Target
Maternal embryonic leucine zipper kinase
Ligand
BDBM158154
Substrate
n/a
Meas. Tech.
ChEMBL_1577180 (CHEMBL3807442)
IC50
>10000±n/a nM
Citation
 Menichincheri, MArdini, EMagnaghi, PAvanzi, NBanfi, PBossi, RBuffa, LCanevari, GCeriani, LColombo, MCorti, LDonati, DFasolini, MFelder, EFiorelli, CFiorentini, FGalvani, AIsacchi, ABorgia, ALMarchionni, CNesi, MOrrenius, CPanzeri, APesenti, ERusconi, LSaccardo, MBVanotti, EPerrone, EOrsini, P Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. J Med Chem 59:3392-408 (2016) [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:
BDBM158154
Synonyms:
US10081622, Compound 11 | US10370379, Entrectinib | US11059827, Compound Entrectinib | US11267806, Compound T-12 | US9029356, 11 | US9255087, 11 | US9616059, 11
Type:
Small organic molecule
Emp. Form.:
C31H34F2N6O2
Mol. Mass.:
560.6375
SMILES:
CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1
Structure:
Search PDB for entries with ligand similarity: