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 |
---|---|---|---|---|
Loa Loa (eye worm) | CYP4Cod1 | 0.00248392 | 1 | 1 |
Brugia malayi | Cytochrome P450 family protein | 0.00248392 | 1 | 0.5 |
Trypanosoma brucei | cytochrome P450, putative | 0.00248392 | 1 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.00248392 | 1 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.00248392 | 1 | 0.5 |
Brugia malayi | Cytochrome P450 family protein | 0.00248392 | 1 | 0.5 |
Leishmania major | cytochrome p450-like protein | 0.00248392 | 1 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.00248392 | 1 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.00248392 | 1 | 1 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.00248392 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI infected in Swiss mouse model of Chagas disease assessed as increase in host survival at 50 mg/kg once daily for 5 consecutive days through oral gavage starting on day 8 post infection measured 14 days post infection | ChEMBL. | 23462713 | |
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI infected in Swiss mouse model of Chagas disease assessed as increase in host survival at 100 mg/kg once daily for 5 consecutive days through oral gavage starting on day 8 post infection measured 14 days post infection | ChEMBL. | 23462713 | |
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI infected in Swiss mouse model of Chagas disease assessed as increase in host survival at 20 mg/kg once daily for 5 consecutive days through oral gavage starting on day 8 post infection measured 14 days post infection | ChEMBL. | 23462713 | |
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI infected in Swiss mouse model of Chagas disease assessed as decrease in blood parasitemia level at 100 mg/kg once daily for 5 consecutive days through oral gavage starting on day 8 post infection measured 14 days post infection | ChEMBL. | 23462713 | |
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI infected in Swiss mouse model of Chagas disease assessed as decrease in blood parasitemia level at 50 mg/kg once daily for 5 consecutive days through oral gavage starting on day 8 post infection measured 14 days post infection | ChEMBL. | 23462713 | |
Activity (functional) | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI infected in Swiss mouse model of Chagas disease assessed as decrease in blood parasitemia level at 20 mg/kg once daily for 5 consecutive days through oral gavage starting on day 8 post infection measured 14 days post infection | ChEMBL. | 23462713 | |
IC50 (functional) | = 0.24 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC50 (functional) | = 0.24 uM | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI extracellular trypomastigotes forms transfected with beta-galactosidase gene infected in rat L6 cells assessed as inhibition of parasite growth after 4 days | ChEMBL. | 23462713 |
IC50 (functional) | = 0.39 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC50 (functional) | = 0.49 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC50 (functional) | = 0.54 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC50 (ADMET) | = 7.4 uM | Inhibition of CYP3A4/5 in human liver microsomes assessed as reduction in testosterone-beta-hydroxylation | ChEMBL. | 23462713 |
IC90 (functional) | = 0.52 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC90 (functional) | = 0.82 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC90 (functional) | = 0.93 uM | DNDI: Inhibition of Chagas Disease parasite Trypanosoma cruzi (Tulahuen LacZ, Clone C4), in vitro. | ChEMBL. | No reference |
IC90 (functional) | = 0.96 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 | 23462713 |
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.