sulmazole: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
sulmazole : An imidazopyridine that is 1H-imidazo[4,5-b]pyridine which is substituted at position 2 by a 2-methoxy-4-(methylsulfinyl)phenyl group. An A1 adenosine receptor antagonist, it was formerly used as a cardiotonic agent. [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 | 5353 |
| CHEMBL ID | 286020 |
| CHEBI ID | 34988 |
| SCHEMBL ID | 187165 |
| MeSH ID | M0094722 |
| Synonym |
|---|
| smr001233271 |
| MLS002153927 |
| BRD-A22081593-001-04-6 |
| BPBIO1_000707 |
| DIVK1C_000276 |
| KBIO1_000276 |
| vardax |
| 2-(2-methoxy-4-(methylsulfinyl)phenyl)-1h-imidazo(4,5-b)pyridine |
| sulmazolum [inn-latin] |
| sulmazole [inn] |
| ar-l 115bs |
| ar-l 115-bs |
| sulmazol |
| 1h-imidazo(4,5-b)pyridine, 2-(2-methoxy-4-(methylsulfinyl)phenyl)- |
| sulmazol [inn-spanish] |
| 2-(2-methoxy-4-(methylsulfinyl)phenyl)-3h-imidazo(4,5-b)pyridine |
| einecs 277-406-1 |
| brn 0818370 |
| ar-l-115-bs |
| SPECTRUM_001155 |
| IDI1_000276 |
| PRESTWICK3_000641 |
| PRESTWICK_1012 |
| cas-73384-60-8 |
| NCGC00016924-01 |
| BSPBIO_000641 |
| PRESTWICK2_000641 |
| BSPBIO_002286 |
| 73384-60-8 |
| sulmazole |
| AB00052230 |
| NCGC00095999-01 |
| KBIO2_001635 |
| KBIO2_004203 |
| KBIOGR_001772 |
| KBIO2_006771 |
| KBIOSS_001635 |
| KBIO3_001506 |
| PRESTWICK1_000641 |
| PRESTWICK0_000641 |
| SPECTRUM4_001246 |
| NINDS_000276 |
| SPECTRUM3_000733 |
| SPBIO_002562 |
| SPECTRUM1501159 |
| SPECTRUM5_002074 |
| 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1h-imidazo[4,5-b]pyridine |
| ar-l-115 |
| nsc-757867 |
| CHEMBL286020 , |
| chebi:34988 , |
| ar-l-115bs |
| HMS500N18 |
| HMS1570A03 |
| 2-methyl-6-oxo-1,6-dihydro-[3,4'']bipyridinyl-5-carbonitrile |
| 2-(4-methanesulfinyl-2-methoxy-phenyl)-1h-imidazo[4,5-b]pyridine |
| bdbm50000056 |
| (sulmazole)2-(4-methanesulfinyl-2-methoxy-phenyl)-3h-imidazo[4,5-b]pyridine |
| 2-(4-methanesulfinyl-2-methoxy-phenyl)-3h-imidazo[4,5-b]pyridine |
| 2-(4-methanesulfinyl-2-methoxy-phenyl)-1h-imidazo[4,5-b]pyridine(sulmazole) |
| 2-(4-methanesulfinyl-2-methoxy-phenyl)-1h-imidazo[4,5-b]pyridine (sulmazole) |
| 2-(2-methoxy-4-methylsulfinylphenyl)-1h-imidazo[4,5-b]pyridine |
| NCGC00016924-02 |
| HMS2097A03 |
| pharmakon1600-01501159 |
| nsc757867 |
| dtxcid9020617 |
| tox21_110685 |
| dtxsid1040617 , |
| HMS2230O09 |
| CCG-38446 |
| hk56eh9k44 , |
| unii-hk56eh9k44 |
| nsc 757867 |
| sulmazolum |
| 2-[2-methoxy-4-(methylsulfinyl)phenyl]-3h-imidazo[4,5-b]pyridine |
| sulmazole [mart.] |
| sulmazole [mi] |
| 3h-imidazo(4,5-b)pyridine, 2-(2-methoxy-4-(methylsulfinyl)phenyl)- |
| 3h-imidazo[4,5-b]pyridine,2-[2-methoxy-4-(methylsulfinyl)phenyl]- |
| HMS3371L17 |
| CCG-220641 |
| SCHEMBL187165 |
| XMFCOYRWYYXZMY-UHFFFAOYSA-N |
| 2-(2-methoxy-4-methylsulfinyl-phenyl)-1h-imidazo[4,5-b]pyridine |
| 2-(2-methoxy-4-(methylsulfinyl)phenyl)-3h-imidazo[4,5-b]pyridine |
| SR-01000841215-2 |
| sr-01000841215 |
| SR-01000841215-3 |
| SBI-0051668.P002 |
| HMS3714A03 |
| 2-(2-methoxy-4-(methylsulfinyl)phenyl)-1h-imidazo[4,5-b]pyridine |
| FT-0748740 |
| 2-(2-methoxy-4-[methylsulfinyl]phenyl)-1h-imidazo(4,5-b)pyridine |
| Q27116354 |
| bdbm50225309 |
| BRD-A22081593-001-06-1 |
| 2-methoxy-4-(methylsulfinyl)-phenylimidazo[4,5-b]pyridine |
| CS-0066237 |
| HY-116675 |
| AKOS040749578 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Sulmazole does not generate its positive inotropism by way of an increased slow inward current as do beta-adrenoceptor agonists but rather reduces the slow inward current by means of a negative shift of Eisi and a decrease in isi-driving force after it has affected intracellular calcium." | ( Effects of the new cardiotonic agent sulmazole on the slow inward current of sheep cardiac Purkinje fibres. Achenbach, C; Hauswirth, O; Wiemer, J; Ziskoven, R, 1984) | 1.26 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Present interest focuses on the development of new agents with sufficiently high oral bioavailability and long duration of action." | ( Pharmacological actions of various inotropic agents. Scholz, H, 1983) | 0.27 |
| "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) | 0.51 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " By contrast, carbachol did not alter the dose-response profile to AR-L57." | ( A comparison of the cardiotonic effects of AR-L115 and AR-L57: evidence for distinct inotropic mechanisms. Hayes, JS; Pollock, GD; Wilson, H; Wyss, VL, ) | 0.13 |
| " Ethylmorphine N-demethylation was decreased after dosing with the imidazo[4,5-b]pyridine-containing drug." | ( The induction profile of three orally active imidazopyridine-containing cardiotonic agents in rat hepatic microsomes. Bernstein, JR; Franklin, RB, 1986) | 0.27 |
| " The dose-response curves for synaptosomal 22Na uptake and for the inotropic effect on guinea pig left atria are parallel for sulmazole and the quinazolone drug, with first an increase and then a decrease in activity." | ( Effect of some new cardiotonic agents on synaptosomal sodium uptake. Decker, N; Grima, M; Schwartz, J, 1986) | 0.48 |
| " In either group, the dose-response curve of dP/dt to isoproterenol was shifted upward by AR-L, but the actions of the two drugs were additive without real synergism (e." | ( In vivo interaction of AR-L 115BS (Vardax) with the adrenergic nervous system. Cohn, JN; Francis, GS; From, AH; Petein, M; Pierpont, GL, ) | 0.13 |
| " The effect of sulmazol was greater than the effect of an increased dosage of dobutamine in five patients in whom this was studied." | ( Hemodynamic effects of sulmazol (ARL-115 BS), a new vasodilator and positive inotropic agent, in patients with cardiogenic shock. Hugenholtz, PG; Muskens, G; Simoons, ML, 1983) | 0.27 |
| " The dose-response curve of the inotropy and frequency was very similar in shape to that of theophylline as far as intensity of inotropy and the range of dosage is concerned, but AR-L 115 BS is 10 times as active." | ( [The effect of AR-L 115 BS on the function and oxygen consumption of isolated guinea pig atria as compared to g-strophanthin and theophylline]. Seifart, HJ; Siess, M; Stieler, K, 1981) | 0.26 |
| " In miniature pigs and rats this was only observed at high dosage (mini-pig: 10 and 30 mg/kg; rat: 200 mg/kg)." | ( [Animal studies on the tolerability of AR-L 115 BS (author's transl)]. Bauer, M; Eckenfels, A; Lehmann, H; Lützen, L; Schneider, P; Ueberberg, H, 1981) | 0.26 |
| Role | Description |
|---|---|
| cardiotonic drug | A drug that has a strengthening effect on the heart or that can increase cardiac output. |
| EC 3.1.4.* (phosphoric diester hydrolase) inhibitor | An EC 3.1.* (ester hydrolase) inhibitor that interferes with the action of a phosphoric diester hydrolase (EC 3.1.4.*). |
| adenosine A1 receptor antagonist | An antagonist at the A1 receptor. |
| [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 |
|---|---|
| imidazopyridine | |
| sulfoxide | An organosulfur compound having the structure R2S=O or R2C=S=O (R =/= H). |
| [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] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 10.0000 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 18.9338 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 18.9338 | 0.0251 | 20.2376 | 39.8107 | AID886; AID893 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 24.0682 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 14.1254 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 79.4328 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 20.3865 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 2.1132 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 18.8541 | 0.0018 | 15.6638 | 39.8107 | AID894 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 100.0000 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| transcriptional regulator ERG isoform 3 | Homo sapiens (human) | Potency | 60.4566 | 0.7943 | 21.2757 | 50.1187 | AID624246; AID651804 |
| geminin | Homo sapiens (human) | Potency | 0.8913 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 1.2589 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.2239 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| [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) |
|---|---|---|---|---|---|---|---|
| cGMP-dependent 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 0.0000 | 1.7767 | 9.2000 | AID158290 |
| cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 (µMol) | 21.0000 | 0.0000 | 1.1843 | 9.6140 | AID157161 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.2300 | 2.5105 | 10.0000 | AID158887 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.0000 | 2.1417 | 9.2000 | AID158887 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | IC50 (µMol) | 383.3333 | 0.0000 | 2.0724 | 10.0000 | AID157152; AID158302; AID158303 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Homo sapiens (human) | IC50 (µMol) | 1,000.0000 | 0.2300 | 1.9814 | 9.0000 | AID158887 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | IC50 (µMol) | 383.3333 | 0.0003 | 1.9901 | 10.0000 | AID157152; AID158302; AID158303 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| AID49059 | Response ratio = (percent increase to drug)/(percent increase to 10 E-4 M isoproterenol) | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| AID59623 | Percent change in mean arterial blood pressure in anesthetized dog | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| AID231469 | Relative positive inotropic activity (ED50) and PDE 3 inhibition (IC50) | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
| AID59592 | Maximum percentage change in dP/dt, diastolic blood pressure and heart rate produced by the compound at a dose 3.0 mg/kg | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID47761 | Inotropic activity in cat papillary muscle at 10e-5 M expressed as percent of control | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyrazines: the role of nitrogen position in inotropic activity. |
| AID49060 | Response ratio = (percent increase to drug)/(percent increase to 10 E-5 M isoproterenol) | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| AID157159 | In vitro inhibition of PDE-IV isolated from guinea pig ventricle at 100 uM. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
| AID59288 | In vivo hypotension in anesthetized dog, expressed as the dose of the drug producing a 25% decrease in diastolic arterial pressure (DAP) from control value. | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID60472 | In vivo hypotension in anesthetized dog expressed as % decrease in diastolic arterial pressure (DAP). | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID157154 | Percent inhibition of PDE 3 (phosphodiesterase III) from guinea pig ventricle at 10 uM (or 100 uM) | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
| AID157152 | Inhibition of PDE 3 (phosphodiesterase III) from guinea pig ventricle | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
| AID158302 | Inhibition of low Km cyclic cAMP phosphodiesterase PDE III of guinea pig ventricle | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. |
| AID219845 | Inhibition of dog left ventricle sarcoplasmic reticulum bound low-Km cAMP phosphodiesterase | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | A novel class of cardiotonic agents: synthesis and biological evaluation of 5-substituted 3,6-dihydrothiadiazin-2-ones with cyclic AMP phosphodiesterase inhibiting and myofibrillar calcium sensitizing properties. |
| AID59300 | The effective dose to produce the 30%decrease in diastolic blood pressure | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID76809 | Positive inotropic activity in isolated left guinea pig atria. | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | Cardiotonic agents. 1. Synthesis and structure-activity relationships in a new class of 3-, 4-, and 5-pyridyl-2(1H)-quinolone derivatives. |
| AID59727 | Maximum percentage increase in heart rate produced by the compound at a dose of 3 mg/kg | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID219023 | Shift induced by 200 uM of compound, of the [Ca2+] concentration required for half-maximal activation of the canine cardiac myofibrillar ATPase | 1992 | Journal of medicinal chemistry, Jan, Volume: 35, Issue:1 | A novel class of cardiotonic agents: synthesis and biological evaluation of 5-substituted 3,6-dihydrothiadiazin-2-ones with cyclic AMP phosphodiesterase inhibiting and myofibrillar calcium sensitizing properties. |
| AID80749 | Positive inotropic activity in isolated guinea pig atria, Concentration producing 50% of the maximal effect | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Potential antitumor agents. 24. Synthesis and pharmacological behavior of imidazo[2,1-b]thiazole guanylhydrazones bearing at least one chlorine. |
| AID59845 | In vivo contractility in conscious dog expressed as dose which produced a 50% increase in dP/dt max from the control value | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID79555 | In vitro inotropic activity expressed as the maximal increase in developed tension in isolated left atria from guinea pig. | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID79546 | In vitro inotropic activity in isolated left atria from guinea pig. | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID59872 | Percent increase in contractility was evaluated by effect of Cardiotonic agents on myocardial contractility in conscious dog administered orally at dose of 10 mg/kg | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Cardiotonic agents. 2. Synthesis and structure-activity relationships of 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: a new class of positive inotropic agents. |
| AID158303 | Inhibition of fraction III of guinea pig phosphodiesterase | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure. |
| AID158887 | Inhibition of [Ca(2+)]/calmodulin dependent phosphodiesterase PDE 1 of guinea pig ventricle | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. |
| AID58608 | Evaluated for 50% increase of myocardial contractility in anesthetized dog, administered intravenously | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Cardiotonic agents. 2. Synthesis and structure-activity relationships of 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: a new class of positive inotropic agents. |
| AID59572 | Maximum percentage decrease in diastolic blood pressure produced by the compound at a dose of 3.0 mg/kg | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID62402 | Positive inotropic activity in anesthetized dogs | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure. |
| AID22275 | Compound was tested for initial contractile force 0.4+/-0.1 g (% deltabase line value) | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Potential antitumor agents. 24. Synthesis and pharmacological behavior of imidazo[2,1-b]thiazole guanylhydrazones bearing at least one chlorine. |
| AID59622 | Percent change in heart rate in anesthetized dog | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| AID60445 | In vivo contractility in anesthetized dog expressed as % dP/dt max. | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID19937 | Compound was tested for concentration to obtain Emax (microg) | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14 | Potential antitumor agents. 24. Synthesis and pharmacological behavior of imidazo[2,1-b]thiazole guanylhydrazones bearing at least one chlorine. |
| AID50436 | Compound tested for contractility in isolated cat papillary muscle at 10 e-5 M. | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| AID59844 | In vivo contractility in anesthetized dog expressed as dose which produced a 50% increase in dP/dt max from the control value. | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID158290 | Inhibition of cyclic GMP sensitive phosphodiesterase PDE 2 of guinea pig ventricle | 1985 | Journal of medicinal chemistry, May, Volume: 28, Issue:5 | A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. |
| AID157161 | In vitro inhibition of PDE-V isolated from porcine pulmonary artery. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
| AID59878 | Percent increase in heart rate was evaluated by effect of Cardiotonic agents on myocardial contractility in conscious dog administered orally at dose of 10 mg/kg | 1985 | Journal of medicinal chemistry, Oct, Volume: 28, Issue:10 | Cardiotonic agents. 2. Synthesis and structure-activity relationships of 4,5-dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3(2H)-pyridazinones: a new class of positive inotropic agents. |
| AID80320 | The compound was tested in vitro for chronotropic activity expressed as the maximal increase in beat/min in isolated left atria from guinea pig | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID59123 | The effective dose was measured to produce the 10%increase in heart rate | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID59485 | Compound tested for contractility in anesthetized dog when administered intravenously. | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| AID60175 | The effective dose to produce a maximum increase in dP/dt diastolic blood pressure and heart rate | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID77604 | Maximum response compared to maximum response to isoprenaline. | 1986 | Journal of medicinal chemistry, Dec, Volume: 29, Issue:12 | Cardiotonic agents. 1. Synthesis and structure-activity relationships in a new class of 3-, 4-, and 5-pyridyl-2(1H)-quinolone derivatives. |
| AID79659 | In vitro concentration required to give a 50% increase in basal contractile force in an isolated paced guinea pig papillary muscle preparation | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Inotropic "A" ring substituted sulmazole and isomazole analogues. |
| AID80307 | The compound was tested in vitro for chronotropic activity in isolated right atria from guinea pig | 1992 | Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23 | Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID157151 | Effective dose against PDE-III for increase in contractility following administration to anaesthetised dogs | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
| AID50434 | Compound tested for contractility in isolated cat papillary muscle at 10 e-4 M. | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Structure-activity relationships of arylimidazopyridine cardiotonics: discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine. |
| 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. |
| 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 | |||
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase 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. |
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 152 (76.00) | 18.7374 |
| 1990's | 32 (16.00) | 18.2507 |
| 2000's | 4 (2.00) | 29.6817 |
| 2010's | 10 (5.00) | 24.3611 |
| 2020's | 2 (1.00) | 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 (20.45) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (2.35%) | 5.53% |
| Reviews | 16 (7.51%) | 6.00% |
| Case Studies | 2 (0.94%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 190 (89.20%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||