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Assay Detail

CHEMBL4478166

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

Binding
Inhibition of ATM (unknown origin) using p53 as substrate incubated for 30 mins followed by substrate addition measured after 2 hrs in presence of ATP by HTRF method
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

Target

Serine-protein kinase ATM (CHEMBL3797)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Degorce SL, Barlaam B, Cadogan E, Dishington A, Ducray R, Glossop SC, Hassall LA, Lach F, Lau A, McGuire TM, Nowak T, Ouvry G, Pike KG, Thomason AG.
J Med Chem (2016) 59 : 6281 -6292
PubMed 27259031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.35 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4166405 1 9.22
CHEMBL2140173 1 9.10
CHEMBL4565988 1 8.70
CHEMBL4593348 1 8.10
CHEMBL2143829 1 7.68
CHEMBL4527822 1 7.31
CHEMBL4218734 1 -
CHEMBL222102 KU-55933 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4166405 IC50 = 0.6 nM 9.22
CHEMBL2140173 IC50 = 0.8 nM 9.10
CHEMBL4565988 IC50 = 2.0 nM 8.70
CHEMBL4593348 IC50 = 8.0 nM 8.10
CHEMBL2143829 IC50 = 21.0 nM 7.68
CHEMBL4527822 IC50 = 49.0 nM 7.31
CHEMBL4218734 IC50 < 1.2 nM -
CHEMBL222102 KU-55933 IC50 < 2.0 nM -