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Target
Presenilin-1
Ligand
BDBM50577514
Substrate
n/a
Meas. Tech.
ChEMBL_2130375 (CHEMBL4839804)
EC50
10.0±n/a nM
Citation
 Bursavich, MG; Harrison, BA; Acharya, R; Costa, DE; Freeman, EA; Hrdlicka, LA; Jin, H; Kapadnis, S; Moffit, JS; Murphy, D; Nolan, SJ; Patzke, H; Tang, C; Van Voorhies, HE; Wen, M; Koenig, G; Blain, JF; Burnett, DA Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator. J Med Chem 64:14426-14447 (2021) [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:
BDBM50577514
Synonyms:
CHEMBL4868749
Type:
Small organic molecule
Emp. Form.:
C20H17ClF3N5O2
Mol. Mass.:
451.829
SMILES:
COc1nc(ccc1-n1cnc(C)c1)C1=NOCC(N1)c1ccc(c(Cl)c1)C(F)(F)F |t:16|
Structure:
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