Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL439753 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466] | ||||||||
ChEMBL | Inhibitory activity against caspase-1 | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
ChEMBL | Inhibitory activity against caspase 1 using Ac-YVAD-AMC substrate | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 7637-7647 [PMID:16302804] |
ChEMBL | Inhibition of human recombinant caspase 1 assessed as accumulation of 7-amino-4-methylcoumarin substrate | B | 5.3 | pEC50 | >5000 | nM | EC50 | J Med Chem (2008) 51: 8057-8067 [PMID:19049429] |
Caspase 2/Caspase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4884] [GtoPdb: 1618] [UniProtKB: P42575] | ||||||||
ChEMBL | Inhibitory activity against caspase-2 | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
Caspase 3/Caspase-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2334] [GtoPdb: 1619] [UniProtKB: P42574] | ||||||||
ChEMBL | Inhibitory activity against caspase-3 | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
ChEMBL | Inhibition of human recombinant caspase 3 assessed as accumulation of fluorogenic product by fluorometric assay | B | 7.84 | pIC50 | 14.5 | nM | IC50 | J Med Chem (2009) 52: 2188-2191 [PMID:19326941] |
ChEMBL | Inhibition of caspase3 | B | 7.91 | pIC50 | 12.3 | nM | IC50 | Bioorg Med Chem (2012) 20: 5410-5415 [PMID:22503362] |
ChEMBL | Inhibitory activity against caspase 3 using Ac-DEVD-AMC substrate | B | 7.91 | pIC50 | 12.2 | nM | IC50 | J Med Chem (2005) 48: 7637-7647 [PMID:16302804] |
ChEMBL | Inhibition of recombinant human caspase-3 | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
ChEMBL | Inhibition of staurosporine induced activation of caspase 3 activation in human Hela cells assessed as hydrolysis of Z-DEVD-R110 substrate by microplate fluorescence assay | B | 5.44 | pEC50 | 3670 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2192-2197 [PMID:21441025] |
ChEMBL | Inhibition of human recombinant caspase 3 assessed as accumulation of 7-amino-4-methylcoumarin substrate | B | 7.38 | pEC50 | 41.8 | nM | EC50 | J Med Chem (2008) 51: 8057-8067 [PMID:19049429] |
Caspase 4/Caspase-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2226] [GtoPdb: 1620] [UniProtKB: P49662] | ||||||||
ChEMBL | Inhibitory activity against caspase-4 | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
Caspase 6/Caspase-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308] [GtoPdb: 1622] [UniProtKB: P55212] | ||||||||
ChEMBL | Inhibitory activity against Caspase-6 | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
ChEMBL | Inhibitory activity against caspase 6 using Ac-VEID-AMC substrate | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2005) 48: 7637-7647 [PMID:16302804] |
ChEMBL | Inhibition of human recombinant caspase 6 assessed as accumulation of fluorogenic product by fluorometric assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2009) 52: 2188-2191 [PMID:19326941] |
ChEMBL | Inhibition of human recombinant caspase 6 assessed as accumulation of 7-amino-4-methylcoumarin substrate | B | 5.3 | pEC50 | >5000 | nM | EC50 | J Med Chem (2008) 51: 8057-8067 [PMID:19049429] |
Caspase 7/Caspase-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3468] [GtoPdb: 1623] [UniProtKB: P55210] | ||||||||
GtoPdb | - | - | 8.2 | pKi | 6 | nM | Ki | J Med Chem (2001) 44: 2015-26 [PMID:11384246] |
ChEMBL | Inhibitory activity against Caspase-7 | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
ChEMBL | Inhibitory activity against caspase 7 using Ac-DEVD-AMC substrate | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2005) 48: 7637-7647 [PMID:16302804] |
ChEMBL | Inhibition of human recombinant caspase 7 assessed as accumulation of 7-amino-4-methylcoumarin substrate | B | 7.53 | pEC50 | 29.4 | nM | EC50 | J Med Chem (2008) 51: 8057-8067 [PMID:19049429] |
Caspase 8/Caspase-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3776] [GtoPdb: 1624] [UniProtKB: Q14790] | ||||||||
ChEMBL | Inhibitory activity against Caspase-8 | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
ChEMBL | Inhibitory activity against caspase 8 using Ac-IETD-AMC substrate | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2005) 48: 7637-7647 [PMID:16302804] |
ChEMBL | Inhibition of human recombinant caspase 8 assessed as accumulation of 7-amino-4-methylcoumarin substrate | B | 5.3 | pEC50 | >5000 | nM | EC50 | J Med Chem (2008) 51: 8057-8067 [PMID:19049429] |
Caspase 9/Caspase-9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2273] [GtoPdb: 1625] [UniProtKB: P55211] | ||||||||
GtoPdb | - | - | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2001) 44: 2015-26 [PMID:11384246] |
ChEMBL | Inhibitory activity against Caspase-9 | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2001) 44: 2015-2026 [PMID:11384246] |
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]