Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | farnesyltransferase, CAAX box, beta | References | |
Homo sapiens | farnesyltransferase, CAAX box, alpha | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 2.76 ug hr ml-1 | Area under plasma concentration time curve of the compound was determined in dog upon oral administration | ChEMBL. | 14736242 |
Clp (ADMET) | = 0.31 l hr-1 kg-1 | Plasma clearance of the compound was determined in dog | ChEMBL. | 14736242 |
EC50 (functional) | = 9.1 nM | Effective concentration required for inhibition of farnesylation of Ras protein in NIH3T3 cells | ChEMBL. | 14736242 |
EC50 (functional) | = 9.1 nM | Effective concentration required for inhibition of farnesylation of Ras protein in NIH3T3 cells | ChEMBL. | 14736242 |
F (ADMET) | = 82 % | Bioavailability in dog | ChEMBL. | 14736242 |
IC50 (binding) | = -5.95 | Inhibition of FTase | ChEMBL. | 16455255 |
IC50 (binding) | = 1.1 nM | Inhibition of FTase (unknown origin) | ChEMBL. | 17236767 |
Inhibition (binding) | = 1.1 nM | Inhibitory activity against Farnesyltransferase (FTase) | ChEMBL. | 14736242 |
Inhibition (binding) | = 1.1 nM | Inhibitory activity against Farnesyltransferase (FTase) | ChEMBL. | 14736242 |
Inhibition (binding) | = 2000 nM | Inhibitory concentration required against geranylgeranyltransferase-I (GGTase-I) | ChEMBL. | 14736242 |
Inhibition (binding) | = 2000 nM | Inhibitory concentration required against geranylgeranyltransferase-I (GGTase-I) | ChEMBL. | 14736242 |
Log IC50 (binding) | = 5.95 | Inhibition of FTase | ChEMBL. | 16455255 |
T1/2 (ADMET) | = 1.3 hr | Half-life of the compound was determined in dog upon oral administration | ChEMBL. | 14736242 |
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.
3 literature references were collected for this gene.