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Assay Detail

CHEMBL1670119

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Binding
Inhibition of PI3Kalpha after 80 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.
Clapham KM, Bardos J, Finlay MR, Golding BT, Griffen EJ, Griffin RJ, Hardcastle IR, Menear KA, Ting A, Turner P, Young GL, Cano C.
Bioorg Med Chem Lett (2011) 21 : 966 -970
PubMed 21216595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.34 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1669154 1 7.16
CHEMBL188678 1 6.89
CHEMBL1669161 1 6.82
CHEMBL1669160 1 6.82
CHEMBL1669167 1 6.57
CHEMBL1669159 1 6.54
CHEMBL1669165 1 6.54
CHEMBL1669155 1 6.52
CHEMBL1669156 1 6.46
CHEMBL1669166 1 6.40
CHEMBL1669157 1 6.37
CHEMBL1669158 1 6.33
CHEMBL98350 LY-294002 -1.0 1 6.30
CHEMBL1669162 1 5.96
CHEMBL1669163 1 5.82
CHEMBL1669168 1 5.80
CHEMBL1669169 1 5.52
CHEMBL1669164 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1669154 IC50 = 70.0 nM 7.16
CHEMBL188678 IC50 = 130.0 nM 6.89
CHEMBL1669161 IC50 = 150.0 nM 6.82
CHEMBL1669160 IC50 = 150.0 nM 6.82
CHEMBL1669167 IC50 = 270.0 nM 6.57
CHEMBL1669159 IC50 = 290.0 nM 6.54
CHEMBL1669165 IC50 = 290.0 nM 6.54
CHEMBL1669155 IC50 = 300.0 nM 6.52
CHEMBL1669156 IC50 = 350.0 nM 6.46
CHEMBL1669166 IC50 = 400.0 nM 6.40
CHEMBL1669157 IC50 = 430.0 nM 6.37
CHEMBL1669158 IC50 = 470.0 nM 6.33
CHEMBL98350 LY-294002 IC50 = 500.0 nM 6.30
CHEMBL1669162 IC50 = 1100.0 nM 5.96
CHEMBL1669163 IC50 = 1500.0 nM 5.82
CHEMBL1669168 IC50 = 1600.0 nM 5.80
CHEMBL1669169 IC50 = 3000.0 nM 5.52
CHEMBL1669164 IC50 = 4400.0 nM 5.36