Reaction Details |
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Target | Tyrosine-protein kinase JAK2 |
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Ligand | BDBM50434782 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_962506 (CHEMBL2390548) |
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EC50 | 1700±n/a nM |
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Citation | Zak, M; Hurley, CA; Ward, SI; Bergeron, P; Barrett, K; Balazs, M; Blair, WS; Bull, R; Chakravarty, P; Chang, C; Crackett, P; Deshmukh, G; DeVoss, J; Dragovich, PS; Eigenbrot, C; Ellwood, C; Gaines, S; Ghilardi, N; Gibbons, P; Gradl, S; Gribling, P; Hamman, C; Harstad, E; Hewitt, P; Johnson, A; Johnson, T; Kenny, JR; Koehler, MF; Bir Kohli, P; Labadie, S; Lee, WP; Liao, J; Liimatta, M; Mendonca, R; Narukulla, R; Pulk, R; Reeve, A; Savage, S; Shia, S; Steffek, M; Ubhayakar, S; van Abbema, A; Aliagas, I; Avitabile-Woo, B; Xiao, Y; Yang, J; Kulagowski, JJ Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2. J Med Chem56:4764-85 (2013) [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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BDBM50434782 |
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n/a |
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Name | BDBM50434782 |
Synonyms: | CHEMBL2386640 |
Type | Small organic molecule |
Emp. Form. | C16H20N4O |
Mol. Mass. | 284.3562 |
SMILES | C[C@@H](O)c1nc2cnc3[nH]ccc3c2n1C1CCCCC1 |r| |
Structure |
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