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Target
Cytoplasmic tyrosine-protein kinase BMX
Ligand
BDBM291522
Substrate
n/a
Meas. Tech.
ChEMBL_1857786 (CHEMBL4358515)
Kd
31±n/a nM
Citation
 Angst, D; Gessier, F; Janser, P; Vulpetti, A; Wälchli, R; Beerli, C; Littlewood-Evans, A; Dawson, J; Nuesslein-Hildesheim, B; Wieczorek, G; Gutmann, S; Scheufler, C; Hinniger, A; Zimmerlin, A; Funhoff, EG; Pulz, R; Cenni, B Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. J Med Chem 63:5102-5118 (2020) [PubMed]  Article
Target
Name:
Cytoplasmic tyrosine-protein kinase BMX
Synonyms:
BMX | BMX non-receptor tyrosine kinase | BMX_HUMAN | Bone marrow tyrosine kinase gene in chromosome X protein | Cytoplasmic tyrosine-protein kinase BMX (BMX) | ETK | Epithelial and endothelial tyrosine kinase | NTK38 | Tyrosine Kinase BMX | Tyrosine-protein kinase BMX/ETK
Type:
Tyrosine-protein kinase
Mol. Mass.:
78030.42
Organism:
Homo sapiens (Human)
Description:
P51813
Residue:
675
Sequence:
MDTKSILEELLLKRSQQKKKMSPNNYKERLFVLTKTNLSYYEYDKMKRGSRKGSIEIKKIRCVEKVNLEEQTPVERQYPFQIVYKDGLLYVYASNEESRSQWLKALQKEIRGNPHLLVKYHSGFFVDGKFLCCQQSCKAAPGCTLWEAYANLHTAVNEEKHRVPTFPDRVLKIPRAVPVLKMDAPSSSTTLAQYDNESKKNYGSQPPSSSTSLAQYDSNSKKIYGSQPNFNMQYIPREDFPDWWQVRKLKSSSSSEDVASSNQKERNVNHTTSKISWEFPESSSSEEEENLDDYDWFAGNISRSQSEQLLRQKGKEGAFMVRNSSQVGMYTVSLFSKAVNDKKGTVKHYHVHTNAENKLYLAENYCFDSIPKLIHYHQHNSAGMITRLRHPVSTKANKVPDSVSLGNGIWELKREEITLLKELGSGQFGVVQLGKWKGQYDVAVKMIKEGSMSEDEFFQEAQTMMKLSHPKLVKFYGVCSKEYPIYIVTEYISNGCLLNYLRSHGKGLEPSQLLEMCYDVCEGMAFLESHQFIHRDLAARNCLVDRDLCVKVSDFGMTRYVLDDQYVSSVGTKFPVKWSAPEVFHYFKYSSKSDVWAFGILMWEVFSLGKQPYDLYDNSQVVLKVSQGHRLYRPHLASDTIYQIMYSCWHELPEKRPTFQQLLSSIEPLREKDKH
  
Inhibitor
Name:
BDBM291522
Synonyms:
1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one | US10413562, Compound A250 | US9580449, Example A250 | US9580449, Example A39
Type:
Small organic molecule
Emp. Form.:
C25H27N5O2
Mol. Mass.:
429.5142
SMILES:
Nc1ncnc(NCC2CCN(CC2)C(=O)C=C)c1-c1ccc(Oc2ccccc2)cc1
Structure:
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