Basic Information
ID: ALA3887343
Type: Binding
Description: Cell Based Assay: ATR (Ataxia Telangiectasia+Rad3-related kinase) is a PI3-kinase-related kinase which phosphorylates multiple substrates on serine or threonine residues in response to DNA damage or replication blocks. Chk1, a downstream protein kinase of ATR, plays a key role in DNA damage checkpoint control. Activation of Chk1 involves phosphorylation of Ser317 and Ser345 (the latter regarded as the preferential target for phosphorylation/activation by ATR).This was a cell based assay to measure inhibition of ATR kinase, by measuring a decrease in phosphorylation of Chk1 (Ser 345) in HT29 cells, following treatment with compound and the UV mimetic 4NQO (Sigma #N8141). HT29 cells (ECACC #85061109) were seeded into 384 well assay plates (Costar #3712) at a density of 6000 cells/well in 40 ul EMEM medium containing 1% L glutamine and 10% FBS and allowed to adhere overnight. The following morning compounds in 100% DMSO were added to assay plates by acoustic dispensing.
Organism: Homo sapiens
Cell type: HT-29
Activity Charts
Bioactivity
Activity Types for Assay ALA3887343
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 469.55 | 1.68 | 1.68 |
| 469.55 | 1.77 | 1.77 |
| 455.52 | 1.29 | 1.29 |
| 469.51 | 1.38 | 1.38 |
| 469.55 | 1.68 | 1.68 |
| 469.55 | 1.54 | 1.54 |