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photosensitizing agent
A chemical compound that can be excited by light of a specific wavelength and subsequently transfer energy to a chosen reactant. This is commonly molecular oxygen within a cancer tissue, which is converted to (highly rective) singlet state oxygen. This rapidly reacts with any nearby biomolecules, ultimately killing the cancer cells.
ChEBI ID: 47868
Members (21)
| Member | Definition | Class |
|---|---|---|
| 9,10-diphenylanthracene | A member of the class of anthracenes that is anthracene in which both of the hydrogens on the central ring are substituted by phenyl groups. | 9,10-diphenylanthracene |
| acetophenone | A methyl ketone that is acetone in which one of the methyl groups has been replaced by a phenyl group. | acetophenone |
| aminolevulinic acid | The simplest delta-amino acid in which the hydrogens at the gamma position are replaced by an oxo group. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used (in the form of the hydrochloride salt)in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp. | 5-aminolevulinic acid; 5-ammoniolevulinate |
| aminolevulinic acid hydrochloride | A hydrochloride that is the monohydrochloride of 5-aminolevulinic acid. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp. | 5-aminolevulinic acid hydrochloride |
| benzophenone | The simplest member of the class of benzophenones, being formaldehyde in which both hydrogens are replaced by phenyl groups. | benzophenone |
| carprofen | Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs. | carprofen |
| cidofovir anhydrous | Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | cidofovir anhydrous |
| cisplatin | A diamminedichloroplatinum compound in which the two ammine ligands and two chloro ligands are oriented in a cis planar configuration around the central platinum ion. An anticancer drug that interacts with, and forms cross-links between, DNA and proteins, it is used as a neoplasm inhibitor to treat solid tumours, primarily of the testis and ovary. Commonly but incorrectly described as an alkylating agent due to its mechanism of action (but it lacks alkyl groups). | cisplatin; transplatin |
| diphenylcyclopropenone | A cyclopropenone compound having phenyl substituents at the 2- and 3-positions. | diphenylcyclopropenone |
| docetaxel anhydrous | A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group. | docetaxel anhydrous |
| gemcitabine | A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. | gemcitabine |
| lomefloxacin | A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery. | lomefloxacin |
| lomefloxacin hydrochloride | The hydrochloride salt of lomefloxacin. It is administered by mouth to treat bacterial infections including bronchitis and urinary tract infections. It is also used topically as eye drops for the treatment of bacterial conjunctivitis, and as ear drops for the treatment of otitis externa and otitis media. | lomefloxacin hydrochloride |
| lucanthone | A thioxanthen-9-one compound having a methyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. Formerly used for the treatment of schistosomiasis. It is a prodrug, being metabolised to hycanthone. | lucanthone |
| methoxsalen | A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis. | methoxsalen |
| methyl 5-aminolevulinate | The methyl ester of 5-aminolevulinic acid. A prodrug, it is metabolised to protoporphyrin IX, a photosensitizer, and is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Topical application (often as the hydrochloride salt) results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells. | methyl 5-aminolevulinate |
| methyl 5-aminolevulinate hydrochloride | The hydrochloride salt of methyl 5-aminolevulinate. A prodrug, it is metabolised to protoporphyrin IX, a photosensitizer, and is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Topical application results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells. | methyl 5-aminolevulinate hydrochloride |
| phenosafranine | An organic chloride salt having 3,7-diamino-5-phenylphenazin-5-ium as the counterion. It is commonly used for staining Gram negative bacteria red in smears to contrast with the blue Gram positive organisms. | phenosafranine |
| riboflavin | D-Ribitol in which the hydroxy group at position 5 is substituted by a 7,8-dimethyl-2,4-dioxo-3,4-dihydrobenzo[g]pteridin-10(2H)-yl moiety. It is a nutritional factor found in milk, eggs, malted barley, liver, kidney, heart, and leafy vegetables, but the richest natural source is yeast. The free form occurs only in the retina of the eye, in whey, and in urine; its principal forms in tissues and cells are as flavin mononucleotide and flavin-adenine dinucleotide. | riboflavin |
| trioxsalen | 7H-Furo[3,2-g]chromen-7-one in which positions 2, 5, and 9 are substituted by methyl groups. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered orally in conjunction with UV-A for phototherapy treatment of vitiligo. After photoactivation it creates interstrand cross-links in DNA, inhibiting DNA synthesis and cell division, and can lead to cell injury; recovery from the cell injury may be followed by increased melanisation of the epidermis. | trioxsalen |
| vinorelbine | A vinca alkaloid with a norvinblastine skeleton. | vinorelbine |
Research
Studies (44,340)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 6,512 (14.69) | 18.7374 |
| 1990's | 3,961 (8.93) | 18.2507 |
| 2000's | 11,305 (25.50) | 29.6817 |
| 2010's | 17,086 (38.53) | 24.3611 |
| 2020's | 5,476 (12.35) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 8,169 (16.86%) | 5.53% |
| Reviews | 4,494 (9.28%) | 6.00% |
| Case Studies | 3,948 (8.15%) | 4.05% |
| Observational | 234 (0.48%) | 0.25% |
| Other | 31,601 (65.23%) | 84.16% |
Protein Targets (249)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 20.2567 | 1 | 4 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 20.3025 | 1 | 2 |
| 67.9K protein | Vaccinia virus | Potency | 8.1555 | 2 | 6 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 43.2002 | 2 | 11 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 34.5770 | 2 | 6 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 18.8725 | 1 | 6 |
| Amyloid-beta precursor protein | Homo sapiens (human) | Potency | 20.5962 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 22.5515 | 10 | 38 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 13.1008 | 2 | 7 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 18.3489 | 1 | 1 |
| Ataxin-2 | Homo sapiens (human) | Potency | 35.5348 | 1 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 3.7933 | 1 | 1 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 35.5348 | 1 | 2 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 2 | 2 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 16.7878 | 1 | 2 |
| caspase-1 isoform alpha precursor | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| caspase-3 | Cricetulus griseus (Chinese hamster) | Potency | 13.3332 | 1 | 1 |
| caspase-3 | Homo sapiens (human) | Potency | 16.7878 | 1 | 2 |
| Caspase-7 | Cricetulus griseus (Chinese hamster) | Potency | 13.3332 | 1 | 1 |
| Caspase-7 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 24.1337 | 2 | 12 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 17.7475 | 1 | 6 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 32.4648 | 1 | 2 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 21.1183 | 1 | 3 |
| Chain A, Breast cancer type 1 susceptibility protein | Homo sapiens (human) | Potency | 7.9433 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 18.2472 | 2 | 4 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 22.7328 | 2 | 4 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 7.9960 | 1 | 2 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 18.2472 | 2 | 4 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 77.4325 | 2 | 5 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 8.8006 | 1 | 2 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 12.8832 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.1563 | 1 | 3 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 22.4113 | 1 | 2 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 14.0222 | 2 | 15 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 7.1071 | 2 | 6 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 46.5757 | 1 | 4 |
| DNA polymerase III, partial | Bacillus subtilis | Potency | 18.8876 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 57.1220 | 1 | 2 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 63.4054 | 1 | 2 |
| endonuclease IV | Escherichia coli | Potency | 3.5180 | 1 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 20.8593 | 10 | 40 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 48.7071 | 2 | 5 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 16.9822 | 6 | 19 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.9950 | 1 | 3 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 10.9105 | 4 | 7 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 28.1105 | 4 | 7 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 31.7363 | 2 | 4 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 12.8832 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 13.3946 | 1 | 8 |
| geminin | Homo sapiens (human) | Potency | 7.1024 | 2 | 6 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 12.0199 | 2 | 9 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 5.6294 | 1 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 28.7303 | 2 | 9 |
| glucokinase regulatory protein | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 22.0412 | 1 | 2 |
| Glycoprotein hormones alpha chain | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 25.8518 | 1 | 2 |
| guanine nucleotide-binding protein G(i) subunit alpha-1 isoform 1 | Homo sapiens (human) | Potency | 1.9953 | 1 | 1 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 21.1755 | 1 | 2 |
| hexokinase-4 isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 25.7877 | 1 | 2 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 30.0474 | 2 | 2 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 51.1948 | 2 | 3 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 12.8832 | 1 | 2 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| hypothetical protein, conserved | Trypanosoma brucei | Potency | 1.9012 | 1 | 1 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 32.1271 | 2 | 4 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 12.8832 | 1 | 4 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 11.6044 | 3 | 9 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 11.8379 | 1 | 3 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 31.6228 | 1 | 2 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 36.6968 | 3 | 7 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 2.6157 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 25.3320 | 2 | 5 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 14.0982 | 1 | 4 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.1413 | 1 | 1 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 11.2202 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 31.7453 | 4 | 7 |
| nuclear factor NF-kappa-B p105 subunit isoform 1 | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 46.9762 | 1 | 2 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 44.1556 | 1 | 2 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 19.5543 | 2 | 3 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 21.9556 | 3 | 19 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 18.7728 | 1 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 13.9089 | 2 | 3 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 80.3039 | 1 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 27.0275 | 4 | 13 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 24.6371 | 5 | 13 |
| phosphoglycerate kinase | Trypanosoma brucei brucei TREU927 | Potency | 26.8545 | 1 | 1 |
| polyprotein | Zika virus | Potency | 15.8489 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 13.1088 | 1 | 4 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 36.0462 | 3 | 12 |
| progesterone receptor | Homo sapiens (human) | Potency | 38.6820 | 2 | 6 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 20.6585 | 2 | 12 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 1.5003 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 21.5580 | 3 | 16 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 26.0420 | 4 | 12 |
| RGS12 | Homo sapiens (human) | Potency | 1.9953 | 1 | 1 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 38.6026 | 3 | 6 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 38.6026 | 3 | 6 |
| Smad3 | Homo sapiens (human) | Potency | 0.7079 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 4.3866 | 1 | 3 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 6.8660 | 1 | 2 |
| TDP1 protein | Homo sapiens (human) | Potency | 14.5244 | 2 | 18 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 3.5481 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 15.0572 | 4 | 10 |
| Thrombopoietin | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 5.3968 | 3 | 7 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 19.9057 | 2 | 2 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 38.3212 | 6 | 10 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 15.4331 | 2 | 5 |
| tumor necrosis factor | Homo sapiens (human) | Potency | 53.0804 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 12.2066 | 2 | 3 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 19.7328 | 5 | 17 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 49.8808 | 1 | 3 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 22.0412 | 1 | 2 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 10 kDa chaperonin | Escherichia coli | IC50 | 59.0000 | 2 | 2 |
| 10 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 | 2.3560 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 1.2340 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 | 2.3560 | 1 | 1 |
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 1.2340 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli K-12 | IC50 | 250.0000 | 1 | 1 |
| 60 kDa chaperonin | Escherichia coli | IC50 | 59.0000 | 2 | 2 |
| 60 kDa heat shock protein, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 27.3800 | 2 | 2 |
| Acetylcholinesterase | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 1.3120 | 1 | 1 |
| Adenosine receptor A2a | Homo sapiens (human) | Ki | 0.7370 | 1 | 1 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.7000 | 1 | 1 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.7000 | 1 | 1 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.7000 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 42.9705 | 2 | 2 |
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 | 128.8250 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 3 |
| Beta-secretase 1 | Homo sapiens (human) | IC50 | 500.0000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 208.0250 | 2 | 4 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 3 |
| Cathepsin B | Homo sapiens (human) | IC50 | 288.8000 | 1 | 1 |
| Chain A, DEOXYNUCLEOSIDE KINASE | Drosophila melanogaster (fruit fly) | IC50 | 0.7600 | 1 | 1 |
| Chain A, ODORANT-BINDING PROTEIN | Sus scrofa (pig) | IC50 | 3.6000 | 1 | 5 |
| Chain B, Odorant-binding Protein | Sus scrofa (pig) | IC50 | 3.6000 | 1 | 1 |
| Cholinesterase | Homo sapiens (human) | IC50 | 0.7000 | 1 | 1 |
| Cholinesterase | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| Coagulation factor XII | Homo sapiens (human) | Ki | 100.0000 | 1 | 5 |
| Cocaine esterase | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
| Cytochrome P450 2A13 | Homo sapiens (human) | Ki | 0.0400 | 1 | 1 |
| Cytochrome P450 2A6 | Homo sapiens (human) | Ki | 0.9833 | 3 | 3 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| DNA-(apurinic or apyrimidinic site) endonuclease | Homo sapiens (human) | IC50 | 5.0000 | 2 | 2 |
| Equilibrative nucleoside transporter 1 | Homo sapiens (human) | IC50 | 0.1900 | 1 | 1 |
| Fatty-acid amide hydrolase 1 | Rattus norvegicus (Norway rat) | IC50 | 27.1500 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit rho-1 | Homo sapiens (human) | IC50 | 12.9000 | 1 | 1 |
| Glutamate receptor 1 | Homo sapiens (human) | Ki | 790.0000 | 1 | 1 |
| Glutamate receptor 2 | Homo sapiens (human) | Ki | 790.0000 | 1 | 1 |
| Glutamate receptor 3 | Homo sapiens (human) | Ki | 790.0000 | 1 | 1 |
| Glutamate receptor 4 | Homo sapiens (human) | Ki | 790.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 3 | Rattus norvegicus (Norway rat) | Ki | 790.0000 | 1 | 1 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Indoleamine 2,3-dioxygenase 1 | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| Kinesin-like protein KIF11 | Homo sapiens (human) | IC50 | 0.0014 | 8 | 8 |
| Liver carboxylesterase 1 | Homo sapiens (human) | Ki | 100.0000 | 2 | 6 |
| Liver carboxylesterase 1 | Oryctolagus cuniculus (rabbit) | Ki | 100.0000 | 2 | 6 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 89.6667 | 1 | 3 |
| Nucleotide-binding oligomerization domain-containing protein 2 | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| Papain | Carica papaya (papaya) | IC50 | 3,465.0000 | 1 | 1 |
| Polyphenol oxidase 2 | Agaricus bisporus | IC50 | 850.0000 | 1 | 1 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 2,398.8300 | 1 | 1 |
| Prostaglandin G/H synthase 1 | Homo sapiens (human) | IC50 | 13.2000 | 1 | 1 |
| Prostaglandin G/H synthase 1 | Ovis aries (sheep) | IC50 | 16.1667 | 3 | 3 |
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | IC50 | 1.0510 | 4 | 4 |
| Riboflavin-binding protein | Gallus gallus (chicken) | Ki | 0.3500 | 1 | 1 |
| Serum paraoxonase/arylesterase 1 | Homo sapiens (human) | Ki | 291.0000 | 1 | 1 |
| Solute carrier family 15 member 1 | Homo sapiens (human) | Ki | 790.0000 | 1 | 1 |
| Solute carrier family 15 member 1 | Rattus norvegicus (Norway rat) | Ki | 2,200.0000 | 1 | 1 |
| Solute carrier family 15 member 2 | Rattus norvegicus (Norway rat) | Ki | 230.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | IC50 | 60.0000 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 1.6062 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | Ki | 0.5356 | 1 | 1 |
| Thiosulfate sulfurtransferase | Homo sapiens (human) | IC50 | 8.8000 | 1 | 1 |
| Thymidine kinase | Macacine alphaherpesvirus 1 | IC50 | 900.0000 | 1 | 1 |
| Tubulin alpha-1A chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin alpha-1B chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin alpha-1C chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin alpha-3C chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin alpha-3E chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin alpha-4A chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-1 chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-2A chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-2B chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-3 chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-4A chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-4B chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-6 chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| Tubulin beta-8 chain | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 2-C-methyl-D-erythritol 2,4-cyclodiphosphate synthase | Escherichia coli K-12 | Kd | 40,000.0000 | 1 | 1 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 | 3.0800 | 1 | 2 |
| Chain A, 6,7-Dimethyl-8-ribityllumazine Synthase | Schizosaccharomyces pombe (fission yeast) | Kd | 1.2000 | 1 | 1 |
| Chain A, DODECIN | Halobacterium salinarum R1 | Kd | 1.2680 | 1 | 2 |
| Chain A, DODECIN | Halorhodospira halophila | Kd | 1.2680 | 1 | 2 |
| Chain B, 6,7-Dimethyl-8-ribityllumazine Synthase | Schizosaccharomyces pombe (fission yeast) | Kd | 1.2000 | 1 | 1 |
| Chain C, DODECIN | Halorhodospira halophila | Kd | 1.2680 | 1 | 2 |
| Chain E, DODECIN | Halorhodospira halophila | Kd | 1.2680 | 1 | 2 |
| Chain H, Immunoglobulin Igg1 Heavy chain | Homo sapiens (human) | Kd | 0.0018 | 1 | 1 |
| Chain L, Immunoglobulin Igg1 Lambda Light Chain | Homo sapiens (human) | Kd | 0.0018 | 1 | 1 |
| Complement C5 | Homo sapiens (human) | Kd | 0.5800 | 1 | 1 |
| Cytochrome P450 2A13 | Homo sapiens (human) | Kd | 1.6000 | 1 | 1 |
| Cytochrome P450 2A6 | Homo sapiens (human) | Kd | 11.0000 | 1 | 1 |
| DNA-(apurinic or apyrimidinic site) endonuclease | Homo sapiens (human) | Kd | 0.0890 | 1 | 1 |
| NPYLR7B | Aedes aegypti (yellow fever mosquito) | EC50 | 0.5080 | 1 | 1 |
| Polyphenol oxidase 2 | Agaricus bisporus | EC50 | 14.8000 | 1 | 1 |
| Procathepsin L | Homo sapiens (human) | EC50 | 3.0800 | 1 | 2 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 | 3.0800 | 1 | 2 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 | 3.0800 | 1 | 2 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 | 3.0800 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 3.0800 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 3.0800 | 1 | 2 |
| Riboflavin-binding protein | Gallus gallus (chicken) | Kd | 0.0229 | 4 | 4 |
| Spike glycoprotein | Betacoronavirus England 1 | EC50 | 3.0800 | 1 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 | 3.0800 | 1 | 2 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 | 3.0800 | 1 | 2 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 3-alpha-hydroxysteroid dehydrogenase | Rattus norvegicus (Norway rat) | Km | 10,400.0000 | 1 | 1 |
| AAA family ATPase | Staphylococcus aureus | Km | 192.0000 | 1 | 1 |
| Cytidine deaminase | Homo sapiens (human) | Km | 600.6667 | 3 | 3 |
| Deoxycytidine kinase | Homo sapiens (human) | Km | 1.7750 | 2 | 2 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | Km | 54.0000 | 3 | 3 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | Km | 238.0000 | 1 | 1 |
| Thymidine kinase | Vaccinia virus WR | Km | 158.0000 | 1 | 1 |