Target
Tyrosine-protein kinase JAK2 [808-1132]
Ligand
BDBM127677
Substrate
n/a
Meas. Tech.
Inhibition Assay
IC50
186±n/a nM
Citation
 Allen, SAndrews, SWCondroski, KRHaas, JHuang, LJiang, YKercher, TSeo, J Substituted pyrazolo[l,5-a]pyrimidine compounds as Trk kinase inhibitors US Patent  US10758542 Publication Date 9/1/2020 
Target
Name:
Tyrosine-protein kinase JAK2 [808-1132]
Synonyms:
JAK2 | JAK2_HUMAN | Janus kinase 2 (JAK2) | Tyrosine-protein kinase JAK2 | Tyrosine-protein kinase JAK2 (808-1132)
Type:
n/a
Mol. Mass.:
37984.02
Organism:
Homo sapiens (Human)
Description:
808-1132 aa of O60674
Residue:
325
Sequence:
LFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
  
Inhibitor
Name:
BDBM127677
Synonyms:
US10251889, Example 51 | US10758542, Example 51 | US8791123, 50 | US9782415, Example 51 | US9796724, Example 51
Type:
Small organic molecule
Emp. Form.:
C24H27F2N5O2
Mol. Mass.:
455.5003
SMILES:
C[C@@]1(O)CCC(CC1)NC(=O)c1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F |r,w:8.8,wU:1.0,wD:24.28,1.1,(7.04,-6.19,;5.95,-5.1,;5.55,-6.59,;4.46,-4.7,;4.06,-3.21,;5.15,-2.12,;6.64,-2.52,;7.04,-4.01,;4.75,-.64,;3.27,-.24,;2.18,-1.33,;2.87,1.25,;3.77,2.5,;2.87,3.74,;1.4,3.27,;.07,4.04,;-1.26,3.27,;-1.26,1.73,;.07,.96,;1.4,1.73,;-2.6,.96,;-2.6,-.58,;-4.06,-1.06,;-4.97,.19,;-4.06,1.43,;-4.46,2.92,;-3.37,4.01,;-3.77,5.5,;-2.68,6.59,;-5.26,5.9,;-6.35,4.81,;-5.95,3.32,;-7.04,2.23,)|
Structure:
Search PDB for entries with ligand similarity: