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Assay Detail

CHEMBL662174

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Binding
Inhibition of DNA dependent protein kinase activity without hsp90 alpha protein
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

DNA-dependent protein kinase catalytic subunit (CHEMBL3142)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.
Chiosis G, Rosen N, Sepp-Lorenzino L.
Bioorg Med Chem Lett (2001) 11 : 909 -913
PubMed 11294389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.31 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174207 1 7.70
CHEMBL173055 1 5.76
CHEMBL366754 1 5.52
CHEMBL263287 1 5.43
CHEMBL367315 1 5.37
CHEMBL355195 1 5.21
CHEMBL262054 1 5.00
CHEMBL422731 1 4.91
CHEMBL366755 1 4.87
CHEMBL366637 1 4.86
CHEMBL173928 1 4.55
CHEMBL424579 1 4.48
CHEMBL109480 TANESPIMYCIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174207 IC50 = 20.0 nM 7.70
CHEMBL173055 IC50 = 1750.0 nM 5.76
CHEMBL366754 IC50 = 3000.0 nM 5.52
CHEMBL263287 IC50 = 3700.0 nM 5.43
CHEMBL367315 IC50 = 4300.0 nM 5.37
CHEMBL355195 IC50 = 6100.0 nM 5.21
CHEMBL262054 IC50 = 10000.0 nM 5.00
CHEMBL422731 IC50 = 12200.0 nM 4.91
CHEMBL366755 IC50 = 13400.0 nM 4.87
CHEMBL366637 IC50 = 13900.0 nM 4.86
CHEMBL173928 IC50 = 28000.0 nM 4.55
CHEMBL424579 IC50 = 33000.0 nM 4.48
CHEMBL109480 TANESPIMYCIN IC50 > 40000.0 nM -