Target
Serine/threonine-protein kinase haspin
Ligand
BDBM50442758
Substrate
n/a
Meas. Tech.
ChEMBL_989477 (CHEMBL2444004)
IC50
>10.0±n/a nM
Citation
 Brasca, MGMantegani, SAmboldi, NBindi, SCaronni, DCasale, ECeccarelli, WColombo, NDe Ponti, ADonati, DErmoli, AFachin, GFelder, ERFerguson, RDFiorelli, CGuanci, MIsacchi, APesenti, EPolucci, PRiceputi, LSola, FVisco, CZuccotto, FFogliatto, G Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90). Bioorg Med Chem 21:7047-63 (2013) [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:
BDBM50442758
Synonyms:
CHEMBL2443139
Type:
Small organic molecule
Emp. Form.:
C25H30N4O5
Mol. Mass.:
466.5295
SMILES:
CC(C)Nc1ccc(Oc2cc(O)cc(O)c2-c2cc(no2)C(=O)NC2CCN(C)CC2)cc1
Structure:
Search PDB for entries with ligand similarity: