AZ-4217 [Ligand Id: 6939] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2152903 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817] | ||||||||
| GtoPdb | - | - | 8.74 | pKi | 1.8 | nM | Ki | J Neurosci (2013) 33: 10075-84 [PMID:23761903] |
| ChEMBL | Inhibition of human recombinant BACE1 using (europium)CEVNLDAEFK(Qsy7) as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by TR-FRET assay | B | 8.61 | pIC50 | 2.44 | nM | IC50 | J Med Chem (2012) 55: 9346-9361 [PMID:22924815] |
| ChEMBL | Inhibition of BACE1 by diluted TR-FRET assay | B | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2012) 3: 869-870 [PMID:24900394] |
| ChEMBL | Inhibition of BACE1 by secreted AAPbeta release assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | ACS Med Chem Lett (2012) 3: 869-870 [PMID:24900394] |
| ChEMBL | Inhibition of BACE1 in human SH-SY5Y cells assessed as inhibition of sAPPbeta release after 16 hrs by immunoassay | B | 9.8 | pIC50 | 0.16 | nM | IC50 | J Med Chem (2012) 55: 9346-9361 [PMID:22924815] |
| beta-secretase 1/Beta-secretase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4593] [GtoPdb: 2330] [UniProtKB: P56818] | ||||||||
| ChEMBL | Inhibition of BACE1-mediated amyloid beta 40 release in C57/BL6 mouse primary cortical neurons after overnight incubation by ELISA | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (2012) 55: 9346-9361 [PMID:22924815] |
| beta-secretase 2/Beta secretase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2525] [GtoPdb: 2331] [UniProtKB: Q9Y5Z0] | ||||||||
| ChEMBL | Inhibition of human recombinant BACE2 using (europium)CEVNLDAEFK(Qsy7) as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by TR-FRET assay | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2012) 55: 9346-9361 [PMID:22924815] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells by IonWorks assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2012) 55: 9346-9361 [PMID:22924815] |
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]
