Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | caspase 3, apoptosis-related cysteine peptidase | Starlite/ChEMBL | References |
Homo sapiens | caspase 6, apoptosis-related cysteine peptidase | Starlite/ChEMBL | No references |
Homo sapiens | caspase 1, apoptosis-related cysteine peptidase | Starlite/ChEMBL | References |
Homo sapiens | caspase 8, apoptosis-related cysteine peptidase | Starlite/ChEMBL | No references |
Homo sapiens | caspase 7, apoptosis-related cysteine peptidase | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | caspase 8 | caspase 1, apoptosis-related cysteine peptidase | 383 aa | 312 aa | 26.6 % |
Brugia malayi | Cell death protein 3 precursor | caspase 3, apoptosis-related cysteine peptidase | 277 aa | 253 aa | 38.7 % |
Brugia malayi | Cell death protein 3 precursor | caspase 7, apoptosis-related cysteine peptidase | 303 aa | 256 aa | 37.1 % |
Brugia malayi | Cell death protein 3 precursor | caspase 6, apoptosis-related cysteine peptidase | 293 aa | 270 aa | 34.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | ERG2 and Sigma1 receptor like protein | 0.1121 | 0.5492 | 0.5492 |
Schistosoma mansoni | vesicular acetylcholine transporter | 0.1886 | 1 | 1 |
Onchocerca volvulus | Vesicular acetylcholine transporter homolog | 0.1886 | 1 | 1 |
Trypanosoma cruzi | C-8 sterol isomerase, putative | 0.1121 | 0.5492 | 0.5 |
Schistosoma mansoni | caspase-7 (C14 family) | 0.0315 | 0.0741 | 0.0741 |
Echinococcus granulosus | caspase | 0.0315 | 0.0741 | 0.0741 |
Echinococcus multilocularis | vesicular acetylcholine transporter | 0.1886 | 1 | 1 |
Loa Loa (eye worm) | vesicular acetylcholine transporter unc-17 | 0.1886 | 1 | 1 |
Trypanosoma brucei | C-8 sterol isomerase, putative | 0.1121 | 0.5492 | 0.5 |
Leishmania major | C-8 sterol isomerase-like protein | 0.1121 | 0.5492 | 0.5 |
Schistosoma mansoni | caspase-3 (C14 family) | 0.0315 | 0.0741 | 0.0741 |
Echinococcus multilocularis | caspase 3, apoptosis cysteine peptidase | 0.0315 | 0.0741 | 0.0741 |
Loa Loa (eye worm) | hypothetical protein | 0.1121 | 0.5492 | 0.5492 |
Loa Loa (eye worm) | hypothetical protein | 0.0573 | 0.2264 | 0.2264 |
Echinococcus multilocularis | caspase | 0.0315 | 0.0741 | 0.0741 |
Echinococcus granulosus | caspase 3 apoptosis cysteine peptidase | 0.0315 | 0.0741 | 0.0741 |
Echinococcus granulosus | vesicular acetylcholine transporter | 0.1886 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | 0 | Inhibition of caspase 3 processing in apoptotic HUVEC at 10 uM | ChEMBL. | 17154501 |
Activity (functional) | 0 | Inhibition of caspase 8 processing in apoptotic HUVEC at 50 uM | ChEMBL. | 17154501 |
Activity (functional) | 0 | Inhibition of caspase 8 processing in apoptotic HUVEC at 100 uM | ChEMBL. | 17154501 |
Activity (functional) | 0 | Inhibition of caspase 9 processing in apoptotic HUVEC at 50 uM | ChEMBL. | 17154501 |
Activity (functional) | 0 | Inhibition of caspase 9 processing in apoptotic HUVEC at 100 uM | ChEMBL. | 17154501 |
Activity (functional) | 0 | Inhibition of PARP cleavage in apoptotic HUVEC at 50 uM | ChEMBL. | 17154501 |
Activity (functional) | 0 | Inhibition of lamin A/C cleavage in apoptotic HUVEC at 50 uM | ChEMBL. | 17154501 |
IC50 (binding) | = 4 nM | Inhibition of caspase 7 | ChEMBL. | 17154501 |
IC50 (binding) | = 4 nM | Inhibition of caspase 7 | ChEMBL. | 17154501 |
IC50 (binding) | = 6.1 nM | Inhibition of recombinant human caspase-7 expressed in Escherichia coli using Ac-DEVD-AMC as substrate preincubated for 30 mins before substrate addition measured after 2 hrs | ChEMBL. | No reference |
IC50 (binding) | = 17.6 nM | Inhibition of recombinant human caspase-3 expressed in Escherichia coli using Ac-DEVD-AMC as substrate preincubated for 30 mins before substrate addition measured after 2 hrs | ChEMBL. | No reference |
IC50 (binding) | = 18.4 nM | Inhibition of caspase 3 | ChEMBL. | 17154501 |
IC50 (binding) | = 18.4 nM | Inhibition of caspase 3 | ChEMBL. | 17154501 |
IC50 (binding) | > 10000 nM | Inhibition of caspase 1 | ChEMBL. | 17154501 |
IC50 (binding) | > 10000 nM | Inhibition of caspase 1 | ChEMBL. | 17154501 |
IC50 (binding) | > 10000 nM | Inhibition of recombinant human caspase-8 expressed in Escherichia coli using Ac-IETD-AMC as substrate preincubated for 30 mins before substrate addition measured after 2 hrs | ChEMBL. | No reference |
IC50 (binding) | > 10000 nM | Inhibition of recombinant human caspase-6 expressed in Escherichia coli using Ac-VEID-AMC as substrate preincubated for 30 mins before substrate addition measured after 2 hrs | ChEMBL. | No reference |
IC50 (binding) | > 10000 nM | Inhibition of recombinant human caspase-1 expressed in Escherichia coli using Ac-YVAD-AMC as substrate preincubated for 30 mins before substrate addition measured after 2 hrs | ChEMBL. | No reference |
IC50 (binding) | > 500000 nM | Inhibition of caspase 6 | ChEMBL. | 17154501 |
IC50 (binding) | > 500000 nM | Inhibition of caspase 8 | ChEMBL. | 17154501 |
IC50 (binding) | > 500000 nM | Inhibition of caspase 6 | ChEMBL. | 17154501 |
IC50 (binding) | > 500000 nM | Inhibition of caspase 8 | ChEMBL. | 17154501 |
Ki (binding) | = 9 nM | Binding affinity to human caspase 3 | ChEMBL. | 17154501 |
Ki (binding) | = 9 nM | Binding affinity to human caspase 3 | ChEMBL. | 17154501 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.