Cefsulodin: A pyridinium-substituted semisynthetic, broad-spectrum antibacterial used especially for Pseudomonas infections in debilitated patients. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
cefsulodin : A pyridinium-substituted semi-synthetic, broad-spectrum, cephalosporin antibiotic. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 656575 |
| CHEMBL ID | 3351077 |
| CHEBI ID | 3507 |
| SCHEMBL ID | 65525 |
| MeSH ID | M0003727 |
| PubMed CID | 24776146 |
| MeSH ID | M0003727 |
| Synonym |
|---|
| cefsulodinum |
| cefsulodino |
| 7beta-{[(2r)-2-phenyl-2-sulfoacetyl]amino}-3-(4-carbamoylpyridinium-1-yl)methyl-3,4-didehydrocepham-4-carboxylate |
| CHEBI:3507 , |
| (6r,7r)-3-[(4-carbamoylpyridinium-1-yl)methyl]-8-oxo-7-{[(2r)-2-phenyl-2-sulfoacetyl]amino}-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate |
| cefsulodine |
| cefsulodin (inn) |
| D07653 |
| cefsulodin |
| cefsulodino [inn-spanish] |
| (6r,7r)-3-((4-carbamoylpyridinio)methyl)-8-oxo-7-((r)-2-phenyl-2-sulfoacetamido)-5-thia-1-azabicyclo(4.2.0)oct-2-en-2-carboxylat |
| cgp-7174-e |
| pyridinium, 4-(aminocarbonyl)-1-((2-carboxy-8-oxo-7-((phenylsulfoacetyl)amino)-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methyl)-, inner salt, (6r-(6alpha,7beta(r*)))- |
| cefsulodine [inn-french] |
| cefsulodinum [inn-latin] |
| 4-carbamoyl-1-(((6r,7r)-2-carboxy-8-oxo-7-((2r)-2-phenyl-2-sulfoacetaido)-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methyl)pyridinium hydroxide, inner salt |
| cefsulodin [inn:ban] |
| (6r,7r)-3-[(4-carbamoylpyridin-1-ium-1-yl)methyl]-8-oxo-7-[[(2r)-2-phenyl-2-sulfoacetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate |
| unii-ov42lhe42b |
| ov42lhe42b , |
| EPITOPE ID:120379 |
| cefsulodin [who-dd] |
| 4-carbamoyl-1-(((6r,7r)-2-carboxy-8-oxo-7-((2r)-2-phenyl-2-sulfoacetamido)-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methylpyridinium hydroxide, inner salt |
| cefsulodin [jan] |
| j01dd03 |
| cefsulodin [inn] |
| cefsulodin [mi] |
| SCHEMBL65525 |
| DTXSID6022769 |
| CHEMBL3351077 |
| DB13499 |
| gtpl10783 |
| cgp7174/e |
| cefonomil |
| 52152-93-9 |
| AB00513925 |
| 62587-73-9 |
| NCGC00162106-02 |
| cefsulodin sodium salt hydrate |
| NCGC00162106-01 |
| NCGC00162106-03 |
| CCG-204354 |
| NCGC00162106-07 |
| NCGC00162106-17 |
| (6r,7r)-3-[(4-carbamoylpyridin-1-ium-1-yl)methyl]-8-oxo-7-[[(2r)-2-phenyl-2-sulfonatoacetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate |
| sodium;(6s,7r)-3-[(4-carbamoylpyridin-1-ium-1-yl)methyl]-8-oxo-7-[[(2s)-2-phenyl-2-sulfonatoacetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate |
Cefsulodin is a cephalosporin with a spectrum of antibacterial activity largely limited to Pseudomonas aeruginosa and Staphylococcus aureus. It contains a pyridinomethyl substituent at position 3 of the dihydrothiazine ring and a sulfo group on the acyl side chain.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cefsulodin (SCE-129) is a cephalosporin with a spectrum of antibacterial activity largely limited to Pseudomonas aeruginosa and Staphylococcus aureus. " | ( Cefsulodin: antibacterial activity and tentative interpretive zone standards for the disk susceptibility test. Barry, AL; Jones, RN; Thornsberry, C, 1981) | 3.15 |
| "Cefsulodin is a narrow-spectrum cephalosporin with activity against Staphylococcus aureus and Ps." | ( Cefsulodin and ceftazidime, two antipseudomonal cephalosporins. Smith, BR, ) | 2.3 |
| "Cefsulodin sodium is a narrow-spectrum cephalosporin with marked in vitro activity against clinical isolates of Pseudomonas aeruginosa. " | ( Cefsulodin sodium therapy in cystic fibrosis patients. Cabezudo, I; Guenthner, SH; Selden, RF; Thompson, RL; Wenzel, RP, 1984) | 3.15 |
| "Cefsulodin is a novel cephalosporin that contains a pyridinomethyl substituent at position 3 of the dihydrothiazine ring and a sulfo group on the acyl side chain. " | ( Activity of cefsulodin and other agents against Pseudomonas aeruginosa. Neu, HC; Scully, BE, ) | 1.95 |
| "Cefsulodin is a useful agent for the treatment of chronic osteomyelitis associated with P." | ( Cefsulodin therapy for osteomyelitis due to Pseudomonas aeruginosa. Karakusis, PH; Pottage, JC; Trenholme, GM, ) | 2.3 |
| "Cefsulodin appears to be an effective agent for the treatment of selected patients with invasive external otitis." | ( Treatment of invasive external otitis with cefsulodin. Hirschman, SZ; Mendelson, MH; Meyers, BR; Parisier, SC; Shapiro, ER, ) | 1.12 |
| "Cefsulodin is a third-generation cephalosporin with a unique specificity for Pseudomonas aeruginosa. " | ( Determination of cefsulodin in biological fluids by high-pressure liquid chromatography. Ackers, IM; Blumer, JL; Myers, CM, 1984) | 2.05 |
| "Cefsulodin is a new second generation cephalosporin with a narrow antibacterial spectrum. " | ( [Cefsulodin, a new antibiotic of the group of cephalosporins: its action on Pseudomonas aeruginosa (author's transl)]. Foz, A; Fuster, C; Roy, C; Segura, C; Tirado, M, 1981) | 2.62 |
| "Cefsulodin thus appears to be an effective alternative to carbenicillin in the treatment of severe P." | ( Treatment of pulmonary Pseudomonas aeruginosa infection in cystic fibrosis with cefsulodin. Jensen, K; Koch, C; Møller, NE; Vesterhauge, S, 1982) | 1.21 |
| "Cefsulodin is a third generation cephalosporin with specific antipseudomonas activity. " | ( [Treatment of superinfections caused by pyocyanic bacillus in patients with mucoviscidosis. Efficacy of cefsulodin in combination with an aminoglycoside]. Jehanne, M, 1989) | 1.93 |
| "Cefsulodin is a narrow-spectrum, third-generation cephalosporin with activity virtually restricted to Pseudomonas aeruginosa." | ( Cefsulodin. Wright, DB, 1986) | 2.44 |
Cefsulodin has a high affinity for penicillin-binding proteins of Pseudomonas aeruginosa. It binds poorly to those of other bacteria.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cefsulodin has a high affinity for penicillin-binding proteins of Pseudomonas aeruginosa but binds poorly to those of other bacteria." | ( Activity of cefsulodin and other agents against Pseudomonas aeruginosa. Neu, HC; Scully, BE, ) | 1.23 |
| "Cefsulodin has been used successfully in the treatment of various Ps." | ( Cefsulodin and ceftazidime, two antipseudomonal cephalosporins. Smith, BR, ) | 2.3 |
| "Cefsulodin has a high affinity for penicillin-binding proteins of Pseudomonas aeruginosa but binds poorly to those of other bacteria." | ( Activity of cefsulodin and other agents against Pseudomonas aeruginosa. Neu, HC; Scully, BE, ) | 1.23 |
Simultaneous administration of cefotiam and cefsulodin does not alter the pharmacokinetic parameters of either compound.
The in-vitro activity of cefsulodin combined with sulbactam, cefoxitin or cefotaxime was investigated against 32 strains of beta-lactamase-producing Bacteroides species. The present study shows the interest of use in combination with aminoglycosides in this pathology.
| Excerpt | Reference | Relevance |
|---|---|---|
| " We used cefsulodin in combination with aminoglycosides in 15 cystic fibrosis patients treatments." | ( [Treatment of superinfections caused by pyocyanic bacillus in patients with mucoviscidosis. Efficacy of cefsulodin in combination with an aminoglycoside]. Jehanne, M, 1989) | 0.91 |
| " The present study shows the interest of cefsulodin use in combination with aminoglycosides in this pathology." | ( [Treatment of superinfections caused by pyocyanic bacillus in patients with mucoviscidosis. Efficacy of cefsulodin in combination with an aminoglycoside]. Jehanne, M, 1989) | 0.76 |
| "The in-vitro activity of cefsulodin combined with sulbactam, cefoxitin or cefotaxime was investigated against 32 strains of beta-lactamase-producing Bacteroides species." | ( Synergistic activity of cefsulodin combined with cefoxitin and sulbactam against Bacteroides species. Fu, KP; Kimble, EF; Konopka, EA; Zoganas, H, 1984) | 0.88 |
| "The activities of ticarcillin, cefsulodin, ceftazidime, aztreonam, and imipenem, formerly known as N-formimidoyl thienamycin, were evaluated alone and in combination with aminoglycosides against 56 clinical isolates of Pseudomonas aeruginosa, which were characterized by aminoglycoside susceptibility and content of aminoglycoside-modifying enzymatic activities." | ( Effect of highly potent antipseudomonal beta-lactam agents alone and in combination with aminoglycosides against Pseudomonas aeruginosa. Berndt, KD; Boisvert, WE; Dudek, EJ; Lerner, SA, ) | 0.42 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cefpiramide (SR 95445) (CPM) is a new cephalosporin with activity against Pseudomonas and a good bioavailability following parenteral administration." | ( [Beta-lactamase induction in Pseudomonas aeruginosa by cefpiramide and 3 other antipyocyanic cephalosporins]. Combes, T; Drigues, P; Lanau, C; Roche, G; Salhi, A, 1986) | 0.27 |
Daily dosage of cefsulodin was usually 60-100 mg/kg of body weight given in three to four divided doses. While progressive renal failure slows the elimination, there is a linear relationship between elimination and GFR such that dosage nomograms can be developed.
| Excerpt | Relevance | Reference |
|---|---|---|
| " It appeared, therefore, that this dosage regimen was useful for the treatment of refractory complicated urinary tract infection." | ( [Concomitant therapy with cefmenoxime and cefsulodin for refractory complicated urinary tract infection (especially caused by Pseudomonas aeruginosa)]. Arakawa, S; Fujii, A; Harada, M; Ishigami, J; Kamidono, S; Kataoka, N; Kawabata, G; Miyazaki, S; Takasaki, N; Umezu, K, 1986) | 0.54 |
| " These sensitivities seem good enough for a clinical application of the method considering usual dosage levels of the drugs." | ( [High performance liquid chromatographic determination of astromicin and cefsulodin used in combination in blood samples]. Inoue, A; Kobayashi, S; Takai, K, 1986) | 0.5 |
| " The antibiotic dosage was calculated so that the serum level remained constant for a given period of time." | ( [Intraocular penetration of systemically administered cephalosporins under steady-state conditions in animal experiments]. Mendel, N; Mester, U; Völker, B, 1985) | 0.27 |
| " These results suggest that the pharmacokinetics of the two drugs are not modified by their simultaneous administration and that the dosing schedule previously proposed for administration of the two cephalosporins alone in the presence of renal insufficiency can be applied without modification when they are given together." | ( Pharmacokinetics of cefotiam and cefsulodin after simultaneous administration to patients with impaired renal function. Binswanger, U; Guibert, J; Lecaillon, JB; Rouan, MC; Schoeller, JP, 1984) | 0.55 |
| " These zone standards are still tentative since the dosage schedule has not yet been defined and sufficient clinical experience has not yet been gathered to support the validity of these MIC breakpoints." | ( Cefsulodin: antibacterial activity and tentative interpretive zone standards for the disk susceptibility test. Barry, AL; Jones, RN; Thornsberry, C, 1981) | 1.71 |
| " Based on CFS pharmacokinetic data and the recommended dosage schedule (less than 2 g a day), MIC break points less than 3 micrograms/ml and less than 15 micrograms/ml, appear to be more useful than that of less than or equal to 8 micrograms/ml and less than 32 micrograms/ml for evaluating a proper administrative dose level." | ( [Clinical laboratory approach for estimating effective administrative dose of cefsulodin]. Matsuo, K; Uete, T, 1984) | 0.5 |
| " While progressive renal failure slows the elimination of cefsulodin, there is a linear relationship between elimination of cefsulodin and GFR such that dosage nomograms can be developed." | ( Kinetics of cefsulodin in patients with renal impairment. Gibson, TP; Granneman, GR; Kallal, JE; Sennello, LT, ) | 0.75 |
| " Daily dosage of cefsulodin was usually 60-100 mg/kg of body weight given in three to four divided doses." | ( Clinical and pharmacokinetic study of parenteral administration of cefsulodin in pediatric patients in Japan. Fujii, R; Nishimura, T, ) | 0.71 |
| "9566) can be utilized to revise dosage schedules for patients with any degree of renal impairment." | ( Cefsulodin pharmacokinetics in patients with various degrees of renal function. Keane, WF; Matzke, GR, 1983) | 1.71 |
| " As the measured perilymph concentrations of cefsulodin and gentamicin are comparable on a weight for weight basis and as the clinical dosage of cefsulodin is much higher than that of gentamicin, the perilymph concentrations of cefsulodin reached in man are probably much higher than those of gentamicin." | ( Cefsulodin pharmacokinetics and otitis media. Federspil, P; Schätzle, W; Tiesler, E, 1982) | 1.97 |
| " aeruginosa and administration and dosage of CFS was 47 to 86 mg/kg/day, 2 to 4 times daily by intravenous injection or intravenous drip infusion for 5 to 11 days." | ( [Clinical studies of cefsulodin in the pediatric field]. Hachimori, K; Minamitani, M; Suzuki, M, 1982) | 0.58 |
| " Typically, promising compounds are identified in a primary screen and then more fully characterized in a dose-response analysis with 7-10 data points per compound." | ( High-resolution dose-response screening using droplet-based microfluidics. Baret, JC; Dieu, P; El Debs, B; El Harrak, A; Frenz, L; Galvan, M; Griffiths, AD; Link, DR; Mangeat, T; Mayot, E; Miller, OJ; Rooney, EK; Samuels, ML, 2012) | 0.38 |
| Role | Description |
|---|---|
| antibacterial drug | A drug used to treat or prevent bacterial infections. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| cephalosporin | A class of beta-lactam antibiotics differing from the penicillins in having a 6-membered, rather than a 5-membered, side ring. Although cephalosporins are among the most commonly used antibiotics in the treatment of routine infections, and their use is increasing over time, they can cause a range of hypersensitivity reactions, from mild, delayed-onset cutaneous reactions to life-threatening anaphylaxis in patients with immunoglobulin E (IgE)-mediated allergy. |
| primary carboxamide | A carboxamide resulting from the formal condensation of a carboxylic acid with ammonia; formula RC(=O)NH2. |
| organosulfonic acid | An organic derivative of sulfonic acid in which the sulfo group is linked directly to carbon. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| peptidoglycan maturation (meso-diaminopimelate containing) | 16 | 41 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 5.3289 | 0.1000 | 20.8793 | 79.4328 | AID488773; AID588453 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 15.0030 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.7686 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 70.7946 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 50.1187 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 9.5283 | 0.4256 | 12.0591 | 28.1838 | AID504536 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 26.6795 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 5.3582 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
| [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) |
|---|---|---|---|---|---|---|---|
| Receptor-type tyrosine-protein phosphatase F | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 1.3000 | 2.6660 | 4.2300 | AID1242494 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 (µMol) | 190.0000 | 0.0005 | 3.4984 | 9.7600 | AID1242485 |
| Receptor-type tyrosine-protein phosphatase alpha | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 4.6000 | 4.6000 | 4.6000 | AID1242489 |
| Receptor-type tyrosine-protein phosphatase beta | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 0.0000 | 0.0000 | 0.0000 | AID1242490 |
| Low molecular weight phosphotyrosine protein phosphatase | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 2.8600 | 9.6336 | 17.2000 | AID1242497 |
| Tyrosine-protein phosphatase non-receptor type 6 | Homo sapiens (human) | IC50 (µMol) | 21.0000 | 0.2900 | 2.2075 | 4.2300 | AID1242484 |
| Solute carrier family 15 member 1 | Homo sapiens (human) | Ki | 30,000.0000 | 0.1800 | 3.3933 | 9.8000 | AID681115 |
| Dual specificity protein phosphatase 3 | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 4.0000 | 5.9750 | 8.5000 | AID1242495 |
| Tyrosine-protein phosphatase non-receptor type 11 | Homo sapiens (human) | IC50 (µMol) | 16.8000 | 0.3180 | 4.0042 | 9.6000 | AID1242483 |
| Tyrosine-protein phosphatase non-receptor type 11 | Homo sapiens (human) | Ki | 6.6000 | 5.2000 | 5.9000 | 6.6000 | AID1242499 |
| Solute carrier family 15 member 2 | Rattus norvegicus (Norway rat) | Ki | 30,000.0000 | 3.0000 | 6.4778 | 8.5000 | AID681114 |
| Tyrosine-protein phosphatase non-receptor type 22 | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 1.1000 | 4.6900 | 9.5400 | AID1242486 |
| Lethal(3)malignant brain tumor-like protein 1 | Homo sapiens (human) | IC50 (µMol) | 0.0980 | 0.0980 | 4.2996 | 8.9000 | AID1506809 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1242499 | Competitive inhibition of phosphatase activity of SHP2 (unknown origin) using pNPP as a substrate Lineweaver-Burk plot analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1506809 | Inhibition of L3MBTL1 (unknown origin) by AlphaScreen assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Methyllysine binding domains: Structural insight and small molecule probe development. |
| AID1242487 | Inhibition of phosphatase activity of human HePTP using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242484 | Inhibition of phosphatase activity of human SHP1 using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242486 | Inhibition of phosphatase activity of human LYP using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1209735 | Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics. |
| AID1242493 | Inhibition of phosphatase activity of human PTPmu using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242483 | Inhibition of phosphatase activity of SHP2 (unknown origin) using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID681682 | TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, Cefsulodin: 500 uM) in OCTN2-expressing HEK293 cells | 1999 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2 | Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1242502 | Selectivity ratio of IC50 for human HePTP to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242509 | Selectivity ratio of IC50 for human LAR to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242511 | Selectivity ratio of IC50 for human CDC14A to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242496 | Inhibition of phosphatase activity of human CDC14A using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242494 | Inhibition of phosphatase activity of human LAR using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID1209736 | Inhibition of human OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics. |
| AID1242489 | Inhibition of phosphatase activity of human PTPalpha using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242513 | Selectivity ratio of IC50 for human PP5 to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID660263 | Ratio of MIC for wild type Salmonella typhimurium SH5014 to MIC for Salmonella typhimurium SH7616 harboring missense mutation in acrA/acrB gene by two-fold serial dilution method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1242490 | Inhibition of phosphatase activity of human PTPbeta using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1242505 | Selectivity ratio of IC50 for human PTPbeta to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242485 | Inhibition of phosphatase activity of human PTP1B using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242495 | Inhibition of phosphatase activity of human VHR using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1242500 | Selectivity ratio of IC50 for human PTP1B to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242497 | Inhibition of phosphatase activity of human LMWPTP using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1242506 | Selectivity ratio of IC50 for human PTPepsilon to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242491 | Inhibition of phosphatase activity of human PTPepsilon using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242503 | Selectivity ratio of IC50 for human Meg2 to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242504 | Selectivity ratio of IC50 for human PTPalpha to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1209734 | Inhibition of mouse OAT1 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics. |
| AID681114 | TP_TRANSPORTER: inhibition of Gly-Sar uptake (pH6.0) in SKPT cells | 2005 | European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, Jan, Volume: 59, Issue:1 | Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID681115 | TP_TRANSPORTER: inhibition of Gly-Sar uptake (pH6.0) in Caco-2 cells | 2005 | European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, Jan, Volume: 59, Issue:1 | Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1. |
| AID660261 | Ratio of MIC for wild type Escherichia coli JC7623 to MIC for acrAB-deficient Escherichia coli JZM120 | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics. |
| AID1209733 | Binding affinity to mouse OAT3 expressed in CHO cells at 10 to 1000 uM measured over 20 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1242488 | Inhibition of phosphatase activity of human Meg2 using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242501 | Selectivity ratio of IC50 for human LYP to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1242512 | Selectivity ratio of IC50 for human LMWPTP to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242508 | Selectivity ratio of IC50 for human PTPmu to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1242507 | Selectivity ratio of IC50 for human PTPgamma to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID1242510 | Selectivity ratio of IC50 for human VHR to IC50 for SHP2 (unknown origin) | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1242492 | Inhibition of phosphatase activity of human PTPgamma using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID660265 | Antimicrobial activity against wild type Escherichia coli expressing AcrAB-TolC efflux pump | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics. |
| AID1242498 | Inhibition of phosphatase activity of human PP5 using pNPP as a substrate after 10 mins by spectrophotometer analysis | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7 | Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| 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. |
| 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. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| 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. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| 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. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| 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. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 195 (73.31) | 18.7374 |
| 1990's | 27 (10.15) | 18.2507 |
| 2000's | 15 (5.64) | 29.6817 |
| 2010's | 20 (7.52) | 24.3611 |
| 2020's | 9 (3.38) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (33.86) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 17 (6.09%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 11 (3.94%) | 6.00% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 16 (5.73%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 235 (84.23%) | 84.16% |
| Other | 11 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||