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Target
Tyrosine-protein kinase FRK
Ligand
BDBM255338
Substrate
n/a
Meas. Tech.
ChEMBL_2071889 (CHEMBL4727423)
IC50
154±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 FRK
Synonyms:
FRK | FRK_HUMAN | FYN-related kinase | Nuclear tyrosine protein kinase RAK | PTK5 | RAK | SRC | Tyrosine Kinase FRK
Type:
Tyrosine-protein kinase
Mol. Mass.:
58254.41
Organism:
Homo sapiens (Human)
Description:
P42685
Residue:
505
Sequence:
MSNICQRLWEYLEPYLPCLSTEADKSTVIENPGALCSPQSQRHGHYFVALFDYQARTAEDLSFRAGDKLQVLDTLHEGWWFARHLEKRRDGSSQQLQGYIPSNYVAEDRSLQAEPWFFGAIGRSDAEKQLLYSENKTGSFLIRESESQKGEFSLSVLDGAVVKHYRIKRLDEGGFFLTRRRIFSTLNEFVSHYTKTSDGLCVKLGKPCLKIQVPAPFDLSYKTVDQWEIDRNSIQLLKRLGSGQFGEVWEGLWNNTTPVAVKTLKPGSMDPNDFLREAQIMKNLRHPKLIQLYAVCTLEDPIYIITELMRHGSLQEYLQNDTGSKIHLTQQVDMAAQVASGMAYLESRNYIHRDLAARNVLVGEHNIYKVADFGLARVFKVDNEDIYESRHEIKLPVKWTAPEAIRSNKFSIKSDVWSFGILLYEIITYGKMPYSGMTGAQVIQMLAQNYRLPQPSNCPQQFYNIMLECWNAEPKERPTFETLRWKLEDYFETDSSYSDANNFIR
  
Inhibitor
Name:
BDBM255338
Synonyms:
US9481682, 116 | US9481682, 88
Type:
Small organic molecule
Emp. Form.:
C28H26F3N7O3
Mol. Mass.:
565.5463
SMILES:
COc1cc(ccc1-c1nc([C@@H]2CC[C@H]3CCC(=O)N3C2)n2ccnc(N)c12)C(=O)Nc1cc(ccn1)C(F)(F)F |r|
Structure:
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