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Target
Serine/threonine-protein kinase Chk2 [209-531,Q209M]
Ligand
BDBM16591
Substrate
Histone H1
Meas. Tech.
In Vitro Protein Kinase Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
420±n/a nM
Citation
 Jobson, AG; Cardellina, JH; Scudiero, D; Kondapaka, S; Zhang, H; Kim, H; Shoemaker, R; Pommier, Y Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. Mol Pharmacol 72:876-84 (2007) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase Chk2 [209-531,Q209M]
Synonyms:
CDS1 | CHEK2 | CHK2 | CHK2_HUMAN | Checkpoint Kinase (Chk2) | Checkpoint Kinase 2 | RAD53
Type:
Serine/threonine-protein kinase
Mol. Mass.:
36511.81
Organism:
Homo sapiens (Human)
Description:
O96017[209-531,Q209M]
Residue:
323
Sequence:
MSVYPKALRDEYIMSKTLGSGACGEVKLAFERKTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIVLELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEEDCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFICLSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEALRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAE
  
Inhibitor
Name:
BDBM16591
Synonyms:
(4Z)-4-(2-amino-5-oxo-3,5-dihydro-4H-imidazol-4-ylidene)-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8(1H)-one | 2-amino-5-[(4Z)-8-oxo-1H,4H,5H,6H,7H,8H-pyrrolo[2,3-c]azepin-4-ylidene]-4,5-dihydro-1H-imidazol-4-one | B722657K110 | CHEMBL255465 | Debromohymenialdisine (DBH) | Hymenialdisine, 8 | NSC607174
Type:
Small organic molecule
Emp. Form.:
C11H11N5O2
Mol. Mass.:
245.2373
SMILES:
NC1=NC(=O)C(N1)=C1CCNC(=O)c2[nH]ccc12 |w:7.18,t:1|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA