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Target
Presenilin-1
Ligand
BDBM50458159
Substrate
n/a
Meas. Tech.
ChEMBL_745116 (CHEMBL1772295)
IC50
1.2±n/a nM
Citation
 Brodney, MA; Auperin, DD; Becker, SL; Bronk, BS; Brown, TM; Coffman, KJ; Finley, JE; Hicks, CD; Karmilowicz, MJ; Lanz, TA; Liston, D; Liu, X; Martin, BA; Nelson, RB; Nolan, CE; Oborski, CE; Parker, CP; Richter, KE; Pozdnyakov, N; Sahagan, BG; Schachter, JB; Sokolowski, SA; Tate, B; Wood, DE; Wood, KM; Van Deusen, JW; Zhang, 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:
Human
Description:
P49768
Residue:
467
Sequence:
MTELPAPLSYFQNAQMSEDNHLSNTVRSQNDNRERQEHNDRRSLGHPEPLSNGRPQGNSRQVVEQDEEEDEELTLKYGAKHVIMLFVPVTLCMVVVVATIKSVSFYTRKDGQLIYTPFTEDTETVGQRALHSILNAAIMISVIVVMTILLVVLYKYRCYKVIHAWLIISSLLLLFFFSFIYLGEVFKTYNVAVDYITVALLIWNFGVVGMISIHWKGPLRLQQAYLIMISALMALVFIKYLPEWTAWLILAVISVYDLVAVLCPKGPLRMLVETAQERNETLFPALIYSSTMVWLVNMAEGDPEAQRRVSKNSKYNAESTERESQDTVAENDDGGFSEEWEAQRDSHLGPHRSTPESRAAVQELSSSILAGEDPEERGVKLGLGDFIFYSVLVGKASATASGDWNTTIACFVAILIGLCLTLLLLAIFKKALPALPISITFGLVFYFATDYLVQPFMDQLAFHQFYI
  
Inhibitor
Name:
BDBM50458159
Synonyms:
Nirogacestat | PF 03084014 | PF 3084014 | PF-03084014 | PF-3084014
Type:
Small organic molecule
Emp. Form.:
C27H41F2N5O
Mol. Mass.:
489.6441
SMILES:
CCC[C@H](N[C@H]1CCc2cc(F)cc(F)c2C1)C(=O)Nc1cn(cn1)C(C)(C)CNCC(C)(C)C |r|
Structure:
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