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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM325516
Substrate
n/a
Meas. Tech.
JAK2 Inhibition Assay
IC50
55±n/a nM
Citation
 Allen, S; Boys, ML; Chicarelli, MJ; Fell, JB; Fischer, JP; Gaudino, J; Hicken, EJ; Hinklin, RJ; Kraser, CF; Laird, E; Robinson, JE; Tang, TP; Burgess, LE; Rieger, RA; Pheneger, J; Satoh, Y; Leftheris, K; Raheja, RK; Bennett, BL 4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors US Patent  US11028093 Publication Date 6/8/2021 
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:
BDBM325516
Synonyms:
(cis-3- hydroxycyclobutyl)(3- (4-(4-(1-(pentan-3-yl)- 1H-pyrazol-4- yl)pyrazolo[1,5- a]pyrazin-6-yl)-1H- pyrazol-1-yl)azetidin-1- yl)methanone | US10189845, Example 178 | US10730880, Example 179 | US11028093, Example 179
Type:
Small organic molecule
Emp. Form.:
C25H30N8O2
Mol. Mass.:
474.5581
SMILES:
CCC(CC)n1cc(cn1)-c1nc(cn2nccc12)-c1cnn(c1)C1CN(C1)C(=O)C1C[C@H](O)C1 |r,wU:32.37,(2.16,9,;1.07,7.91,;-.41,8.31,;-.81,9.8,;.28,10.89,;-1.5,7.22,;-1.03,5.76,;-2.27,4.85,;-3.52,5.76,;-3.04,7.22,;-2.27,3.31,;-.94,2.54,;-.94,1,;-2.27,.23,;-3.61,1,;-5.07,.53,;-5.98,1.77,;-5.07,3.02,;-3.61,2.54,;.39,.23,;1.86,.71,;2.76,-.54,;1.86,-1.78,;.39,-1.31,;2.63,-3.12,;2.23,-4.6,;3.72,-5,;4.12,-3.51,;4.49,-6.34,;5.98,-6.73,;3.72,-7.67,;2.23,-8.07,;2.63,-9.56,;1.86,-10.89,;4.12,-9.16,)|
Structure:
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