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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] |
ChEMBL | Inhibition of caspase-1 (unknown origin) | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
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 caspase-3 (unknown origin) | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of caspase3 | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2006) 49: 1613-1623 [PMID:16509578] |
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 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 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 | Inhibition of caspase-7 (unknown origin) | B | 7.06 | pIC50 | 87 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
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 | Inhibition of caspase-8 (unknown origin) | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
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]