An EC 3.6.3.* (acid anhydride hydrolase catalysing transmembrane movement of substances) inhibitor that interferes with the action of xenobiotic-transporting ATPase (EC 3.6.3.44).
| Member | Definition | Class |
|---|
| dexverapamil | A 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile that has R configuration. It competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1, EC 3.6.3.44), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms. Dexverapamil exhibits lower calcium antagonistic activity and toxicity than racemic verapamil. | dexverapamil |
| 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 |
| quinidine | A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | quinidine |
| 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 | 12.5893 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 3.5297 | 4 | 4 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 33.3278 | 2 | 2 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 10.5909 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 8.9125 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 0.0316 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.9640 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 0.0550 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 2 | 3 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.6918 | 1 | 1 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 8.4127 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 5.5629 | 9 | 12 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 2.9849 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 29.6153 | 6 | 13 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 0.8333 | 1 | 1 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 8.4120 | 1 | 1 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 29.5659 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 10.9640 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| GALC protein | Homo sapiens (human) | Potency | 0.6310 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 2 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 16.2292 | 2 | 5 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 7.5624 | 1 | 1 |
| 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 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 27.9362 | 1 | 1 |
| 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 | 10.9640 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 6.3703 | 3 | 3 |
| 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 | 4.6141 | 2 | 6 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 20.5808 | 2 | 3 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 1.2589 | 1 | 1 |
| polyprotein | Zika virus | Potency | 29.5659 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 9.5818 | 1 | 2 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 22.4666 | 3 | 4 |
| 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 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 68.0511 | 1 | 1 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 68.0511 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 21.8959 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 20.7347 | 2 | 4 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 31.9600 | 2 | 4 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 1.2589 | 1 | 1 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 1.2589 | 1 | 1 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 3.7578 | 1 | 1 |