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Target
Tyrosine-protein kinase Fgr
Ligand
BDBM267959
Substrate
n/a
Meas. Tech.
ChEMBL_1706725 (CHEMBL4057958)
IC50
28±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 Fgr
Synonyms:
FGR | FGR_HUMAN | Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homolog | Proto-oncogene c-Fgr | SRC | SRC2 | p55-Fgr | p58-Fgr | p58c-Fgr
Type:
protein
Mol. Mass.:
59469.88
Organism:
Homo sapiens (Human)
Description:
P09769
Residue:
529
Sequence:
MGCVFCKKLEPVATAKEDAGLEGDFRSYGAADHYGPDPTKARPASSFAHIPNYSNFSSQAINPGFLDSGTIRGVSGIGVTLFIALYDYEARTEDDLTFTKGEKFHILNNTEGDWWEARSLSSGKTGCIPSNYVAPVDSIQAEEWYFGKIGRKDAERQLLSPGNPQGAFLIRESETTKGAYSLSIRDWDQTRGDHVKHYKIRKLDMGGYYITTRVQFNSVQELVQHYMEVNDGLCNLLIAPCTIMKPQTLGLAKDAWEISRSSITLERRLGTGCFGDVWLGTWNGSTKVAVKTLKPGTMSPKAFLEEAQVMKLLRHDKLVQLYAVVSEEPIYIVTEFMCHGSLLDFLKNPEGQDLRLPQLVDMAAQVAEGMAYMERMNYIHRDLRAANILVGERLACKIADFGLARLIKDDEYNPCQGSKFPIKWTAPEAALFGRFTIKSDVWSFGILLTELITKGRIPYPGMNKREVLEQVEQGYHMPCPPGCPASLYEAMEQTWRLDPEERPTFEYLQSFLEDYFTSAEPQYQPGDQT
  
Inhibitor
Name:
BDBM267959
Synonyms:
4-(8-amino-3-{(3R)-1-[(3-methyloxetan-3-yl)carbonyl]azepan-3-yl}imidazo[1,5-a]pyrazin-1-yl)-N-[4-(trifluoromethyl)pyridin-2-yl]benzamide | US9718828, Example, 575
Type:
Small organic molecule
Emp. Form.:
C27H25F4N7O3
Mol. Mass.:
571.5261
SMILES:
COCC(=O)N1CCC[C@H](C1)c1nc(-c2ccc(cc2F)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12 |r|
Structure:
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