LY2886721 [Ligand Id: 6475] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2396989 (Ly-2886721, Ly2886721, LY2886721) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817] | ||||||||
| ChEMBL | Inhibition of Fc domain of IgG1-fused human BACE1 (1 to 460) expressed in HEK293 cells preincubated for 10 mins followed by enzyme addition measured after 16 to 24 hrs by FRET assay | B | 7.69 | pIC50 | 20.3 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2033-2045 [PMID:24704031] |
| ChEMBL | Inhibition of human BACE1 (1 to 460 residues) expressed in HEK293 cells using mcaFRET peptide as substrate after 20 hrs by FRET assay | B | 7.69 | pIC50 | 20.3 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
| ChEMBL | Inhibition of human recombinant BACE1 by FRET assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5729-5731 [PMID:27816517] |
| GtoPdb | - | - | 7.7 | pIC50 | 20.3 | nM | IC50 | Alzheimers Dement (2012) 8: 95 |
| ChEMBL | Inhibition of BACE1 (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5729-5731 [PMID:27816517] |
| ChEMBL | Inhibition of recombinant human BACE1 using (MCA)-S-E-V-N-L-D-A-E-F-R-K(dinitrophenol)-R-R-R-R-NH2 as substrate incubated for 8 hrs by FRET assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
| beta-secretase 1/Beta-secretase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4593] [GtoPdb: 2330] [UniProtKB: P56818] | ||||||||
| ChEMBL | Inhibition of BACE1 in mouse primary cortical neuron assessed as reduction in Amyloid-beta level incubated for 24 hrs by sandwich ELISA assay | B | 7.97 | pIC50 | 10.7 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
| beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
| ChEMBL | Inhibition of human BACE2 | B | 7.99 | pIC50 | 10.2 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
