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 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]
