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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM230084
Substrate
n/a
Meas. Tech.
Jak2 Tyrosine Kinase Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
>2000±n/a nM
Comments
extracted
Citation
 Batt, DG; Bertrand, MB; Delucca, GV; Galella, MA; Ko, SS; Langevine, CM; Liu, Q; Shi, Q; Srivastava, AS; Tino, JA; Watterson, SH Substituted tetrahydrocarbazole and carbazole carboxamide compounds US Patent  US10106559 Publication Date 10/23/2018 
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:
BDBM230084
Synonyms:
US10106559, Example 6 | US10435415, Example 6 | US9334290, 5 | US9850258, Example 6
Type:
Small organic molecule
Emp. Form.:
C33H29ClN4O5
Mol. Mass.:
597.06
SMILES:
COc1ccc2c(c1)n(C)c(=O)n(-c1cccc(c1C)-c1c(Cl)cc(C(N)=O)c3[nH]c4cc(ccc4c13)C(C)(C)O)c2=O |(9.42,-4.62,;8.09,-5.39,;6.75,-4.62,;6.75,-3.08,;5.42,-2.31,;4.09,-3.08,;4.09,-4.62,;5.42,-5.39,;2.75,-5.39,;2.75,-6.93,;1.42,-4.62,;.08,-5.39,;1.42,-3.08,;.08,-2.31,;-1.25,-3.08,;-2.58,-2.31,;-2.58,-.77,;-1.25,,;.08,-.77,;1.42,,;-1.25,1.54,;.08,2.31,;1.42,1.54,;.08,3.85,;-1.25,4.62,;-1.25,6.16,;.08,6.93,;-2.58,6.93,;-2.58,3.85,;-4.05,4.33,;-4.95,3.08,;-6.48,2.92,;-7.11,1.51,;-6.21,.27,;-4.67,.43,;-4.05,1.83,;-2.58,2.31,;-8.65,1.51,;-9.42,.18,;-7.88,.18,;-9.42,2.85,;2.75,-2.31,;2.75,-.77,)|
Structure:
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