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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM322910
Substrate
n/a
Meas. Tech.
Enzymatic JAK2 Kinase Activity
IC50
<10±n/a nM
Citation
 Venkatesan, A; Smith, R; Hosahalli, S; Potluri, V; Panigrahi, SK; Basetti, V; Kunta, K Pyrimido-pyridazinone compounds and methods of use thereof US Patent  US10647720 Publication Date 5/12/2020 
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:
BDBM322910
Synonyms:
2-(1-(4-((4-(4,4-difluoropiperidin-1-yl) phenyl)amino)-5-oxo-5,6- dihydropyrimido[4,5-d]pyridazin-2-yl) piperidin-4-yl)acetonitrile | US10183944, Example 280 | US10647720, Ex. # 280
Type:
Small organic molecule
Emp. Form.:
C24H26F2N8O
Mol. Mass.:
480.513
SMILES:
FC1(F)CCN(CC1)c1ccc(Nc2nc(nc3cn[nH]c(=O)c23)N2CCC(CC#N)CC2)cc1
Structure:
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