CHF-5074 [Ligand Id: 7339] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL196945
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Beta amyloid A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
ChEMBL Inhibitory concentration against beta-amyloid-42 (Abeta42) secretion was evaluated in human neuroglioma cells (H4-APP695NL) F 4.39 pIC50 41000 nM IC50 J Med Chem (2005) 48: 5705-5720 [PMID:16134939]
ChEMBL Concentration required to inhibit A beta 40 peptide 100 uM B 4.85 pIC50 14000 nM IC50 J Med Chem (2005) 48: 5705-5720 [PMID:16134939]
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 4.4 pIC50 40000 nM IC50 Eur J Med Chem (2018) 148: 436-452 [PMID:29477076]
GtoPdb - - 4.4 pEC50 40000 nM EC50 Bioorg Med Chem Lett (2011) 21: 7277-80 [PMID:22061640]

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]