Reaction Details |
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Target | Tyrosine-protein kinase JAK2 |
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Ligand | BDBM50307987 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_608408 (CHEMBL1064437) |
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IC50 | >10000±n/a nM |
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Citation | Brasca, MG; Albanese, C; Alzani, R; Amici, R; Avanzi, N; Ballinari, D; Bischoff, J; Borghi, D; Casale, E; Croci, V; Fiorentini, F; Isacchi, A; Mercurio, C; Nesi, M; Orsini, P; Pastori, W; Pesenti, E; Pevarello, P; Roussel, P; Varasi, M; Volpi, D; Vulpetti, A; Ciomei, M Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem18:1844-53 (2010) [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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BDBM50307987 |
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n/a |
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Name | BDBM50307987 |
Synonyms: | CHEMBL604712 | N-[5-(2,2-Dimethylpropanoyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-3,5-difluorobenzamide |
Type | Small organic molecule |
Emp. Form. | C19H22F2N4O2 |
Mol. Mass. | 376.4004 |
SMILES | CC(C)(C)C(=O)N1Cc2c(NC(=O)c3cc(F)cc(F)c3)[nH]nc2C1(C)C |
Structure |
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