Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1104618

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

Binding
Inhibition of ATR by DELFIA assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, Zask A.
J Med Chem (2009) 52 : 8010 -8024
PubMed 19894727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.88 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL563985 1 5.32
CHEMBL1095932 1 5.11
CHEMBL1095627 1 4.94
CHEMBL1095933 1 4.93
CHEMBL562999 1 4.58
CHEMBL561907 1 4.38
CHEMBL1095626 1 -
CHEMBL1094981 1 -
CHEMBL1098242 1 -
CHEMBL1097942 1 -
CHEMBL1098243 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL563985 IC50 = 4800.0 nM 5.32
CHEMBL1095932 IC50 = 7700.0 nM 5.11
CHEMBL1095627 IC50 = 11400.0 nM 4.94
CHEMBL1095933 IC50 = 11700.0 nM 4.93
CHEMBL562999 IC50 = 26200.0 nM 4.58
CHEMBL561907 IC50 = 41500.0 nM 4.38
CHEMBL1095626 IC50 > 50000.0 nM -
CHEMBL1094981 IC50 > 50000.0 nM -
CHEMBL1098242 IC50 > 50000.0 nM -
CHEMBL1097942 IC50 > 50000.0 nM -
CHEMBL1098243 IC50 > 50000.0 nM -