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Target
Serine/threonine-protein kinase Chk2
Ligand
BDBM33212
Substrate
biotinylated CDC25C peptide
Meas. Tech.
CHK Kinase Inhibition Assay
pH
7.4±n/a
Temperature
296.15±n/a K
IC50
74000±n/a nM
Citation
Matthews, TP; Klair, S; Burns, S; Boxall, K; Cherry, M; Fisher, M; Westwood, IM; Walton, MI; McHardy, T; Cheung, KM; Van Montfort, R; Williams, D; Aherne, GW; Garrett, MD; Reader, J; Collins, I Identification of inhibitors of checkpoint kinase 1 through template screening. J Med Chem 52:4810-9 (2009) [PubMed] Article
Target
Name:
Serine/threonine-protein kinase Chk2
Synonyms:
CDS1 | CHEK2 | CHK2 | CHK2_HUMAN | Checkpoint Kinase (Chk2) | RAD53 | Serine/threonine-protein kinase Chek2 | Serine/threonine-protein kinase Chk1/2
Type:
Protein
Mol. Mass.:
60908.59
Organism:
Homo sapiens (Human)
Description:
O96017
Residue:
543
Sequence:
MSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTLSSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKSCEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKRRPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFERKTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIVLELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEEDCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFICLSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEALRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCAAVL
Inhibitor
Name:
BDBM33212
Synonyms:
pyrazolo pyridine, 11
Type:
Small organic molecule
Emp. Form.:
C14H19N5O3
Mol. Mass.:
305.3324
SMILES:
CCOC(=O)c1cnc2[nH]ncc2c1N1CCOC(CN)C1
Substrate
Name:
biotinylated CDC25C peptide
Synonyms:
n/a
Type:
biotinylated peptide
Mol. Mass.:
3148.69
Organism:
n/a
Description:
n/a
Residue:
27
Sequence:
ITINKKKVSRSGLYRSPSMPENLNRPR