Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cytochrome P450, family 2, subfamily D, polypeptide 6 | Starlite/ChEMBL | References |
Homo sapiens | glutamate receptor, metabotropic 1 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | Starlite/ChEMBL | References |
Rattus norvegicus | Metabotropic glutamate receptor 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 4 | 502 aa | 492 aa | 24.2 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 2, subfamily D, polypeptide 6 | 497 aa | 425 aa | 32.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0025 | 0.0587 | 0.0587 |
Loa Loa (eye worm) | hypothetical protein | 0.012 | 1 | 1 |
Brugia malayi | metabotropic glutamate receptor subtype 5a (mGluR5a), putative | 0.0089 | 0.686 | 0.8831 |
Loa Loa (eye worm) | receptor family ligand binding region containing protein | 0.0025 | 0.0587 | 0.0587 |
Schistosoma mansoni | metabotropic glutamate receptor 2 3 (mglur group 2) | 0.0111 | 0.9092 | 1 |
Echinococcus multilocularis | metabotropic glutamate receptor 5 | 0.012 | 1 | 1 |
Brugia malayi | Metabotropic glutamate receptor precursor. | 0.0098 | 0.7768 | 1 |
Loa Loa (eye worm) | glutamate receptor | 0.0038 | 0.191 | 0.191 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0019 | 0 | 0.5 |
Trypanosoma brucei | cytochrome P450, putative | 0.0019 | 0 | 0.5 |
Leishmania major | cytochrome p450-like protein | 0.0019 | 0 | 0.5 |
Brugia malayi | Receptor family ligand binding region containing protein | 0.0025 | 0.0587 | 0.0755 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0019 | 0 | 0.5 |
Loa Loa (eye worm) | metabotropic GABA-B receptor subtype 2 | 0.0025 | 0.0587 | 0.0587 |
Schistosoma mansoni | metabotropic glutamate receptor | 0.0082 | 0.6201 | 0.5392 |
Brugia malayi | metabotropic glutamate receptor type 2 | 0.0048 | 0.2818 | 0.3628 |
Loa Loa (eye worm) | glutamate receptor | 0.0098 | 0.7768 | 0.7768 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0019 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Negative allosteric modulation of mGluR6 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
Activity (binding) | Negative allosteric modulation of mGluR5 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
Activity (binding) | Negative allosteric modulation of mGluR8 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
Activity (binding) | Negative allosteric modulation of mGluR4 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
Activity (binding) | Negative allosteric modulation of mGluR7 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
Activity (binding) | Negative allosteric modulation of mGluR3 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
Activity (binding) | Negative allosteric modulation of mGluR2 (unknown origin) at 10 uM by cell based assay | ChEMBL. | 23727046 | |
IC50 (binding) | = 7.01 | Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization | ChEMBL. | 23727046 |
IC50 (binding) | = 99 nM | Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization | ChEMBL. | 23727046 |
IC50 (binding) | = 99 nM | Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins | ChEMBL. | 23932792 |
IC50 (binding) | > 10000 nM | Negative allosteric modulation of rat mGlu1 receptor | ChEMBL. | 23932792 |
IC50 (ADMET) | = 7 uM | Inhibition of CYP3A4 in human liver microsomes in presence of NADPH | ChEMBL. | 23932792 |
IC50 (ADMET) | = 12.4 uM | Inhibition of CYP2D6 in human liver microsomes in presence of NADPH | ChEMBL. | 23932792 |
IC50 (ADMET) | > 30 uM | Inhibition of CYP1A2 in human liver microsomes in presence of NADPH | ChEMBL. | 23932792 |
IC50 (ADMET) | > 30 uM | Inhibition of CYP2C9 in human liver microsomes in presence of NADPH | ChEMBL. | 23932792 |
Inhibition (binding) | = 2.8 % | Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization at 30 uM relative to glutamate | ChEMBL. | 23727046 |
Inhibition (binding) | < 41 % | Binding affinity to sigma1 receptor (unknown origin) at 10 uM by radioligand binding assay | ChEMBL. | 23727046 |
Inhibition (binding) | < 41 % | Binding affinity to adenosine A1 receptor (unknown origin) at 10 uM by radioligand binding assay | ChEMBL. | 23727046 |
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.
2 literature references were collected for this gene.