RO5508887 [Ligand Id: 9821] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2347215 |
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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] | ||||||||
| GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | J Neurosci (2014) 34: 11621-30 [PMID:25164658] |
| ChEMBL | Inhibition of human BACE1 using MR121-labeled substrate incubated for 4 mins prior to substrate addition measured after 2 mins by spectrophotometric analysis | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2013) 56: 3980-3995 [PMID:23590342] |
| ChEMBL | Inhibition of human BACE1 in HEK293 cells transfected with wild type APP assessed as reduction of amyloid beta40 level after 18 to 20 hrs by AlphaLISA technique | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2013) 56: 3980-3995 [PMID:23590342] |
| beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
| GtoPdb | - | - | 7.4 | pIC50 | 40 | nM | IC50 | J Neurosci (2014) 34: 11621-30 [PMID:25164658] |
| ChEMBL | Inhibition of human BACE2 using MR121-labeled substrate incubated for 4 mins prior to substrate addition measured after 2 mins by spectrophotometric analysis | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2013) 56: 3980-3995 [PMID:23590342] |
| presenilin 1/presenilin 2/Gamma-secretase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094135] [GtoPdb: 2402, 2403] [UniProtKB: P49768, P49810, Q8WW43, Q92542, Q96BI3, Q9NZ42] | ||||||||
| ChEMBL | Inhibition of gamma-secretase (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2018) 148: 436-452 [PMID:29477076] |
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]
