ELND006 [Ligand Id: 7337] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2396778 |
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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 partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA | B | 8.18 | pIC50 | 6.6 | nM | IC50 | J Med Chem (2013) 56: 5261-5274 [PMID:23713656] |
| ChEMBL | Inhibition of gamma-secretase in human IMR32 cell membrane using Notch as substrate after 2 hrs by ELISA | B | 8.28 | pIC50 | 5.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 996-1000 [PMID:23312944] |
| ChEMBL | Inhibition of gamma-secretase in human IMR32 cell membrane using APP as substrate after 2 hrs by ELISA | B | 9.47 | pIC50 | 0.34 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 996-1000 [PMID:23312944] |
| ChEMBL | Inhibition of partially purified human gamma-secretase-mediated cleavage of MBP-APPc125Sw fusion protein measured after overnight incubation by ELISA | B | 9.47 | pIC50 | 0.34 | nM | IC50 | J Med Chem (2013) 56: 5261-5274 [PMID:23713656] |
| GtoPdb | A-beta release assay | - | 9.47 | pIC50 | 0.34 | nM | IC50 | J Med Chem (2013) 56: 5261-74 [PMID:23713656] |
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]
