Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Adrenergic receptor alpha-2 | Starlite/ChEMBL | References |
Bos taurus | Alpha-2a adrenergic receptor | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Schistosoma japonicum | ko:K04145 dopamine receptor D2, putative | Adrenergic receptor alpha-2 | 450 aa | 473 aa | 24.1 % |
Echinococcus multilocularis | neuropeptides capa receptor | Adrenergic receptor alpha-2 | 450 aa | 486 aa | 20.6 % |
Schistosoma japonicum | ko:K04207 neuropeptide Y receptor Y5, putative | Alpha-2a adrenergic receptor | 452 aa | 381 aa | 21.8 % |
Echinococcus granulosus | alpha 1A adrenergic receptor | Alpha-2a adrenergic receptor | 452 aa | 456 aa | 21.1 % |
Onchocerca volvulus | Alpha-2a adrenergic receptor | 452 aa | 426 aa | 18.3 % | |
Echinococcus multilocularis | serotonin receptor | Alpha-2a adrenergic receptor | 452 aa | 421 aa | 33.0 % |
Schistosoma mansoni | amine GPCR | Alpha-2a adrenergic receptor | 452 aa | 440 aa | 29.1 % |
Onchocerca volvulus | Alpha-2a adrenergic receptor | 452 aa | 471 aa | 27.4 % | |
Schistosoma mansoni | biogenic amine (5HT) receptor | Adrenergic receptor alpha-2 | 450 aa | 433 aa | 27.9 % |
Echinococcus multilocularis | alpha 1A adrenergic receptor | Alpha-2a adrenergic receptor | 452 aa | 452 aa | 20.6 % |
Echinococcus multilocularis | fmrfamide receptor | Alpha-2a adrenergic receptor | 452 aa | 453 aa | 19.2 % |
Echinococcus multilocularis | fmrfamide receptor | Adrenergic receptor alpha-2 | 450 aa | 366 aa | 19.9 % |
Loa Loa (eye worm) | TYRA-2 protein | Alpha-2a adrenergic receptor | 452 aa | 491 aa | 24.4 % |
Echinococcus granulosus | biogenic amine 5HT receptor | Alpha-2a adrenergic receptor | 452 aa | 420 aa | 32.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | prolyl oligopeptidase (S09 family) | 0.0805 | 0.1543 | 0.1543 |
Echinococcus multilocularis | prolyl endopeptidase | 0.0805 | 0.1543 | 0.1543 |
Toxoplasma gondii | preprocathepsin c precursor, putative | 0.1333 | 0.3433 | 1 |
Trichomonas vaginalis | Clan CA, family C1, cathepsin B-like cysteine peptidase | 0.0828 | 0.1627 | 0.5 |
Mycobacterium tuberculosis | Probable protease II PtrBa [first part] (oligopeptidase B) | 0.0484 | 0.0393 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0856 | 0.1726 | 0.1561 |
Echinococcus granulosus | Dipeptidyl peptidase 9 | 0.1285 | 0.3264 | 0.3264 |
Plasmodium falciparum | dipeptidyl aminopeptidase 2 | 0.1333 | 0.3433 | 1 |
Echinococcus multilocularis | Dipeptidyl peptidase 9 | 0.1285 | 0.3264 | 0.3264 |
Toxoplasma gondii | prolyl endopeptidase | 0.0805 | 0.1543 | 0.36 |
Echinococcus granulosus | dipeptidyl aminopeptidaseprotein | 0.3165 | 1 | 1 |
Leishmania major | prolyl oligopeptidase, putative,serine peptidase clan SC, family S9A, putative | 0.0805 | 0.1543 | 0.4041 |
Onchocerca volvulus | Dipeptidyl peptidase family member 1 homolog | 0.3165 | 1 | 1 |
Toxoplasma gondii | cathepsin CPC1 | 0.1333 | 0.3433 | 1 |
Plasmodium vivax | dipeptidyl aminopeptidase 2, putative | 0.1333 | 0.3433 | 1 |
Trypanosoma cruzi | prolyl endopeptidase | 0.0805 | 0.1543 | 0.4041 |
Schistosoma mansoni | subfamily S9B unassigned peptidase (S09 family) | 0.3165 | 1 | 1 |
Giardia lamblia | Dipeptidyl-peptidase I precursor | 0.1333 | 0.3433 | 1 |
Toxoplasma gondii | dipeptidyl peptidase iv (dpp iv) n-terminal region domain-containing protein | 0.1177 | 0.2876 | 0.8114 |
Loa Loa (eye worm) | prolyl oligopeptidase | 0.3165 | 1 | 1 |
Mycobacterium ulcerans | protease II (oligopeptidase B), PtrB | 0.0479 | 0.0376 | 0.5 |
Echinococcus multilocularis | dipeptidyl aminopeptidaseprotein | 0.3165 | 1 | 1 |
Leishmania major | dipeptidyl-peptidase 8-like serine peptidase, putative,serine peptidase, Clan SC, Family S9B | 0.1285 | 0.3264 | 1 |
Plasmodium falciparum | dipeptidyl aminopeptidase 1 | 0.1333 | 0.3433 | 1 |
Brugia malayi | prolyl oligopeptidase family protein | 0.1285 | 0.3264 | 0.2035 |
Loa Loa (eye worm) | hypothetical protein | 0.0805 | 0.1543 | 0.1374 |
Mycobacterium leprae | PROBABLE PROTEASE II PTRBB (OLIGOPEPTIDASE B) | 0.0479 | 0.0376 | 0.5 |
Echinococcus granulosus | prolyl endopeptidase | 0.0805 | 0.1543 | 0.1543 |
Trypanosoma brucei | prolyl endopeptidase | 0.0805 | 0.1543 | 0.4041 |
Trypanosoma cruzi | serine peptidase, Clan SC, Family S9B | 0.1285 | 0.3264 | 1 |
Schistosoma mansoni | dipeptidyl-peptidase I (C01 family) | 0.1333 | 0.3433 | 0.3433 |
Schistosoma mansoni | dipeptidyl-peptidase 9 (S09 family) | 0.1285 | 0.3264 | 0.3264 |
Trypanosoma cruzi | dipeptidyl-peptidase 8-like serine peptidase | 0.1285 | 0.3264 | 1 |
Schistosoma mansoni | prolyl oligopeptidase (S09 family) | 0.0805 | 0.1543 | 0.1543 |
Plasmodium vivax | dipeptidyl aminopeptidase 1, putative | 0.1333 | 0.3433 | 1 |
Trypanosoma brucei | serine peptidase, Clan SC, Family S9B | 0.1285 | 0.3264 | 1 |
Trypanosoma brucei | Dipeptidyl-peptidase 8-like, putative | 0.1285 | 0.3264 | 1 |
Brugia malayi | hypothetical protein | 0.0856 | 0.1726 | 0.0217 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AD50 (functional) | > 3 mg kg-1 | Antagonistic activity against central alpha-2 adrenergic receptor, in anesthetized rats (reversal of clonidine-induced mydriasis) | ChEMBL. | 6139479 |
AD50 (functional) | > 3 mg kg-1 | Antagonistic activity against central alpha-2 adrenergic receptor, in anesthetized rats (reversal of clonidine-induced mydriasis) | ChEMBL. | 6139479 |
Kd (functional) | > 5.8 | Presynaptic antagonistic activity against alpha-2 adrenergic receptor from rat, isolated, field-stimulated vas deferens, using clonidine as the agonist | ChEMBL. | 6139479 |
Ki (binding) | = 440 nM | Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]-clonidine as the radioligand | ChEMBL. | 6139479 |
Ki (binding) | = 440 nM | Binding activity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]-clonidine as the radioligand | ChEMBL. | 6139479 |
Ki (binding) | = 31000 nM | Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand | ChEMBL. | 6139479 |
Ki (binding) | = 31000 nM | Binding activity against alpha-1 adrenergic receptor from calf cerebral cortex, using [3H]-prazosin as the radioligand | ChEMBL. | 6139479 |
pA2 (functional) | < 5.8 | Presynaptic antagonistic activity against alpha-2 adrenergic receptor from rat, isolated, field-stimulated vas deferens, using clonidine as the agonist | ChEMBL. | 6139479 |
Selectivity ratio (binding) | = 70 | Selectivity ratio of compound towards alpha2 adrenoceptor over alpha1 adrenoceptor of calf cerebral cortex | ChEMBL. | 6139479 |
Selectivity ratio (binding) | = 70 | Selectivity ratio of compound towards alpha2 adrenoceptor over alpha1 adrenoceptor of calf cerebral cortex | ChEMBL. | 6139479 |
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.