Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | proprotein convertase subtilisin/kexin type 7 | Starlite/ChEMBL | References |
Homo sapiens | proprotein convertase subtilisin/kexin type 6 | Starlite/ChEMBL | References |
Homo sapiens | proprotein convertase subtilisin/kexin type 2 | Starlite/ChEMBL | References |
Homo sapiens | furin (paired basic amino acid cleaving enzyme) | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | endoprotease bli-4 precursor | proprotein convertase subtilisin/kexin type 2 | 619 aa | 600 aa | 43.3 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | furin-1 (S08 family) | 0.0282 | 0.2978 | 0.2492 |
Echinococcus multilocularis | 0.0458 | 0.7071 | 1 | |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0329 | 0.406 | 1 |
Echinococcus multilocularis | neuroendocrine convertase 2 | 0.0437 | 0.6587 | 0.9247 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0182 | 0.0647 | 0.1594 |
Echinococcus granulosus | neuroendocrine convertase 2 | 0.0437 | 0.6587 | 0.6351 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0182 | 0.0647 | 0.1594 |
Brugia malayi | celfurPC protein | 0.0458 | 0.7071 | 0.2842 |
Echinococcus granulosus | proprotein convertase subtilisin:kexin type 5 | 0.0329 | 0.406 | 0.3649 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0182 | 0.0647 | 0.1594 |
Loa Loa (eye worm) | hypothetical protein | 0.0284 | 0.3011 | 0.2527 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0182 | 0.0647 | 0.1594 |
Giardia lamblia | High cysteine membrane protein Group 2 | 0.0175 | 0.0484 | 1 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0182 | 0.0647 | 0.1594 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0182 | 0.0647 | 0.1594 |
Brugia malayi | proprotein convertase 2 | 0.0437 | 0.6587 | 0.1661 |
Echinococcus multilocularis | proprotein convertase subtilisin:kexin type 5 | 0.0329 | 0.406 | 0.5313 |
Trichomonas vaginalis | Clan SB, family S8, subtilisin-like serine peptidase | 0.0329 | 0.406 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 200 uM | Cytotoxicity against human PC3 cells after 72 hrs by MTT assay | ChEMBL. | 24350995 |
Ki (binding) | = 1.7 nM | Inhibition of human PC2 expressed in drosophila schneider 2 cells using pyroGlu-Arg-Thr-Lys-Arg-AMC as substrate after 1 hr | ChEMBL. | 24350995 |
Ki (binding) | = 5.3 nM | Inhibition of human recombinant PACE4 expressed in drosophila schneider 2 cells using pyroGlu-Arg-Thr-Lys-Arg-AMC as substrate after 1 hr | ChEMBL. | 24350995 |
Ki (binding) | = 27 nM | Inhibition of human recombinant furin expressed in drosophila schneider 2 cells using pyroGlu-Arg-Thr-Lys-Arg-AMC as substrate after 1 hr | ChEMBL. | 24350995 |
Ki (binding) | = 72 nM | Inhibition of human PC7 expressed in drosophila schneider 2 cells using pyroGlu-Arg-Thr-Lys-Arg-AMC as substrate after 1 hr | ChEMBL. | 24350995 |
T1/2 (ADMET) | = 7.2 hr | Half life in CD-1 mouse plasma at 0.5 ug/uL by RP-HPLC analysis | ChEMBL. | 24350995 |
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.