Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 5 | References | |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 5 | 502 aa | 458 aa | 24.4 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 4 | 502 aa | 492 aa | 24.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trypanosoma cruzi | cytochrome P450, putative | 0.00248392 | 1 | 0.5 |
Brugia malayi | Cytochrome P450 family protein | 0.00248392 | 1 | 0.5 |
Loa Loa (eye worm) | CYP4Cod1 | 0.00248392 | 1 | 1 |
Brugia malayi | Cytochrome P450 family protein | 0.00248392 | 1 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.00248392 | 1 | 1 |
Trypanosoma brucei | cytochrome P450, putative | 0.00248392 | 1 | 0.5 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.00248392 | 1 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.00248392 | 1 | 1 |
Leishmania major | cytochrome p450-like protein | 0.00248392 | 1 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.00248392 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 6 infected in Swiss mouse assessed as reduction in blood parasitemia at 20 mg/kg, po qd administered on day 8 post-infection for 10 days by microscopic analysis | ChEMBL. | 24304150 | |
Activity (functional) | > 99 % | Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen infected in Swiss mouse model of chagas disease assessed as decrease in parasite level in blood at 20 mg/kg, po administered 8 day after post infection qd for 20 days | ChEMBL. | 22536986 |
Cp (ADMET) | = 0.03 uM | Plasma concentration in Swiss mouse at 20 mg/kg, po after 24 hrs by LC/MS analysis | ChEMBL. | 24304150 |
Cp (ADMET) | = 2.5 uM | Plasma concentration in Swiss mouse at 20 mg/kg, po after 1 hr | ChEMBL. | 22536986 |
IC50 (functional) | = 0.012 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC50 (functional) | = 0.012 uM | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 6 amastigotes infected in rat L6 cells after 96 hrs by colorimetric method | ChEMBL. | 24304150 |
IC50 (functional) | = 0.012 uM | Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen expressing the beta- galactosidase gene infected rat L6 cells after 96 hrs | ChEMBL. | 22536986 |
IC50 (functional) | = 0.018 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC50 (ADMET) | = 7.6 uM | Inhibition of CYP3A4/5 in human liver microsomes | ChEMBL. | 22536986 |
IC90 (functional) | = 0.032 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC90 (functional) | = 0.033 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Trypanosoma cruzi | ChEMBL23 | 22536986 |
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.