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TargetCytoplasmic tyrosine-protein kinase BMX
LigandBDBM348593
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2186315 (CHEMBL5098397)
Kd 2700±n/a nM
Citation Hopkins, BTBame, EBell, NBohnert, TBowden-Verhoek, JKBui, MCancilla, MTConlon, PCullen, PErlanson, DAFan, JFuchs-Knotts, THansen, SHeumann, SJenkins, TJGua, CLiu, YLiu, YLulla, MMarcotte, DMarx, IMcDowell, BMertsching, ENegrou, ERomanowski, MJScott, DSilvian, LYang, WZhong, M Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors. Bioorg Med Chem44:0 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cytoplasmic tyrosine-protein kinase BMX
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:
MDTKSILEELLLKRSQQKKKMSPNNYKERLFVLTKTNLSYYEYDKMKRGSRKGSIEIKKI
RCVEKVNLEEQTPVERQYPFQIVYKDGLLYVYASNEESRSQWLKALQKEIRGNPHLLVKY
HSGFFVDGKFLCCQQSCKAAPGCTLWEAYANLHTAVNEEKHRVPTFPDRVLKIPRAVPVL
KMDAPSSSTTLAQYDNESKKNYGSQPPSSSTSLAQYDSNSKKIYGSQPNFNMQYIPREDF
PDWWQVRKLKSSSSSEDVASSNQKERNVNHTTSKISWEFPESSSSEEEENLDDYDWFAGN
ISRSQSEQLLRQKGKEGAFMVRNSSQVGMYTVSLFSKAVNDKKGTVKHYHVHTNAENKLY
LAENYCFDSIPKLIHYHQHNSAGMITRLRHPVSTKANKVPDSVSLGNGIWELKREEITLL
KELGSGQFGVVQLGKWKGQYDVAVKMIKEGSMSEDEFFQEAQTMMKLSHPKLVKFYGVCS
KEYPIYIVTEYISNGCLLNYLRSHGKGLEPSQLLEMCYDVCEGMAFLESHQFIHRDLAAR
NCLVDRDLCVKVSDFGMTRYVLDDQYVSSVGTKFPVKWSAPEVFHYFKYSSKSDVWAFGI
LMWEVFSLGKQPYDLYDNSQVVLKVSQGHRLYRPHLASDTIYQIMYSCWHELPEKRPTFQ
QLLSSIEPLREKDKH
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  Blast E-value cutoff:
BDBM348593
n/a
NameBDBM348593
Synonyms:US10577374, Compound 316 | US9790229, Compound 316
TypeSmall organic molecule
Emp. Form.C22H24ClFN6O
Mol. Mass.442.917
SMILESFc1cc(Cl)cc(N[C@@H]2CCCN([C@@H]3CCCN(C3)c3ncnc4[nH]ccc34)C2=O)c1 |r|
Structure
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