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TargetCytoplasmic tyrosine-protein kinase BMX
LigandBDBM50194720
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1616894 (CHEMBL3858963)
IC50 32±n/a nM
Citation Watterson, SH; De Lucca, GV; Shi, Q; Langevine, CM; Liu, Q; Batt, DG; Beaudoin Bertrand, M; Gong, H; Dai, J; Yip, S; Li, P; Sun, D; Wu, DR; Wang, C; Zhang, Y; Traeger, SC; Pattoli, MA; Skala, S; Cheng, L; Obermeier, MT; Vickery, R; Discenza, LN; D'Arienzo, CJ; Zhang, Y; Heimrich, E; Gillooly, KM; Taylor, TL; Pulicicchio, C; McIntyre, KW; Galella, MA; Tebben, AJ; Muckelbauer, JK; Chang, C; Rampulla, R; Mathur, A; Salter-Cid, L; Barrish, JC; Carter, PH; Fura, A; Burke, JR; Tino, JA Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke J Med Chem59:9173-9200 (2016) [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:
BDBM50194720
n/a
NameBDBM50194720
Synonyms:CHEMBL3900554
TypeSmall organic molecule
Emp. Form.C32H30F2N4O4
Mol. Mass.572.6018
SMILES[H][C@@]1(CCc2c(C1)[nH]c1c(cc(F)c(-c3cccc(c3C)-n3c(=O)n(C)c4c(F)cccc4c3=O)c21)C(O)=N)C(C)(C)O |r,wU:1.0,(7.64,3.3,;7.24,1.81,;5.84,2.47,;4.58,1.59,;4.71,.05,;6.1,-.6,;7.37,.28,;4.84,-1.48,;3.3,-1.34,;2.9,-2.83,;1.41,-3.22,;.33,-2.13,;-1.16,-2.53,;.73,-.64,;-.36,.45,;.05,1.93,;-1.04,3.03,;-2.53,2.63,;-2.93,1.15,;-1.85,.05,;-2.25,-1.43,;-4.42,.75,;-4.82,-.73,;-3.74,-1.83,;-6.31,-1.13,;-6.71,-2.62,;-7.4,-.04,;-8.89,-.43,;-9.29,-1.92,;-9.97,.66,;-9.57,2.15,;-8.08,2.54,;-6.99,1.45,;-5.51,1.84,;-5.1,3.33,;2.22,-.25,;3.99,-3.92,;5.48,-3.53,;3.58,-5.41,;8.77,1.67,;8.91,3.21,;8.63,.14,;10.3,1.53,)|
Structure
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