Target
Serine/threonine-protein kinase haspin [470-798]
Ligand
BDBM224009
Substrate
n/a
Meas. Tech.
Kinetic Assay with Fluorescence Anisotropy
pH
7.5000±n/a
Kd
0.100±0.0 nM
Comments
extracted
Citation
 Kestav, KViht, KKonovalov, AEnkvist, EUri, ALavogina, D Slowly on, Slowly off: Bisubstrate-Analogue Conjugates of 5-Iodotubercidin and Histone H3 Peptide Targeting Protein Kinase Haspin. Chembiochem 18:790-798 (2017) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase haspin [470-798]
Synonyms:
HASP_HUMAN | HASPIN | GSG2
Type:
Enzyme
Mol. Mass.:
37470.17
Organism:
Human
Description:
Human haspin (470-798 aa)
Residue:
329
Sequence:
KGPVPFSHCLPTEKLQRCEKIGEGVFGEVFQTIADHTPVAIKIIAIEGPDLVNGSHQKTFEEILPEIIISKELSLLSGEVCNRTEGFIGLNSVHCVQGSYPPLLLKAWDHYNSTKGSANDRPDFFKDDQLFIVLEFEFGGIDLEQMRTKLSSLATAKSILHQLTASLAVAEASLRFEHRDLHWGNVLLKKTSLKKLHYTLNGKSSTIPSCGLQVSIIDYTLSRLERDGIVVFCDVSMDEDLFTGDGDYQFDIYRLMKKENNNRWGEYHPYSNVLWLHYLTDKMLKQMTFKTKCNTPAMKQIKRKIQEFHRTMLNFSSATDLLCQHSLFK
  
Inhibitor
Name:
BDBM224009
Synonyms:
ARC-3430
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
C[C@H]([NH3+])C(=O)N[C@@H](CCCNC(N)=[NH2+])C(=O)N[C@@H](CCCCNC(=O)C[C@@H](NC(=O)CCCCCNC(=O)[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(I)c2c(N)ncnc12)C([O-])=O)C(=O)N[C@@H](CCCNC(N)=[NH2+])C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)O)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNC(=O)c1ccc(c(c1)C(O)=O)-c1c2ccc(cc2oc2cc(ccc12)=[N+](C)C)N(C)C)C(N)=O |r,wU:6.5,62.64,82.84,38.37,40.45,wD:17.16,1.1,73.75,89.92,94.96,26.26,41.41,43.44,(11.91,-18.78,;11.91,-17.24,;10.58,-16.47,;13.25,-16.47,;13.25,-14.93,;14.58,-17.24,;15.92,-16.47,;15.92,-14.93,;14.58,-14.16,;14.58,-12.62,;13.25,-11.85,
Structure:
Search PDB for entries with ligand similarity: