Target
Glutathione S-transferase P/Tyrosine-protein kinase SYK
Ligand
BDBM255586
Substrate
n/a
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
8.476±n/a nM
Comments
extracted
Citation
 Arrington, KLDuBois, BDebenham, JSLiu, PNorthrup, ABSzewczyk, JWWang, LWang, M Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors US Patent  US9499534 Publication Date 11/22/2016 
Target
Name:
Glutathione S-transferase P/Tyrosine-protein kinase SYK
Synonyms:
GST-Tyrosine-protein kinase SYK
Type:
Enzyme
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Glutathione S-transferase P
Synonyms:
FAEES3 | GST class-pi | GST3 | GSTP1 | GSTP1-1 | GSTP1_HUMAN | Glutathione S-transferase | Glutathione S-transferase (GST) | Glutathione S-transferase P | Glutathione S-transferase Pi | Glutathione transferase (GST)
Type:
Enzyme
Mol. Mass.:
23353.53
Organism:
Homo sapiens (Human)
Description:
P09211
Residue:
210
Sequence:
MPPYTVVYFPVRGRCAALRMLLADQGQSWKEEVVTVETWQEGSLKASCLYGQLPKFQDGDLTLYQSNTILRHLGRTLGLYGKDQQEAALVDMVNDGVEDLRCKYISLIYTNYEAGKDDYVKALPGQLKPFETLLSQNQGGKTFIVGDQISFADYNLLDLLLIHEVLAPGCLDAFPLLSAYVGRLSARPKLKAFLASPEYVNLPINGNGKQ
  
Component 2
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:
BDBM255586
Synonyms:
US9499534, 1.7
Type:
Small organic molecule
Emp. Form.:
C22H18F3N5O3S
Mol. Mass.:
489.47
SMILES:
OC(=O)C1CCC(O)(CC1)c1ncc(s1)-c1cc(Nc2nccc(n2)C(F)(F)F)cc(c1)C#N |(-4.06,-5.27,;-2.99,-6.38,;-3.42,-7.86,;-1.5,-6,;-.43,-7.11,;1.07,-6.74,;1.49,-5.26,;2.87,-5.93,;.42,-4.15,;-1.07,-4.52,;2.4,-4.01,;3.94,-4.01,;4.41,-2.55,;3.17,-1.64,;1.92,-2.55,;3.17,-.1,;1.83,.67,;1.83,2.21,;.5,2.98,;.5,4.52,;-.84,5.29,;-.84,6.83,;.5,7.6,;1.83,6.83,;1.83,5.29,;3.17,7.6,;4.5,8.37,;2.4,8.93,;3.94,6.26,;3.17,2.98,;4.5,2.21,;4.5,.67,;5.83,2.98,;7.17,3.75,)|
Structure:
Search PDB for entries with ligand similarity: