Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cholesteryl ester transfer protein, plasma | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Brugia malayi | LBP / BPI / CETP family, C-terminal domain containing protein | 0.0041 | 1 | 1 |
Onchocerca volvulus | 0.0041 | 1 | 1 | |
Loa Loa (eye worm) | LBP/BPI/CETP family domain-containing protein | 0.0041 | 1 | 1 |
Brugia malayi | LBP / BPI / CETP family, N-terminal domain containing protein | 0.0041 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0041 | 1 | 1 |
Onchocerca volvulus | 0.0041 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 19 nM | BindingDB_Patents: Scintillation Proximity Assay. Compounds of the present invention inhibit CETP-dependent cholesterol ester transfer from HDL to LDL as described here. Dilutions of compounds in DMSO (1 µl) are added to BD plates (#353232). To this is added 20 µl of a mixture containing 3H-CE/HDL (0.15 µl), biotinylated LDL (5 µg protein/ml final concentration) and unlabeled HDL (16 µg/ml final concentration) in a buffer containing 50 mM HEPES, pH 7.4, 150 mM NaCl and 0.05% sodium azide. Reactions are initiated by the addition of 10 µl of buffer containing purified human recombinant CETP, and incubated at 37 C. At the end of the reaction, 60 µl of LEADseeker beads (#RPNQ0261, 2 mg/ml in buffer containing 1 mg/ml BSA and 0.05 mg protein/ml HDL) are added, the plates are covered and subsequently read. Background activity is determined in a set of wells that receive buffer but no CETP. | ChEMBL. | No reference |
IC50 (binding) | = 19 nM | BindingDB_Patents: Scintillation Proximity Assay. Compounds of the present invention inhibit CETP-dependent cholesterol ester transfer from HDL to LDL as described here. Dilutions of compounds in DMSO (1 µl) are added to BD plates (#353232). To this is added 20 µl of a mixture containing 3H-CE/HDL (0.15 µl), biotinylated LDL (5 µg protein/ml final concentration) and unlabeled HDL (16 µg/ml final concentration) in a buffer containing 50 mM HEPES, pH 7.4, 150 mM NaCl and 0.05% sodium azide. Reactions are initiated by the addition of 10 µl of buffer containing purified human recombinant CETP, and incubated at 37 C. At the end of the reaction, 60 µl of LEADseeker beads (#RPNQ0261, 2 mg/ml in buffer containing 1 mg/ml BSA and 0.05 mg protein/ml HDL) are added, the plates are covered and subsequently read. Background activity is determined in a set of wells that receive buffer but no CETP. | ChEMBL. | No reference |
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.