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Target
Presenilin-1
Ligand
BDBM50498592
Substrate
n/a
Meas. Tech.
ChEMBL_1512247 (CHEMBL3611643)
IC50
470±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:
BDBM50498592
Synonyms:
CHEMBL3609642
Type:
Small organic molecule
Emp. Form.:
C30H34N6O2
Mol. Mass.:
510.63
SMILES:
[H][C@@]12CCCC[C@@]1([H])N(Cc1ccccc1)C(=O)C(CC2)n1cc(nn1)-c1ccc(c(OC)c1)-n1cnc(C)c1 |r|
Structure:
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