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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM50402424
Substrate
n/a
Meas. Tech.
ChEMBL_886512 (CHEMBL2214787)
IC50
4.4±n/a nM
Citation
 Forsyth, T; Kearney, PC; Kim, BG; Johnson, HW; Aay, N; Arcalas, A; Brown, DS; Chan, V; Chen, J; Du, H; Epshteyn, S; Galan, AA; Huynh, TP; Ibrahim, MA; Kane, B; Koltun, ES; Mann, G; Meyr, LE; Lee, MS; Lewis, GL; Noguchi, RT; Pack, M; Ridgway, BH; Shi, X; Takeuchi, CS; Zu, P; Leahy, JW; Nuss, JM; Aoyama, R; Engst, S; Gendreau, SB; Kassees, R; Li, J; Lin, SH; Martini, JF; Stout, T; Tong, P; Woolfrey, J; Zhang, W; Yu, P SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett 22:7653-8 (2012) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase JAK2
Synonyms:
JAK-2 | JAK2 | JAK2_HUMAN | Janus kinase 2 | Janus kinase 2 (JAK2) | Janus kinase 2 (a protein tyrosine kinase)
Type:
Protein
Mol. Mass.:
130684.68
Organism:
Homo sapiens (Human)
Description:
O60674
Residue:
1132
Sequence:
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLREALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNCYQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
  
Inhibitor
Name:
BDBM50402424
Synonyms:
CHEMBL2208027
Type:
Small organic molecule
Emp. Form.:
C22H22FN5O2
Mol. Mass.:
407.4408
SMILES:
CC(=O)Nc1ccc(cc1)-c1nc(Nc2ccc(cc2)N2CCOCC2)ncc1F
Structure:
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