Cirazoline is an α2-adrenergic agonist that is used as a nasal decongestant. It works by constricting blood vessels in the nasal passages, which reduces swelling and congestion. Cirazoline is available over the counter as a nasal spray. Research on cirazoline has focused on its efficacy and safety as a decongestant, as well as its potential for other uses, such as treatment of migraines and glaucoma. Cirazoline is a synthetic compound, meaning it is not naturally occurring but rather is manufactured. Its synthesis involves several steps, including the use of starting materials like 2-chloro-6-methylpyridine and 2-phenylethylamine. '
cirazoline: posseses agonist properties at alpha-adrenoreceptor sites; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 2765 |
| CHEMBL ID | 13852 |
| CHEBI ID | 92950 |
| SCHEMBL ID | 126496 |
| MeSH ID | M0062711 |
| Synonym |
|---|
| BRD-K54142781-001-02-1 |
| gtpl515 |
| ld-3098 |
| cirazolina [inn-spanish] |
| cirazoline [inn] |
| cirazolinum [inn-latin] |
| 1h-imidazole, 2-((2-cyclopropylphenoxy)methyl)-4,5-dihydro- |
| 2-((o-cyclopropylphenoxy)methyl)-2-imidazoline |
| LOPAC0_000354 |
| NCGC00015196-01 |
| BIO1_000412 |
| tocris-0888 |
| BIO2_000786 |
| lopac-c-223 |
| NCGC00024847-01 |
| BIO2_000306 |
| BIO1_000901 |
| BIO1_001390 |
| BSPBIO_001586 |
| cirazoline |
| IDI1_034056 |
| NCGC00024847-04 |
| NCGC00024847-03 |
| KBIOGR_000306 |
| KBIO3_000612 |
| KBIO2_005442 |
| KBIO2_002874 |
| KBIOSS_000306 |
| KBIO2_000306 |
| KBIO3_000611 |
| NCGC00024847-05 |
| NCGC00024847-02 |
| HMS1989P08 |
| HMS2089E21 |
| NCGC00015196-07 |
| L000800 |
| CHEMBL13852 , |
| HMS1361P08 |
| HMS1791P08 |
| 59939-16-1 |
| 2-[(2-cyclopropylphenoxy)methyl]-4,5-dihydro-1h-imidazole |
| bdbm50027060 |
| 2-(2-cyclopropyl-phenoxymethyl)-4,5-dihydro-1h-imidazole (cirazoline) |
| 2-(2-cyclopropyl-phenoxymethyl)-4,5-dihydro-1h-imidazole |
| NCGC00015196-04 |
| dtxsid4045131 , |
| cas-59939-16-1 |
| dtxcid2025131 |
| tox21_110095 |
| CCG-204449 |
| NCGC00015196-06 |
| NCGC00015196-02 |
| NCGC00015196-05 |
| NCGC00015196-03 |
| NCGC00015196-08 |
| qk318gvy3y , |
| cirazolinum |
| cirazolina |
| unii-qk318gvy3y |
| FT-0602943 |
| SCHEMBL126496 |
| tox21_110095_1 |
| NCGC00015196-09 |
| HMS3402P08 |
| DB09202 |
| CHEBI:92950 |
| Q5121338 |
| BRD-K54142781-003-08-4 |
| BRD-K54142781-003-02-7 |
| SDCCGSBI-0050342.P002 |
| NCGC00015196-13 |
| 1h-imidazole, 2-[(2-cyclopropylphenoxy)methyl]-4,5-dihydro- |
Cirazoline was found to be a full agonist at alpha-1 receptors having an ED50, dissociation constant (KA) and relative efficacy similar to that of (-)-norepinephrine.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cirazoline was found to be a full agonist at alpha-1 receptors having an ED50, dissociation constant (KA) and relative efficacy similar to that of (-)-norepinephrine." | ( Receptor interactions of imidazolines. IX. Cirazoline is an alpha-1 adrenergic agonist and an alpha-2 adrenergic antagonist. Ruffolo, RR; Waddell, JE, 1982) | 1.25 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cirazoline has additional high affinity for imidazoline receptors and has good brain penetrance when administered systemically." | ( The alpha-1 adrenergic agonist, cirazoline, impairs spatial working memory performance in aged monkeys. Arnsten, AF; Jentsch, JD, 1997) | 1.3 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Cirazoline did not produce a significant depolarisation in blood vessels of either normotensive or hypertensive rats." | ( Effects of chloride substitution on electromechanical responses in the pulmonary artery of Dahl normotensive and hypertensive rats. Bieger, D; Duggan, JA; Tabrizchi, R, 2004) | 1.04 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 |
Dose-response curves for the alpha1-adrenoceptor-mediated vasoconstrictor effects of cirazoline were shifted in a rightward direction with no depression of the maximum response. The acute or chronic administration of phenoxybenzamine alone displaced the dose-response curve to Cirazoline to the right in a dose-dependent manner.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The acute or chronic administration of phenoxybenzamine alone displaced the dose-response curve to cirazoline to the right in a dose-dependent manner, while reducing the slope function and maximum response to the agonist." | ( A comparison of the effects of acute versus chronic administration of phenoxybenzamine on pressor responses elicited by the selective alpha 1-adrenoceptor agonist cirazoline in the pithed rat preparation. Tabrizchi, R; Triggle, CR, 1992) | 0.7 |
| " After the administration of carvedilol on day 8, the cirazoline vasopressor response was 2 +/- 1 mmHg and the isoproterenol-induced tachycardia was 4 +/- 3 beats/min, indicating effective alpha 1- and beta-adrenergic blockade after chronic dosing with carvedilol." | ( Single and repeated doses of the vasodilator/beta-adrenergic antagonist, carvedilol, block cirazoline- and isoproterenol-mediated hemodynamic responses in the conscious rat. Gagnon, R; Slivjak, MJ; Smith, EF, 1992) | 0.75 |
| " Treatment with captopril was found to attenuate pressor responses produced by the administration of either alpha 1- or alpha 2-adrenoceptor agonists, resulting in the displacement to the right of the agonist dose-response curves and significantly increasing the calculated ED50 values." | ( The interrelationship between the effects of captopril and nifedipine on pressor responses elicited by selective alpha-adrenoceptor agonists in the pithed rat preparation. Tabrizchi, R; Triggle, CR, 1992) | 0.28 |
| " The ED50 value for the dose-response curves to B-HT 920 and St587 were found to be significantly increased after the administration of staurosporine." | ( Effects of staurosporine on the pressor responses to alpha-adrenoceptor agonists in pithed rats: a comparison with nifedipine. Tabrizchi, R; Triggle, CR, 1991) | 0.28 |
| " (-)-Pindolol (30 and 100 nmol/kg) shifted the dose-response curves of both drugs significantly and in a similar manner to the right." | ( Involvement of 5-HT1A receptors in blood pressure reduction by 8-OH-DPAT and urapidil in cats. Beller, KD; Kolassa, N; Sanders, KH, 1990) | 0.28 |
| " Cumulative dose-response curves of the alpha 1-agonists l-phenylephrine or cirazoline applied luminally in rat tail arteries and in side branches of canine femoral arteries were identical to those obtained by adventitial application in the intact arteries, and were not modified by removal of the endothelium (eliminating acetylcholine-induced dilations)." | ( Endothelium-mediated dilations contribute to the polarity of the arterial wall in vasomotion induced by alpha 2-adrenergic agonists. Busse, R; Holtz, J; Kuon, E; Matsuda, H, ) | 0.36 |
| " Dose-response studies indicated clonidine was 100 times more potent than norepinephrine or cirazoline at inhibiting N-acetyltransferase activity." | ( Regulation of chicken pineal arylalkylamine-N-acetyl transferase by postsynaptic alpha 2-adrenergic receptors. Collin, JP; Voisin, P, 1986) | 0.49 |
| " Although administered in a dosage range 100 to 1000 times that of alpha-1 agonists, the alpha-2 agonists (B-HT 920, UK 14,304 and guanabenz) produced only minimal renal vasoconstriction before systemic pressor effects." | ( In vivo assessment of rat renal alpha adrenoceptors. Gesek, FA; Strandhoy, JW; Wolff, DW, 1987) | 0.27 |
| " Papaverine, calmidazolium and W-7 did not influence the dose-response curves for the agonists in the pithed rat experiments." | ( Interaction of calmodulin antagonists with alpha-adrenergic responses in pithed rats and in the perfused hindquarters of the rat. Korstanje, C; Ten Brink, EM; Van Zwieten, PA, 1988) | 0.27 |
| "1 mg/kg) and of yohimbine (1 mg/kg) on the dose-response curves for cirazoline in the pithed rat, and for phenylephrine in the anaesthetized dog were compared, after various doses of phenoxybenzamine." | ( Loss of selectivity of so-called selective alpha 1-adrenoceptor agonists after phenoxybenzamine. Gonçalves, J; Guimarães, S; Nunes, JP; Paiva, MQ, 1988) | 0.51 |
| " Furthermore, the norepinephrine dose-response curve was shifted to the right in the presence of cirazoline, without affecting the maximal response." | ( Pharmacologic characterization of cirazoline-activated inositol phospholipid hydrolysis in rat brain cortical slices. Li, PP; Sibony, D; Warsh, JJ, 1988) | 0.77 |
| " Dose-response curves for the alpha1-adrenoceptor-mediated vasoconstrictor effects of cirazoline were shifted in a rightward direction with no depression of the maximum response by lower does of phenoxybenzamine (0." | ( Existence of spare alpha 1-adrenoreceptors, but not alpha 2-adrenoreceptors, for respective vasopressor effects of cirazoline and B-HT 933 in the pithed rat. Ruffolo, RR; Yaden, EL, ) | 0.56 |
| " Where pA2 values (-log dose antagonist evoking a twofold shift for the agonist dose-response curve) could be calculated, no significantly different pA2 values against either agonist resulted." | ( Calcium influx-dependent and -independent alpha 1-adrenoceptor-mediated processes of vasoconstriction in vivo do not operate via different alpha 1-adrenoceptor subtypes. de Jonge, A; Korstanje, C; Thoolen, MJ; Timmermans, PB; van Zwieten, PA; Wilffert, B, ) | 0.13 |
| "5 micrograms/kg per min) that was continued while dose-response curves to M-7 and cirazoline were generated." | ( Differential inhibition of vascular smooth muscle responses to alpha 1- and alpha 2-adrenoceptor agonists by diltiazem and verapamil. Cavero, I; Langer, SZ; Lefèvre-Borg, F; Shepperson, N, 1983) | 0.49 |
| ", dose of WB-4101 isomer in mg/kg required to produce a 2-fold rightward shift in the dose-response curves of cirazoline and UK-14,304) obtained in vivo from Schild regressions, alpha 1/alpha 2 selectivity ratios were calculated." | ( Blockade and postjunctional vascular alpha 1- and alpha 2-adrenoceptors in pithed rat by the enantiomers of WB-4101. Nelson, WL; Ruffolo, RR; Yaden, EL, 1983) | 0.48 |
| " In contrast, the dose-response curves to tiamenidine and clonidine were flatter and bell-shaped with maxima of 30 and 60 min, respectively." | ( Sleeping times evoked by alpha adrenoceptor agonists in two-day-old chicks: an experimental model to evaluate full and partial agonists at central alpha-2 adrenoceptors. Cavero, I; Doxey, JC; Roach, AG; Strachan, DA, 1983) | 0.27 |
| " Pretreatment with captopril reduced the pressor responses to cirazoline and displaced the dose-response curve for this agonist to the right, significantly increasing the ED50 without altering the maximum response." | ( Pressor responses to the alpha 1-adrenoceptor agonist cirazoline: effects of captopril, phenoxybenzamine and nifedipine. Tabrizchi, R; Triggle, CR, 1994) | 0.78 |
| Class | Description |
|---|---|
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| [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, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 50.1187 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID886 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID886 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 27.5404 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395 |
| GALC protein | Homo sapiens (human) | Potency | 0.6310 | 28.1838 | 28.1838 | 28.1838 | AID1159614 |
| TDP1 protein | Homo sapiens (human) | Potency | 30.3001 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 0.9439 | 0.0007 | 14.5928 | 83.7951 | AID1259392 |
| Thrombopoietin | Homo sapiens (human) | Potency | 25.1189 | 0.0251 | 7.3048 | 31.6228 | AID917; AID918 |
| AR protein | Homo sapiens (human) | Potency | 7.4978 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 0.0013 | 18.0743 | 39.8107 | AID926 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 1.8888 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 2.7202 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1259401 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 23.8911 | 0.0002 | 29.3054 | 16,493.5996 | AID743075 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 4.3649 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| arylsulfatase A | Homo sapiens (human) | Potency | 0.0953 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 33.5875 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 14.4409 | 0.0016 | 28.0151 | 77.1139 | AID1224843; AID1224895; AID1259393 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 15.0654 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 0.0013 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 36.4261 | 0.0100 | 39.5371 | 1,122.0200 | AID1469; AID1479 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 12.9244 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| [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) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 0.0347 | 0.0001 | 0.5326 | 10.0000 | AID772375 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 0.0589 | 0.0001 | 0.8074 | 10.0000 | AID443916; AID772379 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 0.5248 | 0.0002 | 0.7257 | 10.0000 | AID443915; AID772378 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | Ki | 0.5495 | 0.0003 | 0.4834 | 10.0000 | AID443913; AID772377 |
| Nischarin | Homo sapiens (human) | Ki | 0.0990 | 0.0042 | 0.2192 | 3.8019 | AID342861 |
| [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) |
|---|---|---|---|---|---|---|---|
| Alpha-2B adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 1.0000 | 0.0005 | 1.3644 | 6.7100 | AID443912; AID772381 |
| Alpha-2C adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.3981 | 0.0005 | 0.5541 | 6.7100 | AID443911; AID772380 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0378 | 0.0054 | 3.2510 | 20.9400 | AID36629; AID37345 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.1259 | 0.0015 | 1.7227 | 5.6000 | AID32972; AID35390; AID35445; AID35453 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0126 | 0.0126 | 0.0379 | 0.0631 | AID36629 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0126 | 0.0013 | 0.0388 | 0.0970 | AID36629 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0126 | 0.0126 | 0.0319 | 0.0631 | AID36629 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.0126 | 0.0001 | 0.5098 | 7.1000 | AID32967; AID35381; AID36626; AID36629 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 0.0631 | 0.0001 | 1.3010 | 5.6000 | AID32970; AID35384; AID37345; AID37350 |
| [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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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. |
| 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. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID37350 | In vitro activation of human Alpha-1B receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | 2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series. |
| AID35384 | Activation of human alpha-1B adrenergic receptors expressed in rat-1 fibroblasts | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
| AID443915 | Displacement of [3H]RX821002 from human alpha2B adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID772382 | Antagonist activity at human alpha2A AR | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID443912 | Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID772375 | Binding affinity at human 5HT1A receptor | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID772379 | Binding affinity at human alpha2A AR | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID35331 | Ability to activate human alpha-1D receptor expressed in rat-1 fibroblasts as calcium mobilization through Gq coupled PLC pathway relative to phenylephrine response | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3 | alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
| AID772377 | Binding affinity at human alpha2C AR | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID23715 | Apparent partion coefficient of compound was evaluated in octanol/buffer at pH of 7.4 at 37 degree Centigrade | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID197169 | Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats. | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID342861 | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | QSAR study of imidazoline antihypertensive drugs. |
| AID443905 | Intrinsic activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry relative to noradrenaline | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID32971 | Tested for efficacy against alpha 1D-adrenoceptor in human expressed as phenylephrine response at the dose of 40 uM | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
| AID180899 | The dose required to increase diastolic blood pressure by 50 mmHg in pithed rats after intravenous administration | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | N-substituted imidazolines and ethylenediamines and their action on alpha- and beta-adrenergic receptors. |
| AID36629 | In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | 2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series. |
| AID174088 | Tested for alpha1 adrenoceptor-Mediated Pressor Response in Pithed Rats; Dose ratio subsequent administration of antagonist (Prazosin) intravenously at a dose of 0.1 mg/kg | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | N-substituted imidazolines and ethylenediamines and their action on alpha- and beta-adrenergic receptors. |
| AID35453 | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4 | 2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series. |
| AID32967 | Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts. | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
| AID772372 | Binding affinity to I2 imidazoline binding site in rat brain membrane | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID35381 | Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
| AID342863 | Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | QSAR study of imidazoline antihypertensive drugs. |
| AID772378 | Binding affinity at human alpha2B AR | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID32970 | Potency against cloned human alpha 1B adrenoceptor expressed in rat-1 fibroblasts. | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
| AID772381 | Agonist activity at human alpha2B AR | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID443913 | Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID772380 | Agonist activity at human alpha2C AR | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID443910 | Antagonist activity at human alpha2A adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID36626 | Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3 | alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
| AID37345 | Activation of recombinant human adrenergic, alpha-1B receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3 | alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
| AID36726 | Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.2 nM) to rat isolated brain membranes by 50% was reported; 8.9*10e-7 | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID36620 | Ability to activate cloned human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through Gq coupled PLC pathway expressed as percent of phenylephrine (40 uM) response | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3 | alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
| AID443911 | Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID174091 | Tested for alpha-2 adrenoceptor-Mediated PressorResponse in Pithed Rats; Dose ratio by subsequent administration of antagonist (yohimbine) intravenously at a dose of 1 mg/kg | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | N-substituted imidazolines and ethylenediamines and their action on alpha- and beta-adrenergic receptors. |
| AID35383 | Activation of human alpha-1B-adrenoceptor receptors expressed in rat-1 fibroblasts as percent maximal effect relative to phenylephrine | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
| AID35390 | Activation of human Alpha-1D adrenergic receptors expressed in rat-1 fibroblasts | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
| AID342860 | Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | QSAR study of imidazoline antihypertensive drugs. |
| AID443916 | Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID36793 | Binding affinity against Alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]-clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported; 5.9*10e-8 | 1984 | Journal of medicinal chemistry, Apr, Volume: 27, Issue:4 | Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. |
| AID772358 | Agonist activity at human 5HT1A receptor assessed as intrinsic activity | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID91715 | Binding affinity for imidazoline receptor I-2 in rabbit kidney homogenate (relative to [3H]-Idazoxan radioligand) | 2000 | Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6 | 3D-QSAR CoMFA study on imidazolinergic I(2) ligands: a significant model through a combined exploration of structural diversity and methodology. |
| AID35445 | Activation of recombinant human adrenergic, alpha-1D receptor expressed in rat-1 fibroblasts assayed via calcium mobilization through Gq coupled PLC pathway | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3 | alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
| AID32972 | Potency against cloned human alpha 1D-adrenoceptor expressed in rat-1 fibroblasts. | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
| AID37338 | Activation of human alpha-1B receptor expressed in rat-1 fibroblasts by calcium mobilization of Gq coupled PLC as percent phenylephrine (40 uM) response | 2002 | Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3 | alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines. |
| AID35380 | Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts; expressed as a percent of the maximal effect of the phenylephrine | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
| AID235537 | The selectivity was evaluated against alpha 1 and alpha 2 adrenoceptor | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | N-substituted imidazolines and ethylenediamines and their action on alpha- and beta-adrenergic receptors. |
| AID443906 | Intrinsic activity at human alpha2B adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry relative to noradrenaline | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine? |
| AID35389 | Activation of human alpha-1D-adrenoceptor receptor expressed in rat-1 fibroblasts relative to phenylephrine | 2002 | Bioorganic & medicinal chemistry letters, Dec-02, Volume: 12, Issue:23 | Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines. |
| AID32969 | Efficacy against alpha 1B-adrenoceptor in human expressed as phenylephrine response at the dose of 40 uM. | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
| AID32966 | Efficacy against alpha 1A adrenoceptor in human expressed as phenylephrine response at the dose of 40 uM | 2001 | Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21 | 2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides. |
| AID36312 | Selective Alpha-1 adrenergic receptor agonistic activity;no data | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives. |
| AID1345920 | Rat alpha1D-adrenoceptor (Adrenoceptors) | 1994 | Molecular pharmacology, Nov, Volume: 46, Issue:5 | Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. |
| 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. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 62 (28.57) | 18.7374 |
| 1990's | 68 (31.34) | 18.2507 |
| 2000's | 56 (25.81) | 29.6817 |
| 2010's | 24 (11.06) | 24.3611 |
| 2020's | 7 (3.23) | 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 (22.28) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 226 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||