Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | gamma-aminobutyric acid (GABA) A receptor, beta 3 | Starlite/ChEMBL | References |
Homo sapiens | gamma-aminobutyric acid (GABA) A receptor, alpha 2 | Starlite/ChEMBL | References |
Homo sapiens | gamma-aminobutyric acid (GABA) A receptor, gamma 2 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Brugia malayi | gamma-aminobutyric-acid receptor beta subunit precursor | Get druggable targets OG5_129441 | All targets in OG5_129441 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_129441 | All targets in OG5_129441 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_131775 | All targets in OG5_131775 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_129441 | All targets in OG5_129441 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | Neurotransmitter-gated ion-channel ligand binding domain containing protein | gamma-aminobutyric acid (GABA) A receptor, gamma 2 | 467 aa | 449 aa | 27.6 % |
Brugia malayi | Neurotransmitter-gated ion-channel ligand binding domain containing protein | gamma-aminobutyric acid (GABA) A receptor, alpha 2 | 451 aa | 393 aa | 25.9 % |
Brugia malayi | excitatory GABA receptor EXP-1A | gamma-aminobutyric acid (GABA) A receptor, beta 3 | 473 aa | 441 aa | 29.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | cyclin domain-containing protein | 0.0173 | 0.3407 | 0.3407 |
Loa Loa (eye worm) | hypothetical protein | 0.022 | 0.4705 | 0.4705 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0082 | 0.0961 | 0.3764 |
Echinococcus multilocularis | cyclin dependent kinase 1 | 0.0082 | 0.0961 | 0.0869 |
Plasmodium vivax | protein kinase Crk2 | 0.0082 | 0.0961 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0067 | 0.0548 | 0.078 |
Loa Loa (eye worm) | CMGC/CDK/CDK5 protein kinase | 0.0082 | 0.0961 | 0.0961 |
Leishmania major | CYC2-like cyclin, putative,cyclin 6, putative | 0.0114 | 0.1824 | 1 |
Brugia malayi | Cyclin, N-terminal domain containing protein | 0.0114 | 0.1824 | 0.2003 |
Brugia malayi | hypothetical protein | 0.0116 | 0.1872 | 0.2114 |
Echinococcus multilocularis | cyclin dependent kinase | 0.0082 | 0.0961 | 0.0869 |
Trichomonas vaginalis | cyclins, putative | 0.0114 | 0.1824 | 1 |
Trichomonas vaginalis | cyclins, putative | 0.0114 | 0.1824 | 1 |
Echinococcus multilocularis | cyclin dependent kinase 5 activator 1 | 0.0242 | 0.53 | 1 |
Brugia malayi | Cyclin, N-terminal domain containing protein | 0.0114 | 0.1824 | 0.2003 |
Plasmodium falciparum | protein kinase 5 | 0.0082 | 0.0961 | 1 |
Echinococcus granulosus | cyclin dependent kinase | 0.0082 | 0.0961 | 0.0869 |
Giardia lamblia | G2/mitotic-specific cyclin B | 0.0114 | 0.1824 | 1 |
Echinococcus granulosus | cyclin dependent kinase 5 activator 1 | 0.0242 | 0.53 | 1 |
Entamoeba histolytica | cyclin, putative | 0.0114 | 0.1824 | 1 |
Schistosoma mansoni | cyclin B3 | 0.0173 | 0.3407 | 0.6016 |
Trichomonas vaginalis | cyclins, putative | 0.0067 | 0.0548 | 0.078 |
Loa Loa (eye worm) | CMGC/CDK/CDC2 protein kinase | 0.0082 | 0.0961 | 0.0961 |
Trypanosoma cruzi | cyclin, putative | 0.0114 | 0.1824 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0116 | 0.1872 | 0.1872 |
Toxoplasma gondii | cell-cycle-associated protein kinase CDK, putative | 0.0082 | 0.0961 | 1 |
Trichomonas vaginalis | cyclin B3, putative | 0.0067 | 0.0548 | 0.078 |
Trichomonas vaginalis | cyclin B, putative | 0.0114 | 0.1824 | 1 |
Trichomonas vaginalis | cyclin A, putative | 0.0114 | 0.1824 | 1 |
Trichomonas vaginalis | cyclins, putative | 0.0114 | 0.1824 | 1 |
Schistosoma mansoni | cyclin-dependent kinase 5 activator | 0.0242 | 0.53 | 1 |
Brugia malayi | Cyclin, N-terminal domain containing protein | 0.0173 | 0.3407 | 0.5675 |
Trichomonas vaginalis | cyclin D, putative | 0.0067 | 0.0548 | 0.078 |
Trypanosoma cruzi | cyclin, putative | 0.0114 | 0.1824 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0114 | 0.1824 | 0.1824 |
Loa Loa (eye worm) | hypothetical protein | 0.0116 | 0.1872 | 0.1872 |
Giardia lamblia | Kinase, CMGC CDK | 0.0082 | 0.0961 | 0.3236 |
Trichomonas vaginalis | cyclin B, putative | 0.0114 | 0.1824 | 1 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0082 | 0.0961 | 0.3764 |
Entamoeba histolytica | cell division protein kinase 2, putative | 0.0082 | 0.0961 | 0.3236 |
Entamoeba histolytica | cell division protein kinase 2, putative | 0.0082 | 0.0961 | 0.3236 |
Echinococcus granulosus | G2:mitotic specific cyclin B3 | 0.0173 | 0.3407 | 0.6016 |
Echinococcus granulosus | 5'partial|cyclin dependent kinase 1 | 0.0082 | 0.0961 | 0.0869 |
Loa Loa (eye worm) | hypothetical protein | 0.0081 | 0.0918 | 0.0918 |
Loa Loa (eye worm) | hypothetical protein | 0.0114 | 0.1824 | 0.1824 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0082 | 0.0961 | 0.3764 |
Echinococcus granulosus | cyclin dependent kinase 5 | 0.0082 | 0.0961 | 0.0869 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0082 | 0.0961 | 0.0869 |
Brugia malayi | gamma-aminobutyric-acid receptor beta subunit precursor | 0.0241 | 0.527 | 1 |
Schistosoma mansoni | cyclin B | 0.0114 | 0.1824 | 0.2685 |
Loa Loa (eye worm) | hypothetical protein | 0.0241 | 0.527 | 0.527 |
Trichomonas vaginalis | cyclin B, putative | 0.0067 | 0.0548 | 0.078 |
Trichomonas vaginalis | cyclin B, putative | 0.0114 | 0.1824 | 1 |
Echinococcus multilocularis | G2:mitotic specific cyclin B3 | 0.0173 | 0.3407 | 0.6016 |
Loa Loa (eye worm) | hypothetical protein | 0.0242 | 0.53 | 0.53 |
Trypanosoma cruzi | cyclin 6, putative | 0.0114 | 0.1824 | 1 |
Trypanosoma brucei | mitotic cyclin 6 | 0.0114 | 0.1824 | 1 |
Trichomonas vaginalis | cyclin D, putative | 0.0067 | 0.0548 | 0.078 |
Loa Loa (eye worm) | CMGC/CDK/CDC2 protein kinase | 0.0082 | 0.0961 | 0.0961 |
Echinococcus multilocularis | cyclin dependent kinase 1 | 0.0082 | 0.0961 | 0.0869 |
Giardia lamblia | Kinase, CMGC CDK | 0.0082 | 0.0961 | 0.3236 |
Leishmania major | cyclin | 0.0114 | 0.1824 | 1 |
Echinococcus granulosus | cyclin dependent kinase 1 | 0.0082 | 0.0961 | 0.0869 |
Trypanosoma cruzi | CYC2-like cyclin, putative | 0.0114 | 0.1824 | 1 |
Trichomonas vaginalis | cyclins, putative | 0.0114 | 0.1824 | 1 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0082 | 0.0961 | 0.0869 |
Echinococcus granulosus | cyclin B | 0.0114 | 0.1824 | 0.2685 |
Onchocerca volvulus | 0.0114 | 0.1824 | 0.5 | |
Echinococcus multilocularis | cyclin dependent kinase 5 | 0.0082 | 0.0961 | 0.0869 |
Echinococcus multilocularis | cyclin B | 0.0114 | 0.1824 | 0.2685 |
Trichomonas vaginalis | cyclin B, putative | 0.0114 | 0.1824 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Efficacy (functional) | = 12.4 % | Efficacy against human recombinant GABAA alpha1 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | ChEMBL. | 16392789 |
Efficacy (functional) | = 12.4 % | Efficacy against human recombinant GABAA alpha1 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | ChEMBL. | 16392789 |
Efficacy (functional) | = 14 % | Efficacy against human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | ChEMBL. | 16392789 |
Efficacy (functional) | = 14 % | Efficacy against human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | ChEMBL. | 16392789 |
Efficacy (functional) | = 43 % | Efficacy against human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | ChEMBL. | 16392789 |
Efficacy (functional) | = 43 % | Efficacy against human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells by whole cell patch clamp method | ChEMBL. | 16392789 |
Ki (binding) | = 0.2 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.2 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha5 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.34 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.34 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.5 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.5 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.52 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
Ki (binding) | = 0.52 nM | Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells | ChEMBL. | 16392789 |
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.