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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM50355501
Substrate
n/a
Meas. Tech.
ChEMBL_856880 (CHEMBL2160361)
Ki
0.1±n/a nM
Citation
 Zak, M; Mendonca, R; Balazs, M; Barrett, K; Bergeron, P; Blair, WS; Chang, C; Deshmukh, G; Devoss, J; Dragovich, PS; Eigenbrot, C; Ghilardi, N; Gibbons, P; Gradl, S; Hamman, C; Hanan, EJ; Harstad, E; Hewitt, PR; Hurley, CA; Jin, T; Johnson, A; Johnson, T; Kenny, JR; Koehler, MF; Bir Kohli, P; Kulagowski, JJ; Labadie, S; Liao, J; Liimatta, M; Lin, Z; Lupardus, PJ; Maxey, RJ; Murray, JM; Pulk, R; Rodriguez, M; Savage, S; Shia, S; Steffek, M; Ubhayakar, S; Ultsch, M; van Abbema, A; Ward, SI; Xiao, L; Xiao, Y Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. J Med Chem 55:6176-93 (2012) [PubMed]  Article 
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:
BDBM50355501
Synonyms:
INCB-018424 | RUXOLITINIB | RUXOLITINIB PHOSPHATE | US10112907, Example 00016 | US10766894, Compound TABLE 1.1 | US10875847, Compound JAKAFI | US11203595, TABLE 1.1 | US11279703, TABLE 6.147
Type:
Small organic molecule
Emp. Form.:
C17H18N6
Mol. Mass.:
306.365
SMILES:
N#CC[C@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12 |r|
Structure:
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