Target
Tyrosine-protein kinase JAK2
Ligand
BDBM264154
Substrate
n/a
Meas. Tech.
Jak2 Tyrosine Kinase Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
470±n/a nM
Comments
extracted
Citation
 Ko, SSBatt, DGBertrand, MBDelucca, GLangevine, CMLiu, QSrivastava, ASWatterson, SH Carbazole carboxamide compounds US Patent  US9714234 Publication Date 7/25/2017 
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:
BDBM264154
Synonyms:
US9714234, 29
Type:
Small organic molecule
Emp. Form.:
C30H24FN5O3
Mol. Mass.:
521.5417
SMILES:
CN(C)c1ccc2c(c1)[nH]c1c(ccc(-c3cccc(c3C)-n3c(=O)cc4c(F)cccn4c3=O)c21)C(N)=O |(-8.22,2.2,;-7.13,1.11,;-7.53,-.37,;-5.64,1.51,;-4.74,.27,;-3.21,.43,;-2.58,1.83,;-3.49,3.08,;-5.02,2.92,;-2.58,4.33,;-1.12,3.85,;.22,4.62,;1.55,3.85,;1.55,2.31,;.22,1.54,;.22,,;-1.12,-.77,;-1.12,-2.31,;.22,-3.08,;1.55,-2.31,;1.55,-.77,;2.89,,;2.89,-3.08,;2.89,-4.62,;1.55,-5.39,;4.22,-5.39,;5.55,-4.62,;6.89,-5.39,;6.89,-6.93,;8.22,-4.62,;8.22,-3.08,;6.89,-2.31,;5.55,-3.08,;4.22,-2.31,;4.22,-.77,;-1.12,2.31,;.22,6.16,;1.55,6.93,;-1.12,6.93,)|
Structure:
Search PDB for entries with ligand similarity: