Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase JAK2
Ligand
BDBM322895
Substrate
n/a
Meas. Tech.
Enzymatic JAK2 Kinase Activity
IC50
<10±n/a nM
Citation
Venkatesan, A; Smith, R; Hosahalli, S; Potluri, V; Panigrahi, SK; Basetti, V; Kunta, K Pyrimido-pyridazinone compounds and methods of use thereof US Patent US10647720 Publication Date 5/12/2020
More Info.:
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:
BDBM322895
Synonyms:
2-(azepan-1-yl)-4-((4-(4-(1-hydroxy-2- methylpropan-2-yl)piperazin-1-yl)phenyl) amino)pyrimido[4,5-d]pyridazin-5(6H)- one | US10183944, Example 265 | US10647720, Ex. # 265
Type:
Small organic molecule
Emp. Form.:
C26H36N8O2
Mol. Mass.:
492.6164
SMILES:
CC(C)(CO)N1CCN(CC1)c1ccc(Nc2nc(nc3cn[nH]c(=O)c23)N2CCCCCC2)cc1