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Assay Detail

CHEMBL3372399

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

Binding
Inhibition of full-length Chk1 in HeLa S3 cells assessed as phosphorylation at Ser345 after 4 hrs
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa S3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Barsanti PA, Pan Y, Lu Y, Jain R, Cox M, Aversa RJ, Dillon MP, Elling R, Hu C, Jin X, Knapp M, Lan J, Ramurthy S, Rudewicz P, Setti L, Subramanian S, Mathur M, Taricani L, Thomas G, Xiao L, Yue Q.
ACS Med Chem Lett (2015) 6 : 42 -46
PubMed 25589928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.07 7.10
EC50 2 5.86 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355474 1 7.10
CHEMBL3355475 1 7.08
CHEMBL3355476 1 7.02
CHEMBL3355473 1 6.24
CHEMBL3355472 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355474 IC50 = 80.0 nM 7.10
CHEMBL3355475 IC50 = 84.0 nM 7.08
CHEMBL3355476 IC50 = 96.0 nM 7.02
CHEMBL3355473 EC50 = 570.0 nM 6.24
CHEMBL3355472 EC50 = 3300.0 nM 5.48