LY2811376 [Ligand Id: 6936] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2333941 (J3.079.793K, Ly-2811376, Ly2811376, LY2811376) |
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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 human BACE1 using MOCA-SEV-NL-DAEFR-DNP-RR as substrate measured after 2 hrs by FRET assay | B | 6.21 | pIC50 | 620 | nM | IC50 | J Nat Prod (2018) 81: 1937-1945 [PMID:30207465] |
| ChEMBL | Inhibition of BACE-1 in HEK293 cells expressing human APP751 cDNA harboring N670L671 mutation pretreated for 2 hrs followed by measuring after 2 hrs by sandwich ELISA | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2018) 61: 619-637 [PMID:28749667] |
| ChEMBL | Inhibition of human recombinant BACE1 using MBP-C125Swe as substrate | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5729-5731 [PMID:27816517] |
| ChEMBL | Inhibition of BACE1 (unknown origin) | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 761-777 [PMID:30709653] |
| ChEMBL | Inhibition of BACE1 in human H4 cells expressing APP751 Swedish mutant assessed as inhibition of amyloid beta 40 or amyloid beta 42 production incubated for 19 hrs by microplate reader analysis | B | 6.57 | pIC50 | 270 | nM | IC50 | ACS Med Chem Lett (2016) 7: 271-276 [PMID:26985314] |
| ChEMBL | Inhibition of 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 | B | 6.57 | pIC50 | 269.3 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126772-126772 [PMID:31711785] |
| ChEMBL | Inhibition of human BACE-1 | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2018) 61: 619-637 [PMID:28749667] |
| ChEMBL | Inhibition of recombinant human BACE1 by 7-methoxycoumarin-4-yl-acetyl-based FRET assay | B | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2033-2045 [PMID:24704031] |
| ChEMBL | Inhibition of IgG1 Fc-fused human recombinant BACE1 (1 to 460 residues) expressed in HEK293 cells using methylcoumarin peptide harboring Swedish mutant as substrate incubated for 20 hrs by FRET assay | B | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2016) 7: 271-276 [PMID:26985314] |
| GtoPdb | - | - | 6.62 | pIC50 | 239 | nM | IC50 | J Neurosci (2011) 31: 16507-16 [PMID:22090477] |
| 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 | 6.62 | pIC50 | 239 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
| ChEMBL | Inhibition of human BACE1 | B | 6.62 | pIC50 | 239 | nM | IC50 | J Med Chem (2018) 61: 4476-4504 [PMID:29613789] |
| 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 | 6.62 | pIC50 | 239 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
| ChEMBL | Inhibition of BACE 1 (unknown origin) using 250 nM of Rh-EVNLDAEFK-Quencher as substrate after 1 hr by FRET assay | B | 6.76 | pIC50 | 173 | nM | IC50 | Bioorg Med Chem (2018) 26: 4823-4840 [PMID:30181028] |
| ChEMBL | Inhibition of BACE1 in HEK293 cells expressing APPswedish mutant assessed as inhibition of amyloid beta production by ELISA | B | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2033-2045 [PMID:24704031] |
| 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 | 6.9 | pIC50 | 126 | 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 | 6.54 | pIC50 | 288 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
| cathepsin D/Cathepsin D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2581] [GtoPdb: 2345] [UniProtKB: P07339] | ||||||||
| ChEMBL | Inhibition of human cathepsin D | B | 4.8 | pIC50 | 15700 | nM | IC50 | Bioorg Med Chem (2020) 28: 115194-115194 [PMID:31786008] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
