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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM325506
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  US10730880 Publication Date 8/4/2020 
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:
BDBM325506
Synonyms:
(1s,3s)-3-(4-(4-(1-(pentan- 3-yl)-1H-pyrazol-4- yl)pyrazolo[1,5-a]pyrazin- 6-yl)-1H-pyrazol-1- yl)cyclobutanecarboxamide | US10189845, Example 168 | US10730880, Example 168 | US11028093, Example 168
Type:
Small organic molecule
Emp. Form.:
C22H26N8O
Mol. Mass.:
418.4948
SMILES:
CCC(CC)n1cc(cn1)-c1nc(cn2nccc12)-c1cnn(c1)C1C[C@@H](C1)C(N)=O |r,wU:26.32,(.75,4.49,;-.33,3.4,;-1.82,3.8,;-2.22,5.29,;-1.13,6.38,;-2.91,2.71,;-2.43,1.25,;-3.68,.34,;-4.93,1.25,;-4.45,2.71,;-3.68,-1.2,;-2.35,-1.97,;-2.35,-3.51,;-3.68,-4.28,;-5.01,-3.51,;-6.48,-3.98,;-7.38,-2.74,;-6.48,-1.49,;-5.01,-1.97,;-1.01,-4.28,;-1.01,-5.82,;.45,-6.29,;1.36,-5.05,;.45,-3.8,;2.9,-5.05,;3.99,-6.13,;5.07,-5.05,;3.99,-3.96,;6.61,-5.05,;7.38,-6.38,;7.38,-3.71,)|
Structure:
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