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Target
Tyrosine-protein kinase SYK
Ligand
BDBM212271
Substrate
n/a
Meas. Tech.
ChEMBL_1972894 (CHEMBL4605712)
EC50
26±n/a nM
Citation
Blomgren, P; Chandrasekhar, J; Di Paolo, JA; Fung, W; Geng, G; Ip, C; Jones, R; Kropf, JE; Lansdon, EB; Lee, S; Lo, JR; Mitchell, SA; Murray, B; Pohlmeyer, C; Schmitt, A; Suekawa-Pirrone, K; Wise, S; Xiong, JM; Xu, J; Yu, H; Zhao, Z; Currie, KS Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases. ACS Med Chem Lett 11:506-513 (2020) [PubMed] Article
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:
BDBM212271
Synonyms:
6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine | US10342794, Example Ex.-2 | US10828299, Example Ex.-2 | US11517570, Example Ex.-2: | US9290505, Ex.-2 | US9504684, Ex.-2 | US9931338, Ex.-2
Type:
Small organic molecule
Emp. Form.:
C23H25N9O
Mol. Mass.:
443.5043
SMILES:
Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1