Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cytochrome P450, family 26, subfamily A, polypeptide 1 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 2, subfamily D, polypeptide 6 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | cytochrome P450 | cytochrome P450, family 2, subfamily D, polypeptide 6 | 497 aa | 425 aa | 32.0 % |
Trypanosoma brucei | cytochrome P450, putative | cytochrome P450, family 26, subfamily A, polypeptide 1 | 497 aa | 515 aa | 21.9 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 4 | 502 aa | 492 aa | 24.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Leishmania major | cytochrome p450-like protein | 0.0023 | 0.5 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0023 | 0.5 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0023 | 0.5 | 0.5 |
Loa Loa (eye worm) | CYP4Cod1 | 0.0023 | 0.5 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0023 | 0.5 | 0.5 |
Trypanosoma brucei | cytochrome P450, putative | 0.0023 | 0.5 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0023 | 0.5 | 0.5 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0023 | 0.5 | 0.5 |
Brugia malayi | Cytochrome P450 family protein | 0.0023 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | = 3.51 uM | Inhibition of CYP26A1-mediated ATRA metabolism in human HL60 cells assessed as ATRA level at 5 uM incubated for 96 hrs by HPLC method (Rvb = 1.21 uM) | ChEMBL. | 26365710 |
Activity (binding) | = 5.67 uM | Inhibition of CYP26A1-mediated ATRA metabolism in human HL60 cells assessed as ATRA level at 5 uM incubated for 72 hrs by HPLC method (Rvb = 3.6 uM) | ChEMBL. | 26365710 |
Activity (binding) | = 7.45 uM | Inhibition of CYP26A1-mediated ATRA metabolism in human HL60 cells assessed as ATRA level at 5 uM incubated for 48 hrs by HPLC method (Rvb = 4.95 uM) | ChEMBL. | 26365710 |
Activity (binding) | = 9.3 uM | Inhibition of CYP26A1-mediated ATRA metabolism in human HL60 cells assessed as ATRA level at 5 uM incubated for 24 hrs by HPLC method (Rvb = 7.19 uM) | ChEMBL. | 26365710 |
GI (functional) | = 10.86 % | Growth inhibition of human HL60 cells at 10 uM incubated for 48 hrs by MTT assay | ChEMBL. | 26365710 |
IC50 (binding) | = 0.22 uM | Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins in dark condition with NADPH and ATRA by HPLC method | ChEMBL. | 26365710 |
IC50 (ADMET) | = 1.17 uM | Inhibition of CYP3A4 (unknown origin) incubated for 45 mins using NADPH by fluorescence assay | ChEMBL. | 26365710 |
IC50 (ADMET) | = 5.56 uM | Inhibition of CYP2D6 (unknown origin) incubated for 45 mins using NADPH and ATRA by HPLC assay | ChEMBL. | 26365710 |
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.