Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mus musculus | diacylglycerol lipase, beta | References | |
Homo sapiens | diacylglycerol lipase, alpha | References | |
Homo sapiens | abhydrolase domain containing 6 | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Plasmodium falciparum | epoxide hydrolase 1 | abhydrolase domain containing 6 | 337 aa | 275 aa | 21.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | lipase | 0.0518 | 1 | 0.5 |
Leishmania major | hypothetical protein, conserved | 0.0518 | 1 | 0.5 |
Mycobacterium tuberculosis | 4,9-DHSA hydrolase | 0.0499 | 0 | 0.5 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0518 | 1 | 0.5 |
Mycobacterium ulcerans | 2-hydroxy-6-oxo-6-phenylhexa-2,4-dienoate hydrolase BphD | 0.0507 | 0.4239 | 0.5 |
Trypanosoma brucei | lipase domain protein, putative | 0.0518 | 1 | 0.5 |
Onchocerca volvulus | 0.0518 | 1 | 0.5 | |
Echinococcus granulosus | sn1 specific diacylglycerol lipase beta | 0.0518 | 1 | 0.5 |
Trypanosoma brucei | lipase domain protein, putative | 0.0518 | 1 | 0.5 |
Trichomonas vaginalis | lipase containing protein, putative | 0.0518 | 1 | 0.5 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0518 | 1 | 0.5 |
Echinococcus multilocularis | sn1 specific diacylglycerol lipase beta | 0.0518 | 1 | 0.5 |
Trichomonas vaginalis | lipase containing protein, putative | 0.0518 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 5.6 | Inhibition of HT-01 probe binding to recombinant human DAGLalpha expressed in HEK293T cell membrane proteomes preincubated for 30 mins followed by HT-01 probe addition measured after 30 mins by gel-based competitive activity based protein profiling assay | LITERATURE. | 27992221 |
IC50 (binding) | = 6.9 | Inhibition of recombinant human DAGLalpha expressed in HEK293T cell membranes overexpressing MAGL using natural substrate 1-stearoyl-2-arachidonoly-sn-glycerol by fluorescence based assay | LITERATURE. | 27992221 |
IC50 (binding) | = 7.1 | Inhibition of recombinant mouse DAGLbeta expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay | LITERATURE. | 27992221 |
IC50 (binding) | = 7.4 | Inhibition of human ABHD6 using 2-AG as natural substrate by fluorescence based assay | LITERATURE. | 27992221 |
IC50 (binding) | = 7.4 | Inhibition of HT-01 probe binding to recombinant mouse DAGLbeta expressed in HEK293T cell membrane proteomes preincubated for 30 mins followed by HT-01 probe addition measured after 30 mins by gel-based competitive activity based protein profiling assay | LITERATURE. | 27992221 |
IC50 (binding) | = 8.2 | Inhibition of full length recombinant human DAGLalpha expressed in HEK293T cell membranes using PNP butyrate as substrate by colorimetric assay | LITERATURE. | 27992221 |
IC50 (functional) | 0.043 uM | PubChem BioAssay. Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based dose-response biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of DAGLb in vitro. (Class of assay: confirmatory) | ChEMBL. | No reference |
IC50 (functional) | 0.1 uM | PubChem BioAssay. Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based biochemical dose response assay. (Class of assay: confirmatory) | ChEMBL. | No reference |
IC50 (binding) | = 2.3 uM | Inhibition of HT-01 probe binding to recombinant human DAGLalpha expressed in HEK293T cell membrane proteomes preincubated for 30 mins followed by HT-01 probe addition measured after 30 mins by gel-based competitive activity based protein profiling assay | LITERATURE. | 27992221 |
Inhibition (binding) | Inhibition of DH379 probe binding to full length recombinant human DAGLalpha expressed in HEK293T cell membranes at 0 | LITERATURE. | 27992221 | |
Inhibition (binding) | Inhibition of DH379 probe binding to full length recombinant human DAGLbeta expressed in HEK293T cell membranes at 0 | LITERATURE. | 27992221 |
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.