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Target
Tyrosine-protein kinase Fgr
Ligand
BDBM255303
Substrate
n/a
Meas. Tech.
ChEMBL_2071888 (CHEMBL4727422)
IC50
34±n/a nM
Citation
 Liu, J; Guiadeen, D; Krikorian, A; Gao, X; Wang, J; Babu Boga, S; Alhassan, AB; Yu, W; Selyutin, O; Yu, Y; Anand, R; Xu, J; Kelly, J; Duffy, JL; Liu, S; Yang, C; Wu, H; Cai, J; Bennett, C; Maloney, KM; Tyagarajan, S; Gao, YD; Fischmann, TO; Presland, J; Mansueto, M; Xu, Z; Leccese, E; Zhang-Hoover, J; Knemeyer, I; Garlisi, CG; Stivers, P; Brandish, PE; Hicks, A; Kim, R; Kozlowski, JA Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes. Bioorg Med Chem Lett 30:0 (2020) [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:
BDBM255303
Synonyms:
US9481682, 52
Type:
Small organic molecule
Emp. Form.:
C28H26F3N7O3
Mol. Mass.:
565.5463
SMILES:
CC1(C)OC(=O)N2C[C@@H](CC[C@@H]12)c1nc(-c2ccc(cc2)C(=O)Nc2cc(ccn2)C(F)(F)F)c2c(N)nccn12 |r|
Structure:
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