Page last updated: 2024-12-07
sch 28080
Description
Research Excerpts
Clinical Trials
Roles
Classes
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Study Profile
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Description
Sch 28080: not related structurally to other known anti-ulcer agents; inhibits histamine-stimulated gastric secretion; prevents gastric lesions induced by aspirin, indomethacin & ethanol [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 108137 |
| CHEMBL ID | 47529 |
| CHEBI ID | 92978 |
| SCHEMBL ID | 1815961 |
| MeSH ID | M0108108 |
Synonyms (66)
| Synonym |
|---|
| sch28080 |
| HMS3268O05 |
| BRD-K55748775-001-01-4 |
| sch-28080 |
| EU-0100439 |
| sch-28080, >=98% (hplc), solid |
| lopac-s-4443 |
| tocris-1690 |
| NCGC00025259-01 |
| NCGC00015953-01 |
| 2-methyl-8-(phenylmethoxy)imidazo-(1-2-a)pyrine-3-acetonitrile |
| imidazo(1,2-a)pyridine-3-acetonitrile, 2-methyl-8-(phenylmethoxy)- |
| schering compound 28080 |
| NCGC00025259-03 |
| sch 28080 |
| NCGC00025259-02 |
| s28080 , |
| NCGC00015953-03 |
| S 4443 |
| 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile |
| NCGC00015953-05 |
| CHEMBL47529 , |
| bdbm50008977 |
| (8-benzyloxy-2-methyl-imidazo[1,2-a]pyridin-3-yl)-acetonitrie |
| (8-benzyloxy-2-methyl-imidazo[1,2-a]pyridin-3-yl)-acetonitrile |
| 2-(8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl)acetonitrile |
| 76081-98-6 |
| 2-(2-methyl-8-phenylmethoxyimidazo[1,2-a]pyridin-3-yl)acetonitrile |
| HMS3261G20 |
| CCG-204531 |
| NCGC00015953-02 |
| NCGC00015953-04 |
| FT-0641585 |
| unii-00427x161i |
| 00427x161i , |
| LP00439 |
| NCGC00261124-01 |
| tox21_500439 |
| DTXSID10226971 |
| 8-benzyloxy-3-cyanomethyl-2-methyl-imidazo[1,2-a]pyridine |
| PYKJFEPAUKAXNN-UHFFFAOYSA-N , |
| 8-benzyloxy-3-cyanomethyl-2-methylimidazo[1,2-a]pyridine |
| SCHEMBL1815961 |
| 2-methyl-8-(phenylmethoxy)imidazo(1,2-a)-pyridine-3-acetonitrile |
| c17h15n3o |
| HB1124 |
| AKOS024456748 |
| CHEBI:92978 |
| (8-benzyloxy-2-methylimidazo[1,2-a]pyridin-3-yl)acetonitrile |
| SR-01000076230-3 |
| sr-01000076230 |
| SR-01000076230-1 |
| Q27164711 |
| Z2044772151 |
| HMS3678M11 |
| 2-methyl-8 (phenyl-methoxy) imidazo (1,2-a)-pyridine-3-acetonitrile |
| HY-103261 |
| HMS3414M11 |
| SDCCGSBI-0050424.P002 |
| NCGC00015953-08 |
| CS-0026715 |
| 2-methyl-8-(phenylmethoxy)-imidazo[1,2-a]pyridine-3-acetonitrile |
| MS-23941 |
| EN300-233396 |
| 2-[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]acetonitrile |
| BDA08198 |
Research Excerpts
Overview
SCH 28080 is an H+K(+)-ATPase specific inhibitor. It binds to the high affinity K+ site.
| Excerpt | Reference | Relevance |
|---|---|---|
| "SCH 28080 is an H+,K(+)-ATPase specific inhibitor and binds to the high affinity K+ site." | ( The apical chloride channel as part of the function of gastric H+,K(+)-ATPase. Asano, S; Morii, M; Ohshika, M; Takeguchi, N; Tomiyama, Y, 1994) | 1.01 |
Effects
| Excerpt | Reference | Relevance |
|---|---|---|
| "SCH 28080 has no effect on Mg2(+)-catalyzed dephosphorylation." | ( Interaction of a K(+)-competitive inhibitor, a substituted imidazo[1,2a] pyridine, with the phospho- and dephosphoenzyme forms of H+, K(+)-ATPase. Mendlein, J; Sachs, G, 1990) | 1 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| "8 mM Ca2+, the rate of glycogen breakdown was increased by theophylline in a dose-dependent manner and the dose-response curve was somewhat similar to that obtained with oxygen uptake." | ( Ca2+ requirement for metabolic effects of secretagogues in the amphibian gastric mucosa. Chacín, J; Lobo, P; Subero, O, 1989) | 0.28 |
| " dosing of SCH 28080, 1 mg/kg, indicating that the antisecretory action of SCH 28080 was not secondary to changes in gastric blood flow." | ( Studies on the mechanisms of the antisecretory and cytoprotective actions of SCH 28080. Barnett, A; Casciano, C; Chiu, PJ; Long, JF; Tetzloff, G, 1983) | 0.88 |
| " showed moderate effects, but the dosage also inhibited cysteamine-stimulated acid secretion." | ( Effects of a gastric antisecretory-cytoprotectant 2-methyl-8-(phenylmethoxy)imidazo[1,2-a]pyridine-3-acetonitrile (Sch 28 080) on cysteamine, reserpine and stress ulcers in rats. Barnett, A; Brown, AD; Chiu, PJ; Gerhart, C, 1984) | 0.27 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| imidazopyridine | |
| [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 Targets (37)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Nrf2 | Homo sapiens (human) | Potency | 25.9290 | 0.0920 | 8.2222 | 23.1093 | AID624149 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 37.6858 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0810 | 0.0041 | 10.8903 | 31.5287 | AID493107 |
| GLS protein | Homo sapiens (human) | Potency | 25.1189 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| TDP1 protein | Homo sapiens (human) | Potency | 33.4983 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
| arylsulfatase A | Homo sapiens (human) | Potency | 8.4921 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0011 | 0.5406 | 17.6392 | 96.1227 | AID2364; AID2528 |
| hexokinase-4 isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 2.5119 | 13.8003 | 28.1838 | AID743205 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 60.1198 | 23.9341 | 23.9341 | 23.9341 | AID1967 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 1.1995 | 0.1346 | 10.3950 | 30.1313 | AID1347049 |
| glucokinase regulatory protein | Homo sapiens (human) | Potency | 28.1838 | 2.5119 | 13.8003 | 28.1838 | AID743205 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0398 | 16.7842 | 39.8107 | AID995 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 6.7016 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 0.0010 | 6.0009 | 35.4813 | AID943 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 8.4921 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 2.0000 | 0.0001 | 1.7740 | 10.0000 | AID468397 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 10.5000 | 0.0001 | 1.7536 | 10.0000 | AID468401; AID468402 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 82.0000 | 0.0000 | 2.0151 | 10.0000 | AID468400 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 54.0000 | 0.0000 | 2.8005 | 10.0000 | AID468398 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0000 | 2.3983 | 10.0000 | AID468399 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (42)
Molecular Functions (34)
Ceullar Components (6)
Bioassays (107)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| 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. |
| 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. |
| 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. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1910987 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha A339S mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910981 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha A123V mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID183829 | Antisecretory activity of intraperitoneally injected compound (40 mg/kg) in pylorus-ligated rat | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID78725 | Compound was evaluated for the ability to inhibit purified H+/K+ -ATPase at pH 7.4, by using gastric membrane vesicles prepared from hog stomach. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Antiulcer agents. 5. Inhibition of gastric H+/K(+)-ATPase by substituted imidazo[1,2-a]pyridines and related analogues and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme. |
| AID59342 | Histopathology of the stomach was determined as HGM (Hyperplasia of grandular mucosa)in the presence of the compound. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine. |
| AID178863 | Antisecretory activity in gastric fistula rat when administered perorally | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | Synthesis and biological activity of 3-substituted imidazo[1,2-a]pyridines as antiulcer agents. |
| AID60560 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at dose 2 mg/kg given intravenously | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID468397 | Inhibition of CYP1A2 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID176373 | Cytoprotective activity against ethyle alcohol induced ulcers was determined in rats by peroral administration of the compound | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine. |
| AID183827 | Antisecretory activity in pylorus ligated rats at a 40 mg/kg dose administered intraperitoneally | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID78875 | Inhibition of purified H+/K+ ATPase at pH 7.4 as released inorganic phosphate from ATP using hog stomach gastric membrane vesicles | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies |
| AID60425 | Organ weight ratio was determined for the compound with respect to (8-Benzyloxy-2-methyl-imidazo[1,2-a]pyridin-3-yl) compound | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine. |
| AID468408 | Intrinsic clearance in human liver microsomes | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID60561 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at dose 2 mg/kg given orally | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID59824 | Effective dose required to reduce acid out put when administered perorally in dog;Value ranges from(2.1-14) | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID60554 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 2 mg/kg compound administered perorally | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID468401 | Inhibition of CYP3A4 using diethoxyfluorescein substrate | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID60553 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 2 mg/kg i.v. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID159535 | In vitro inhibition of [14C]- aminopyrine accumulation was determined in gastric vesicles of pig with outside vesicle pH 7 | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines. |
| AID468409 | Dissociation constant, pKa of the compound | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID59997 | Inhibition of gastric acid secretion stimulated by histamine in dog was determined by peroral administration confidence limits (p=0.05.); value ranges from 2.1-14.0 | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine. |
| AID60565 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at dose 5 mg/kg given intravenously | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID59471 | Antisecretory activity in histamine stimulated dogs at 5 mg/kg dose administered orally measured as 50% effective concentration | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID176440 | Oral gastric cytoprotective activity in the rat against ethanol-induced lesions | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID59818 | Effective dose required to reduce acid out put when administered intravenously in dog;Value ranges from(0.01-1.2). | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID59665 | Effective dose against histamine stimulated gastric acid secretion in adult mongrel dogs given orally; value ranges from 2.1-14.0 | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID59663 | Effective dose against histamine stimulated gastric acid secretion in adult mongrel dogs given intravenously; value ranges from 0.01-1.19 | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID176523 | Cytoprotective activity in rats against the ethyl alcohol stimulated ulcers measured as effective dose | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID60072 | Antisecretory activity in histamine stimulated dogs at 2 mg/kg dose administered orally | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID178206 | Effective dose inhibiting ethanol-induced lesions was determined 1 h, after oral administration of absolute ethanol in rat | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID60073 | Antisecretory activity in histamine stimulated dogs at 4 mg/kg dose administered orally | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID468400 | Inhibition of CYP2D6 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID78910 | Inhibition of H+/K+ ATPase as reduced acid formation in rabbit gastric glands | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies |
| AID78726 | Compound was evaluated for the ability to inhibit H+/K+ -ATPase formation in rabbit gastric glands. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Antiulcer agents. 5. Inhibition of gastric H+/K(+)-ATPase by substituted imidazo[1,2-a]pyridines and related analogues and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme. |
| AID1910991 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha Y799F mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910980 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta subunit in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910979 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha A339S mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID25103 | Dissociation constant (pKa) | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies |
| AID1910995 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha I816F mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910990 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha Y799F mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID183520 | Cytoprotective activity in rat when administered 30 mg/kg perorally (Ethyl alcohol as necrotic agent) | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | Synthesis and biological activity of 3-substituted imidazo[1,2-a]pyridines as antiulcer agents. |
| AID1910983 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha V331F mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID183525 | Cytoprotective activity in rats when administered 100 mg/kg perorally (Hydrochloric acid as necrotic agent) | 1989 | Journal of medicinal chemistry, Sep, Volume: 32, Issue:9 | Synthesis and biological activity of 3-substituted imidazo[1,2-a]pyridines as antiulcer agents. |
| AID60555 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 4 mg/kg administered perorally | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID1910989 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha Y799A mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910994 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha I816F mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910982 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha A123V mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID60423 | Organ weight (stomach) was determined after administration of the compound | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine. |
| AID468406 | Intrinsic clearance in rat liver microsomes | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID60559 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at dose 1 mg/kg given intravenously | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID60551 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 0.1 mg/kg compound administered intravenously | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID60068 | Antisecretory activity in histamine stimulated dogs at 0.1 mg/kg dose administered intravenously | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID1910993 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha L809F mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID60552 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 1 mg/kg i.v. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID468402 | Inhibition of CYP3A4 using 7-benzyloxyquinoline substrate | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID183857 | Gastric antisecretory activity in the pylorus-ligated rat and the reduction in acid output was measured after 4 hr by intraperitoneal (ip) administration of 40 mg/kg dose. | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID78903 | In vitro inhibition of H+/K+ ATPase activity was determined in gastric vesicles of pig using ATPase assay with pH 7 | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines. |
| AID78728 | The percent of compound protonated at pH 7.4 in purified H+/K+ -ATPase from rabbit gastric glands. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Antiulcer agents. 5. Inhibition of gastric H+/K(+)-ATPase by substituted imidazo[1,2-a]pyridines and related analogues and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme. |
| AID221913 | Inhibitory activity against histamine-stimulated gastric acid secretion in adult mengrel dogs, with surgically prepared Heidenhain pouches after peroral administration | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Antiulcer agents. 5. Inhibition of gastric H+/K(+)-ATPase by substituted imidazo[1,2-a]pyridines and related analogues and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme. |
| AID468399 | Inhibition of CYP2C19 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID60558 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at dose 0.1 mg/kg given intravenously | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID60074 | Antisecretory activity in histamine stimulated dogs following 5 mg/kg i.v. administration. | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID60556 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 5 mg/kg i.v. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID1910992 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha L809F mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID59469 | Antisecretory activity in histamine stimulated dogs at 5 mg/kg dose administered intravenously | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID468398 | Inhibition of CYP2C9 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID468410 | Chromatographic hydrophobicity index at pH 7.4 by fast gradient HPLC | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID60562 | Inhibition of histamine stimulated gastric acid secretion in mongrel dogs following 4 mg/kg p.o. administration. | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID60069 | Antisecretory activity in histamine stimulated dogs at 1 mg/kg dose administered intravenously | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID60070 | Antisecretory activity in histamine stimulated dogs at 2 mg/kg dose administered intravenously | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID60568 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at dose 8 mg/kg given orally | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines. |
| AID468396 | Inhibition of H+/K+ ATPase in parietal cells assessed as inhibition of pentagastrin-stimulated [14C]aminopyrine accumulation | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID60075 | Antisecretory activity in histamine stimulated dogs at 8 mg/kg dose administered orally | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 2. Gastric antisecretory, cytoprotective, and metabolic properties of substituted imidazo[1,2-a]pyridines and analogues. |
| AID1910984 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha V331F mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID1910985 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha A335V mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID60011 | Intravenous effective dose for gastric antisecretory activity against histamine-stimulated gastric acid secretion in adult mongrel dogs | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies |
| AID1910986 | Ratio of IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha A335V mutant/beta subunit to IC50 for Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta su | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID60025 | Peroral effective dose for gastric antisecretory activity against histamine-stimulated gastric acid secretion in adult mongrel dogs | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies |
| AID1910988 | Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha Y799A mutant/beta subunit activity in HEK293 cells by colorimetric microplate reader | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump. |
| AID468395 | Inhibition of H+/K+ ATPase at pH 7.4 | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID221785 | Inhibitory activity against histamine-stimulated gastric acid secretion in adult mengrel dogs, with surgically prepared Heidenhain pouches after intravenous administration | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Antiulcer agents. 5. Inhibition of gastric H+/K(+)-ATPase by substituted imidazo[1,2-a]pyridines and related analogues and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme. |
| AID26399 | pKa value of the compound. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2 | Antiulcer agents. 5. Inhibition of gastric H+/K(+)-ATPase by substituted imidazo[1,2-a]pyridines and related analogues and its implication in modeling the high affinity potassium ion binding site of the gastric proton pump enzyme. |
| AID60424 | Organ weight ratio was determined for the compound :control | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11 | Antiulcer agents. 3. Structure-activity-toxicity relationships of substituted imidazo[1,2-a]pyridines and a related imidazo[1,2-a]pyrazine. |
| AID60557 | Inhibition of histamine stimulated gastric acid secretion in adult mongrel dogs at 8 mg/kg compound administered perorally | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | Antiulcer agents. 4. Conformational considerations and the antiulcer activity of substituted imidazo[1,2-a]pyridines and related analogues. |
| AID177135 | In vivo antisecretory activity was determined for inhibition of gastric secretion in rat | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines. |
| AID468403 | Inhibition of CYP3A4 assessed as ratio of IC50 at 0 mins to IC50 at 10 mins using diethoxyfluorescein substrate | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs). |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 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. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (214)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 35 (16.36) | 18.7374 |
| 1990's | 100 (46.73) | 18.2507 |
| 2000's | 52 (24.30) | 29.6817 |
| 2010's | 20 (9.35) | 24.3611 |
| 2020's | 7 (3.27) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 24.88
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 (24.88) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 3 (1.38%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 214 (98.62%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||