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Target
Serine/threonine-protein kinase haspin
Ligand
BDBM50466158
Substrate
n/a
Meas. Tech.
ChEMBL_1791729 (CHEMBL4263648)
IC50
36±n/a nM
Citation
 Darwish, SS; Abdel-Halim, M; Salah, M; Abadi, AH; Becker, W; Engel, M Development of novel 2,4-bispyridyl thiophene-based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives. Eur J Med Chem 157:1031-1050 (2018) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase haspin
Synonyms:
GSG2 | Germ cell-specific gene 2 protein | H-haspin | HASPIN | HASP_HUMAN | Haploid germ cell-specific nuclear protein kinase
Type:
PROTEIN
Mol. Mass.:
88531.28
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1510616
Residue:
798
Sequence:
MAASLPGPGSRLFRTYGAADGRRQRRPGREAAQWFPPQDRRRFFNSSGSSDASIGDPSQSDDPDDPDDPDFPGSPVRRRRRRPGGRVPKDRPSLTVTPKRWKLRARPSLTVTPRRLGLRARPPQKCSTPCGPLRLPPFPSRDSGRLSPDLSVCGQPRDGDELGISASLFSSLASPCPGSPTPRDSVISIGTSACLVAASAVPSGLHLPEVSLDRASLPCSQEEATGGAKDTRMVHQTRASLRSVLFGLMNSGTPEDSEFRADGKNMRESCCKRKLVVGNGPEGPGLSSTGKRRATGQDSCQERGLQEAVRREHQEASVPKGRIVPRGIDRLERTRSSRKSKHQEATETSLLHSHRFKKGQKLGKDSFPTQDLTPLQNVCFWTKTRASFSFHKKKIVTDVSEVCSIYTTATSLSGSLLSECSNRPVMNRTSGAPSSWHSSSMYLLSPLNTLSISNKKASDAEKVYGECSQKGPVPFSHCLPTEKLQRCEKIGEGVFGEVFQTIADHTPVAIKIIAIEGPDLVNGSHQKTFEEILPEIIISKELSLLSGEVCNRTEGFIGLNSVHCVQGSYPPLLLKAWDHYNSTKGSANDRPDFFKDDQLFIVLEFEFGGIDLEQMRTKLSSLATAKSILHQLTASLAVAEASLRFEHRDLHWGNVLLKKTSLKKLHYTLNGKSSTIPSCGLQVSIIDYTLSRLERDGIVVFCDVSMDEDLFTGDGDYQFDIYRLMKKENNNRWGEYHPYSNVLWLHYLTDKMLKQMTFKTKCNTPAMKQIKRKIQEFHRTMLNFSSATDLLCQHSLFK
  
Inhibitor
Name:
BDBM50466158
Synonyms:
CHEMBL4290247
Type:
Small organic molecule
Emp. Form.:
C22H16FN3OS
Mol. Mass.:
389.445
SMILES:
Fc1ccc(CC(=O)Nc2cncc(c2)-c2cc(cs2)-c2cccnc2)cc1
Structure:
Search PDB for entries with ligand similarity: