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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM230143
Substrate
n/a
Meas. Tech.
Jak2 Tyrosine Kinase Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
4300±n/a nM
Comments
extracted
Citation
 Batt, DG; Bertrand, MB; Delucca, G; Galella, MA; Ko, SS; Langevine, CM; Liu, Q; Shi, Q; Srivastava, AS; Tino, JA; Watterson, 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:
BDBM230143
Synonyms:
US9334290, 74
Type:
Small organic molecule
Emp. Form.:
C32H26F2N4O4
Mol. Mass.:
568.57
SMILES:
Cc1c(cccc1-n1c(=O)n(C)c2c(F)cccc2c1=O)-c1c(F)cc(C(N)=O)c2[nH]c3cc(ccc3c12)C(C)(C)O |(2.89,,;1.55,-.77,;.22,,;-1.12,-.77,;-1.12,-2.31,;.22,-3.08,;1.55,-2.31,;2.89,-3.08,;2.89,-4.62,;1.55,-5.39,;4.22,-5.39,;4.22,-6.93,;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,;.22,1.54,;1.55,2.31,;2.89,1.54,;1.55,3.85,;.22,4.62,;.22,6.16,;1.55,6.93,;-1.12,6.93,;-1.12,3.85,;-2.58,4.33,;-3.49,3.08,;-5.02,2.92,;-5.64,1.51,;-4.74,.27,;-3.21,.43,;-2.58,1.83,;-1.12,2.31,;-7.13,1.11,;-6.73,-.37,;-8.22,.02,;-8.22,2.2,)|
Structure:
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