Reaction Details |
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Target | Tyrosine-protein kinase JAK2 |
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Ligand | BDBM325453 |
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Substrate/Competitor | n/a |
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Meas. Tech. | JAK2 Inhibition Assay |
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IC50 | 55±n/a nM |
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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 US10189845 Publication Date 1/29/2019 |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase JAK2 |
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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: | MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSG
EYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYF
PRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLG
MAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQF
SQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSR
GKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLR
EALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQT
GLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNC
YQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKI
RNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASM
MSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWA
MHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVP
PECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAEL
ANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRD
PTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIE
ILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQI
CKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFW
YAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIE
LLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
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BDBM325453 |
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n/a |
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Name | BDBM325453 |
Synonyms: | (R)-1-(4-(4-(1-(pentan-3- yl)-1H-pyrazol-4- yl)pyrazolo[1,5- a]pyrazin-6-yl)-1H- pyrazol-1-yl)butan-2-ol | US10189845, Example 115 | US10730880, Example 115 | US11028093, Example 115 |
Type | Small organic molecule |
Emp. Form. | C21H27N7O |
Mol. Mass. | 393.4854 |
SMILES | CC[C@@H](O)Cn1cc(cn1)-c1cn2nccc2c(n1)-c1cnn(c1)C(CC)CC |r| |
Structure |
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