Target
Presenilin-1
Ligand
BDBM50483774
Substrate
n/a
Meas. Tech.
ChEMBL_745115 (CHEMBL1772294)
IC50
19±n/a nM
Citation
 Brodney, MAAuperin, DDBecker, SLBronk, BSBrown, TMCoffman, KJFinley, JEHicks, CDKarmilowicz, MJLanz, TAListon, DLiu, XMartin, BANelson, RBNolan, CEOborski, CEParker, CPRichter, KEPozdnyakov, NSahagan, BGSchachter, JBSokolowski, SATate, BWood, DEWood, KMVan Deusen, JWZhang, L Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as ?-secretase inhibitors: discovery of PF-3084014. Bioorg Med Chem Lett 21:2637-40 (2011) [PubMed]  Article
Target
Name:
Presenilin-1
Synonyms:
3.4.23.- | AD3 | Gamma-Secretase Subunit Presenilin-1 | PS-1 | PS1 | PS1-CTF12 | PSEN1 | PSN1_HUMAN | PSNL1 | Presenilin-1 CTF subunit | Presenilin-1 CTF12 | Presenilin-1 NTF subunit | Protein S182
Type:
n/a
Mol. Mass.:
52657.13
Organism:
Homo sapiens (Human)
Description:
P49768
Residue:
467
Sequence:
MTELPAPLSYFQNAQMSEDNHLSNTVRSQNDNRERQEHNDRRSLGHPEPLSNGRPQGNSRQVVEQDEEEDEELTLKYGAKHVIMLFVPVTLCMVVVVATIKSVSFYTRKDGQLIYTPFTEDTETVGQRALHSILNAAIMISVIVVMTILLVVLYKYRCYKVIHAWLIISSLLLLFFFSFIYLGEVFKTYNVAVDYITVALLIWNFGVVGMISIHWKGPLRLQQAYLIMISALMALVFIKYLPEWTAWLILAVISVYDLVAVLCPKGPLRMLVETAQERNETLFPALIYSSTMVWLVNMAEGDPEAQRRVSKNSKYNAESTERESQDTVAENDDGGFSEEWEAQRDSHLGPHRSTPESRAAVQELSSSILAGEDPEERGVKLGLGDFIFYSVLVGKASATASGDWNTTIACFVAILIGLCLTLLLLAIFKKALPALPISITFGLVFYFATDYLVQPFMDQLAFHQFYI
  
Inhibitor
Name:
BDBM50483774
Synonyms:
CHEMBL1770909
Type:
Small organic molecule
Emp. Form.:
C26H38FN5O
Mol. Mass.:
455.6112
SMILES:
CCC[C@H](NC1CCc2cc(F)ccc2C1)C(=O)Nc1cn(cn1)C(C)(C)CN1CCCC1 |r|
Structure:
Search PDB for entries with ligand similarity: