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Assay Detail

CHEMBL4200472

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

Binding
Inhibition of recombinant human PI3Kgamma using PIP2 as substrate pretreated for 20 mins followed by substrate addition and measured after 80 mins by luminescence assay
2
Total Activities
2
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

Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, Goldberg K, Hassall LA, Hughes GD, MacFaul PA, McGuire TM, Pass M, Patel A, Pearson S, Petersen J, Pike KG, Robb G, Stratton N, Xin G, Zhai B.
ACS Med Chem Lett (2018) 9 : 809 -814
PubMed 30128072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.53 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217549 1 5.54
CHEMBL4218854 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217549 IC50 = 2900.0 nM 5.54
CHEMBL4218854 IC50 = 3000.0 nM 5.52