Target
Serine/threonine-protein kinase MARK2
Ligand
BDBM247045
Substrate
n/a
Meas. Tech.
PAR-1 FLIPR Assay
IC50
104±n/a nM
Citation
 Yang, ZZhang, FDong, GKnowles, SLMaletic, 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:
BDBM247045
Synonyms:
2-((1R,3aR,6S, 7R,7aS)-5,5- difluoro-7- ((E)-2-(2'- methoxy-[3,3'- bipyridin]-6- yl)vinyl)-1,6- dimethyl-3- oxooctahydro- isobenzofuran- 3a-yl)acetamide | US9701669, 16
Type:
Small organic molecule
Emp. Form.:
C25H27F2N3O4
Mol. Mass.:
471.4964
SMILES:
COc1ncccc1-c1ccc(\C=C\[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@]3(CC(N)=O)CC(F)(F)[C@H]2C)nc1 |r|
Structure:
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