Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | coagulation factor II (thrombin) | Starlite/ChEMBL | References |
Bos taurus | Trypsin I | Starlite/ChEMBL | References |
Homo sapiens | coagulation factor X | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Drosophila melanogaster | CG9733 gene product from transcript CG9733-RB | Trypsin I | 246 aa | 262 aa | 30.1 % |
Echinococcus granulosus | transmembrane protease serine 3 | Trypsin I | 246 aa | 233 aa | 33.5 % |
Echinococcus granulosus | glycoprotein Antigen 5 | Trypsin I | 246 aa | 299 aa | 23.4 % |
Schistosoma mansoni | aminopeptidase PILS (M01 family) | Trypsin I | 246 aa | 301 aa | 23.9 % |
Echinococcus multilocularis | glycoprotein Antigen 5 | Trypsin I | 246 aa | 299 aa | 21.7 % |
Drosophila melanogaster | CG30287 gene product from transcript CG30287-RA | Trypsin I | 246 aa | 259 aa | 26.6 % |
Drosophila melanogaster | CG18420 gene product from transcript CG18420-RA | Trypsin I | 246 aa | 243 aa | 28.8 % |
Schistosoma mansoni | cercarial elastase (S01 family) | Trypsin I | 246 aa | 241 aa | 27.0 % |
Drosophila melanogaster | Jonah 65Aiii | Trypsin I | 246 aa | 235 aa | 34.9 % |
Schistosoma mansoni | cercarial elastase (S01 family) | Trypsin I | 246 aa | 241 aa | 27.0 % |
Drosophila melanogaster | Jonah 66Ci | Trypsin I | 246 aa | 272 aa | 30.5 % |
Loa Loa (eye worm) | hypothetical protein | Trypsin I | 246 aa | 217 aa | 24.0 % |
Echinococcus multilocularis | Mastin | Trypsin I | 246 aa | 306 aa | 23.2 % |
Drosophila melanogaster | CG3916 gene product from transcript CG3916-RA | Trypsin I | 246 aa | 269 aa | 31.6 % |
Drosophila melanogaster | CG10405 gene product from transcript CG10405-RB | Trypsin I | 246 aa | 251 aa | 33.9 % |
Drosophila melanogaster | CG31267 gene product from transcript CG31267-RA | Trypsin I | 246 aa | 234 aa | 32.5 % |
Drosophila melanogaster | Spatzle-Processing Enzyme | Trypsin I | 246 aa | 272 aa | 31.6 % |
Onchocerca volvulus | Trypsin I | 246 aa | 266 aa | 22.2 % | |
Drosophila melanogaster | CG31220 gene product from transcript CG31220-RB | Trypsin I | 246 aa | 227 aa | 29.5 % |
Drosophila melanogaster | CG30323 gene product from transcript CG30323-RB | Trypsin I | 246 aa | 208 aa | 23.1 % |
Drosophila melanogaster | CG33458 gene product from transcript CG33458-RA | Trypsin I | 246 aa | 248 aa | 28.2 % |
Echinococcus granulosus | enteropeptidase | Trypsin I | 246 aa | 230 aa | 27.0 % |
Drosophila melanogaster | CG34436 gene product from transcript CG34436-RA | Trypsin I | 246 aa | 208 aa | 24.0 % |
Echinococcus multilocularis | enteropeptidase | Trypsin I | 246 aa | 230 aa | 27.0 % |
Drosophila melanogaster | CG5909 gene product from transcript CG5909-RA | Trypsin I | 246 aa | 261 aa | 28.0 % |
Drosophila melanogaster | CG9673 gene product from transcript CG9673-RB | Trypsin I | 246 aa | 260 aa | 27.7 % |
Brugia malayi | Trypsin family protein | Trypsin I | 246 aa | 270 aa | 23.3 % |
Drosophila melanogaster | Jonah 99Ci | Trypsin I | 246 aa | 237 aa | 32.9 % |
Drosophila melanogaster | Jonah 65Aii | Trypsin I | 246 aa | 265 aa | 34.3 % |
Neospora caninum | glycine cleavage T-protein domain containing protein, putative | Trypsin I | 246 aa | 203 aa | 21.7 % |
Drosophila melanogaster | CG11313 gene product from transcript CG11313-RC | Trypsin I | 246 aa | 223 aa | 31.8 % |
Onchocerca volvulus | Trypsin I | 246 aa | 247 aa | 21.1 % | |
Schistosoma japonicum | Enteropeptidase, putative | Trypsin I | 246 aa | 264 aa | 24.6 % |
Drosophila melanogaster | CG30083 gene product from transcript CG30083-RB | Trypsin I | 246 aa | 209 aa | 31.1 % |
Drosophila melanogaster | CG3505 gene product from transcript CG3505-RA | Trypsin I | 246 aa | 235 aa | 29.8 % |
Drosophila melanogaster | CG30288 gene product from transcript CG30288-RC | Trypsin I | 246 aa | 250 aa | 29.6 % |
Echinococcus granulosus | subfamily S1A unassigned peptidase S01 family | Trypsin I | 246 aa | 287 aa | 27.5 % |
Drosophila melanogaster | CG14990 gene product from transcript CG14990-RA | Trypsin I | 246 aa | 238 aa | 28.6 % |
Schistosoma japonicum | ko:K09637 transmembrane protease, serine 6, putative | Trypsin I | 246 aa | 242 aa | 30.6 % |
Schistosoma mansoni | cercarial elastase (S01 family) | Trypsin I | 246 aa | 234 aa | 26.9 % |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | Trypsin I | 246 aa | 304 aa | 24.0 % |
Echinococcus multilocularis | transmembrane protease serine 3 | Trypsin I | 246 aa | 233 aa | 33.9 % |
Drosophila melanogaster | CG31326 gene product from transcript CG31326-RA | Trypsin I | 246 aa | 249 aa | 24.5 % |
Schistosoma japonicum | ko:K01346 pancreatic elastase II [EC3.4.21.71], putative | Trypsin I | 246 aa | 305 aa | 23.9 % |
Drosophila melanogaster | CG13744 gene product from transcript CG13744-RA | Trypsin I | 246 aa | 249 aa | 31.3 % |
Drosophila melanogaster | CG33465 gene product from transcript CG33465-RC | Trypsin I | 246 aa | 235 aa | 25.1 % |
Drosophila melanogaster | CG32277 gene product from transcript CG32277-RA | Trypsin I | 246 aa | 267 aa | 29.2 % |
Echinococcus multilocularis | subfamily S1A unassigned peptidase (S01 family) | Trypsin I | 246 aa | 287 aa | 27.9 % |
Schistosoma japonicum | Cercarial protease precursor (EC 3.4.21.-) (Cercarial elastase), putative | Trypsin I | 246 aa | 207 aa | 24.6 % |
Echinococcus granulosus | Mastin | Trypsin I | 246 aa | 306 aa | 23.2 % |
Drosophila melanogaster | CG17239 gene product from transcript CG17239-RB | Trypsin I | 246 aa | 223 aa | 34.5 % |
Mycobacterium tuberculosis | Membrane-associated serine protease | Trypsin I | 246 aa | 203 aa | 20.7 % |
Drosophila melanogaster | CG18180 gene product from transcript CG18180-RA | Trypsin I | 246 aa | 233 aa | 30.0 % |
Drosophila melanogaster | CG4914 gene product from transcript CG4914-RA | Trypsin I | 246 aa | 246 aa | 38.2 % |
Onchocerca volvulus | Trypsin I | 246 aa | 210 aa | 21.0 % | |
Drosophila melanogaster | CG4815 gene product from transcript CG4815-RA | Trypsin I | 246 aa | 205 aa | 27.8 % |
Schistosoma japonicum | Transmembrane protease, serine 9, putative | Trypsin I | 246 aa | 250 aa | 23.6 % |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | Trypsin I | 246 aa | 262 aa | 34.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Leishmania major | ribonuclease H1, putative | 0.0654 | 0.2497 | 0.5 |
Echinococcus multilocularis | ribonuclease H1 | 0.0654 | 0.2497 | 1 |
Schistosoma mansoni | phosphoglucomutase | 0.0654 | 0.2497 | 0.2497 |
Treponema pallidum | ribonuclease H (rnhA) | 0.0654 | 0.2497 | 0.5 |
Trypanosoma brucei | ingi protein (ORF1) | 0.0709 | 0.2728 | 0.2728 |
Brugia malayi | Trypsin family protein | 0.012 | 0.0268 | 0.1074 |
Trypanosoma brucei | hypothetical protein, conserved | 0.0709 | 0.2728 | 0.2728 |
Onchocerca volvulus | 0.012 | 0.0268 | 0.1074 | |
Mycobacterium tuberculosis | Possible maturase | 0.0056 | 0 | 0.5 |
Brugia malayi | RNase H family protein | 0.0654 | 0.2497 | 1 |
Echinococcus granulosus | ribonuclease H1 | 0.0654 | 0.2497 | 1 |
Schistosoma mansoni | phosphoglucomutase | 0.0654 | 0.2497 | 0.2497 |
Onchocerca volvulus | Ribonuclease H1 homolog | 0.0654 | 0.2497 | 1 |
Trypanosoma brucei | RNA helicase, putative | 0.2451 | 1 | 1 |
Trypanosoma brucei | unspecified product | 0.0709 | 0.2728 | 0.2728 |
Trypanosoma cruzi | ribonuclease H1, putative | 0.0654 | 0.2497 | 1 |
Trypanosoma brucei | ingi protein (ORF1) | 0.0709 | 0.2728 | 0.2728 |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | 0.012 | 0.0268 | 0.0268 |
Loa Loa (eye worm) | hypothetical protein | 0.012 | 0.0268 | 0.5 |
Brugia malayi | RNase H family protein | 0.0654 | 0.2497 | 1 |
Giardia lamblia | Ribonuclease H | 0.0654 | 0.2497 | 1 |
Trichomonas vaginalis | ribonuclease H1, putative | 0.0654 | 0.2497 | 1 |
Schistosoma mansoni | phosphoglucomutase | 0.0654 | 0.2497 | 0.2497 |
Toxoplasma gondii | ribonuclease HI protein | 0.0654 | 0.2497 | 0.5 |
Trypanosoma brucei | retrotransposon hot spot protein 4 (RHS4), interrupted | 0.0709 | 0.2728 | 0.2728 |
Schistosoma mansoni | subfamily S1A unassigned peptidase (S01 family) | 0.012 | 0.0268 | 0.0268 |
Onchocerca volvulus | 0.0106 | 0.0212 | 0.085 | |
Loa Loa (eye worm) | hypothetical protein | 0.012 | 0.0268 | 0.5 |
Brugia malayi | RNase H family protein | 0.0654 | 0.2497 | 1 |
Trypanosoma brucei | ribonuclease H1 | 0.0654 | 0.2497 | 0.2497 |
Wolbachia endosymbiont of Brugia malayi | ribonuclease HI | 0.0654 | 0.2497 | 0.5 |
Trypanosoma cruzi | ribonuclease H1, putative | 0.0654 | 0.2497 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Ki (binding) | = 0.71 nM | Inhibitory potency was measured against human coagulation factor X | ChEMBL. | 9733480 |
Ki (binding) | = 0.71 nM | Inhibitory potency was measured against human coagulation factor X | ChEMBL. | 9733480 |
Ki (binding) | = 280 nM | Inhibitory potency was measured against human thrombin | ChEMBL. | 9733480 |
Ki (binding) | = 280 nM | Inhibitory potency was measured against human thrombin | ChEMBL. | 9733480 |
Ki (binding) | = 740 nM | Inhibitory potency was measured against bovine trypsin. | ChEMBL. | 9733480 |
Ki (binding) | = 740 nM | Inhibitory potency was measured against bovine trypsin. | ChEMBL. | 9733480 |
Plasma concentration (ADMET) | = 0.1 uM | Inhibitor plasma concentration was measured in dogs on 10 mg/kg oral dosing after 4 hr administration; microM | ChEMBL. | 9733480 |
Plasma concentration (ADMET) | = 0.2 uM | Inhibitor plasma concentration was measured in dogs on 10 mg/kg oral dosing after 2 hr administration; microM | ChEMBL. | 9733480 |
Plasma concentration (ADMET) | = 0.3 uM | Inhibitor plasma concentration was measured in dogs on 10 mg/kg oral dosing after 1 hr administration; microM | ChEMBL. | 9733480 |
PT extension (functional) | = 1400 nM | Prothrombin time concentration of the compound was determined to give a 2-fold extension activity against pooled lyophilized human plasma. | ChEMBL. | 9733480 |
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.