thioperamide: structure given in first source; histamine H3 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 3035905 |
| CHEMBL ID | 260374 |
| CHEBI ID | 81391 |
| SCHEMBL ID | 2235762 |
| MeSH ID | M0147976 |
| Synonym |
|---|
| unii-ii4319bwui |
| ii4319bwui , |
| BRD-K63874012-103-01-5 |
| n-cyclohexyl-4-(3h-imidazol-4-yl)piperidine-1-carbothioamide |
| gtpl1267 |
| bdbm22914 |
| chembl260374 , |
| thioperamide |
| n-cyclohexyl-4-(1h-imidazol-5-yl)piperidine-1-carbothioamide |
| tocris-0644 |
| lopac-t-123 |
| NCGC00015988-01 |
| NCGC00024704-01 |
| LOPAC0_001214 |
| mr 12842 |
| n-cyclohexy-4-(imidazol-4-yl)-1-piperidinecarbothioamide |
| 1-piperidinecarbothioamide, n-cyclohexyl-4-(1h-imidazol-4-yl)- |
| mr-12842 |
| NCGC00024704-03 |
| NCGC00024704-02 |
| NCGC00015988-05 |
| chebi:81391 , |
| fjz , |
| L000596 |
| 106243-16-7 |
| C17933 |
| CCG-205288 |
| NCGC00015988-04 |
| NCGC00015988-03 |
| NCGC00015988-02 |
| 1-piperidinecarbothioamide, n-cyclohexyl-4-(1h-imidazol-5-yl)- |
| SCHEMBL2235762 |
| n-cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide |
| n-cyclohexyl-4-(1h-imidazol-5-yl)-1-piperidinecarbothioamide |
| QKDDJDBFONZGBW-UHFFFAOYSA-N |
| AKOS024458593 |
| DTXSID50147555 |
| AKOS030228083 |
| NCGC00015988-11 |
| n-cyclohexyl-4-(1h-imidazol-4-yl)piperidine-1-carbothioamide |
| thioperamidemaleate |
| HMS3675M08 |
| HY-12206 |
| HMS3411M08 |
| Q7784686 |
| SDCCGSBI-0051181.P002 |
| CS-0010277 |
| NCGC00015988-13 |
| A925117 |
| n-ccyclohexyl-4-(1h-imidazol-4-yl)piperidine-1-carbothioamide maleate |
Thioperamide is an antagonist at AXOR 35. It is a potent and selective H3-receptor antagonist, whose in vivo effects have been reported after systemic administration.
Thioperamide plays a protective role in seizure development and cognitive impairment of PTZ-induced kindling in rats. The increase of acetylcholine release might be exerted via H3-receptors located on cholinergic terminals.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Thioperamide plays a protective role in seizure development and cognitive impairment of PTZ-induced kindling in rats. " | ( Effects of thioperamide on seizure development and memory impairment induced by pentylenetetrazole-kindling epilepsy in rats. Chen, GF; Chen, JF; Ding, MP; Hu, XY; Zhang, LS, 2013) | 2.22 |
| "The thioperamide-induced increase of acetylcholine release might be exerted via H3-receptors located on cholinergic terminals." | ( Release of acetylcholine in the ventral striatum is influenced by histamine receptors. Fischer, H; Philippu, A; Prast, H, 1994) | 0.77 |
Thioperamide (1 mg kg-1, i.v.) blocked (R)-alpha-mHA's inhibitory effect on stimulation-induced sympathetic cardiopressor responses. Pre-treatment with thioperamia augmented (p < 0.02) HFC and this increase was inhibited by alpha-methylhistamine (p = 0.05). Pretreatment with thooperamide attenuated the inhibition of the tail-flick response induced by beta-endorphin or U50, 488H, but not morphine.
| Excerpt | Reference | Relevance |
|---|---|---|
| " Histamine was applied at 10(-9),10(-8), 10(-7),10(-6), and 10(-5) M for 16 h into the cultures and the highest dose was found to be the most toxic one." | ( Contribution of the histaminergic receptor subtypes to histamine-induced cerebellar granular neurotoxicity. Buyukokuroglu, ME; Gepdiremen, A; Hacimuftuoglu, A; Suleyman, H, ) | 0.13 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Our data suggest that thioperamide, at least at 10 mg/kg, increases cocaine-induced locomotion through the combination of pharmacokinetic effects and the blockade of H3 receptors located on non-histaminergic neurons." | ( Effects of the H3 receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions. Alleva, L; Brabant, C; Grisar, T; Jatlow, P; Lakaye, B; Lin, JS; Ohtsu, H; Picciotto, MR; Quertemont, E; Tirelli, E, 2009) | 0.93 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " As ciproxifan and thioperamide are inhibitors of cytochrome P450 enzymes, responsible for metabolizing risperidone and haloperidol, the possibility that the augmentation of antipsychotics by imidazoles resulted from drug-drug interactions was tested." | ( Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs. Ballard, ME; Cowart, M; Decker, MW; Esbenshade, TA; Faghih, R; Fox, GB; Hancock, AA; Pan, L; Roberts, S; Rueter, LE; Zhang, M, 2005) | 0.66 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e." | ( Novel human histamine H(3) receptor antagonists. Breitenbucher, JG; Carruthers, NI; Li, X; Lovenberg, TW; Mazur, C; McAtee, L; Rudolph, D; Shah, C; Wilson, SJ, 2002) | 0.31 |
| "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 |
The drug acts on mechanisms involved in memory consolidation. Methysergide counteracted the effect of thioperamide in the open-field test only at a high dosage (50 mg/kg)
| Excerpt | Relevance | Reference |
|---|---|---|
| " Thioperamide did not alter the dose-response curve to exogenous histamine (0." | ( Histamine H3 receptors modulate antigen-induced bronchoconstriction in guinea pigs. Barnes, PJ; Ichinose, M, 1990) | 1.19 |
| " The results indicate that dimaprit, an H2 agonist, facilitated retention (25 and 50 pg) with a U-shaped dose-response curve typical of drugs acting at postsynaptic receptors." | ( Effect of histamine H2 and H3 receptor modulation in the septum on post-training memory processing. Flood, JF; Morley, JE; Uezu, K, 1998) | 0.3 |
| "), which facilitates histamine release, significantly shifted the methamphetamine dose-response curve to the left when tested together with different doses of methamphetamine and markedly extended the time-course of methamphetamine's discriminative-stimulus effects." | ( Potentiation of the discriminative-stimulus effects of methamphetamine by the histamine H3 receptor antagonist thioperamide in rats. Goldberg, SR; Munzar, P; Nosál, R, 1998) | 0.51 |
| " Methysergide counteracted the effect of thioperamide in the open-field test only at a high dosage (50 mg/kg)." | ( Combined action of thioperamide plus scopolamine, diphenhydramine, or methysergide on memory in mice. Di Carlo, G; Ghi, P; Molinengo, L, 1999) | 0.9 |
| "), showed an anxiogenic-like effect that reached a maximum with the dosage of 5 mg/kg." | ( Mouse light/dark box test reveals anxiogenic-like effects by activation of histamine H1 receptors. Bartolini, A; Ipponi, A; Malmberg-Aiello, P; Schunack, W, ) | 0.13 |
| " The U-shaped dose-response relationship and the time dependency of the effect of thioperamide indicated that the drug acts on mechanisms involved in memory consolidation." | ( Histamine H3-receptor blockade in the rat nucleus basalis magnocellularis improves place recognition memory. Ferretti, C; Gamalero, R; Ghi, P; Orsetti, M, 2002) | 0.54 |
| " In a dose-dependent manner, both the intraperitoneal and oral route of administration resulted in similar ex vivo binding curves and tele-methylhistamine dose-response curves despite the route of administration." | ( Central H3R activation by thioperamide does not affect energy balance. Alexander-Chacko, J; Cramer, JW; Dill, MJ; Gadski, R; Pickard, RT; Shepperd, ML; Sindelar, DK; Smith, DP, 2004) | 0.62 |
| Class | Description |
|---|---|
| primary aliphatic amine | |
| [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) |
|---|---|---|---|---|---|---|---|
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.3162 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
| Thrombopoietin | Homo sapiens (human) | Potency | 3.9811 | 0.0251 | 7.3048 | 31.6228 | AID917; AID918 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 28.1838 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
| arylsulfatase A | Homo sapiens (human) | Potency | 19.0115 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 21.1923 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 14.2191 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 0.0787 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 0.3299 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 56.2341 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 0.3552 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 17.0390 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 7.9433 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 2.2332 | 0.0063 | 8.2350 | 39.8107 | AID881; AID883 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 0.8913 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 0.3552 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [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) |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M2 | Sus scrofa (pig) | Kd | 0.0437 | 0.0001 | 0.0219 | 0.0437 | AID239867 |
| Histamine H3 receptor | Mus musculus (house mouse) | EC50 (µMol) | 0.0110 | 0.0017 | 0.0063 | 0.0110 | AID426159 |
| Histamine H4 receptor | Mus musculus (house mouse) | EC50 (µMol) | 0.1651 | 0.0024 | 2.0716 | 8.7096 | AID1649713; AID1649720 |
| Histamine H4 receptor | Homo sapiens (human) | EC50 (µMol) | 0.1333 | 0.0074 | 0.6016 | 10.0000 | AID1272169; AID1649698; AID414926; AID452998; AID453000; AID453003; AID471098; AID586700 |
| Histamine H3 receptor | Homo sapiens (human) | EC50 (µMol) | 0.0784 | 0.0000 | 0.0947 | 3.1623 | AID414925; AID471097; AID586701 |
| Histamine H3 receptor | Homo sapiens (human) | Kd | 0.0534 | 0.0001 | 0.0138 | 0.0631 | AID239867; AID599205 |
| [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) |
|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | Kb | 0.0620 | 0.0120 | 0.0347 | 0.0620 | AID471111 |
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | Kinact | 0.1250 | 0.0130 | 0.0513 | 0.1250 | AID471111 |
| Histamine H4 receptor | Homo sapiens (human) | Kb | 0.0783 | 0.0028 | 0.0385 | 0.1000 | AID1300590; AID1300597; AID471111 |
| Histamine H4 receptor | Homo sapiens (human) | Kinact | 0.1250 | 0.0130 | 0.0513 | 0.1250 | AID471111 |
| Histamine H3 receptor | Homo sapiens (human) | Kb | 0.0428 | 0.0002 | 0.2097 | 2.0000 | AID1300581; AID1728989 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| AID425224 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. |
| AID270363 | Displacement of [3H]histamine form human H4 receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID586693 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. |
| AID365344 | Displacement of [3H]tiotidine from human histamine H2 receptor | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1300590 | Antagonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 assessed as inhibition of histamine-induced [35S]GTPgammaS binding incubated for 90 mins | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID408970 | Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. |
| AID132793 | To increase N-methyl-histamine levels in mouse brain cortex after po administration as an index of increased histaminergic neuron activity. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency. |
| AID1300577 | Intrinsic activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 at 10 uM preincubated for 2 mins followed by [gamma-32P]GTP addition measured after 20 mins by liquid scintillation counting method relative to histamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID586701 | Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. |
| AID1633204 | Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells at 10 uM incubated for 30 mins by beta-lactamase complementation technology relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1300580 | Intrinsic activity at human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas at 10 uM incubated for 90 mins by [35S]GTPgammaS binding assay relative to histamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID365342 | Displacement of [3H]NAMH from histamine H3 receptor in rat cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID239987 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID426159 | Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies. |
| AID765078 | Invivo inhibition of histamine H3 receptor in po dosed mouse assessed as Nt-methylhistamine level in brain | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol. |
| AID475123 | Displacement of [3H]histamine human recombinant histamine H4 receptor | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. |
| AID468415 | Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
| AID635818 | Antagonist activity at histamine H4 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID765076 | Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Gai2 and Gb1c2 subunit | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol. |
| AID1633201 | Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID635813 | Inverse agonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID780103 | Awakening activity in rat assessed as decrease in slow wave and REM sleep at 10 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders. |
| AID1829881 | Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H |
| AID327691 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. |
| AID471098 | Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists. |
| AID86627 | In vivo effects in mice against H3 receptor on N6-methylhistamine levels in brain (following oral dosing of compound) | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds. |
| AID89718 | In vitro inhibitory activity against histamine H3 receptor using [3H]histamine as radioligand from rat cerebral cortex synaptosomes | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain. |
| AID1125547 | Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties. |
| AID89559 | Antagonistic activity was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 1 | 1998 | Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10 | New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine. |
| AID1572220 | Inverse agonist activity at recombinant human Histamine 3 receptor expressed in CHO-K1 cells assessed as inhibition of RAMH-induced agonist activity preincubated for 20 mins and measured after 60 mins by [35S]-GTPgammaS binding assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H |
| AID1649750 | Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H3R expressed in HEK293T cells by Nano-BRET assay | |||
| AID181164 | Histamine level after treatment was determined in hypothalamus. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? |
| AID428564 | Inhibition of CYP3A4 | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques. |
| AID86283 | Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE. |
| AID765079 | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol. |
| AID86466 | Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells | 2003 | Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8 | Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds. |
| AID1300582 | Agonist activity at human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 90 mins by [35S]GTPgammaS binding assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID270364 | Inhibition of histamine agonist activity at human H4 receptor at 100 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID89714 | In vitro binding affinity against rat histamine H3 receptor | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists. |
| AID89569 | Inhibition of rat Histamine H3 receptor using [3H]N-alpha-methyl histamine | 2003 | Journal of medicinal chemistry, May-08, Volume: 46, Issue:10 | Cyclopropane-based conformational restriction of histamine. (1S,2S)-2-(2-aminoethyl)-1-(1H-imidazol-4-yl)cyclopropane, a highly selective agonist for the histamine H3 receptor, having a cis-cyclopropane structure. |
| AID1300581 | Antagonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 assessed as inhibition of histamine-induced [35S]GTPgammaS binding incubated for 90 mins | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID1300613 | Displacement of [3H]histamine from human histamine H4 receptor expressed in sf9 cells co-expressing mammalian Galphai2 and Gbeta1gamma2 | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID1300576 | Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 assessed as increase in 32Pi level preincubated for 2 mins followed by [gamma-32P]GTP addition measured after 20 mins by liquid scintillation counting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID586700 | Inverse agonist activity at human histamine H4 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. |
| AID1633203 | Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate at 10 uM measured after 30 mins by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1581337 | Antagonist activity at human H4 receptor expressed in CHO-K1 cells co-expressing G protein alpha16 assessed as inhibition of histamine-induced calcium mobilization incubated for 16 hrs by aequorin-based functional assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H |
| AID89723 | In vitro antagonism of the histamine H3-receptor in the rat cerebral cortex. | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17 | Design of potent non-thiourea H3-receptor histamine antagonists. |
| AID468416 | Selectivity, ratio of Ki for human histaminee H4 receptor to Ki for human histamine H3 receptor | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
| AID86459 | Binding affinity to the human histamine H3 receptor | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | The first potent and selective non-imidazole human histamine H4 receptor antagonists. |
| AID365346 | Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID89560 | Antagonistic activity was evaluated against histamine H3 receptor using [3H]- N-alpha-methylhistamine as radioligand in experiment 2 | 1998 | Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10 | New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine. |
| AID635815 | Antagonist activity at histamine H1 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID1637849 | Displacement of [3H]-Nalpha-Methylhistamine from recombinant human histamine H3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Design, synthesis, and |
| AID181165 | Histamine level after treatment was determined in lung. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? |
| AID1649759 | Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 | |||
| AID89573 | Effect on histamine H3 receptors in vitro, on synaptosomes of rat cerebral cortex for the release of [3H]histamine | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds. |
| AID374272 | Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | Non-imidazole histamine H3 ligands, part IV: SAR of 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives. |
| AID765080 | Antagonist activity at histamine H1 receptor in guinea pig ileum | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol. |
| AID1829899 | Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H |
| AID692494 | Binding affinity to human histamine H3 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Histamine H3 receptor as a drug discovery target. |
| AID1637848 | Displacement of [3H]-Nalpha-Methylhistamine from rat histamine H3 receptor expressed in HEK293T cell membranes after 60 mins by liquid scintillation counting analysis | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Design, synthesis, and |
| AID765077 | Antagonist activity at histamine H2 receptor in guinea pig atrium | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol. |
| AID597168 | Antagonist activity at histamine H3 receptor in po dosed 24 hrs fasted Swiss mouse brain assessed as N-methylhistamine level after 90 mins by radioimmunoassay | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
| AID365355 | Antagonist activity at rat full length histamine H3 receptor expressed in HEK cells assessed as inhibition of forskolin-induced intracellular calcium release by SPA | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID88659 | Binding affinity against H3 receptor in guinea pig brain using [3H]N-alpha-methyl histamine as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12 | Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine. |
| AID365358 | Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID599205 | Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists. |
| AID414926 | Agonist activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. |
| AID181166 | Histamine level after treatment was determined in spleen | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? |
| AID127844 | In vivo evaluation for effect on brain tele-methylhistamine levels in mice | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists. |
| AID89561 | Binding affinity to rat Histamine H3 receptor in CHO-K1 cells using [125I]iodoproxyfan as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Different antagonist binding properties of human and rat histamine H3 receptors. |
| AID89571 | Effect at histamine H3 receptors (in vitro) on synaptosomes of rat cerebral cortex assayed by functional H3-receptor assay. | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity. |
| AID86456 | Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay | 2004 | Journal of medicinal chemistry, May-20, Volume: 47, Issue:11 | 1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists. |
| AID1649757 | Displacement of [3H]-histamine from human recombinant H4R expressed in HEK293T cell homogenates | |||
| AID462453 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists. |
| AID1300586 | Intrinsic activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 at 10 uM incubated for 90 mins by [35S]GTPgammaS binding assay relative to histamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID270361 | Displacement of [3H]Nalpha-methylhistamine form human H3 receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID89711 | In vitro antagonist potency at Histamine H3 receptor measured as K+-evoked [3H]histamine release from synaptosomes of rat cerebral cortex. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | 4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity. |
| AID1300589 | Intrinsic activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 at 10 uM incubated for 90 mins by [35S]GTPgammaS binding assay relative to histamine | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID89712 | In vitro antagonistic activity against Histamine H3 receptor on Synaptosomes of rat cerebral cortex. | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5 | Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity. |
| AID1540386 | Antagonist activity at rat H4R by [35S]-GTPgammaS-binding assay | |||
| AID404336 | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening. |
| AID238933 | Antagonist potency against human H3 receptor in GTPgamma-S-Assay | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists. |
| AID599203 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists. |
| AID453000 | Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of GTPase by [gamma-32P]GTP spontaneous degradation assay | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. |
| AID1649698 | Agonist activity at human H4R expressed in HEK293-SF-hH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay | |||
| AID89900 | Binding affinity to the human histamine H4 receptor | 2003 | Journal of medicinal chemistry, Sep-11, Volume: 46, Issue:19 | The first potent and selective non-imidazole human histamine H4 receptor antagonists. |
| AID692511 | Binding affinity to human histamine H4 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Histamine H3 receptor as a drug discovery target. |
| AID1649755 | Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell homogenates | |||
| AID1633207 | Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID113518 | In vivo inhibition of brain N-methyl-histamine formation in mice when administered perorally in presence of oxalate salt | 2004 | Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12 | Meta-substituted aryl(thio)ethers as potent partial agonists (or antagonists) for the histamine H3 receptor lacking a nitrogen atom in the side chain. |
| AID414933 | Intrinsic activity at human H4 receptor expressed in insect Sf9 cells co-expressing RGS19 fusion protein and Gialpha2, Gbeta1gamma2 assessed as gamma[32P]GTP binding at 10 uM by liquid scintillation counting relative to histamine | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. |
| AID1272169 | Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | 2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity. |
| AID270375 | Agonist activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay at 10 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID426169 | Inverse agonist activity at mouse histamine H3 receptor overexpressed in HEK293 cells by [35S]GTPgammaS binding assay relative to basal level | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies. |
| AID436615 | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | 2009 | European journal of medicinal chemistry, Oct, Volume: 44, Issue:10 | Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines. |
| AID481085 | Antagonist activity at human histamine H3 receptor expressed in human HEK293-EBNA cells assessed as inhibition of histamine-induced response at 100 uM by luciferase reporter gene assay | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy. |
| AID586694 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity. |
| AID239936 | Mean binding affinity for human H3 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | 4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists. |
| AID270374 | Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay at 10 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID1495454 | Displacement of [125I]-iodoproxyfan from human striatal full length H3 receptor expressed in CHOK1 cells after 60 mins | |||
| AID365340 | Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1633202 | Inhibition of mouse brain AChE using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID365343 | Displacement of [3H]mepyramine from human histamine H1 receptor | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID635814 | Inhibition of BACE1 at 20 ug/mL by FRET assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID86633 | In vivo antagonist activity at Histamine H3 receptor was screened by measuring the effect on brain histamine turnover after oral application to mice. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21 | 4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity. |
| AID181163 | Histamine level after treatment was determined in colon. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? |
| AID1649748 | Inhibition of UR-DEBa242 binding to mouse recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay | |||
| AID1633232 | Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate measured after 30 mins by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID365345 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1649749 | Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H3R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS4 measured after 60 mins by microbeta scintillation counting method | |||
| AID246007 | Tested for their ability to enhance memory in the adult rats using social recognition memory test | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID89708 | Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes. | 2000 | Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17 | New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency. |
| AID270365 | Selectivity index, Ki for human H3 receptor/Ki for human H4 receptor | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID239988 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID181161 | Histamine level after treatment was determined in adbominal skin. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? |
| AID88633 | In vivo Histamine H3 receptor antagonism, dose required to increase in N-t-methylhistamine levels in Swiss mice brains 90 min after p.o. administration | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists. |
| AID1649720 | Antagonist activity at mouse H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment preincubated for 15 mins followed by histamine addition by luciferase reporter gene a | |||
| AID452843 | Binding affinity to histamine H4 receptor | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. |
| AID89550 | Ex-vivo effective dose required for rat histamine H3 receptor occupancy by the compound using [3H]R-alpha-methylhistamine upon subcutaneous administration | 2002 | Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22 | Novel human histamine H(3) receptor antagonists. |
| AID87710 | Agonistic activity against histamine H2 receptor on guinea pig atrium | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. |
| AID365349 | Displacement of [3H]LY278584 from 5HT2 receptor in rat frontal cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID481083 | Displacement of [3H]N-alpha-methyl-histamine from human histamine H3 receptor expressed in human HEK293-EBNA cells | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Investigation of the bioactive conformation of histamine H3 receptor antagonists by the cyclopropylic strain-based conformational restriction strategy. |
| AID86248 | Agonistic activity against histamine H1 receptor on guinea pig ileum | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. |
| AID597171 | Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
| AID86631 | In vivo Histamine H3 receptor antagonistic activity as increase in N'-methylhistamine levels in Swiss mice after peroral administration | 1998 | Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15 | General construction pattern of histamine H3-receptor antagonists: change of a paradigm. |
| AID86630 | Compound was tested for its effect at histamine H3 receptors (in vivo) on mice by central H3-receptor test. | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity. |
| AID131007 | Potency after oral administration in vivo in mice | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | 4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists. |
| AID1649754 | Displacement of [3H]-UR-PI294 from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes co-expressing RGS19 measured after 60 mins by microbeta scintillation counting method | |||
| AID181162 | Histamine level after treatment was determined in cerebral cortex | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Histamine H3 ligands: just pharmacological tools or potential therapeutic agents? |
| AID1649746 | Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H3R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay | |||
| AID414932 | Intrinsic activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding at 10 uM by liquid scintillation counting relative to histamine | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. |
| AID638346 | Antagonist activity at human H4 receptor expressed in HEK293T cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics. |
| AID1637851 | Selectivity ratio of Ki for recombinant human histamine H4 receptor expressed in CHO cell membranes to Ki for recombinant human histamine H3 receptor expressed in HEK293 cells | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Design, synthesis, and |
| AID1649756 | Displacement of [3H]-histamine from human recombinant H4R stably expressed in human SK-N-MC cell membranes | |||
| AID638337 | Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1 | Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics. |
| AID86457 | Binding affinity to human Histamine H3 receptor in CHO-K1 cells using [125I]iodoproxyfan as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Different antagonist binding properties of human and rat histamine H3 receptors. |
| AID468419 | Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23 | Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates. |
| AID1649705 | Displacement of [3H]-histamine from Galphai2/Gbeta1gamma2-coupled human recombinant H4R expressed in baculovirus infected Sf9 insect cell membranes | |||
| AID270377 | Activity at human H4 receptor expressed in 293-EBNA cells by luciferase reporter gene assay at 100 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID1649760 | Displacement of UR-DEBa176 from mouse recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells | |||
| AID239893 | Tested for its ability to block human histamine H3 receptor activation by the agonist R-alpha-methyl histamine in a [Ca2+] flux assay | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID365357 | Antagonist activity at rat full length histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced intracellular calcium release by FLIPR | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID86644 | In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. |
| AID365350 | Displacement of [3H]LY278584 from 5HT3 receptor in rat frontal cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID246006 | Lowest dose to induce CNS side effects was assessed in a general behavioral screen in rats | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID365348 | Displacement of [3H]LY278584 from 5HT1 receptor in rat frontal cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID86635 | In vivo antagonistic activity was tested against histamine H3 receptor after oral administration to mouse | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. |
| AID635810 | Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID365353 | Antagonist activity at rat full length histamine H3 receptor expressed in rat C6 cells assessed as inhibition of [35S]gammaGTP binding relative to control | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID767822 | Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19 | Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers. |
| AID1637846 | Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as effect on pyrilamine-induced inhibition of electrically evoked contraction treated 20 mins after pyrilamine stimulation | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Design, synthesis, and |
| AID1125546 | Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties. |
| AID471111 | Antagonist activity at human histamine H4 receptor expressed in Sf9 cell membrane coexpressing RGS19 protein assessed as inhibition of 2-Cyano-1-[4-(1H-imidazol-4-yl)butyl]-3-(2-phenylthioethyl)-guanidine-stimulated GTP hydrolysis by steady-state GTPase a | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists. |
| AID1649716 | Inverse agonist activity at human H4R expressed in HEK293 cells co-expressing ELucC/ELucN-beta-arrestin2 assessed as inhibition of histamine-induced beta-arrestin recruitment by luciferase reporter gene assay | |||
| AID1649753 | Displacement of clobenpropit-BODIPY-630/650 from recombinant human NLuc-fused H4R expressed in HEK293T cells by Nano-BRET assay | |||
| AID89719 | Rat Histamine H3 receptor antagonism determined by [K+] - evoked depolarization-induced release of [3H]histamine from rat cerebral cortex synaptosomes | 1996 | Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19 | A novel series of (phenoxyalkyl)imidazoles as potent H3-receptor histamine antagonists. |
| AID1300612 | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cell membrane incubated for 60 mins | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID1649713 | Agonist activity at mouse H4R expressed in HEK293-SF-mH4R-His6-CRE-Luc cells incubated for 5 hrs by luciferase reporter gene assay | |||
| AID597172 | Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins | 2011 | Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9 | N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands. |
| AID365347 | Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID231506 | Ratio of binding affinity of rat H3 receptor to that of human H3 receptor binding affinities; 1:9 | 2001 | Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7 | Different antagonist binding properties of human and rat histamine H3 receptors. |
| AID1633209 | Selectivity index, ratio of CC50 for human SH-SY5Y cells to IC50 for inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID425225 | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11 | Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. |
| AID471097 | Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists. |
| AID1649752 | Displacement of [3H]-N-alpha-methylhistamine from human recombinant H3R expressed in human SK-N-MC cell membranes | |||
| AID239867 | Mean functional activity against human H3 receptor | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | 4-phenoxypiperidines: potent, conformationally restricted, non-imidazole histamine H3 antagonists. |
| AID635812 | Antagonist activity at histamine H3 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID1300597 | Antagonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 assessed as inhibition of UR-RG98-induced [35S]GTPgammaS binding incubated for 90 mins | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Conformational Restriction and Enantioseparation Increase Potency and Selectivity of Cyanoguanidine-Type Histamine H4 Receptor Agonists. |
| AID132754 | In vivo antagonistic activity against Histamine H3 receptor in mouse after peroral administration was assessed from the brain histamine turnover | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5 | Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity. |
| AID89716 | In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex | 2000 | Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20 | Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists. |
| AID270376 | Activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay at 100 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID692493 | Binding affinity to rat cortical histamine H3 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Histamine H3 receptor as a drug discovery target. |
| AID1649747 | Inhibition of UR-DEBa242 binding to human recombinant NLuc/GPCR-fused H4R expressed in HEK293T cells measured after 30 mins by furimazine substrate based BRET assay | |||
| AID89709 | In vitro Histamine H3 receptor antagonist activity in an assay with K+-evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex | 1998 | Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15 | General construction pattern of histamine H3-receptor antagonists: change of a paradigm. |
| AID239562 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID1649758 | Displacement of UR-DEBa176 from human recombinant H4R expressed in HEK293T-SF-His6-CRE-Luc cells | |||
| AID692510 | Binding affinity to rat histamine H4 receptor | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Histamine H3 receptor as a drug discovery target. |
| AID1272170 | Antagonist activity at human histamine 4 receptor expressed in Sf9 cell membranes co-expressing Galphai2 and Gbeta1gamma2 assessed as [35S]GTPgammaS binding by scintillation counting relative to control histamine | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | 2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity. |
| AID414925 | Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent. |
| AID1819613 | Inhibition of CH24H expressing human 293-F cells for 15 minutes using [14C] cholesterol as substrate and measured after 5 hrs by trypan blue staining based thin-layer chromatography | |||
| AID1649711 | Inverse agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells assessed as reduction in histamine-induced inhibition of forskolin stimulated luciferase activity by luciferase reporter gene assay | |||
| AID635816 | Antagonist activity at histamine H2 receptor expressed in HEK293 cells co-transfected with pCRE-Luc gene assessed as inhibition of forskolin/histamine-induced cAMP accumulation at 1 uM after 5 hrs by luciferase reporter gene assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H₃R and BACE 1 inhibitory activities. |
| AID365352 | Antagonist activity at human full length histamine H3 receptor expressed in HEK cells assessed as inhibition of [35S]gammaGTP binding relative to control | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1495453 | Displacement of [3H]-(R)alpha-MeHA from rat brain H3 receptor | |||
| AID1637850 | Displacement of [3H]-Nalpha-Methylhistamine from human recombinant histamine H4 receptor expressed in CHO cell membranes after 1 hrs by liquid scintillation counting analysis | 2019 | MedChemComm, Feb-01, Volume: 10, Issue:2 | Design, synthesis, and |
| AID88663 | Inhibition of N-alpha-methylhistamine binding to histamine H3 receptor of guinea pig brain membranes | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | 4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor. |
| AID86629 | Histamine H3 receptor antagonist potency in vivo in mice after peroral administration | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21 | Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds. |
| AID453003 | Inverse agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. |
| AID365341 | Displacement of [3H]NAMH from histamine H3 receptor in human cortex | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID452998 | Agonist activity at human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2 assessed as stimulation of [35S]GTPgammaS binding | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. |
| AID86645 | In vitro antagonistic activity against histamine H3 receptor on rat cerebral cortex | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6 | [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. |
| AID1633205 | Inhibition of mouse brain AChE at 10 uM using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1728989 | Antagonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as reduction in (R)-(-)-alpha-methylhistamine dihydrobromide-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by LANCE ultra cAMP TR-FRET as | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
| AID765075 | Anticonvulsant activity in Wistar rat assessed as protection against maximum electric shock-induced tonic hind limb extension at 10 mg/kg, ip | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | Anticonvulsant properties of histamine H3 receptor ligands belonging to N-substituted carbamates of imidazopropanol. |
| AID77117 | In vivo antihistaminic (Histamine H3) activity was determined in guinea pig | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16 | 4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: novel antagonists of the histamine H3 receptor. |
| AID270362 | Inhibition of histamine agonist activity at human H3 receptor at 100 uM | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID426166 | Displacement of 3-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone from mouse histamine H3 receptor expressed in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies. |
| AID1540385 | Antagonist activity at mouse H4R by [35S]-GTPgammaS-binding assay | |||
| AID365339 | Displacement of [3H]NAMH from human full length histamine H3 receptor expressed in rat C6 cells | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1125545 | Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in HEK-293 cell membrane after 90 mins by liquid scintillation counting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties. |
| AID239591 | In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID246008 | Tested for their ability to enhance learning in the rat pups using inhibitory avoidance acquisition model | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | 4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention. |
| AID365354 | Antagonist activity at human full length histamine H3 receptor expressed in rat C6 cells assessed as inhibition of forskolin-induced cAMP release by SPA | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1540384 | Antagonist activity at human H4R by [35S]-GTPgammaS-binding assay | |||
| AID780104 | Awakening activity in rat assessed as increased wakefulness at 10 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22 | Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders. |
| AID270373 | Antagonist activity at human H4 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID365356 | Antagonist activity at human full length histamine H3 receptor expressed in HEK293 cells assessed as inhibition of (R)-alpha-methylhistamine-induced intracellular calcium release by FLIPR | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID462454 | Inverse agonist activity at human histamine H4 receptor expressed in HEK293T cells by CRE-beta-galactosidase assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists. |
| AID1728991 | Agonist activity at recombinant human H3R expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by LANCE ultra cAMP TR-FRET assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Structural modifications in the distal, regulatory region of histamine H |
| AID452842 | Binding affinity to histamine H3 receptor | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20 | 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization. |
| AID270372 | Antagonist activity at human H3 receptor expressed in 293-EBNA cells assessed as inhibition of histamine agonist activity by luciferase reporter gene assay | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18 | Stereochemical diversity-oriented conformational restriction strategy. Development of potent histamine H3 and/or H4 receptor antagonists with an imidazolylcyclopropane structure. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3 | Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2000 | British journal of pharmacology, Dec, Volume: 131, Issue:7 | Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 299, Issue:3 | Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 299, Issue:3 | Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3 | Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | Molecular pharmacology, Mar, Volume: 59, Issue:3 | Cloning, expression, and pharmacological characterization of a novel human histamine receptor. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 296, Issue:3 | Cloning and characterization of a novel human histamine receptor. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2003 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3 | Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2000 | British journal of pharmacology, Dec, Volume: 131, Issue:7 | Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1 | Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2004 | Biochemical pharmacology, Sep-01, Volume: 68, Issue:5 | Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. |
| AID1346044 | Mouse H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1 | Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2004 | Biochemical pharmacology, Sep-01, Volume: 68, Issue:5 | Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2004 | Biochemical pharmacology, Sep-01, Volume: 68, Issue:5 | Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2001 | The Biochemical journal, Apr-15, Volume: 355, Issue:Pt 2 | Genomic organization and characterization of splice variants of the human histamine H3 receptor. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2001 | Biochemical and biophysical research communications, Jan-12, Volume: 280, Issue:1 | The rat H3 receptor: gene organization and multiple isoforms. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2000 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 293, Issue:3 | Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles. |
| AID1346088 | Mouse H3 receptor (Histamine receptors) | 2004 | Journal of neurochemistry, Sep, Volume: 90, Issue:6 | Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2002 | European journal of pharmacology, Oct-18, Volume: 453, Issue:1 | Characteristics of recombinantly expressed rat and human histamine H3 receptors. |
| AID1346028 | Rat H4 receptor (Histamine receptors) | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1 | Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. |
| AID1346017 | Rat H3 receptor (Histamine receptors) | 2000 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 293, Issue:3 | Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles. |
| AID1346055 | Human H4 receptor (Histamine receptors) | 2001 | Molecular pharmacology, Mar, Volume: 59, Issue:3 | Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. |
| AID1346107 | Human H3 receptor (Histamine receptors) | 2002 | European journal of pharmacology, Oct-18, Volume: 453, Issue:1 | Characteristics of recombinantly expressed rat and human histamine H3 receptors. |
| 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. |
| 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. |
| AID1347159 | Primary screen GU Rhodamine 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. |
| AID1347160 | Primary screen NINDS Rhodamine 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. |
| 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. |
| AID1798786 | Radioligand Binding Assay from Article 10.1021/jm8003625: \\The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.\\ | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17 | The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. |
| AID1798266 | H3R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\ | 2005 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3 | Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. |
| AID1798265 | H4R Radioligand Binding Assay from Article 10.1124/jpet.105.087965: \\Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.\\ | 2005 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 314, Issue:3 | Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 11 (2.37) | 18.7374 |
| 1990's | 187 (40.22) | 18.2507 |
| 2000's | 176 (37.85) | 29.6817 |
| 2010's | 78 (16.77) | 24.3611 |
| 2020's | 13 (2.80) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (38.29) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (0.21%) | 5.53% |
| Reviews | 6 (1.24%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 476 (98.55%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||