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ChEMBL ligand: CHEMBL417149 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466] | ||||||||
ChEMBL | Amidolytic activity of THP.1 cell lysate against IL-1 beta converting enzyme using C1-Asp-AMC as a substrate | B | 4.15 | pIC50 | 70000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1477-1482 [PMID:9873373] |
ChEMBL | Inhibitory activity against caspase-1 | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 805-808 [PMID:14741294] |
Caspase 3/Caspase-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2334] [GtoPdb: 1619] [UniProtKB: P42574] | ||||||||
ChEMBL | Inhibition of recombinant human caspase-3 activity using Ac-DEVD-AMC as substrate preincubated for 10 mins by fluorescence assay | B | 7.12 | pIC50 | 75.7 | nM | IC50 | Bioorg Med Chem (2014) 22: 6735-6745 [PMID:25468037] |
ChEMBL | Inhibitory concentration of compound against caspase-3 | B | 7.36 | pIC50 | 43.9 | nM | IC50 | J Med Chem (2004) 47: 2466-2474 [PMID:15115390] |
ChEMBL | Inhibitory concentration required against human Caspase-3 | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2137-2140 [PMID:12798321] |
ChEMBL | Inhibitory activity against caspase-3 | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 805-808 [PMID:14741294] |
ChEMBL | Inhibition of caspase3 | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2006) 49: 1613-1623 [PMID:16509578] |
ChEMBL | Inhibition of human recombinant caspase 3 assessed as accumulation of fluorogenic product by fluorometric assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2009) 52: 2188-2191 [PMID:19326941] |
ChEMBL | Inhibition of human caspase 3 by fluorometric assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2192-2197 [PMID:21441025] |
ChEMBL | Inhibition of His-tagged human recombinant caspase 3 expressed in Escherichia coli using acetyl-Asp-Glu-Val-Asp-7- amido-4-methylcoumarin (Ac-DEVD-AMC) as substrate by fluorimetric assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3195-3201 [PMID:27216999] |
ChEMBL | Inhibition of human recombinant caspase 3 assessed as fluorescent 7-amido-4-methylcoumarin release | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Eur J Med Chem (2010) 45: 3858-3863 [PMID:20541849] |
ChEMBL | Inhibition of recombinant human caspase-3 using Ac-LDEVD-AMC as substrate assessed as accumulation of 7-AMC incubated for 10 mins followed by substrate addition measured for 10 mins by fluorimetric analysis | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2013) 21: 2960-2967 [PMID:23632366] |
GtoPdb | - | - | 9.8 | pIC50 | 0.16 | nM | IC50 | Eur J Med Chem (2010) 45: 3858-63 [PMID:20541849] |
Caspase 7/Caspase-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3468] [GtoPdb: 1623] [UniProtKB: P55210] | ||||||||
ChEMBL | Inhibition of recombinant human caspase-7 activity using Ac-DEVD-AMC as substrate preincubated for 10 mins by fluorescence assay | B | 6.81 | pIC50 | 155.2 | nM | IC50 | Bioorg Med Chem (2014) 22: 6735-6745 [PMID:25468037] |
ChEMBL | Inhibitory activity against caspase-7 | B | 7.06 | pIC50 | 87 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 805-808 [PMID:14741294] |
ChEMBL | Inhibition of His-tagged human recombinant caspase 7 expressed in Escherichia coli using acetyl-Asp-Glu-Val-Asp-7- amido-4-methylcoumarin (Ac-DEVD-AMC) as substrate by fluorimetric assay | B | 7.22 | pIC50 | 60.4 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3195-3201 [PMID:27216999] |
ChEMBL | Inhibition of human recombinant caspase 7 assessed as fluorescent 7-amido-4-methylcoumarin release | B | 7.23 | pIC50 | 59.1 | nM | IC50 | Eur J Med Chem (2010) 45: 3858-3863 [PMID:20541849] |
ChEMBL | Inhibition of human recombinant caspase 7 assessed as accumulation of fluorogenic product by fluorometric assay | B | 8.53 | pIC50 | 2.95 | nM | IC50 | J Med Chem (2009) 52: 2188-2191 [PMID:19326941] |
ChEMBL | Inhibition of caspase 7 by fluorometric assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2192-2197 [PMID:21441025] |
Caspase 8/Caspase-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3776] [GtoPdb: 1624] [UniProtKB: Q14790] | ||||||||
ChEMBL | Inhibitory activity against caspase-8 | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 805-808 [PMID:14741294] |
ChEMBL data shown on this page come from version 32:
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]