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ChEMBL ligand: CHEMBL4452566 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817] | ||||||||
GtoPdb | Inhibition of BACE1 enzyme activity in a biochemical assay. | - | 6.21 | pIC50 | 615 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
ChEMBL | Inhibition of human BACE1 (1 to 460 residues) expressed in HEK293 cells after 16 to 24 hrs by FRET assay | B | 9.21 | pIC50 | 0.61 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 761-777 [PMID:30709653] |
ChEMBL | Inhibition of recombinant human BACE1 using (MCA)-S-E-V-N-L-D-A-E-F-R-K(dinitrophenol)-R-R-R-R-NH2 as substrate incubated for 8 hrs by FRET assay | B | 9.21 | pIC50 | 0.61 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
beta-secretase 1/Beta-secretase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4593] [GtoPdb: 2330] [UniProtKB: P56818] | ||||||||
ChEMBL | Inhibition of BACE1 in mouse primary cortical neuron assessed as reduction in Amyloid-beta level incubated for 24 hrs by sandwich ELISA assay | B | 9.56 | pIC50 | 0.28 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
ChEMBL | Inhibition of recombinant human BACE2 using (MCA)-S-E-V-N-L-D-A-E-F-R-K(dinitrophenol)-R-R-R-R-NH2 as substrate by FRET assay | B | 9.06 | pIC50 | 0.87 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2021) 64: 8076-8100 [PMID:34081466] |
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]