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Assay Detail

CHEMBL1767685

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

Binding
Inhibition of ATR in human HT-29 cells assessed as hydroxyurea-induced phosphorylation of H2AX by immunofluorescence microscopy
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase ATR (CHEMBL5024)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.
Charrier JD, Durrant SJ, Golec JM, Kay DP, Knegtel RM, MacCormick S, Mortimore M, O'Donnell ME, Pinder JL, Reaper PM, Rutherford AP, Wang PS, Young SC, Pollard JR.
J Med Chem (2011) 54 : 2320 -2330
PubMed 21413798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.81 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766798 1 6.42
CHEMBL1766797 1 6.38
CHEMBL1766799 1 6.34
CHEMBL1766786 1 6.00
CHEMBL1766793 1 6.00
CHEMBL1766796 1 6.00
CHEMBL1766788 1 5.85
CHEMBL1766792 1 5.82
CHEMBL1766795 1 5.80
CHEMBL1766787 1 5.70
CHEMBL1766794 1 5.70
CHEMBL1766791 1 5.27
CHEMBL1766789 1 5.19
CHEMBL1766790 1 4.92
CHEMBL1766784 1 -
CHEMBL1766785 1 -
CHEMBL1766759 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766798 IC50 = 380.0 nM 6.42
CHEMBL1766797 IC50 = 420.0 nM 6.38
CHEMBL1766799 IC50 = 460.0 nM 6.34
CHEMBL1766786 IC50 = 1000.0 nM 6.00
CHEMBL1766793 IC50 = 1000.0 nM 6.00
CHEMBL1766796 IC50 = 1000.0 nM 6.00
CHEMBL1766788 IC50 = 1400.0 nM 5.85
CHEMBL1766792 IC50 = 1500.0 nM 5.82
CHEMBL1766795 IC50 = 1600.0 nM 5.80
CHEMBL1766787 IC50 = 2000.0 nM 5.70
CHEMBL1766794 IC50 = 2000.0 nM 5.70
CHEMBL1766791 IC50 = 5400.0 nM 5.27
CHEMBL1766789 IC50 = 6500.0 nM 5.19
CHEMBL1766790 IC50 = 12000.0 nM 4.92
CHEMBL1766784 IC50 - -
CHEMBL1766785 IC50 - -
CHEMBL1766759 IC50 > 2500.0 nM -