Reaction Details
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Serine/threonine-protein kinase haspin [470-798]
Ligand
BDBM224008
Substrate
n/a
Meas. Tech.
Equilibrium Binding/Displacement Assay with Fluorescence Anisotropy
pH
7.5±n/a
Kd
0.14±0.05 nM
Comments
extracted
Citation
Kestav, K; Viht, K; Konovalov, A; Enkvist, E; Uri, A; Lavogina, 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 More Info.:
Target
Name:
Serine/threonine-protein kinase haspin [470-798]
Synonyms:
GSG2 | HASPIN | HASP_HUMAN
Type:
Enzyme
Mol. Mass.:
37470.17
Organism:
Homo sapiens (Human)
Description:
Human haspin (470-798 aa)
Residue:
329
Sequence:
KGPVPFSHCLPTEKLQRCEKIGEGVFGEVFQTIADHTPVAIKIIAIEGPDLVNGSHQKTFEEILPEIIISKELSLLSGEVCNRTEGFIGLNSVHCVQGSYPPLLLKAWDHYNSTKGSANDRPDFFKDDQLFIVLEFEFGGIDLEQMRTKLSSLATAKSILHQLTASLAVAEASLRFEHRDLHWGNVLLKKTSLKKLHYTLNGKSSTIPSCGLQVSIIDYTLSRLERDGIVVFCDVSMDEDLFTGDGDYQFDIYRLMKKENNNRWGEYHPYSNVLWLHYLTDKMLKQMTFKTKCNTPAMKQIKRKIQEFHRTMLNFSSATDLLCQHSLFK
Inhibitor
Name:
BDBM224008
Synonyms:
ARC-3429
Type:
Small organic molecule
Emp. Form.:
C60H104IN24O18
Mol. Mass.:
1576.5206
SMILES:
CC(O)[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[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)NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@H](C)[NH3+])C(=O)N[C@@H](C)C(=O)N[C@H](CCCC[NH3+])C(N)=O |r|
Structure:
