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Target
Tyrosine-protein kinase Blk
Ligand
BDBM267935
Substrate
n/a
Meas. Tech.
ChEMBL_1706717 (CHEMBL4057950)
IC50
78±n/a nM
Citation
 Boga, SB; Alhassan, AB; Liu, J; Guiadeen, D; Krikorian, A; Gao, X; Wang, J; Yu, Y; Anand, R; Liu, S; Yang, C; Wu, H; Cai, J; Zhu, H; Desai, J; Maloney, K; Gao, YD; Fischmann, TO; Presland, J; Mansueto, M; Xu, Z; Leccese, E; Knemeyer, I; Garlisi, CG; Bays, N; Stivers, P; Brandish, PE; Hicks, A; Cooper, A; Kim, RM; Kozlowski, JA Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis. Bioorg Med Chem Lett 27:3939-3943 (2017) [PubMed]  Article
Target
Name:
Tyrosine-protein kinase Blk
Synonyms:
B lymphoid tyrosine kinase | BLK | BLK_HUMAN | SRC | Tyrosine-protein kinase BLK (BLK) | p55-Blk
Type:
Protein
Mol. Mass.:
57711.88
Organism:
Homo sapiens (Human)
Description:
P51451
Residue:
505
Sequence:
MGLVSSKKPDKEKPIKEKDKGQWSPLKVSAQDKDAPPLPPLVVFNHLTPPPPDEHLDEDKHFVVALYDYTAMNDRDLQMLKGEKLQVLKGTGDWWLARSLVTGREGYVPSNFVARVESLEMERWFFRSQGRKEAERQLLAPINKAGSFLIRESETNKGAFSLSVKDVTTQGELIKHYKIRCLDEGGYYISPRITFPSLQALVQHYSKKGDGLCQRLTLPCVRPAPQNPWAQDEWEIPRQSLRLVRKLGSGQFGEVWMGYYKNNMKVAIKTLKEGTMSPEAFLGEANVMKALQHERLVRLYAVVTKEPIYIVTEYMARGCLLDFLKTDEGSRLSLPRLIDMSAQIAEGMAYIERMNSIHRDLRAANILVSEALCCKIADFGLARIIDSEYTAQEGAKFPIKWTAPEAIHFGVFTIKADVWSFGVLLMEVVTYGRVPYPGMSNPEVIRNLERGYRMPRPDTCPPELYRGVIAECWRSRPEERPTFEFLQSVLEDFYTATERQYELQP
  
Inhibitor
Name:
BDBM267935
Synonyms:
4-{8-amino-3-[(2R)-4-oxetan-3-ylmorpholin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide | US9718828, Example, 551
Type:
Small organic molecule
Emp. Form.:
C26H23F4N7O4
Mol. Mass.:
573.4989
SMILES:
COCC(=O)N1CCO[C@H](C1)c1nc(-c2ccc(cc2F)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12 |r|
Structure:
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