Target family: A1: Pepsin (type: enzyme)
Target: beta-secretase 1

Ligand: AM-6494 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Published in: J Med Chem

Ligand: AM-6494 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.4399995803833 pIC50
Reference (Journal): Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Published in: J Med Chem

Ligand: AM-6494 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.210000038146973 pIC50
Reference (Journal): Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Published in: J Med Chem

Ligand: AMG-8718 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).
Published in: J Med Chem

Ligand: atabecestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.010000228881836 pIC50
Reference (Webpage): Discovery and synthesis of JNJ-​54861911, a novel orally active BACE1 inhibitor

Ligand: atabecestat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Discovery of Extremely Selective Fused Pyridine-Derived β-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Published in: J Med Chem

Ligand: AZ3971 (Synthetic organic)
Interaction type: Inhibitor
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 7.519999980926514 pIC50
Reference (Patent): 5h-pyrrolo[3,4- gbp >]pyrazin-7-amine derivatives inhibitors of beta-secretase.

Ligand: AZ-4217 (Synthetic organic)
Interaction type: Inhibitor
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 8.739999771118164 pKi
Reference (Journal): AZ-4217: a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice.
Published in: J Neurosci

Ligand: AZD3839 (Synthetic organic)
Interaction type: Inhibitor
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 7.579999923706055 pKi
Reference (Journal): Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease.
Published in: J Biol Chem

Ligand: β-secretase inhibitor IV (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.630000114440918 pKi
Reference (Journal): Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.
Published in: J Med Chem

Ligand: compound 11d [PMID: 23981898] (Synthetic organic)
Interaction type: Inhibitor
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.
Published in: Bioorg Med Chem Lett

Ligand: Compound 12 [PMID:28626832] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 3.299999952316284 pIC50
Reference (Journal): Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.
Published in: ACS Omega