Target
Maternal embryonic leucine zipper kinase
Ligand
BDBM4815
Substrate
n/a
Meas. Tech.
ChEMBL_1679543 (CHEMBL4029820)
IC50
760±n/a nM
Citation
 Edupuganti, RTaliaferro, JMWang, QXie, XCho, EJVidhu, FRen, PAnslyn, EVBartholomeusz, CDalby, KN Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth. Bioorg Med Chem 25:2609-2616 (2017) [PubMed]  Article 
Target
Name:
Maternal embryonic leucine zipper kinase
Synonyms:
KIAA0175 | MELK | MELK_HUMAN | Maternal embryonic leucine zipper kinase | Maternal embryonic leucine zipper kinase (MELK)
Type:
Enzyme
Mol. Mass.:
74665.45
Organism:
Homo sapiens (Human)
Description:
Q14680
Residue:
651
Sequence:
MKDYDELLKYYELHETIGTGGFAKVKLACHILTGEMVAIKIMDKNTLGSDLPRIKTEIEALKNLRHQHICQLYHVLETANKIFMVLEYCPGGELFDYIISQDRLSEEETRVVFRQIVSAVAYVHSQGYAHRDLKPENLLFDEYHKLKLIDFGLCAKPKGNKDYHLQTCCGSLAYAAPELIQGKSYLGSEADVWSMGILLYVLMCGFLPFDDDNVMALYKKIMRGKYDVPKWLSPSSILLLQQMLQVDPKKRISMKNLLNHPWIMQDYNYPVEWQSKNPFIHLDDDCVTELSVHHRNNRQTMEDLISLWQYDHLTATYLLLLAKKARGKPVRLRLSSFSCGQASATPFTDIKSNNWSLEDVTASDKNYVAGLIDYDWCEDDLSTGAATPRTSQFTKYWTESNGVESKSLTPALCRTPANKLKNKENVYTPKSAVKNEEYFMFPEPKTPVNKNQHKREILTTPNRYTTPSKARNQCLKETPIKIPVNSTGTDKLMTGVISPERRCRSVELDLNQAHMEETPKRKGAKVFGSLERGLDKVITVLTRSKRKGSARDGPRRLKLHYNVTTTRLVNPDQLLNEIMSILPKKHVDFVQKGYTLKCQTQSDFGKVTMQFELEVCQLQKPDVVGIRRQRLKGDAWVYKRLVEDILSSCKV
  
Inhibitor
Name:
BDBM4815
Synonyms:
5-{[(3Z)-5-chloro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | CHEMBL13485 | SU11248 analog 12c | US10981896, Compound 572660
Type:
Small organic molecule
Emp. Form.:
C22H27ClN4O2
Mol. Mass.:
414.928
SMILES:
CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(Cl)cc23)c1C
Structure:
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