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 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]
