NB-360 [Ligand Id: 9822] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3261067 |
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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 | Inhibition of wild type APP751 (unknown origin) expressed in CHO cells | B | 7.01 | pIC50 | 98 | nM | IC50 | J Med Chem (2021) 64: 15262-15279 [PMID:34648711] |
| ChEMBL | Inhibition of wild type human APP expressed in CHO cells assessed as reduction in soluble APP beta level incubated for 24 hrs by immunoassay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
| ChEMBL | Inhibition of wild type human APP751 expressed in CHO cells incubated for 24 hrs by immunoassay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
| ChEMBL | Inhibition of wild type human APP expressed in CHO cells assessed as reduction in amyloid beta 40 secretion incubated for 24 hrs by immunoassay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
| ChEMBL | Inhibition of wild type human APP expressed in CHO cells assessed as reduction in amyloid beta 42 secretion incubated for 24 hrs by immunoassay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
| beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817] | ||||||||
| ChEMBL | Inhibition of recombinant human BACE1 extracellular domain expressed in baculovirus using fluorescence-quenched peptide substrate derived from APP sequence preincubated for 1 hr followed by substrate addition measured every 1 min for 5 to 30 mins by spectrofluorimetric analysis | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2033-2045 [PMID:24704031] |
| ChEMBL | Inhibition Assay: Recombinant BACE-1 (extracellular domain, expressed in baculovirus and purified using standard methods) at 0.1 to 10 nM concentrations is incubated with the test compound at various concentrations for 1 hour at room temperature in 10 to 100 mM acetate buffer, pH 4.5, containing 0.1% CHAPS. Synthetic fluorescence-quenched peptide substrate, derived from the sequence of APP and containing a suitable fluorophore-quencher pair, is added to a final concentration of 1 to 5 μM, and the increase in fluorescence is recorded at a suitable excitation/emission wavelength in a microplate spectro-fluorimeter for 5 to 30 minutes in 1-minute intervals. | B | 8 | pIC50 | 10 | nM | IC50 | US-8846658-B2. Oxazine derivatives and their use in the treatment of neurological disorders (2014) |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Mol Neurodegener (2015) 10: 44 [PMID:26336937] |
| ChEMBL | Inhibition of human BACE1 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2018) 61: 4476-4504 [PMID:29613789] |
| ChEMBL | Inhibition of human recombinant BACE1 catalytic domain using FRET substrate with BACE-cleavable sequence | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 15262-15279 [PMID:34648711] |
| ChEMBL | Inhibition of human recombinant BACE1 catalytic domain using FRET substrate | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
| beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Mol Neurodegener (2015) 10: 44 [PMID:26336937] |
| ChEMBL | Inhibition of human recombinant BACE2 catalytic domain using FRET substrate with BACE-cleavable sequence | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 15262-15279 [PMID:34648711] |
| ChEMBL | Inhibition of human recombinant BACE2 catalytic domain using FRET substrate | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by patch clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2021) 64: 4677-4696 [PMID:33844524] |
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]
