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Assay Detail

CHEMBL5720980

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

Binding
Inhibition of human VPS34 assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P ELISA assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Inhibition of Human Class I vs Class III Phosphatidylinositol 3'-Kinases.
Hassett MR, Sternberg AR, Roepe PD.
Biochemistry (2017) 56 : 4326 -4334
PubMed 28719179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.19 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3622372 1 8.96
CHEMBL3218578 BGT-226 FREE BASE 2.0 1 8.15
CHEMBL3781415 1 8.03
CHEMBL1765602 1 7.94
CHEMBL1229535 1 6.66
CHEMBL1236962 OMIPALISIB 2.0 1 6.44
CHEMBL5723005 1 6.11
CHEMBL3545097 SAPANISERTIB 2.0 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3622372 EC50 = 1.11 nM 8.96
CHEMBL3218578 BGT-226 FREE BASE EC50 = 7.03 nM 8.15
CHEMBL3781415 EC50 = 9.4 nM 8.03
CHEMBL1765602 EC50 = 11.5 nM 7.94
CHEMBL1229535 EC50 = 220.0 nM 6.66
CHEMBL1236962 OMIPALISIB EC50 = 364.0 nM 6.44
CHEMBL5723005 EC50 = 784.0 nM 6.11
CHEMBL3545097 SAPANISERTIB EC50 = 5620.0 nM 5.25