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Target
Presenilin-1
Ligand
BDBM50498594
Substrate
n/a
Meas. Tech.
ChEMBL_1512248 (CHEMBL3611644)
IC50
150±n/a nM
Citation
 Fischer, C; Zultanski, SL; Zhou, H; Methot, JL; Shah, S; Hayashi, I; Hughes, BL; Moxham, CM; Bays, NW; Smotrov, N; Hill, AD; Pan, BS; Wu, Z; Moy, LY; Tanga, F; Kenific, C; Cruz, JC; Walker, D; Bouthillette, M; Nikov, GN; Deshmukh, SV; Jeliazkova-Mecheva, VV; Diaz, D; Michener, MS; Cook, JJ; Munoz, B; Shearman, MS Discovery of novel triazolobenzazepinones as ?-secretase modulators with central A?42 lowering in rodents and rhesus monkeys. Bioorg Med Chem Lett 25:3488-94 (2015) [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:
BDBM50498594
Synonyms:
CHEMBL3609625
Type:
Small organic molecule
Emp. Form.:
C25H24F2N6O2
Mol. Mass.:
478.4939
SMILES:
COc1cc(ccc1-n1cnc(C)c1)-c1cn(nn1)C1CCc2ccccc2N(CC(F)F)C1=O
Structure:
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