Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | arachidonate 5-lipoxygenase-activating protein | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 2, subfamily D, polypeptide 6 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 2, subfamily C, polypeptide 9 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Mycobacterium tuberculosis | Probable cytochrome P450 136 Cyp136 | cytochrome P450, family 2, subfamily C, polypeptide 9 | 490 aa | 441 aa | 21.8 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 2, subfamily D, polypeptide 6 | 497 aa | 425 aa | 32.0 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 4 | 502 aa | 492 aa | 24.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | Cytochrome P450 family protein | 0.0036 | 0.1115 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0023 | 0 | 0.5 |
Schistosoma mansoni | membrane associated proteins in eicosanoid and glutathione metabolism family member | 0.0135 | 1 | 0.5 |
Echinococcus multilocularis | microsomal glutathione S transferase 3 | 0.0135 | 1 | 0.5 |
Trypanosoma brucei | cytochrome P450, putative | 0.0023 | 0 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0036 | 0.1115 | 1 |
Schistosoma mansoni | microsomal glutathione s-transferase | 0.0135 | 1 | 0.5 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0023 | 0 | 0.5 |
Toxoplasma gondii | MAPEG family protein | 0.0135 | 1 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0023 | 0 | 0.5 |
Leishmania major | cytochrome p450-like protein | 0.0023 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.5 nM | Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 10 mins by ELISA | ChEMBL. | 22059882 |
IC50 (binding) | = 2.2 nM | Displacement of [3H]-3-[5-(pyrid-2-ylmethoxy)-3-tert-butylthio-1-benzylindol-2-yl]-2,2-dimethylpropionic acid from FLAP in human polymorphonuclear cell membranes after 1 hr by scintillation counting | ChEMBL. | 22059882 |
IC50 (ADMET) | = 8.5 nM | Inhibition of human CYP3A4 | ChEMBL. | 22059882 |
IC50 (ADMET) | = 12 nM | Inhibition of human CYP2C9 | ChEMBL. | 22059882 |
IC50 (ADMET) | > 50 nM | Inhibition of human CYP2D6 | ChEMBL. | 22059882 |
IC50 (binding) | = 130 nM | Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionophore A23187-induced LTB4 production preincubated for 5 hrs by ELISA | ChEMBL. | 22059882 |
IC50 (binding) | = 283 nM | Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionophore A23187-induced LTB4 production preincubated for 15 mins by ELISA | ChEMBL. | 22059882 |
Inhibition (binding) | = 33 % | Inhibition of COX1-mediated TXB2 production in human whole blood at 10 uM after 30 mins by competitive enzyme immunoassay | ChEMBL. | 22059882 |
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.