Target family: A22: Presenilin (type: enzyme)
Target: presenilin 1

Ligand: avagacestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.5 pIC50
Reference (Webpage): DRUGS IN CLINICAL TRIALS: BMS-708163.

Ligand: ELND006 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.470000267028809 pIC50
Reference (Journal): Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Published in: J Med Chem

Ligand: CHF-5074 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 4.400000095367432 pEC50
Reference (Journal): Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach.
Published in: Bioorg Med Chem Lett

Ligand: begacestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.829999923706055 pEC50
Reference (Journal): Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Published in: J Pharmacol Exp Ther

Ligand: AZ4800 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.590000152587891 pIC50
Reference (Journal): First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms.
Published in: J Biol Chem

Ligand: SCH-900229 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Published in: ACS Med Chem Lett

Ligand: RO4929097 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties.
Published in: Cancer Res

Ligand: PF-06648671 (Synthetic organic)
Interaction type: Allosteric modulator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.010000228881836 pIC50
Reference (Journal): Discovery of Clinical Candidate PF-06648671: A Potent &#x3b3;-Secretase Modulator for the Treatment of Alzheimer's Disease.
Published in: J Med Chem

Ligand: semagacestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
Published in: J Med Chem