Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase JAK2
Ligand
BDBM50261777
Substrate
n/a
Meas. Tech.
ChEBML_1696338
IC50
>2000±n/a nM
Citation
 Kempson, J; Ovalle, D; Guo, J; Wrobleski, ST; Lin, S; Spergel, SH; Duan, JJ; Jiang, B; Lu, Z; Das, J; Yang, BV; Hynes, J; Wu, H; Tokarski, J; Sack, JS; Khan, J; Schieven, G; Blatt, Y; Chaudhry, C; Salter-Cid, LM; Fura, A; Barrish, JC; Carter, PH; Pitts, WJ Discovery of highly potent, selective, covalent inhibitors of JAK3. Bioorg Med Chem Lett 27:4622-4625 (2017) [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:
BDBM50261777
Synonyms:
CHEMBL4088027
Type:
Small organic molecule
Emp. Form.:
C21H21N7O2
Mol. Mass.:
403.4371
SMILES:
CN(C)\C=C(\C#N)C(=O)Nc1cccc(CNc2c(cnn3cccc23)C(N)=O)c1
Structure:
Search PDB for entries with ligand similarity: