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Target
Tyrosine-protein kinase ITK/TSK
Ligand
BDBM2579
Substrate
SAM68 Peptide Substrate
Meas. Tech.
Radiometric Kinase Assay
pH
8±n/a
Temperature
298.15±n/a K
Ki
2.2±0.4 nM
Km
7800000±1300000 nM
Comments
Kcat=0.12 1/min.
Citation
 Brown, K; Long, JM; Vial, SC; Dedi, N; Dunster, NJ; Renwick, SB; Tanner, AJ; Frantz, JD; Fleming, MA; Cheetham, GM Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors. J Biol Chem 279:18727-32 (2004) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase ITK/TSK
Synonyms:
EMT | ITK | ITK_HUMAN | Kinase EMT | LYK | T-cell-specific kinase | Tyrosine-protein kinase ITK | Tyrosine-protein kinase ITK (ITK) | Tyrosine-protein kinase Lyk
Type:
Protein
Mol. Mass.:
71839.20
Organism:
Homo sapiens (Human)
Description:
Q08881
Residue:
620
Sequence:
MNNFILLEEQLIKKSQQKRRTSPSNFKVRFFVLTKASLAYFEDRHGKKRTLKGSIELSRIKCVEIVKSDISIPCHYKYPFQVVHDNYLLYVFAPDRESRQRWVLALKEETRNNNSLVPKYHPNFWMDGKWRCCSQLEKLATGCAQYDPTKNASKKPLPPTPEDNRRPLWEPEETVVIALYDYQTNDPQELALRRNEEYCLLDSSEIHWWRVQDRNGHEGYVPSSYLVEKSPNNLETYEWYNKSISRDKAEKLLLDTGKEGAFMVRDSRTAGTYTVSVFTKAVVSENNPCIKHYHIKETNDNPKRYYVAEKYVFDSIPLLINYHQHNGGGLVTRLRYPVCFGRQKAPVTAGLRYGKWVIDPSELTFVQEIGSGQFGLVHLGYWLNKDKVAIKTIREGAMSEEDFIEEAEVMMKLSHPKLVQLYGVCLEQAPICLVFEFMEHGCLSDYLRTQRGLFAAETLLGMCLDVCEGMAYLEEACVIHRDLAARNCLVGENQVIKVSDFGMTRFVLDDQYTSSTGTKFPVKWASPEVFSFSRYSSKSDVWSFGVLMWEVFSEGKIPYENRSNSEVVEDISTGFRLYKPRLASTHVYQIMNHCWKERPEDRPAFSRLLRQLAEIAESGL
  
Inhibitor
Name:
BDBM2579
Synonyms:
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine
Type:
Small organic molecule
Emp. Form.:
C28H26N4O3
Mol. Mass.:
466.531
SMILES:
CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
SAM68 Peptide Substrate
Synonyms:
Src-associated in mitosis 68-kDa protein, residues 332Â?443
Type:
Other Protein Type
Mol. Mass.:
12597.27
Organism:
Mus musculus (mouse)
Description:
n/a
Residue:
112
Sequence:
GVPPPPTVRGAPTPRARTAGIQRIPLPPTPAPETYEDYGYDDTYAEQSYEGYEGYYSQSQGESEYYDYGHGELQDSYEAYGQDDWNGTRPSLKAPPARPVKGAYREHPYGRY