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Assay Detail

CHEMBL906674

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

Binding
Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Intermediate

Publication

Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.
Hayakawa M, Kawaguchi K, Kaizawa H, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI, Parker P, Workman P, Waterfield MD.
Bioorg Med Chem (2007) 15 : 5837 -5844
PubMed 17601739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.71 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555968 1 9.59
CHEMBL556399 1 9.52
CHEMBL536070 1 9.11
CHEMBL541643 1 8.60
CHEMBL224769 1 8.51
CHEMBL538346 1 8.44
CHEMBL535170 1 8.28
CHEMBL559361 1 8.22
CHEMBL541642 1 7.85
CHEMBL229046 1 7.77
CHEMBL229097 1 7.68
CHEMBL229098 1 7.09
CHEMBL387636 1 6.77
CHEMBL535171 1 6.47
CHEMBL389843 1 6.40
CHEMBL98350 LY-294002 -1.0 1 6.20
CHEMBL427066 1 6.17
CHEMBL558174 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555968 IC50 = 0.26 nM 9.59
CHEMBL556399 IC50 = 0.3 nM 9.52
CHEMBL536070 IC50 = 0.77 nM 9.11
CHEMBL541643 IC50 = 2.5 nM 8.60
CHEMBL224769 IC50 = 3.1 nM 8.51
CHEMBL538346 IC50 = 3.6 nM 8.44
CHEMBL535170 IC50 = 5.3 nM 8.28
CHEMBL559361 IC50 = 6.0 nM 8.22
CHEMBL541642 IC50 = 14.0 nM 7.85
CHEMBL229046 IC50 = 17.0 nM 7.77
CHEMBL229097 IC50 = 21.0 nM 7.68
CHEMBL229098 IC50 = 81.0 nM 7.09
CHEMBL387636 IC50 = 170.0 nM 6.77
CHEMBL535171 IC50 = 340.0 nM 6.47
CHEMBL389843 IC50 = 400.0 nM 6.40
CHEMBL98350 LY-294002 IC50 = 630.0 nM 6.20
CHEMBL427066 IC50 = 670.0 nM 6.17
CHEMBL558174 IC50 = 780.0 nM 6.11