Target
Tyrosine-protein kinase SYK
Ligand
BDBM182243
Substrate
n/a
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
1±n/a nM
Comments
extracted
Citation
 Deschenes, DAltman, MDEllis, JMFischer, CHaidle, AMKattar, SDNorthrup, ABSchell, AJSmith, GFTaoka, BMBienstock, CDi Francesco, MEDonofrio, APeterson, SSpencer, KBJewell, JPAli, ABennett, DJDang, QWai, J Bipyridylaminopyridines as Syk inhibitors US Patent  US9145391 Publication Date 9/29/2015 
Target
Name:
Tyrosine-protein kinase SYK
Synonyms:
KSYK_HUMAN | SYK | Spleen Tyrosine Kinase | Spleen tyrosine kinase (SYK) | Tyrosine-protein kinase SYK (Syk)
Type:
Enzyme
Mol. Mass.:
72079.99
Organism:
Homo sapiens (Human)
Description:
P43405
Residue:
635
Sequence:
MASSGMADSANHLPFFFGNITREEAEDYLVQGGMSDGLYLLRQSRNYLGGFALSVAHGRKAHHYTIERELNGTYAIAGGRTHASPADLCHYHSQESDGLVCLLKKPFNRPQGVQPKTGPFEDLKENLIREYVKQTWNLQGQALEQAIISQKPQLEKLIATTAHEKMPWFHGKISREESEQIVLIGSKTNGKFLIRARDNNGSYALCLLHEGKVLHYRIDKDKTGKLSIPEGKKFDTLWQLVEHYSYKADGLLRVLTVPCQKIGTQGNVNFGGRPQLPGSHPATWSAGGIISRIKSYSFPKPGHRKSSPAQGNRQESTVSFNPYEPELAPWAADKGPQREALPMDTEVYESPYADPEEIRPKEVYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNEANDPALKDELLAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKALRADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSYGQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPGFAAVELRLRNYYYDVVN
  
Inhibitor
Name:
BDBM182243
Synonyms:
US9145391, 15
Type:
Small organic molecule
Emp. Form.:
C26H27BrF2N4O3
Mol. Mass.:
561.418
SMILES:
Cc1cc(Nc2cc(ccn2)C(F)F)nc(-c2ccc(nc2)C(C)(O)[C@H]2CC[C@@H](CC2)C(O)=O)c1Br |r,wU:28.33,wD:25.26,(5.37,-1.95,;4.04,-1.18,;4.04,.36,;2.7,1.13,;2.7,2.67,;4.04,3.44,;4.04,4.98,;5.37,5.75,;6.71,4.98,;6.71,3.44,;5.37,2.67,;5.37,7.29,;4.04,8.06,;6.71,8.06,;1.37,.36,;1.37,-1.18,;.04,-1.95,;-1.3,-1.18,;-2.63,-1.95,;-2.63,-3.49,;-1.3,-4.26,;.04,-3.49,;-3.96,-4.26,;-4.73,-2.92,;-3.19,-5.59,;-5.3,-5.03,;-6.63,-4.26,;-7.97,-5.03,;-7.97,-6.57,;-6.63,-7.34,;-5.3,-6.57,;-9.3,-7.34,;-9.3,-8.88,;-10.63,-6.57,;2.7,-1.95,;2.7,-3.49,)|
Structure:
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