lomofungin: antibiotic obtained from Streptomyces species; reported effective against bacteria as well as fungi & yeasts; probably inhibits nucleic acid & protein synthesis; minor descriptor (76-85); on-line & Index Medicus search PHENAZINES (76-85) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 135426834 |
| SCHEMBL ID | 14973446 |
| SCHEMBL ID | 393820 |
| MeSH ID | M0262982 |
| Synonym |
|---|
| AB00642035-09 |
| NCIMECH_000010 |
| SMP2_000090 |
| D04767 |
| lomondomycin |
| lomofungin |
| 1-phenazinecarboxylic acid,7,9-trihydroxy-, methyl ester |
| methyl 6-formyl-4,9-trihydroxy-1-phenazinecarboxylate |
| nsc106995 , |
| 26786-84-5 |
| mls002701957 , |
| mls000766240 , |
| nsc156939 |
| NCGC00160392-01 |
| NCGC00160392-02 |
| smr000528852 |
| NCI60_000168 |
| HMS2089A15 |
| methyl 6-formyl-4,7-dihydroxy-9-oxo-5h-phenazine-1-carboxylate |
| NCGC00160392-03 |
| CCG-35333 |
| A245 |
| glycopeptide, 4 |
| methyl 6-methanoyl-4,7-bis(oxidanyl)-9-oxidanylidene-5h-phenazine-1-carboxylate |
| 6-formyl-4,7-dihydroxy-9-oxo-5h-phenazine-1-carboxylic acid methyl ester |
| cid_5351222 |
| 6-formyl-4,7-dihydroxy-9-keto-5h-phenazine-1-carboxylic acid methyl ester |
| bdbm43865 |
| SCHEMBL14973446 |
| SCHEMBL393820 |
| sr-01000762031 |
| SR-01000762031-2 |
| methyl 6-formyl-4,7,9-trihydroxyphenazine-1-carboxylate |
| methyl (6z)-7-hydroxy-6-(hydroxymethylidene)-4,9-dioxo-10h-phenazine-1-carboxylate |
| A937080 |
| DTXSID90949590 |
| Excerpt | Reference |
|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 22.9833 | 0.0032 | 45.4673 | 12,589.2998 | AID2517; AID2572 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 0.1000 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 56.2341 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 0.6310 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 8.9125 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 39.8107 | 0.1259 | 19.1169 | 125.8920 | AID2549 |
| endonuclease IV | Escherichia coli | Potency | 22.3872 | 0.7079 | 12.4324 | 31.6228 | AID2565 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 56.2341 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| WRN | Homo sapiens (human) | Potency | 63.0957 | 0.1683 | 31.2583 | 100.0000 | AID651768 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 44.6684 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0810 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 31.6228 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
| GLS protein | Homo sapiens (human) | Potency | 5.0119 | 0.3548 | 7.9355 | 39.8107 | AID624170 |
| TDP1 protein | Homo sapiens (human) | Potency | 24.8446 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 50.1187 | 0.1000 | 22.9075 | 100.0000 | AID485364 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 1.2589 | 0.7079 | 12.1943 | 39.8107 | AID720542 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 35.4813 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 0.7079 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.7943 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 17.7828 | 0.5406 | 17.6392 | 96.1227 | AID2528 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 22.5358 | 0.0100 | 39.5371 | 1,122.0200 | AID1469; AID1479 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 50.1187 | 5.8048 | 36.1306 | 65.1308 | AID540263 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 39.8107 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 18.8876 | 0.1683 | 16.4040 | 67.0158 | AID720504 |
| snurportin-1 | Homo sapiens (human) | Potency | 50.1187 | 5.8048 | 36.1306 | 65.1308 | AID540263 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 7.0795 | 0.4256 | 12.0591 | 28.1838 | AID504891 |
| tumor susceptibility gene 101 protein | Homo sapiens (human) | Potency | 79.4328 | 0.1298 | 10.8331 | 32.6090 | AID493005 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 2.8184 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| geminin | Homo sapiens (human) | Potency | 8.1995 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 2.2864 | 0.0041 | 9.9625 | 28.1838 | AID2675; AID493199; AID493205 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 79.4328 | 6.3096 | 60.2008 | 112.2020 | AID720709 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 0.0141 | 8.6024 | 39.8107 | AID2572 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 0.0015 | 51.7393 | 15,848.9004 | AID2572 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 0.0141 | 8.6024 | 39.8107 | AID2572 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 0.0141 | 8.6024 | 39.8107 | AID2572 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Mcl-1 | Homo sapiens (human) | IC50 (µMol) | 3.4951 | 0.4000 | 7.1344 | 54.0000 | AID1417; AID1418 |
| RAD51 | Homo sapiens (human) | IC50 (µMol) | 33.6700 | 1.3990 | 17.7214 | 32.1000 | AID1436; AID1437 |
| microphthalmia-associated transcription factor isoform 9 | Homo sapiens (human) | IC50 (µMol) | 2.1348 | 0.0048 | 1.3710 | 4.9290 | AID1259371; AID1259373; AID1259375 |
| dual specificity protein phosphatase 3 | Homo sapiens (human) | IC50 (µMol) | 1.6450 | 0.4000 | 9.3610 | 90.0000 | AID1654; AID1878 |
| Vif | Human immunodeficiency virus 1 | IC50 (µMol) | 0.3500 | 0.2700 | 34.0015 | 100.0000 | AID1117319 |
| Tat | Human immunodeficiency virus 1 | IC50 (µMol) | 20.3430 | 0.9960 | 39.8009 | 100.0000 | AID1117361 |
| DNA dC->dU-editing enzyme APOBEC-3G isoform 1 | Homo sapiens (human) | IC50 (µMol) | 0.3500 | 0.2700 | 26.3638 | 100.0000 | AID1117319 |
| dual specificity protein phosphatase 6 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 48.2000 | 0.8320 | 24.1190 | 48.2000 | AID425 |
| Renin | Homo sapiens (human) | IC50 (µMol) | 2.0600 | 0.0000 | 0.7796 | 8.2000 | AID1654 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.2300 | 0.0005 | 2.7739 | 25.1700 | AID1418 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.2300 | 0.0005 | 2.8919 | 25.1700 | AID1418 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.2300 | 0.0005 | 2.7478 | 25.1700 | AID1418 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.2300 | 0.0005 | 2.7802 | 25.1700 | AID1418 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 3.2300 | 0.0005 | 3.3142 | 49.5000 | AID1418 |
| Dolichyl-diphosphooligosaccharide--protein glycosyltransferase subunit 1 | Saccharomyces cerevisiae S288C | Ki | 0.0620 | 0.0410 | 1.3677 | 4.0000 | AID1799481 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| guanyl-nucleotide exchange factor activity | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| protein binding | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| protein domain specific binding | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| cAMP binding | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| aspartic-type endopeptidase activity | Renin | Homo sapiens (human) |
| signaling receptor binding | Renin | Homo sapiens (human) |
| insulin-like growth factor receptor binding | Renin | Homo sapiens (human) |
| protein binding | Renin | Homo sapiens (human) |
| peptidase activity | Renin | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1799481 | Competition Assay from Article 10.1016/S1074-5521(02)00281-8: \\Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition.\\ | 2002 | Chemistry & biology, Dec, Volume: 9, Issue:12 | Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (14.29) | 29.6817 |
| 2010's | 10 (71.43) | 24.3611 |
| 2020's | 2 (14.29) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||