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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM325351
Substrate
n/a
Meas. Tech.
JAK2 Inhibition Assay
IC50
<10±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:
BDBM325351
Synonyms:
3-(4-(4-(1-(pentan-3-yl)-1H- pyrazol-4-yl)pyrazolo[1,5- a]pyrazin-6-yl)-1H-pyrazol- 1-yl)thietane 1,1-dioxide | US10189845, Example 13 | US10730880, Example 13 | US11028093, Example 13
Type:
Small organic molecule
Emp. Form.:
C20H23N7O2S
Mol. Mass.:
425.507
SMILES:
CCC(CC)n1cc(cn1)-c1nc(cn2nccc12)-c1cnn(c1)C1CS(=O)(=O)C1
Structure:
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