Any pathway inhibitor that inhibits the Hedgehog signalling pathway.
ChEBI ID: 140921
| Member | Definition | Class |
|---|---|---|
| gant 61 | An aminal that is hexahydropyrimidine which is substituted on each nitrogen by a 2-(dimethylamino)benzyl group, and at the aminal carbon by a pyridin-4-yl group. A Hedgehog signaling pathway and Gli protein inhibitor. | 2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline; GANT61 |
| 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 |
| itraconazole | An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis. | itraconazole |
| 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 |
| u 18666a | A hydrochloride obtained by reaction of 3beta-(2-diethylaminoethoxy)androst-5-en-17-one with one equivalent of hydrochloric acid. It is a cholesterol synthesis and transport inhibitor. | 3beta-(2-diethylaminoethoxy)androst-5-en-17-one hydrochloride |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 174 (2.49) | 18.7374 |
| 1990's | 1,351 (19.36) | 18.2507 |
| 2000's | 1,918 (27.48) | 29.6817 |
| 2010's | 2,576 (36.91) | 24.3611 |
| 2020's | 960 (13.76) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 766 (9.95%) | 5.53% |
| Reviews | 932 (12.10%) | 6.00% |
| Case Studies | 2,314 (30.05%) | 4.05% |
| Observational | 24 (0.31%) | 0.25% |
| Other | 3,664 (47.58%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| activating transcription factor 6 | Homo sapiens (human) | Potency | 7.5624 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 3.5481 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 5.6319 | 2 | 2 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 10.5909 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.9640 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 1.2589 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 3.1623 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 4.3176 | 2 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 5.6228 | 7 | 8 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 2.9849 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 4.5728 | 5 | 5 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 12.3327 | 4 | 12 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 8.4120 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 20.6682 | 1 | 2 |
| G | Vesicular stomatitis virus | Potency | 10.9640 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| GALC protein | Homo sapiens (human) | Potency | 0.6310 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 1.5059 | 2 | 2 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 3.7578 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 5.9553 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 1 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 10.9640 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 6.0070 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 10.9640 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 22.4002 | 2 | 4 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 2.0755 | 2 | 2 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 6.0070 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 2.4926 | 2 | 2 |
| polyprotein | Zika virus | Potency | 20.6682 | 1 | 2 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 26.2123 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 2.4901 | 2 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 1.4334 | 2 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 1.5916 | 2 | 2 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 2.3914 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 13.1880 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 10.9143 | 2 | 4 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 3.7578 | 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 | 1.0057 | 3 | 5 |
| Zinc finger protein GLI1 | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| Zinc finger protein GLI1 | Mus musculus (house mouse) | IC50 | 5.0000 | 1 | 1 |
| Zinc finger protein GLI2 | Mus musculus (house mouse) | IC50 | 5.0000 | 1 | 1 |
| 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 |
| Cytochrome P450 144 | Mycobacterium tuberculosis CDC1551 | Kd | 30.2000 | 1 | 1 |
| 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 |
| Steroid C26-monooxygenase | Mycobacterium tuberculosis CDC1551 | Kd | 30.2000 | 1 | 2 |
| 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 |