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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM325510
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:
BDBM325510
Synonyms:
(1s,3s)-N-(2- hydroxyethyl)-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 172 | US10730880, Example 172 | US11028093, Example 172
Type:
Small organic molecule
Emp. Form.:
C24H30N8O2
Mol. Mass.:
462.5474
SMILES:
CCC(CC)n1cc(cn1)-c1nc(cn2nccc12)-c1cnn(c1)C1C[C@@H](C1)C(=O)NCCO |r,wU:26.32,(-1.17,5.16,;-2.26,4.07,;-3.75,4.47,;-4.15,5.96,;-3.06,7.05,;-4.84,3.38,;-4.36,1.92,;-5.61,1.01,;-6.85,1.92,;-6.38,3.38,;-5.61,-.53,;-4.27,-1.3,;-4.27,-2.84,;-5.61,-3.61,;-6.94,-2.84,;-8.4,-3.31,;-9.31,-2.07,;-8.4,-.82,;-6.94,-1.3,;-2.94,-3.61,;-2.94,-5.15,;-1.47,-5.62,;-.57,-4.38,;-1.47,-3.13,;.97,-4.38,;2.06,-5.47,;3.15,-4.38,;2.06,-3.29,;4.69,-4.38,;5.46,-3.05,;5.46,-5.71,;7,-5.71,;7.77,-7.05,;9.31,-7.05,)|
Structure:
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