Assay ID | Title | Year | Journal | Article |
AID497568 | Inhibition of BACE1 at 2 ug/ml by FRET assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease. |
AID44236 | Compound was tested for its inhibitory activity against human beta-Secretase (BACE) | 2003 | Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
| Human beta-secretase (BACE) and BACE inhibitors. |
AID739031 | Inhibition of BACE1 (unknown origin) expressed in baculovirus expression system using Rh-EVNLDAEFK-Quencher as substrate after 90 mins by FRET assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of β-secretase (BACE1). |
AID754474 | Inhibition of human BACE1 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
| Structure-based design of β-site APP cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease. |
AID241087 | Inhibitory concentration against human Membrane-associated aspartic protease 2 | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics. |
AID635810 | Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
AID1378349 | Inhibition of human BACE1 (1 to 460 residues) expressed in baculovirus expression system using Rh-EVNLDAEFK-quencher as substrate after 90 mins by FRET assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis. |
AID739030 | Inhibition of BACE1 in mouse Neuro2a cells expressing APP Swedish mutant assessed as inhibition of amyloid beta (1 to 40) production at 10 uM after 24 hrs by sandwich ELISA relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of β-secretase (BACE1). |
AID412435 | Inhibition of BACE1 at 2 ug/ml by FRET assay | 2008 | Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
| Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors. |
AID238396 | Binding affinity against Beta-secretase | 2004 | Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
| Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity. |
AID1360333 | Inhibition of recombinant human BACE1 (1 to 460 residues) expressed in baculovirus-infected insect cells using Rh-EVNLDAEFK-quencher as substrate measured after 90 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
AID629956 | Inhibition of BACE-1 | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors. |
AID392811 | Inhibition of human recombinant C-terminal histidine-tagged BACE1 expressed in baculovirus-infected insect cells by FRET assay | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase. |
AID44256 | Binding affinity towards Beta-secretase 1 expressed in HEK293 (Human Embryonic Kidney) cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
| Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR. |
AID469063 | Inhibition of BACE1 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening. |
AID1504221 | Inhibition of recombinant human BACE1 (1 to 460 residues) expressed in baculovirus infected insect cells using Rh-EVNLDAEFK-Quencher as substrate incubated under dark condition for 90 mins by FRET assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Multifunctional iminochromene-2H-carboxamide derivatives containing different aminomethylene triazole with BACE1 inhibitory, neuroprotective and metal chelating properties targeting Alzheimer's disease. |
AID238867 | Binding affinity for human brain memapsin 2 | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
| Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase). |
AID739028 | Cytotoxicity against mouse Neuro2a cells expressing APP Swedish mutant assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of β-secretase (BACE1). |
AID739027 | Cytotoxicity against mouse Neuro2a cells expressing APP Swedish mutant assessed as cell viability at 5 uM after 24 hrs by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of β-secretase (BACE1). |
AID318154 | Binding affinity to BACE1 by surface plasmon resonance method | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
| Tyramine fragment binding to BACE-1. |
AID635814 | Inhibition of BACE1 at 20 ug/mL by FRET assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
AID240496 | Inhibitory concentration against human Cathepsin D | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics. |
AID1233547 | Inhibition of pro-BACE1 (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Peptidomimetic β-Secretase Inhibitors Comprising a Sequence of Amyloid-β Peptide for Alzheimer's Disease. |
AID635811 | Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
AID635813 | Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
AID1486227 | Inhibition of human BACE1 using Rh-EVNLDAEFK-quencher as substrate measured after 60 mins by FRET assay | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
| Synthesis, docking study and neuroprotective effects of some novel pyrano[3,2-c]chromene derivatives bearing morpholine/phenylpiperazine moiety. |
AID1545066 | Inhibition of recombinant human BACE1 (1 to 460 residues) expressed in baculovirus-infected insect cells using Rh-EVNLDAEFK-quencher as substrate measured after 90 mins by FRET assay relative to control | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
| Design, synthesis, and biological evaluation of novel 4-oxobenzo[d]1,2,3-triazin-benzylpyridinum derivatives as potent anti-Alzheimer agents. |
AID1233548 | Inhibition of active BACE1 (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
| Peptidomimetic β-Secretase Inhibitors Comprising a Sequence of Amyloid-β Peptide for Alzheimer's Disease. |
AID44241 | Inhibitory activity against human brain beta-APP (amyloid precursor protein) cleaving enzyme Beta-secretase | 2003 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
| Design and synthesis of statine-containing BACE inhibitors. |
AID314082 | Binding affinity to recombinant memapsin 2 | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation. |
AID675251 | Inhibition of recombinant beta-secretase 1 | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potent β-secretase inhibitors. |
AID303947 | Inhibition of BACE1 | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
| Discovery of a novel warhead against beta-secretase through fragment-based lead generation. |
AID415235 | Inhibition of recombinant memapsin 2 | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease. |
AID668997 | Inhibition of human recombinant BACE1 ectodomain after 1 hr by fluorescence analysis | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
| Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides. |
AID438118 | Inhibition of human recombinant BACE1 by FRET assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors. |
AID739029 | Inhibition of BACE1 in mouse Neuro2a cells expressing APP Swedish mutant assessed as inhibition of amyloid beta (1 to 40) production at 5 uM after 24 hrs by sandwich ELISA relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of β-secretase (BACE1). |
AID761335 | Inhibition of BACE1 (unknown origin) by fluorescence spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Hydroxyethylamine-based inhibitors of BACE1: P₁-P₃ macrocyclization can improve potency, selectivity, and cell activity. |
AID438582 | Inhibition of human BACE1 by FRET | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors. |
AID42091 | Binding affinity for human brain memapsin 2 beta-Secretase (BACE) | 2003 | Journal of medicinal chemistry, May-22, Volume: 46, Issue:11
| Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method. |
AID392813 | Inhibition of AChE in rat cortex at 25 uM preincubated for 20 mins by Ellman method | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase. |
AID636691 | Inhibition of human recombinant BACE1 ectodomain (1 to 460 amino acids) assessed as inhibition of proteolytic cleavage of Rhodamine-EVNLDAEFK-Quencher substrate after 35 mins by FRET assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| On a possible neutral charge state for the catalytic dyad in β-secretase when bound to hydroxyethylene transition state analogue inhibitors. |
AID241737 | Inhibitory concentration against hamster memapsin 2 | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
| Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase). |
AID497567 | Inhibition of BACE1 at 20 ug/ml by FRET assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease. |
AID445876 | Inhibition of human BACE1 by FRET based peptide cleavage assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors. |
AID705007 | Inhibition of BACE1 | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Structure-based design of highly selective β-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure. |
AID1414174 | Inhibition of recombinant human BACE1 using Mca-S-E-VeN-L-D-AEF-R-K(Dnp)-R-R-NH2 as substrate after 60 mins by fluorescence assay | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | A phenotypic approach to the discovery of compounds that promote non-amyloidogenic processing of the amyloid precursor protein: Toward a new profile of indirect β-secretase inhibitors. |
AID418180 | Inhibition of BACE1 | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
| Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors. |
AID238793 | Binding affinity for hamster memapsin 2 | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
| Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase). |
AID1797486 | Enzyme Inhibition Measurements from Article 10.1021/ja058636j: \\Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.\\ | 2006 | Journal of the American Chemical Society, Apr-26, Volume: 128, Issue:16
| Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors. |
AID1797556 | Enzyme Inhibition Measurements from Article 10.1021/jm0101803: \\Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).\\ | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase). |
AID1797461 | Enzyme Inhibition Measurements from Article 10.1021/jm050142+: \\Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.\\ | 2005 | Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
| Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics. |
AID1801911 | AChE and BChE Inhibition Assay from Article 10.1016/j.bioorg.2016.06.001: \\Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.\\ | 2016 | Bioorganic chemistry, 08, Volume: 67 | Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2000 | Science (New York, N.Y.), Oct-06, Volume: 290, Issue:5489
| Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2000 | Science (New York, N.Y.), Oct-06, Volume: 290, Issue:5489
| Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |