Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | Starlite/ChEMBL | References |
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled | 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 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | sodium bile acid cotransporter | 0.919 | 1 | 1 |
Onchocerca volvulus | 0.919 | 1 | 0.5 | |
Trypanosoma cruzi | cytochrome P450, putative | 0.0015 | 0.0005 | 0.5 |
Leishmania major | cytochrome p450-like protein | 0.0015 | 0.0005 | 0.5 |
Echinococcus granulosus | sodium bile acid cotransporter | 0.919 | 1 | 1 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0015 | 0.0005 | 0.0005 |
Trypanosoma brucei | cytochrome P450, putative | 0.0015 | 0.0005 | 0.5 |
Echinococcus granulosus | sodium bile acid cotransporter | 0.919 | 1 | 1 |
Schistosoma mansoni | sodium-bile acid cotransporter related | 0.919 | 1 | 1 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0015 | 0.0005 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.919 | 1 | 1 |
Loa Loa (eye worm) | CYP4Cod1 | 0.0015 | 0.0005 | 0.0005 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0015 | 0.0005 | 0.0005 |
Echinococcus granulosus | sodium bile acid cotransporter | 0.919 | 1 | 1 |
Schistosoma mansoni | sodium-bile acid cotransporter | 0.5463 | 0.594 | 0.3179 |
Echinococcus multilocularis | sodium bile acid cotransporter | 0.919 | 1 | 1 |
Echinococcus multilocularis | sodium bile acid cotransporter | 0.919 | 1 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0015 | 0.0005 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 310 nM | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry | ChEMBL. | 21134749 |
IC50 (ADMET) | = 5.54 uM | Inhibition of human CYP3A4 | ChEMBL. | 21134749 |
IC50 (ADMET) | = 39.2 uM | Inhibition of human CYP2D6 | ChEMBL. | 21134749 |
Kb (functional) | = 0.53 nM | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated cAMP accumulation by luminometry | ChEMBL. | 21134749 |
Ki (binding) | = 3.4 nM | Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in human HeLa cells by glass fiber filtration assay | ChEMBL. | 21134749 |
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.