Target
Tyrosine-protein kinase JAK2
Ligand
BDBM230099
Substrate
n/a
Meas. Tech.
Jak2 Tyrosine Kinase Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
440±n/a nM
Comments
extracted
Citation
 Batt, DGBertrand, MBDelucca, GGalella, MAKo, SSLangevine, CMLiu, QShi, QSrivastava, ASTino, JAWatterson, SH Substituted tetrahydrocarbazole and carbazole carboxamide compounds US Patent  US9334290 Publication Date 5/10/2016 
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:
BDBM230099
Synonyms:
US10106559, Example 24 | US10435415, Example 24 | US9334290, 23 | US9334290, 24 | US9850258, Example 24
Type:
Small organic molecule
Emp. Form.:
C33H26ClFN4O4
Mol. Mass.:
597.035
SMILES:
Cc1c(cccc1-n1c(=O)ccn(-c2ccc(F)cc2)c1=O)-c1c(Cl)cc(C(N)=O)c2[nH]c3cc(ccc3c12)C(C)(C)O |(1.42,-.77,;.08,-1.54,;-1.25,-.77,;-2.58,-1.54,;-2.58,-3.08,;-1.25,-3.85,;.08,-3.08,;1.42,-3.85,;1.42,-5.39,;.08,-6.16,;2.75,-6.16,;4.09,-5.39,;4.09,-3.85,;5.42,-3.08,;6.75,-3.85,;8.09,-3.08,;8.09,-1.54,;9.42,-.77,;6.75,-.77,;5.42,-1.54,;2.75,-3.08,;2.75,-1.54,;-1.25,.77,;.08,1.54,;1.42,.77,;.08,3.08,;-1.25,3.85,;-1.25,5.39,;.08,6.16,;-2.58,6.16,;-2.58,3.08,;-4.05,3.56,;-4.95,2.31,;-6.48,2.15,;-7.11,.74,;-6.21,-.5,;-4.67,-.34,;-4.05,1.06,;-2.58,1.54,;-8.65,.74,;-9.42,-.59,;-7.88,-.59,;-9.42,2.08,)|
Structure:
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