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Target
Tyrosine-protein kinase JAK2
Ligand
BDBM472735
Substrate
n/a
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Assay
IC50
>20.0±n/a nM
Citation
 Zhu, L; Hu, Y; Wu, W; Dai, L; Duan, X; Yang, Y; Sun, Y; Han, Y; Peng, Y; Kong, F; Luo, H; Yang, L; Xu, H; Guo, M; Zhong, Z; Wang, S Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor US Patent  US10829492 Publication Date 11/10/2020 
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:
BDBM472735
Synonyms:
2-amino-5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-N-((trans)-4-hydroxycyclohexyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide | US10829492, Example 12
Type:
Small organic molecule
Emp. Form.:
C23H26F2N6O2
Mol. Mass.:
456.4883
SMILES:
Nc1nn2ccc(nc2c1C(=O)N[C@H]1CC[C@H](O)CC1)N1CCC[C@@H]1c1cc(F)ccc1F |r,wU:13.14,wD:24.28,16.18,(3.91,3.31,;2.44,2.83,;1.2,3.74,;-.05,2.83,;-1.56,3.15,;-2.59,2.01,;-2.11,.54,;-.6,.22,;.43,1.37,;1.97,1.37,;2.87,.12,;2.24,-1.29,;4.4,.28,;5.31,-.96,;6.84,-.8,;7.74,-2.05,;7.12,-3.46,;8.02,-4.7,;5.59,-3.62,;4.68,-2.37,;-3.14,-.6,;-2.67,-2.07,;-3.91,-2.97,;-5.16,-2.07,;-4.68,-.6,;-5.59,.64,;-4.96,2.05,;-5.87,3.3,;-5.24,4.7,;-7.4,3.13,;-8.02,1.73,;-7.12,.48,;-7.74,-.92,)|
Structure:
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