Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | matrix metallopeptidase 13 (collagenase 3) | Starlite/ChEMBL | References |
Homo sapiens | matrix metallopeptidase 9 (gelatinase B, 92kDa gelatinase, 92kDa type IV collagenase) | Starlite/ChEMBL | References |
Homo sapiens | ADAM metallopeptidase domain 17 | Starlite/ChEMBL | References |
Homo sapiens | matrix metallopeptidase 2 (gelatinase A, 72kDa gelatinase, 72kDa type IV collagenase) | Starlite/ChEMBL | References |
Sus scrofa | ADAM17 | Starlite/ChEMBL | References |
Homo sapiens | matrix metallopeptidase 1 (interstitial collagenase) | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus granulosus | adam 17 protease | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Echinococcus multilocularis | adam 17 protease | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Schistosoma japonicum | ko:K06059 a disintegrin and metalloproteinase domain 17, putative | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Schistosoma mansoni | ADAM17 peptidase (M12 family) | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Echinococcus multilocularis | Blood coagulation inhibitor, Disintegrin | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Echinococcus granulosus | Blood coagulation inhibitor Disintegrin | Get druggable targets OG5_132656 | All targets in OG5_132656 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Onchocerca volvulus | ADAM17 | 112 aa | 98 aa | 41.8 % | |
Trypanosoma congolense | hypothetical protein, conserved | ADAM17 | 112 aa | 100 aa | 29.0 % |
Brugia malayi | Matrixin family protein | matrix metallopeptidase 1 (interstitial collagenase) | 403 aa | 401 aa | 27.7 % |
Echinococcus granulosus | matrix metallopeptidase 7 M10 family | matrix metallopeptidase 13 (collagenase 3) | 471 aa | 448 aa | 34.1 % |
Onchocerca volvulus | Putative glutaminase 3 | ADAM17 | 112 aa | 105 aa | 45.7 % |
Plasmodium yoelii | A/G-specific adenine glycosylase, putative | ADAM17 | 112 aa | 109 aa | 24.8 % |
Echinococcus granulosus | disintegrin and metalloproteinase | ADAM17 | 112 aa | 99 aa | 42.4 % |
Echinococcus multilocularis | disintegrin and metalloproteinase | ADAM17 | 112 aa | 99 aa | 42.4 % |
Brugia malayi | Disintegrin family protein | ADAM metallopeptidase domain 17 | 824 aa | 724 aa | 27.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | fructose-1,6-bisphosphatase | 0.0491 | 0.5613 | 0.5803 |
Schistosoma mansoni | tyrosine kinase | 0.0413 | 0.452 | 0.4647 |
Echinococcus granulosus | fructose 16 bisphosphatase 1 | 0.0491 | 0.5613 | 0.5252 |
Trypanosoma cruzi | fructose-1,6-bisphosphatase, cytosolic, putative | 0.0491 | 0.5613 | 1 |
Schistosoma mansoni | matrix metallopeptidase-9 (M10 family) | 0.01 | 0.0109 | 0.0077 |
Echinococcus multilocularis | matrix metallopeptidase 7 (M10 family) | 0.0344 | 0.3551 | 0.3126 |
Onchocerca volvulus | 0.0134 | 0.0592 | 0.3568 | |
Brugia malayi | Matrixin family protein | 0.0229 | 0.1926 | 0.1968 |
Echinococcus multilocularis | 0.0241 | 0.2089 | 0.1488 | |
Brugia malayi | Furin-like cysteine rich region family protein | 0.0777 | 0.9648 | 1 |
Schistosoma mansoni | tyrosine kinase | 0.0413 | 0.452 | 0.4647 |
Echinococcus multilocularis | fructose 1,6 bisphosphatase 1 | 0.0491 | 0.5613 | 0.5436 |
Brugia malayi | Protein kinase domain containing protein | 0.0248 | 0.2199 | 0.2251 |
Echinococcus granulosus | lysosomal alpha glucosidase | 0.016 | 0.0947 | 0.0202 |
Loa Loa (eye worm) | hypothetical protein | 0.0115 | 0.0325 | 0.0302 |
Echinococcus multilocularis | epidermal growth factor receptor | 0.0777 | 0.9648 | 0.9956 |
Brugia malayi | Hemopexin family protein | 0.0134 | 0.0592 | 0.058 |
Loa Loa (eye worm) | matrixin family protein | 0.0229 | 0.1926 | 0.1968 |
Loa Loa (eye worm) | glycosyl hydrolase family 31 protein | 0.016 | 0.0947 | 0.095 |
Schistosoma mansoni | ADAM17 peptidase (M12 family) | 0.078 | 0.9687 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0146 | 0.0761 | 0.0755 |
Echinococcus granulosus | insulin growth factor 1 receptor beta | 0.0248 | 0.2199 | 0.1556 |
Echinococcus granulosus | matrix metallopeptidase 7 M10 family | 0.0344 | 0.3551 | 0.302 |
Schistosoma mansoni | fructose-16-bisphosphatase-related | 0.0491 | 0.5613 | 0.5779 |
Echinococcus multilocularis | a disintegrin and metalloproteinase with | 0.0368 | 0.3889 | 0.3504 |
Schistosoma mansoni | tyrosine kinase | 0.0248 | 0.2199 | 0.2242 |
Echinococcus multilocularis | lysosomal alpha glucosidase | 0.016 | 0.0947 | 0.0209 |
Echinococcus granulosus | epidermal growth factor receptor | 0.0418 | 0.4582 | 0.4136 |
Echinococcus multilocularis | lysosomal alpha glucosidase | 0.016 | 0.0947 | 0.0209 |
Schistosoma mansoni | tyrosine kinase | 0.0418 | 0.4582 | 0.4711 |
Loa Loa (eye worm) | matrixin family protein | 0.021 | 0.1659 | 0.169 |
Loa Loa (eye worm) | TK/INSR protein kinase | 0.0248 | 0.2199 | 0.2251 |
Brugia malayi | Glycosyl hydrolases family 31 protein | 0.016 | 0.0947 | 0.095 |
Echinococcus granulosus | Blood coagulation inhibitor Disintegrin | 0.0434 | 0.4812 | 0.4385 |
Schistosoma mansoni | alpha-glucosidase | 0.0137 | 0.0634 | 0.0622 |
Schistosoma mansoni | alpha-glucosidase | 0.0137 | 0.0634 | 0.0622 |
Schistosoma mansoni | ADAMTS5 peptidase (M12 family) | 0.0368 | 0.3889 | 0.3993 |
Echinococcus granulosus | insulin receptor | 0.0248 | 0.2199 | 0.1556 |
Schistosoma mansoni | tyrosine kinase | 0.0413 | 0.452 | 0.4647 |
Schistosoma mansoni | hypothetical protein | 0.0134 | 0.0592 | 0.0578 |
Mycobacterium tuberculosis | Probable peptidoglycan hydrolase | 0.0115 | 0.0325 | 0.5 |
Trypanosoma cruzi | fructose-1,6-bisphosphatase, cytosolic, putative | 0.0491 | 0.5613 | 1 |
Echinococcus granulosus | a disintegrin and metalloproteinase with | 0.0368 | 0.3889 | 0.3385 |
Brugia malayi | Matrix metalloprotease, N-terminal domain containing protein | 0.0115 | 0.0325 | 0.0302 |
Loa Loa (eye worm) | hypothetical protein | 0.0146 | 0.0761 | 0.0755 |
Onchocerca volvulus | Matrix metalloproteinase homolog | 0.021 | 0.1659 | 1 |
Loa Loa (eye worm) | fructose-1,6-bisphosphatase | 0.0491 | 0.5613 | 0.5803 |
Echinococcus multilocularis | insulin receptor | 0.0248 | 0.2199 | 0.1611 |
Echinococcus multilocularis | Blood coagulation inhibitor, Disintegrin | 0.0434 | 0.4812 | 0.4538 |
Brugia malayi | Muscleblind-like protein | 0.0146 | 0.0761 | 0.0755 |
Toxoplasma gondii | fructose-bisphospatase II | 0.0491 | 0.5613 | 1 |
Echinococcus granulosus | epidermal growth factor receptor | 0.0777 | 0.9648 | 0.9619 |
Loa Loa (eye worm) | hypothetical protein | 0.0763 | 0.9438 | 0.9782 |
Schistosoma mansoni | tyrosine kinase | 0.0777 | 0.9648 | 0.9959 |
Loa Loa (eye worm) | TK/EGFR protein kinase | 0.0777 | 0.9648 | 1 |
Echinococcus granulosus | melanoma receptor tyrosine protein kinase | 0.0418 | 0.4582 | 0.4136 |
Brugia malayi | metalloprotease disintegrin 16 with thrombospondin type I motif | 0.0368 | 0.3889 | 0.4009 |
Onchocerca volvulus | 0.0095 | 0.0034 | 0.0208 | |
Mycobacterium leprae | PROBABLE HYDROLASE | 0.0115 | 0.0325 | 0.5 |
Leishmania major | 0.0491 | 0.5613 | 0.5 | |
Onchocerca volvulus | Matrilysin homolog | 0.0095 | 0.0034 | 0.0208 |
Echinococcus multilocularis | epidermal growth factor receptor | 0.0418 | 0.4582 | 0.4281 |
Trypanosoma brucei | fructose-1,6-bisphosphatase | 0.0491 | 0.5613 | 1 |
Mycobacterium ulcerans | hydrolase | 0.0115 | 0.0325 | 0.5 |
Echinococcus multilocularis | insulin growth factor 1 receptor beta | 0.0248 | 0.2199 | 0.1611 |
Schistosoma mansoni | tyrosine kinase | 0.0248 | 0.2199 | 0.2242 |
Schistosoma mansoni | tyrosine kinase | 0.0418 | 0.4582 | 0.4711 |
Onchocerca volvulus | Matrilysin homolog | 0.021 | 0.1659 | 1 |
Echinococcus multilocularis | adam 17 protease | 0.078 | 0.9687 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Caco-2 Papp (functional) | = 0.0000001 cm s-1 | Permeability action of the compound in Caco-2 cells | ChEMBL. | 15357971 |
Caco-2 Papp (functional) | = 0.0000001 cm s-1 | Permeability action of the compound in Caco-2 cells | ChEMBL. | 15357971 |
IC50 (binding) | = 1.5 nM | Inhibition of porcine Tumor necrosis factor- alpha converting enzyme (TACE, ADAM17) | ChEMBL. | 15357971 |
IC50 (binding) | = 1.5 nM | Inhibition of porcine Tumor necrosis factor- alpha converting enzyme (TACE, ADAM17) | ChEMBL. | 15357971 |
IC50 (functional) | = 76 nM | Effect on TNF-Alpha release in LPS-stimulated human whole blood assay | ChEMBL. | 15357971 |
IC50 (functional) | = 76 nM | Effect on TNF-Alpha release in LPS-stimulated human whole blood assay | ChEMBL. | 15357971 |
Inhibition (functional) | = 34 % | Compound was tested for anti TNF-alpha activity using LPS mouse model at 5 mg/kg p.o. | ChEMBL. | 15357971 |
Inhibition (functional) | = 34 % | Compound was tested for anti TNF-alpha activity using LPS mouse model at 5 mg/kg p.o. | ChEMBL. | 15357971 |
Ki (binding) | > 2100 nM | Inhibition of Matrix metalloproteinase-9 (MMP-9) | ChEMBL. | 15357971 |
Ki (binding) | > 2100 nM | Inhibition of Matrix metalloproteinase-9 (MMP-9) | ChEMBL. | 15357971 |
Ki (binding) | = 3266 nM | Inhibition of Matrix metalloproteinase-13 (MMP-13) | ChEMBL. | 15357971 |
Ki (binding) | = 3266 nM | Inhibition of Matrix metalloproteinase-13 (MMP-13) | ChEMBL. | 15357971 |
Ki (binding) | > 3300 nM | inhibition of Matrix metalloproteinase-2 (MMP-2) | ChEMBL. | 15357971 |
Ki (binding) | > 3300 nM | inhibition of Matrix metalloproteinase-2 (MMP-2) | ChEMBL. | 15357971 |
Ki (binding) | > 4900 nM | Inhibition of Matrix metalloproteinase-1 (MMP-1) | ChEMBL. | 15357971 |
Ki (binding) | > 4900 nM | Inhibition of Matrix metalloproteinase-1 (MMP-1) | ChEMBL. | 15357971 |
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.