SCH-900229 [Ligand Id: 8848] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2159511 (SCH-900229) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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-mediated amyloid beta40 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 844-849 [PMID:23265892] |
| ChEMBL | Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 850-853 [PMID:23265902] |
| ChEMBL | Inhibition of gamma secretase-mediated amyloid beta40 production in HEK293 cell membranes transfected with human APPSOW and APPLON mutant after 5 hrs by sandwich immunoassay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 844-849 [PMID:23265892] |
| ChEMBL | Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cell membrane co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-40 production | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 850-853 [PMID:23265902] |
| GtoPdb | Data range indicates inhibition of Aβ42 or Aβ40 production. | - | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2012) 3: 892-6 [PMID:24900404] |
| ChEMBL | Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells transfected with human APPSOW and APPLON after 5 hrs by sandwich immunoassay | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 844-849 [PMID:23265892] |
| ChEMBL | Inhibition of gamma-secretase (unknown origin) expressed in HEK293 cells co-expressing Awe-Lon mutant assessed as reduction of amyloid beta-42 production | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 850-853 [PMID:23265902] |
| presenilin 1/Presenilin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2473] [GtoPdb: 2402] [UniProtKB: P49768] | ||||||||
| ChEMBL | Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as notch cleavage | B | 7.34 | pIC50 | 46 | nM | IC50 | ACS Med Chem Lett (2012) 3: 892-896 [PMID:24900404] |
| ChEMBL | Inhibition of PS1 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-40 production | B | 8.4 | pIC50 | 4 | nM | IC50 | ACS Med Chem Lett (2012) 3: 892-896 [PMID:24900404] |
| ChEMBL | Inhibition of PS1 gamma-secretase assessed as reduction of amyloid beta-40 production by membrane based assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | ACS Med Chem Lett (2012) 3: 892-896 [PMID:24900404] |
| GtoPdb | Data range indicates inhibition of Aβ42 or Aβ40 production. | - | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2012) 3: 892-6 [PMID:24900404] |
| presenilin 2/Presenilin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3708] [GtoPdb: 2403] [UniProtKB: P49810] | ||||||||
| ChEMBL | Inhibition of PS2 gamma-secretase expressed in HEK cells harboring Awe-Lon gene assessed as reduction of amyloid beta-42 production | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2012) 3: 892-896 [PMID:24900404] |
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]
