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Assay Detail

CHEMBL1810296

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

Binding
Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.
Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, Yu K, Hollander I, Feldberg L, Lucas J, Mallon R.
Bioorg Med Chem Lett (2011) 21 : 4773 -4778
PubMed 21763134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.87 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1808983 1 8.40
CHEMBL1808977 1 8.32
CHEMBL1808990 1 8.22
CHEMBL1808988 1 8.19
CHEMBL1808979 1 8.15
CHEMBL1808989 1 8.10
CHEMBL589258 1 8.05
CHEMBL1808984 1 8.02
CHEMBL1808981 1 8.02
CHEMBL1808980 1 7.98
CHEMBL592445 GEDATOLISIB 3.0 1 7.96
CHEMBL1808982 1 7.87
CHEMBL1808991 1 7.84
CHEMBL1808986 1 7.75
CHEMBL1808978 1 7.69
CHEMBL1808987 1 7.61
CHEMBL1808985 1 7.30
CHEMBL1808992 1 7.14
CHEMBL1808993 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1808983 IC50 = 4.0 nM 8.40
CHEMBL1808977 IC50 = 4.8 nM 8.32
CHEMBL1808990 IC50 = 6.0 nM 8.22
CHEMBL1808988 IC50 = 6.5 nM 8.19
CHEMBL1808979 IC50 = 7.0 nM 8.15
CHEMBL1808989 IC50 = 8.0 nM 8.10
CHEMBL589258 IC50 = 9.0 nM 8.05
CHEMBL1808984 IC50 = 9.5 nM 8.02
CHEMBL1808981 IC50 = 9.5 nM 8.02
CHEMBL1808980 IC50 = 10.5 nM 7.98
CHEMBL592445 GEDATOLISIB IC50 = 11.0 nM 7.96
CHEMBL1808982 IC50 = 13.5 nM 7.87
CHEMBL1808991 IC50 = 14.3 nM 7.84
CHEMBL1808986 IC50 = 18.0 nM 7.75
CHEMBL1808978 IC50 = 20.5 nM 7.69
CHEMBL1808987 IC50 = 24.5 nM 7.61
CHEMBL1808985 IC50 = 49.5 nM 7.30
CHEMBL1808992 IC50 = 72.5 nM 7.14
CHEMBL1808993 IC50 = 96.5 nM 7.01