Quinelorane is a selective serotonin reuptake inhibitor (SSRI) that has been studied for its potential use in the treatment of depression, anxiety, and other mental health conditions. It is a synthetic compound that was first developed in the 1980s. Quinelorane is thought to work by increasing the levels of serotonin in the brain, which is a neurotransmitter that plays a role in regulating mood, sleep, appetite, and other functions. Research on quinelorane has been limited due to concerns about its potential side effects. However, some studies have shown that it may be effective in treating depression and anxiety. Further research is needed to determine the safety and efficacy of quinelorane for these conditions.'
quinelorane: LY 175887 is dextrorotary isomer; LY 137157 is a racemic mixture [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 57242 |
| CHEMBL ID | 155731 |
| CHEBI ID | 92230 |
| SCHEMBL ID | 378583 |
| MeSH ID | M0137707 |
| Synonym |
|---|
| ly 163502 |
| (5ar-trans)-5,5a,6,7,8,9,9a,10-octahydro-6-propylpyrido(2,3-g)quinazolin-2-amine |
| quineloranum [inn-latin] |
| ly 137157 |
| quinelorane |
| quinelorane [inn:ban] |
| pyrido(2,3-g)quinazolin-2-amine, 5,5a,6,7,8,9,9a,10-octahydro-6-propyl-, (5ar-trans)- |
| quinelorano [inn-spanish] |
| BRD-K13261168-001-01-4 |
| gtpl954 |
| BPBIO1_001213 |
| NCGC00015869-01 |
| lopac-q-110 |
| BIOMOL-NT_000026 |
| LOPAC0_001020 |
| PDSP2_000522 |
| 97466-90-5 |
| NCGC00162319-03 |
| (5ar,9ar)-6-propyl-5a,7,8,9,9a,10-hexahydro-5h-pyrido[2,3-g]quinazolin-2-amine |
| CHEMBL155731 , |
| (5ar,9ar)-6-propyl-5,5a,6,7,8,9,9a,10-octahydropyrido[2,3-g]quinazolin-2-amine |
| 6-propyl-5,5a,6,7,8,9,9a,10-octahydro-pyrido[2,3-g]quinazolin-2-ylamine(quinelorane) |
| quinerolane |
| bdbm50016017 |
| (5ar,9ar)-6-propyl-5,5a,6,7,8,9,9a,10-octahydro-pyrido[2,3-g]quinazolin-2-ylamine |
| NCGC00162319-04 |
| z0x4vt3y1q , |
| quinelorano |
| unii-z0x4vt3y1q |
| quineloranum |
| cas-97466-90-5 |
| dtxcid2026315 |
| dtxsid4046315 , |
| tox21_112009 |
| CCG-205100 |
| (-)-(5ar,9ar)-2-amino-5,5a,6,7,8,9,9a,10-octahydro-6-propylpyrido(2,3-g)quinazoline |
| quinelorane [inn] |
| tox21_112009_1 |
| NCGC00162319-05 |
| SCHEMBL378583 |
| CHEBI:92230 |
| pyrido(2,3-g)quinazolin-2-amine, 5,5a,6,7,8,9,9a,10-octahydro-6-propyl-, trans- |
| ly137157 |
| 97430-52-9 |
| ly175877 |
| pyrido(2,3-g)quinazolin-2-amine, 5,5a,6,7,8,9,9a,10-octahydro-6-propyl-, (5as-trans)- |
| rel-(5ar,9ar)-6-propyl-5,5a,6,7,8,9,9a,10-octahydropyrido[2,3-g]quinazolin-2-amine |
| Q7272223 |
| SDCCGSBI-0050993.P002 |
| NCGC00162319-07 |
| pyrido[2,3-g]quinazolin-2-amine, 5,5a,6,7,8,9,9a,10-octahydro-6-propyl-, (5ar,9ar)- |
| AKOS040753676 |
Quinelorane is a BCD partial ergoline with potent dopaminergic effects in vitro and in vivo.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Quinelorane is a BCD partial ergoline with potent dopaminergic effects in vitro and in vivo. " | ( [3H]-quinelorane binds to D2 and D3 dopamine receptors in the rat brain. Gackenheimer, SL; Gehlert, DR; Schaus, JM, 1995) | 2.25 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Quinelorane (LY163502) has the endocrine, neurochemical and behavioral profile of a potent and highly selective D2-dopaminergic agonist. " | ( Preclinical studies on quinelorane, a potent and highly selective D2-dopaminergic agonist. Clemens, JA; Foreman, MM; Fuller, RW; Gidda, JS; Hynes, MD; Kornfeld, EC; Nichols, CL; Schaus, JM, 1989) | 2.03 |
Quinelorane (IM) treatment produced dose-dependent effects on male sexual responding. Flibanserin as well as buspirone significantly reduced dystonia in wild-type mice.
| Excerpt | Reference | Relevance |
|---|---|---|
| "In quinelorane-treated wild-type mice flibanserin as well as buspirone significantly reduced dystonia (p < 0.05)." | ( The 5-HT1A-receptor agonist flibanserin reduces drug-induced dyskinesia in RGS9-deficient mice. Adamaszek, M; Beck, J; Ohm, S; Schwarz, J; Strecker, K; Wegner, F, 2012) | 0.89 |
| "Quinelorane (IM) treatment produced dose-dependent effects on male sexual responding." | ( Quinelorane (LY163502), a D2 dopamine receptor agonist, acts centrally to facilitate penile erections of male rhesus monkeys. Pomerantz, SM, 1991) | 2.45 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " These experiments provide further evidence that dopaminergic mechanisms may play a role in the regulation of male sexual behavior of rhesus monkeys and, in particular, demonstrate that the direction of the effect depends on the dopamine receptor subtype and dosage of the dopamine agonist being administered." | ( Dopaminergic influences on male sexual behavior of rhesus monkeys: effects of dopamine agonists. Pomerantz, SM, 1992) | 0.28 |
| " Mild and advanced parkinsonism in nonhuman primates can be produced with fixed dosing regimens of MPTP." | ( D(1) dopamine receptor agonists are more effective in alleviating advanced than mild parkinsonism in 1-methyl-4-phenyl-1,2,3, 6-tetrahydropyridine-treated monkeys. Goulet, M; Madras, BK, 2000) | 0.31 |
| " Administration of the D(1) antagonist SCH23390 enhanced the effects of levonantradol, producing a leftward shift of the log dose-response curve." | ( Cannabinoid and dopamine interaction in rodent brain: effects on locomotor activity. Conley, TJ; Howlett, AC; Meschler, JP, 2000) | 0.31 |
| " The dissociation constant (K(B)) and relative intrinsic efficacy (E(r)) for each partial agonist were calculated using a partial agonist interaction null model in which the effects of fixed concentrations of each partial agonist on the dopamine dose-response curve were evaluated." | ( Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells. Abell, C; Avalos, M; Kwan, SW; Mak, C; Randall, PK; Trzeciakowski, JP; Wilcox, RE, ) | 0.13 |
| " The present study was designed to determine the extent to which D2/3 receptor activation and blockade can modulate morphine-induced locomotion using a novel cumulative dosing procedure in Swiss-Webster mice." | ( The modulatory actions of dopamine D2/3 agonists and antagonists on the locomotor-activating effects of morphine and caffeine in mice. Beardsley, PM; Cook, CD, 2003) | 0.32 |
| Class | Description |
|---|---|
| quinazolines | Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. |
| [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) |
|---|---|---|---|---|---|---|---|
| acetylcholinesterase | Homo sapiens (human) | Potency | 2.1216 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347398 |
| dopamine D1 receptor | Homo sapiens (human) | Potency | 9.2000 | 0.0052 | 1.3022 | 8.1995 | AID624455 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 13.0051 | 0.1000 | 20.8793 | 79.4328 | AID588453; AID588456 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 16.1096 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 16.8336 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 24.5454 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 20.9067 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 9.7717 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 10.6213 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 21.1317 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 33.4889 | 0.0006 | 27.2152 | 1,122.0200 | AID743202 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 0.0010 | 6.0009 | 35.4813 | AID943 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 33.4915 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| [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) |
|---|---|---|---|---|---|---|---|
| D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0003 | 0.5026 | 7.7625 | AID61181 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.0009 | 0.0000 | 0.6020 | 10.0000 | AID239943 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1510 | 0.0001 | 0.5494 | 8.4000 | AID64424 |
| [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) |
|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.0306 | 0.0000 | 0.1874 | 3.9000 | AID1189844; AID310686 |
| D(3) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.0010 | 0.0001 | 0.0247 | 0.6690 | AID310687 |
| [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) |
|---|---|---|---|---|---|---|---|
| D | Rattus norvegicus (Norway rat) | K 0.5 | 5.0000 | 0.0004 | 0.0042 | 0.0062 | AID61343 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | K 0.5 | 0.0007 | 0.0004 | 0.0439 | 0.1700 | AID61683 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | K 0.5 | 0.3574 | 0.0002 | 0.4747 | 2.2500 | AID61330; AID64778 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| 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. |
| 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. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| 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. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1189844 | Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease. |
| AID64778 | Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID61330 | Affinity on C6 glioma cells transfected with Dopamine receptor D2L | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID61343 | Inhibition of [3H]SCH-23390 binding to rat striatal membrane Dopamine receptor D1 | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID61683 | Affinity on C6 glioma cells transfected with Dopamine receptor D3 | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5 | Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane. |
| AID61181 | In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Aporphines as antagonists of dopamine D-1 receptors. |
| AID239943 | Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID182829 | Ability to block adenylate cyclase stimulation caused by 10 uM dopamine in rat retinal tissue in vitro at a concentration of 100 uM | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Aporphines as antagonists of dopamine D-1 receptors. |
| AID64424 | In vitro binding affinity towards rat Dopamine receptor D2 by [3H]spiperone displacement. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Aporphines as antagonists of dopamine D-1 receptors. |
| AID310686 | Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
| AID310688 | Selectivity for human dopamine D3 receptor over human dopamine D2 receptor | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
| AID191925 | Ability to stimulate adenylate cyclase in rat retinal tissue over basal levels; NS=no significant stimulation | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Aporphines as antagonists of dopamine D-1 receptors. |
| AID310687 | Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation | 2007 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24 | Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
| 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. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1995 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2 | Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 1992 | European journal of pharmacology, Apr-10, Volume: 225, Issue:4 | Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1992 | European journal of pharmacology, Apr-10, Volume: 225, Issue:4 | Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 1995 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 275, Issue:2 | Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 10 (8.85) | 18.7374 |
| 1990's | 43 (38.05) | 18.2507 |
| 2000's | 38 (33.63) | 29.6817 |
| 2010's | 15 (13.27) | 24.3611 |
| 2020's | 7 (6.19) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.47) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 117 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||