Reaction Details |
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Target | Tyrosine-protein kinase JAK2 |
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Ligand | BDBM50337338 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_726514 (CHEMBL1685409) |
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IC50 | 1.8±n/a nM |
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Citation | Harikrishnan, LS; Kamau, MG; Wan, H; Inghrim, JA; Zimmermann, K; Sang, X; Mastalerz, HA; Johnson, WL; Zhang, G; Lombardo, LJ; Poss, MA; Trainor, GL; Tokarski, JS; Lorenzi, MV; You, D; Gottardis, MM; Baldwin, KF; Lippy, J; Nirschl, DS; Qiu, R; Miller, AV; Khan, J; Sack, JS; Purandare, AV Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3. Bioorg Med Chem Lett21:1425-8 (2011) [PubMed] Article |
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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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BDBM50337338 |
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n/a |
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Name | BDBM50337338 |
Synonyms: | 2-(2,6-difluoro-4-methoxyphenyl)-1-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)piperazin-1-yl)ethanone | 2-(2,6-difluoro-4-methoxyphenyl)-1-(4-{4-[(3-methyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}piperazin-1-yl)ethanone | CHEMBL1615027 |
Type | Small organic molecule |
Emp. Form. | C23H24F2N8O2 |
Mol. Mass. | 482.4859 |
SMILES | COc1cc(F)c(CC(=O)N2CCN(CC2)c2nc(Nc3cc(C)n[nH]3)c3cccn3n2)c(F)c1 |
Structure |
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