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 |
|---|---|---|---|---|---|---|---|---|
| Amyloid-beta 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 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]
