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Target
Presenilin-1
Ligand
BDBM28922
Substrate
n/a
Meas. Tech.
ChEMBL_968577 (CHEMBL2401297)
IC50
1.6±n/a nM
Citation
 Ye, XM; Konradi, AW; Sun, M; Yuan, S; Aubele, DL; Dappen, M; Dressen, D; Garofalo, AW; Jagodzinski, JJ; Latimer, L; Probst, GD; Sham, HL; Wone, D; Xu, YZ; Ness, D; Brigham, E; Kwong, GT; Willtis, C; Tonn, G; Goldbach, E; Quinn, KP; Zhang, HH; Sauer, JM; Bova, M; Basi, GS Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious ?-secretase inhibitors. Bioorg Med Chem Lett 23:996-1000 (2013) [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:
BDBM28922
Synonyms:
(2S)-N-(5-chlorothiophen-2-yl)-4,4,4-trifluoro-1-hydroxy-3-(trifluoromethyl)butane-2-sulfonamido | Begacestat | GSI-953
Type:
Small organic molecule
Emp. Form.:
C9H8ClF6NO3S2
Mol. Mass.:
391.738
SMILES:
OC[C@@H](NS(=O)(=O)c1ccc(Cl)s1)C(C(F)(F)F)C(F)(F)F |r|
Structure:
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