Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase SYK
Ligand
BDBM189863
Substrate
n/a
Meas. Tech.
Time-Resolved Fluorescence (HTRF) Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
13.2±0.0 nM
Comments
extracted
Citation
Miller, TA; Petrocchi, A; Romeo, ET; Vitharana, D; Kattar, SD; Northrup, AB; Altman, MD; Anthony, NJ Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors US Patent US9670196 Publication Date 6/6/2017
More Info.:
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:
BDBM189863
Synonyms:
US9670196, 1.7 (1S,4R or 1R,4S)-4- hydroxy-2,2-dimethyl-4- (5-(3-methyl-5-((4- methylfuro[3,2- d]pyrimidin-2- yl)amino)phenyl)thiazol- 2- yl)cyclohexanecarboxylic acid
Type:
Small organic molecule
Emp. Form.:
C26H28N4O4S
Mol. Mass.:
492.59
SMILES:
Cc1cc(Nc2nc(C)c3occc3n2)cc(c1)-c1cnc(s1)[C@@]1(O)CC[C@H](C(O)=O)C(C)(C)C1 |r|