An antagonist that interferes with the action of smoothened (SMO) receptor.
ChEBI ID: 66908
| Member | Definition | Class |
|---|---|---|
| gdc 0449 | A benzamide obtained by formal condensation between the carboxy group of 2-chloro-4-(methylsulfonyl)benzoic acid and the anilino group of 4-chloro-3-(pyridin-2-yl)aniline. Used for the treatment metastatic basal cell carcinoma. | vismodegib |
| glasdegib | A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a (2R,4S)-4-{[(4-cyanophenyl)carbamoyl]amino}-1-methylpiperidin-2-yl group at position 2. It is a hedgehog signalling pathway inhibitor that acts by binding to Smoothened (SMO) receptors and blocking signal transduction (IC50 = 5 nM). It is used in combination with low-dose cytarabine, for the treatment of newly-diagnosed acute myeloid leukemia (AML) in adult patients (aged >= 75 years), or who have medical conditions that prevent the use of standard chemotherapy. | glasdegib |
| lde225 | A member of the classo of biphenyls that is the amide obtained by formal condensation of the carboxy group of 2-methyl-4'-(trifluoromethoxy)[1,1'-biphenyl]-3-carboxylic acid with the amino group of 6-(2,6-dimethylmorpholin-4-yl)pyridin-3-amine. Used (as its phosphate salt) for treatment of locally advanced basal cell carcinoma. | sonidegib |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 12 (1.51) | 29.6817 |
| 2010's | 548 (69.02) | 24.3611 |
| 2020's | 234 (29.47) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 113 (12.65%) | 5.53% |
| Reviews | 168 (18.81%) | 6.00% |
| Case Studies | 133 (14.89%) | 4.05% |
| Observational | 6 (0.67%) | 0.25% |
| Other | 473 (52.97%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 9.3476 | 4 | 7 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
| Cytochrome P450 2C8 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 25.0000 | 2 | 2 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 33.0000 | 1 | 1 |
| Smoothened homolog | Homo sapiens (human) | IC50 | 0.0222 | 8 | 8 |
| Smoothened homolog | Mus musculus (house mouse) | IC50 | 0.0627 | 8 | 9 |
| Smoothened homolog | Homo sapiens (human) | Ki | 0.0115 | 2 | 3 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
| Sonic hedgehog protein | Homo sapiens (human) | IC50 | 0.8825 | 2 | 2 |
| Sonic hedgehog protein | Mus musculus (house mouse) | IC50 | 0.0072 | 3 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Albumin | Homo sapiens (human) | Kd | 65.3750 | 4 | 4 |
| Albumin | Rattus norvegicus (Norway rat) | Kd | 105.6000 | 3 | 3 |
| Smoothened homolog | Homo sapiens (human) | EC50 | 0.0025 | 2 | 2 |
| Smoothened homolog | Mus musculus (house mouse) | EC50 | 0.0034 | 2 | 2 |
| Smoothened homolog | Homo sapiens (human) | Kd | 0.0975 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 2C9 | Homo sapiens (human) | INH | 20.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | INH | 20.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2B | Rattus norvegicus (Norway rat) | INH | 20.0000 | 1 | 1 |
| Sonic hedgehog protein | Homo sapiens (human) | INH | 0.0028 | 1 | 1 |