An EC 2.7.7.* (nucleotidyltransferase) inhibitor that interferes with the action of RNA polymerase (EC 2.7.7.6).
ChEBI ID: 37416
| Member | Definition | Class |
|---|---|---|
| acetopyrrothine | A dithiolopyrrolone antibiotic that is 4,5-dihydro[1,2]dithiolo[4,3-b]pyrrole in which the hydrogens at positions 4,5 and 6 have been replaced by methyl, oxo and acetamido groups, respectively. It is a potent inhibitor of RNA polymerases, inhibits the angiogenesis of human umbilical vein endothelial cells, and also inhibits JAMM metalloproteases. | thiolutin |
| aureothricin | A dithiolopyrrolone antibiotic that is 4,5-dihydro[1,2]dithiolo[4,3-b]pyrrole in which the hydrogens at positions 4,5 and 6 have been replaced by methyl, oxo and propanoylamino groups, respectively. It is a moderate antimicrobial by-product of the thiolutin fermentation in various Streptomyces species. | aureothricin |
| cx 5461 | An organic heterotetracyclic compound that is 5-oxo-5H-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxylic acid substituted by a 4-methyl-1,4-diazepan-1-yl group at position 2 and in which the carboxy group at position 6 is substituted by a [(5-methylpyrazin-2-yl)methyl]nitrilo group. An inhibitor of ribosomal RNA (rRNA) synthesis which specifically inhibits RNA polymerase I-driven transcription of rRNA in several cancer cell lines. It is currently in phase I/II clinical trials for advanced hematologic malignancies and triple-negative breast cancer with BRCA1/2 mutation. | CX-5461 |
| holomycin | A dithiolopyrrolone antibiotic that is 4,5-dihydro[1,2]dithiolo[4,3-b]pyrrole in which the hydrogens at positions 5 and 6 have been replaced by oxo and acetamido groups, respectively. It is an inhibitor of DNA-dependent RNA polymerase, and exhibits antibacterial and antitumour properties. | holomycin |
| opt 80 | An 18-membered macrolide that is a fermentation product obtained from the Actinomycete Dactylosporangium aurantiacum. A narrow spectrum antibiotic used for treatment of Clostridium difficile-related infections. | fidaxomicin |
| rifampin | A member of the class of rifamycins that is a a semisynthetic antibiotic derived from Amycolatopsis rifamycinica (previously known as Amycolatopsis mediterranei and Streptomyces mediterranei). | rifampicin zwitterion; rifampicin |
| sch 642305 | A macrocyclic lactone isolated from the fermentation broth of the fungal culture Penicillium verrucosum and has been shown to exhibit inhibitory activity against bacterial DNA primase enzyme. | sch 642305 |
| streptolydigin | A monocarboxylic acid amide that is a broad-spectrum antibiotic produced by Streptomyces lydicus. | streptolydigin |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 6,093 (31.54) | 18.7374 |
| 1990's | 2,525 (13.07) | 18.2507 |
| 2000's | 3,517 (18.21) | 29.6817 |
| 2010's | 5,224 (27.04) | 24.3611 |
| 2020's | 1,957 (10.13) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,504 (7.25%) | 5.53% |
| Reviews | 1,275 (6.15%) | 6.00% |
| Case Studies | 2,849 (13.74%) | 4.05% |
| Observational | 106 (0.51%) | 0.25% |
| Other | 14,998 (72.34%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 31.0990 | 2 | 2 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 12.5893 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 0.0050 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 5.2539 | 3 | 3 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 26.6320 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 31.6228 | 1 | 2 |
| interleukin 8 | Homo sapiens (human) | Potency | 66.8242 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 21.7515 | 2 | 3 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 64.7304 | 1 | 2 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 0.3246 | 2 | 2 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 17.7828 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 11.7031 | 1 | 2 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 2.2387 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 25.1189 | 2 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Albumin | Homo sapiens (human) | Kd | 12.0000 | 1 | 1 |
| Cytochrome P450 2B6 | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
| Mobilization protein A | Escherichia coli | EC50 | 70.0000 | 1 | 1 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 2.1656 | 9 | 9 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Arylacetamide deacetylase | Homo sapiens (human) | Km | 200.0000 | 1 | 2 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Km | 7.2500 | 2 | 2 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Km | 2.3000 | 1 | 1 |