Target
Tyrosine-protein kinase JAK2 [V617F]
Ligand
BDBM608218
Substrate
n/a
Meas. Tech.
JAK2 LanthaScreen JH2-V617F Binding Assay
IC50
5500±n/a nM
Citation
 Shepard, SShao, LWu, LYao, W Naphthyridinone compounds as JAK2 V617F inhibitors US Patent  US11691971 Publication Date 7/4/2023 
Target
Name:
Tyrosine-protein kinase JAK2 [V617F]
Synonyms:
JAK2 | JAK2_HUMAN | Tyrosine-protein kinase JAK2 (V617F) | Tyrosine-protein kinase JAK2 [V617F]
Type:
Enzyme Catalytic Domain
Mol. Mass.:
130732.72
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
1132
Sequence:
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLREALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNCYQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCFCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
  
Inhibitor
Name:
BDBM608218
Synonyms:
US11691971, Example 10
Type:
Small organic molecule
Emp. Form.:
C28H29N5O4S
Mol. Mass.:
531.626
SMILES:
COc1c(Nc2cc(NC(=O)C3CC3)nc3ccn(C)c(=O)c23)cccc1-c1cnc(s1)C1CCOCC1
Structure:
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