A membrane transport modulator that restores the chloride ion transport ability of defective cystic fibrosis transmembrane conductance regulator (CFTR) genes.
ChEBI ID: 66902
| Member | Definition | Class |
|---|---|---|
| lumacaftor | An aromatic amide obtained by formal condensation of the carboxy group of 1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropane-1-carboxylic acid with the aromatic amino group of 3-(6-amino-3-methylpyridin-2-yl)benzoic acid. Used for the treatment of cystic fibrosis. | lumacaftor |
| vx-770 | An aromatic amide obtained by formal condensation of the carboxy group of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid with the amino group of 5-amino-2,4-di-tert-butylphenol. Used for the treatment of cystic fibrosis. | ivacaftor |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (0.24) | 29.6817 |
| 2010's | 471 (56.47) | 24.3611 |
| 2020's | 361 (43.29) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 66 (6.59%) | 5.53% |
| Reviews | 139 (13.87%) | 6.00% |
| Case Studies | 75 (7.49%) | 4.05% |
| Observational | 49 (4.89%) | 0.25% |
| Other | 673 (67.17%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 23.9185 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 18.9991 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.0473 | 4 | 4 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 0.0372 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 23.9185 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 23.9185 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 23.9185 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 23.5009 | 2 | 4 |
| polyprotein | Zika virus | Potency | 0.0372 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 23.3617 | 1 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 21.4865 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Cytochrome P450 2C8 | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 26.0000 | 2 | 2 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 20.0000 | 2 | 2 |
| Cytochrome P450 2E1 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 6.5700 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cystic fibrosis transmembrane conductance regulator | Homo sapiens (human) | EC50 | 0.7447 | 17 | 17 |
| Cystic fibrosis transmembrane conductance regulator | Homo sapiens (human) | Kd | 60.3000 | 2 | 2 |