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Target
Serine/threonine-protein kinase MARK2
Ligand
BDBM247043
Substrate
n/a
Meas. Tech.
PAR-1 FLIPR Assay
IC50
13.9±n/a nM
Citation
 Yang, Z; Zhang, F; Dong, G; Knowles, SL; Maletic, M Preparation and use of 7a-amide substituted- 6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists US Patent  US9701669 Publication Date 7/11/2017 
Target
Name:
Serine/threonine-protein kinase MARK2
Synonyms:
ELKL motif kinase 1 | EMK1 | MAP/microtubule affinity-regulating kinase 2 | MARK2 | MARK2_HUMAN | PAR1 homolog | Par-1 | Serine/threonine-protein kinase MARK2
Type:
PROTEIN
Mol. Mass.:
87953.09
Organism:
Homo sapiens (Human)
Description:
ChEMBL_774586
Residue:
788
Sequence:
MSSARTPLPTLNERDTEQPTLGHLDSKPSSKSNMIRGRNSATSADEQPHIGNYRLLKTIGKGNFAKVKLARHILTGKEVAVKIIDKTQLNSSSLQKLFREVRIMKVLNHPNIVKLFEVIETEKTLYLVMEYASGGEVFDYLVAHGRMKEKEARAKFRQIVSAVQYCHQKFIVHRDLKAENLLLDADMNIKIADFGFSNEFTFGNKLDTFCGSPPYAAPELFQGKKYDGPEVDVWSLGVILYTLVSGSLPFDGQNLKELRERVLRGKYRIPFYMSTDCENLLKKFLILNPSKRGTLEQIMKDRWMNVGHEDDELKPYVEPLPDYKDPRRTELMVSMGYTREEIQDSLVGQRYNEVMATYLLLGYKSSELEGDTITLKPRPSADLTNSSAPSPSHKVQRSVSANPKQRRFSDQAAGPAIPTSNSYSKKTQSNNAENKRPEEDRESGRKASSTAKVPASPLPGLERKKTTPTPSTNSVLSTSTNRSRNSPLLERASLGQASIQNGKDSLTMPGSRASTASASAAVSAARPRQHQKSMSASVHPNKASGLPPTESNCEVPRPSTAPQRVPVASPSAHNISSSGGAPDRTNFPRGVSSRSTFHAGQLRQVRDQQNLPYGVTPASPSGHSQGRRGASGSIFSKFTSKFVRRNLSFRFARRNLNEPESKDRVETLRPHVVGSGGNDKEKEEFREAKPRSLRFTWSMKTTSSMEPNEMMREIRKVLDANSCQSELHEKYMLLCMHGTPGHEDFVQWEMEVCKLPRLSLNGVRFKRISGTSMAFKNIASKIANELKL
  
Inhibitor
Name:
BDBM247043
Synonyms:
1-((1R,3aS,6S, 7R,7aS)-5,5- difluoro-7- ((E)-2-(5-(3- fluorophenyl) pyridin-2- yl)vinyl)-1,6- dimethyl-3- oxo-octahydro- isobenzofuran- 3a-yl)azetidine- 3-carboxamide | US9701669, 13
Type:
Small organic molecule
Emp. Form.:
C27H28F3N3O3
Mol. Mass.:
499.5247
SMILES:
C[C@H]1OC(=O)[C@@]2(CC(F)(F)[C@@H](C)[C@H](\C=C\c3ccc(cn3)-c3cccc(F)c3)[C@H]12)N1CC(C1)C(N)=O |r|
Structure:
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