Page last updated: 2024-11-04

quinacrine

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Description

Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9. [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]

Cross-References

ID SourceID
PubMed CID237
CHEMBL ID7568
CHEBI ID8711
SCHEMBL ID19225
MeSH IDM0018330

Synonyms (138)

Synonym
acriquine
quinactine
acrinamine
mepacrine [inn:ban]
haffkinine
1,4-pentanediamine, n4-(6-chloro-2-methoxy-9-acridinyl)-n1,n1-diethyl-
mepacrinum [inn-latin]
antimalarina
einecs 201-508-7
hsdb 3253
akrichin
ai3-04467
st 439
acridine, 6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxy-
mepacrina [inn-spanish]
italchine
AB00053540-08
BRD-A45889380-336-03-4
n*4*-(6-chloro-2-methoxy-acridin-9-yl)-n*1*,n*1*-diethyl-pentane-1,4-diamine
KBIO1_000101
DIVK1C_000101
3-chloro-7-methoxy-9-(1-methyl-4-diethylaminobutylamino)acridine
CHEBI:8711 ,
2-methoxy-6-chloro-9-diethylaminopentylaminoacridine
6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxyacridine
4-n-(6-chloro-2-methoxyacridin-9-yl)-1-n,1-n-diethylpentane-1,4-diamine
n(4)-(6-chloro-2-methoxy-9-acridinyl)-n(1),n(1)-diethyl-1,4-pentanediamine
n~4~-[6-chloro-2-(methyloxy)acridin-9-yl]-n~1~,n~1~-diethylpentane-1,4-diamine
n'-(6-chloro-2-methoxy-acridin-9-yl)-n,n-diethyl-pentane-1,4-diamine dihydrochloride
ccris 3726
SPECTRUM_000929
IDI1_000101
PRESTWICK3_000318
PRESTWICK2_000318
BSPBIO_000316
BSPBIO_002112
CMAP_000067
erion
n4-(6-chloro-2-methoxy-9-acridinyl)-n1,n1-diethyl-1,4-pentanediamine
acirchine
n4-(6-chloro-2-methoxy-acridin-9-yl)-n1,n1-diethyl-pentane-1,4-diamine
sn-390 (dihydrochloride dihydrate)
rp-866 (dihydrochloride dihydrate)
AB00053540
mepacrine
ATABRINE ,
quinacrine
83-89-6
C07339
chinacrin
DB01103
SPECTRUM5_001405
KBIO2_006545
KBIO2_003977
KBIO2_005075
KBIO2_002507
KBIOGR_001011
KBIO2_001409
KBIOGR_002507
KBIO2_007643
NCI60_000926
KBIOSS_002515
KBIOSS_001409
KBIO3_002985
KBIO3_001612
SPECTRUM2_000888
SPBIO_000676
PRESTWICK1_000318
SPBIO_002535
NINDS_000101
SPECTRUM3_000606
PRESTWICK0_000318
SPECTRUM4_000496
BPBIO1_000348
LOPAC0_000970
NCGC00162300-01
HMS2090L03
NCGC00015874-04
gnf-pf-5448 ,
CHEMBL7568 ,
quinacrin
mepacrine (inn)
D08179
STL061087
n~4~-(6-chloro-2-methoxyacridin-9-yl)-n~1~,n~1~-diethylpentane-1,4-diamine
AKOS000541535
6-chloro-2-methoxy-9-acridinyl(4-diethylamino-1-methylbutyl)amine
n*4*-(6-chloro-2-methoxy-acridin-9-yl)-n*1*,n*1*-diethyl-pentane-1,4-diamine (mepacrine)
n*4*-(6-chloro-2-methoxy-acridin-9-yl)-n*1*,n*1*-diethyl-pentane-1,4-diamine ; (mepacrine)
6-chloro-n-(5-(diethylamino)pentan-2-yl)-2-methoxyacridin-9-amine
bdbm50015214
n''-(6-chloro-2-methoxy-acridin-9-yl)-n,n-diethyl-pentane-1,4-diamine
CCG-205050
NCGC00015874-03
NCGC00015874-02
ccris 8633
mepacrina
mepacrinum
unii-h0c805xyde
h0c805xyde ,
AKOS016340229
BBL028456
SCHEMBL19225
quinacrine, mepacrine
MS-1557
quinacrine [vandf]
mepacrine [who-dd]
quinacrine [mi]
65960-39-6
quinacrine [hsdb]
mepacrine [inn]
AB00053540-09
6-chloro-n-[5-(diethylamino)pentan-2-yl]-2-methoxyacridin-9-amine
(.+/-.)-quinacrine
2-methoxy-6-chloro-9-diethylaminopent-2-ylaminoacridine
atebrine (salt/mix)
atebrin (salt/mix)
acridine, 6-chloro-9-[[4-(diethylamino)-1-methylbutyl]amino]-2-methoxy-
AB00053540_10
DTXSID7022627
SBI-0050943.P004
NCGC00015874-08
n4-(6-chloro-2-methoxyacridin-9-yl)-n1,n1-diethylpentane-1,4-diamine
Z31251611
FT-0674264
Q417208
n'-(6-chloro-2-methoxyacridin-9-yl)-n,n-diethylpentane-1,4-diamine
gtpl10172
BRD-A45889380-300-04-8
SDCCGSBI-0050943.P006
NCGC00015874-12
quinacrine (hydrochloride,hydrate)
atabrine hydrochloride dihydrate; mepacrine hydrochloride
FT-0778222
quinacrine,mepacrine
EN300-246511
CS-0007762
HY-13735

Research Excerpts

Overview

Quinacrine (QC) is a tricyclic compound and a derivative of 9-aminoacridine. Quinacrine sterilization is a safe method for the sterilization of HIV-infected women.

ExcerptReferenceRelevance
"Quinacrine is an antimalarial drug that was repositioned for treatment of cancer. "( Lactoferrin/Hyaluronic acid double-coated lignosulfonate nanoparticles of quinacrine as a controlled release biodegradable nanomedicine targeting pancreatic cancer.
Abdallah, OY; Elnaggar, YSR; Etman, SM; Mehanna, RA, 2020
)
2.23
"Quinacrine (QC) is a tricyclic compound and a derivative of 9-aminoacridine. "( Anti-Cancer Stem Cells Potentiality of an Anti-Malarial Agent Quinacrine: An Old Wine in a New Bottle.
Das, B; Kundu, CN, 2021
)
2.3
"Quinacrine is an older antimalarial drug that remains in use for a variety of illnesses including treatment-resistant giardiasis."( A Case of Quinacrine-induced Psychosis: Case Report.
Patel, A; Pedapudi, A; Stewart, J, 2021
)
2.47
"Quinacrine is a repositioned drug with an anticancer activity but suffers a limited ability to reach tumor cells."( Undaria pinnatifida fucoidan nanoparticles loaded with quinacrine attenuate growth and metastasis of pancreatic cancer.
Abdallah, OY; Bary, AA; Elnaggar, YSR; Etman, SM; Mehanna, RA, 2021
)
1.59
"Quinacrine is an effective treatment for nitroimidazole-refractory giardiasis with good tolerability."( Quinacrine Treatment of Nitroimidazole-Refractory Giardiasis.
Asgeirsson, H; Hellgren, U; Ydsten, KA, 2022
)
3.61
"Quinacrine is a formerly used antiparasitic drug that is intensely fluorescent, lipophilic, and a tertiary amine."( Assessment of cation trapping by cellular acidic compartments.
Bouthillier, J; Marceau, F; Roy, C, 2014
)
1.12
"Quinacrine is a relatively non-toxic drug, once given almost exclusively for malaria. "( Quinacrine for extremity melanoma in a mouse model of isolated limb perfusion (ILP).
Blum, AB; Donahue, MJ; Fisher, DT; Haslinger, ML; Kim, M; Park, IY; Skitzki, JJ, 2015
)
3.3
"Quinacrine is an anti-malarial drug with versatile use in the treatment of diseases involving inflammatory response such as rheumatoid arthritis and lupus erythematosus."( Repurposing the anti-malarial drug, quinacrine: new anti-colitis properties.
Chaparala, A; Chumanevich, A; Chumanevich, AA; Hofseth, LJ; Nagarkatti, M; Nagarkatti, P; Witalison, EE, 2016
)
1.43
"Quinacrine sterilization is a safe method for the sterilization of HIV-infected women and has no short-term effect on the pathology of the disease."( Quinacrine sterilization for human immunodeficiency virus-positive women.
Barbosa Magalhães, E; Camargos, AF; Carvalho Ferreira, D; de Carvalho Ferreira, CR; de Magalhães, DR; Lippes, J, 2009
)
3.24
"Quinacrine is a potent antiprion compound in cell culture models of prion disease but has failed to show efficacy in animal bioassays and human clinical trials. "( Continuous quinacrine treatment results in the formation of drug-resistant prions.
Ahn, M; DeArmond, SJ; Ghaemmaghami, S; Giles, K; Legname, G; Lessard, P; Prusiner, SB, 2009
)
2.19
"Quinacrine is a cationic amphiphilic drug."( Mechanisms for Kir channel inhibition by quinacrine: acute pore block of Kir2.x channels and interference in PIP2 interaction with Kir2.x and Kir6.2 channels.
Aréchiga-Figueroa, IA; Ferrer-Villada, T; López-Izquierdo, A; Moreno-Galindo, EG; Ponce-Balbuena, D; Rodríguez-Martínez, M; Rodríguez-Menchaca, AA; Sánchez-Chapula, JA; van der Heyden, MA, 2011
)
1.36
"Quinacrine is a drug that is known to heal neuronal cell culture infected with prions, which are the causative agents of neurodegenerative diseases called transmissible spongiform encephalopathies. "( Quinacrine reactivity with prion proteins and prion-derived peptides.
Bouř, P; Březinová, A; Dvořáková, E; Hlaváček, J; Holada, K; Janoušková, O; Šafařík, M; Sebestík, J; Stibor, I; Zawada, Z, 2013
)
3.28
"Quinacrine is an inhibitor of phospholipase A(2), an enzyme thought to be involved in activity-related injury of skeletal muscles. "( Attenuation of stretch-induced histopathologic changes of skeletal muscles by quinacrine.
Stauber, WT; Willems, ME, 2003
)
1.99
"Quinacrine is an acridine derivative under investigation for its use in nonsurgical female sterilization. "( A one-year neonatal mouse carcinogenesis study of quinacrine dihydrochloride.
Cancel, AM; Dillberger, JE; McClain, RM; Rehkemper, U; Smith, T; Sokal, D,
)
1.83
"Quinacrine sterilization is a procedure that is widely used in the developing world, while hysteroscopic procedures such as the Essure and Adiana procedures are either currently available or emerging as visually controlled, device-dependent methods for reliable transcervical sterilization that may be performed in an outpatient or office setting with minimal anesthesia and high patient acceptability."( Transcervical sterilization.
Abbott, J, 2007
)
1.06
"Quinacrine (QC) is an anti-inflammatory drug that has been used for the treatment of malaria and rheumatoid diseases. "( Quinacrine inhibits the epidermal dendritic cell migration initiating T cell-mediated skin inflammation.
Fairchild, RL; Gasparian, AV; Gorbachev, AV; Gudkov, AV; Gurova, KV, 2007
)
3.23
"Quinacrine mustard is a potent inactivator of the F1-ATPase."( Quinacrine mustard inactivates the bovine heart mitochondrial F1-ATPase with the modification of the beta subunit.
Allison, WS; Laikind, PK, 1983
)
2.43
"Quinacrine is a fluorescent anti-malarial acridine derivative which binds selectively to a population of nerves, presumably peptidergic, and to certain peptide hormone-producing cells. "( Quinacrine accumulates in certain peptide hormone-producing cells.
Ahrén, B; Ekelund, M; Håkanson, R; Lundquist, I; Sundler, F, 1980
)
3.15
"Quinacrine (QU) is an inhibitor of phospholipase A2 (PLA2). "( Quinacrine acts like an acetylcholine receptor antagonist rather than like a phospholipase A2 inhibitor in a passive avoidance task in the chick.
Hölscher, C, 1995
)
3.18
"Quinacrine (QUIN) is a well known inhibitor of PLA2."( Late preventive effects of quinacrine on carbon tetrachloride induced liver necrosis.
Castro, JA; de Toranzo, EG; González Padrón, A, 1993
)
1.3
"Quinacrine is a noncompetitive antagonist of the nicotinic acetylcholine receptor (AChR) which displays severalfold fluorescent enhancement upon binding to AChR-rich membranes from Torpedo californica electric organ. "( Quinacrine and ethidium bromide bind the same locus on the nicotinic acetylcholine receptor from Torpedo californica.
Hareland, ML; Lurtz, MM; Pedersen, SE, 1997
)
3.18
"Quinacrine is a fluorescence probe useful for studying the effect of local anesthetics. "( Quinacrine inhibits the calcium-induced calcium release in heavy sarcoplasmic reticulum vesicles.
Fernandez-Belda, F; Gomez-Fernandez, JC; Soler, F, 1989
)
3.16

Effects

Quinacrine has potential as a chemosensitizer when combined with chemotherapy, but its anti-cancer mechanisms remain unclear. Quinacrine sterilization has the potential to meet the unmet need for female sterilization in developing countries.

ExcerptReferenceRelevance
"Quinacrine (Qx) has been used since the 1930s as preventive antimalarial compound."( Quinacrine as a potential treatment for COVID-19 virus infection.
Hernández Pando, R; Pérez de la Cruz, V; Pineda, B; Sotelo, J, 2021
)
2.79
"Quinacrine has been used for therapeutic drugs in some clinical settings. "( Quinacrine Inhibits ICAM-1 Transcription by Blocking DNA Binding of the NF-κB Subunit p65 and Sensitizes Human Lung Adenocarcinoma A549 Cells to TNF-α and the Fas Ligand.
Harada, M; Hiramatsu, R; Kataoka, T; Kondo, T; Matsuda, I; Morimoto, K; Muko, R; Okina, Y, 2017
)
3.34
"Quinacrine has been widely used in treatment of parasitic diseases such as malaria and giardiasis, and in the treatment of autoimmune diseases. "( Quinacrine-induced occlusive fibrosis in the human fallopian tube is due to a unique inflammatory response and modification of repair mechanisms.
Fail, PA; Growe, RG; Lippes, J; Luster, MI, 2013
)
3.28
"Quinacrine has demonstrable efficacy against melanoma cells in vitro and in a clinically relevant model of ILP. "( Quinacrine for extremity melanoma in a mouse model of isolated limb perfusion (ILP).
Blum, AB; Donahue, MJ; Fisher, DT; Haslinger, ML; Kim, M; Park, IY; Skitzki, JJ, 2015
)
3.3
"Quinacrine has potential as a chemosensitizer when combined with chemotherapy, but its anti-cancer mechanisms remain unclear. "( Quinacrine enhances cisplatin-induced cytotoxicity in four cancer cell lines.
Bi, Q; Dong, L; Fu, J; Ge, X; Li, S; Li, X; Wang, Y; Wu, D; Zhang, X, 2010
)
3.25
"Quinacrine has the potential to be used as a chemotherapy adjuvant when combined with cisplatin."( Quinacrine enhances cisplatin-induced cytotoxicity in four cancer cell lines.
Bi, Q; Dong, L; Fu, J; Ge, X; Li, S; Li, X; Wang, Y; Wu, D; Zhang, X, 2010
)
3.25
"Quinacrine has been widely explored in treatment of malaria, giardiasis, and rheumatic diseases. "( Quinacrine sensitizes hepatocellular carcinoma cells to TRAIL and chemotherapeutic agents.
Abdulghani, J; Allen, JE; Dicker, DT; Dolloff, NG; El-Deiry, WS; Gallant, JN; Hong, B; Katz, SI; Navaraj, A; Smith, CD; Wang, W, 2011
)
3.25
"Quinacrine has been reported as an antiprion agent and proposed as an immediately applicable treatment for Creutzfeldt-Jakob disease (CJD). "( Compassionate use of quinacrine in Creutzfeldt-Jakob disease fails to show significant effects.
Alpérovitch, A; Belorgey, C; Boher, E; Brandel, JP; Delasnerie-Lauprêtre, N; Faucheux, BA; Haïk, S; Hauw, JJ; Laplanche, JL; Salomon, D; Sazdovitch, V; Soubrié, C, 2004
)
2.09
"Quinacrine has evolved from instillations of a solution to the development of pellets to the use of an IUD vector."( Nonsurgical female sterilization.
Cole, LP; Laufe, LE, 1980
)
0.98
"Quinacrine, which has been shown to bind to neurones in the peripheral nervous system, was localized in Purkinje cells in the cerebellum and pyramidal cells in the cerebral cortex and hippocampus of the guinea-pig brain. "( Quinacrine-positive neurones in some regions of the guinea-pig brain.
Burnstock, G; Crowe, R, 1984
)
3.15
"The quinacrine method has the potential to meet estimated developing country needs and also to be widely used in developed countries."( Potential demand for voluntary female sterilization in the 1980s: the compelling need for a nonsurgical method.
Kessel, E; Mumford, SD, 1982
)
0.72
"Quinacrine resistance has been induced in 3 Giardia duodenalis laboratory stocks and 4 lines resistant to other drugs. "( Quinacrine-resistant Giardia duodenalis.
Campbell, RW; Upcroft, JA; Upcroft, P, 1996
)
3.18
"Quinacrine sterilization has the potential to meet the unmet need for female sterilization in developing countries without access to trained personnel and sophisticated surgical equipment."( Quinacrine pellet nonsurgical female sterilization in Wonosobo, Indonesia.
Soejoenoes, A; Suhadi, A, 1997
)
2.36
"Quinacrine has been used for decades and the beneficial effects of this drug are as numerous as its toxic effects. "( Effects of quinacrine on endothelial cell morphology and transcription factor-DNA interactions.
Stuhlmeier, KM, 2001
)
2.14
"Quinacrine has been used for voluntary female non-surgical sterilization for its ability to produce tubal occlusion. "( Re-evaluation of the mutagenic potential of quinacrine dihydrochloride dihydrate.
Campen, DB; Cancel, AM; Clarke, JJ; Gudi, R; Jacobson-Kram, D; San, RH; Sokal, DC; Wagner, VO, 2001
)
2.01
"Quinacrine has been shown to act as a noncompetitive inhibitor of the nicotinic acetylcholine receptor (nAChR). "( The noncompetitive inhibitor quinacrine modifies the desensitization kinetics of muscle acetylcholine receptors.
Bouzat, C; Dilger, JP; Spitzmaul, G, 2001
)
2.04
"Quinacrine has been shown to bind selectively to a population of nerves and ganglion cells in the mouse, rat and guinea-pig gut. "( Semiquantitative estimations of quinacrine fluorescence in intestinal nerve fibres.
Alund, M, 1978
)
1.98

Actions

Quinacrine did not cause supersensitivity to noradrenaline, possibly due to its direct depressant action on the expansor secundariorum muscle. Quinacrine was found to inhibit recovery in cell cultures in exponential growth phase but not, or only slightly, in cells in stationary growth.

ExcerptReferenceRelevance
"Quinacrine, because of its ability to mimic the HIP interactions with heparin, was shown to successfully modulate the HIP-heparin interactions."( Biophysical insight into the heparin-peptide interaction and its modulation by a small molecule.
Kundu, B; Munde, M; Srivastava, A; Tiwari, N, 2018
)
1.2
"In quinacrine group, increase in the SOD1 expression levels was only statistically significant (p < 0.05)."( Expression changes of antioxidant, apoptotic, anti-apoptotic genes and miR-15b-34a-21-98 in over tissue by using erythromycin, quinacrine and tetracycline in non-surgical sterilization.
Atilgan, R; Baspinar, M; Kara, M; Kuloglu, T; Sapmaz, E; Yumrutas, O, 2014
)
1.12
"Quinacrine does not cause retinopathy, but it has more cutaneous side effects than the other two agents."( Antimalarials.
Koranda, FC, 1981
)
0.98
"Quinacrine was found to inhibit recovery in cell cultures in exponential growth phase but not, or only slightly, in cells in stationary growth."( Sensitivity of cells in exponential and stationary growth phase to combined treatment with radiation and quinacrine.
Littbrand, B; Midander, J, 1980
)
1.2
"Quinacrine did not inhibit the degradation by liver homogenates of inositol 1-phosphate, inositol 4,5-bisphosphate or inositol 1,4,5-trisphosphate."( Effects of quinacrine on vasopressin-induced changes in glycogen phosphorylase activity, Ca2+ transport and phosphoinositide metabolism in isolated hepatocytes.
Barritt, GJ; Hughes, BP; Milton, SE, 1988
)
1.39
"Quinacrine did not cause supersensitivity to noradrenaline, possibly due to its direct depressant action on the expansor secundariorum muscle."( The in vitro pharmacology of chloroquine and quinacrine.
Lot, TY, 1986
)
1.25

Treatment

Quinacrine-treated U937 cells showed ROS-mediated p38 MAPK activation and ERK inactivation, which in turn upregulated FOXP3 transcription. Quinacrine treatment decreased the number of alpha-1 receptors in heart and lung but increased alpha-2 receptors in the spleen.

ExcerptReferenceRelevance
"Quinacrine-treated U937 cells showed ROS-mediated p38 MAPK activation and ERK inactivation, which in turn upregulated FOXP3 transcription."( Quinacrine induces the apoptosis of human leukemia U937 cells through FOXP3/miR-183/β-TrCP/SP1 axis-mediated BAX upregulation.
Chang, LS; Chen, YJ; Huang, CH; Lee, YC; Shi, YJ; Wang, LJ, 2017
)
2.62
"The quinacrine-treated group, however, declined less on 2 of 3 functional scales, the modified Rankin and Clinical Dementia Rating, than the placebo group during the first 2 months."( Quinacrine treatment trial for sporadic Creutzfeldt-Jakob disease.
Cheng, HQ; Dearmond, SJ; Devereux, G; Duncan, JL; Finley, R; Forner, SA; Garcia, P; Geschwind, MD; Haman, A; Johnson, DY; Kuo, AL; Miller, BL; Neuhaus, JM; Possin, KL; Prusiner, SB; Raudabaugh, BJ; Thai, JN; Torres-Chae, CC; Wong, KS, 2013
)
2.31
"Quinacrine treatment did not have an effect on the increased sPLA2 level of the sulfite administered group."( Merit of quinacrine in the decrease of ingested sulfite-induced toxic action in rat brain.
Agar, A; Basaranlar, G; Derin, N; Kencebay, C; Kipmen-Korgun, D; Ozsoy, O; Ozturk, N; Sozen, B; Tanriover, G; Yargicoglu-Akkiraz, P, 2013
)
1.53
"Quinacrine treatment cleared PrP(Sc) and restored calcium responses in the ScGT1-1 cultures."( Scrapie-infected GT1-1 cells show impaired function of voltage-gated N-type calcium channels (Ca(v) 2.2) which is ameliorated by quinacrine treatment.
Kristensson, K; Sandberg, MK; Wallén, P; Wikström, MA, 2004
)
1.25
"Quinacrine treatment decreased the number of alpha-1 receptors in heart and lung but increased alpha-2 receptors in the spleen."( Quinacrine-blocked desensitization of adrenoceptors after immobilization stress or repeated injection of isoproterenol in rats.
Axelrod, J; Hirata, F; Kopin, IJ; Torda, T; Yamaguchi, I, 1981
)
2.43
"Quinacrine treatment significantly protected animals against CsA induced biochemical changes."( Quinacrine attenuates cyclosporine-induced nephrotoxicity in rats.
al Khader, A; al Sulaiman, M; Kishore, PN; Morais, C; Tariq, M, 1996
)
2.46
"Quinacrine (16 mg/kg) pretreatment 45 min before intraventral tegmental area melittin injection significantly decreased melittin-induced sensitization of the locomotor and stereotypy response to cocaine."( Evidence for the involvement of phospholipase A2 mechanisms in the development of stimulant sensitization.
Berger, SP; Crawford, CA; Hsu, K; Reid, MS; Tolliver, BK, 1996
)
1.02
"Quinacrine treated rats showed significantly reduced infarct areas in the caudoputamen compared to saline treated rats (P < 0.05, Student's t-test)."( The phospholipase A2 inhibitor, quinacrine, reduces infarct size in rats after transient middle cerebral artery occlusion.
Estevez, AY; Phillis, JW, 1997
)
1.3
"In quinacrine-treated animals phospholipids and CK also fell initially; however, 24 and 48 hr after occlusion they were higher than in controls (phospholipids: 0.99 +/- 0.05 vs."( Inhibition of ischemia-induced phospholipase activation by quinacrine protects jeopardized myocardium in rats with coronary artery occlusion.
Ambrosio, G; Cappelli-Bigazzi, M; Chiariello, M; Condorelli, M; Marone, G; Nevola, E; Perrone-Filardi, P, 1987
)
1.03
"In quinacrine-treated animals left ventricular phospholipids and CK also fell during the first hours post-occlusion; however, 24 and 48 h after the occlusion they were significantly higher than in controls (phospholipids: 0.99 +/- 0.05 vs 0.62 +/- 0.04 microgram P/mg of protein, p less than 0.001, and CK: 7.76 +/- 0.54 vs 4.99 +/- 0.37 IU/mg of protein, p less than 0.001, at 48 h)."( [Limitation of the area of necrosis induced by quinacrine after coronary occlusion in the dog].
Ambrosio, G; Bigazzi, MC; Brigante, F; Chiariello, M; Focaccio, A; Migliaccio, C; Tritto, I, 1985
)
1.04
"Treatment with quinacrine did not prolong the survival times of prion-inoculated, wild-type or MDR(0/0) mice compared to untreated mice."( Continuous quinacrine treatment results in the formation of drug-resistant prions.
Ahn, M; DeArmond, SJ; Ghaemmaghami, S; Giles, K; Legname, G; Lessard, P; Prusiner, SB, 2009
)
1.08
"Treatment by quinacrine alone at concentrations of 10-20 mM for 1-2 d cannot kill hepatocellular carcinoma cells, such as HepG2, Hep3B, Huh7, which are also resistant to TRAIL."( Quinacrine sensitizes hepatocellular carcinoma cells to TRAIL and chemotherapeutic agents.
Abdulghani, J; Allen, JE; Dicker, DT; Dolloff, NG; El-Deiry, WS; Gallant, JN; Hong, B; Katz, SI; Navaraj, A; Smith, CD; Wang, W, 2011
)
2.16
"Treatment with quinacrine or pentosan polysulfate cleared the PrPSc from the ScGT1-1 cell cultures, and the increase in levels of monomeric SNAP-25 and synaptophysin was reversible."( Altered interaction and expression of proteins involved in neurosecretion in scrapie-infected GT1-1 cells.
Löw, P; Sandberg, MK, 2005
)
0.67
"Treatment with quinacrine and chlorpromazine for acquired CJD was ineffective in our patient."( Creutzfeldt-Jakob disease acquired via a dural graft: failure of therapy with quinacrine and chlorpromazine.
Bermejo, J; Contreras, MA; Guerrero, MC; Lunar, A; Martínez Pérez, M; Martínez-Lage, JF; Rábano, A, 2005
)
0.9
"Treatment with quinacrine and BPB leads to decreased synthesis and disturbed breakdown of phospholipids and phosphoinositides."( PLA2 activity in Tetrahymena pyriformis. Effects of inhibitors and stimulators.
Csaba, G; Kovács, P, 1997
)
0.64
"Pretreatment with quinacrine significantly attenuated the formation of stress-, indomethacin- and ethanol-induced gastric lesions."( Effect of quinacrine, a phospholipase A2 inhibitor on stress and chemically induced gastroduodenal ulcers.
Al Moutaery, AR; Tariq, M, 1997
)
1.02

Toxicity

The toxic effects of intraperitoneal, intrauterine and intravenous administration of quinacrine hydrochloride solution were evaluated in female adult rhesus monkeys (Macaca mulatta) Only two of 14 reported serious adverse events were judged quinACrine-related.

ExcerptReferenceRelevance
"The toxic effects of intraperitoneal, intrauterine and intravenous administration of quinacrine hydrochloride solution were evaluated in female adult rhesus monkeys (Macaca mulatta)."( Toxic effects of quinacrine hydrochloride in rhesus monkeys.
Chandra, H; Malaviya, B, 1981
)
0.83
" Maculopathy after short-term therapy was identified as a side-effect which is rarely considered."( Ocular toxicity of antimalarials in dermatology: a survey of current practice.
Cox, NH; Paterson, WD, 1994
)
0.29
" These results indicate that quinacrine pellets are an effective and safe method of nonsurgical sterilization."( Efficacy and safety of repeated transcervical quinacrine pellet insertions for female sterilization.
el Kady, AA; Kessel, E; Nagib, HS, 1993
)
0.83
"Ectopic pregnancies and the occurrence of other adverse health events."( Long-term follow-up after quinacrine sterilization in Vietnam. Part II: interim safety analysis.
Hanenberg, R; Hieu, DT; Huu Vach, T; Sokal, D; Vinh, DQ; Weiner, DH, 2000
)
0.61
" The data on other adverse events are more difficult to interpret."( Long-term follow-up after quinacrine sterilization in Vietnam. Part II: interim safety analysis.
Hanenberg, R; Hieu, DT; Huu Vach, T; Sokal, D; Vinh, DQ; Weiner, DH, 2000
)
0.61
" Previous studies have shown that N-methyl-D-aspartate (NMDA) receptor antagonists can inhibit glutathione depletion and neurotoxicity induced by PrP(TSE) and a toxic prion protein peptide, PrP106-126, in vitro."( Involvement of the 5-lipoxygenase pathway in the neurotoxicity of the prion peptide PrP106-126.
Beyreuther, K; Cappai, R; Collins, SJ; Jobling, MF; Maher, F; Masters, CL; Needham, BE; Stewart, LR; Thyer, J; White, AR, 2001
)
0.31
" When compared clinical effects by quinacrine and the combination therapy, improvement of clinical findings was observed at the same level without any adverse effects."( Toxicity of quinacrine can be reduced by co-administration of P-glycoprotein inhibitor in sporadic Creutzfeldt-Jakob disease.
Eguchi, K; Katamine, S; Kataoka, Y; Nishida, N; Niwa, M; Satoh, K; Shirabe, S; Yamauchi, A, 2004
)
0.98
" The primary endpoints were death and serious adverse events possibly or probably related to the study drug."( Safety and efficacy of quinacrine in human prion disease (PRION-1 study): a patient-preference trial.
Collinge, J; Darbyshire, J; Gorham, M; Hudson, F; Kennedy, A; Keogh, G; Pal, S; Rossor, M; Rudge, P; Siddique, D; Spyer, M; Thomas, D; Walker, S; Webb, T; Wroe, S, 2009
)
0.66
" Only two of 14 reported serious adverse events were judged quinacrine-related."( Safety and efficacy of quinacrine in human prion disease (PRION-1 study): a patient-preference trial.
Collinge, J; Darbyshire, J; Gorham, M; Hudson, F; Kennedy, A; Keogh, G; Pal, S; Rossor, M; Rudge, P; Siddique, D; Spyer, M; Thomas, D; Walker, S; Webb, T; Wroe, S, 2009
)
0.91
" We demonstrate that quinacrine caused a significant reduction of hPrP90-231 toxicity due to its binding to the fragment and the prevention of its conversion in a toxic isoform."( Efficacy of novel acridine derivatives in the inhibition of hPrP90-231 prion protein fragment toxicity.
Aceto, A; Boido, V; Canu, C; Chiovitti, K; Corsaro, A; Florio, T; Novelli, F; Paludi, D; Pino, A; Russo, C; Sparatore, A; Sparatore, F; Tasso, B; Thellung, S; Tonelli, M; Villa, V, 2011
)
0.69
"Renal toxicity is a serious side effect that hinders the use of cisplatin, a commonly used and effective chemotherapeutic agent."( Quinacrine Ameliorates Cisplatin-Induced Renal Toxicity via Modulation of Sirtuin-1 Pathway.
Abo El-Magd, NF; Ebrahim, HA; Eisa, NH; El-Sherbiny, M, 2021
)
2.06

Pharmacokinetics

The lipophilic cationic compound quinacrine has been used as an antimalarial drug for over 75 years. Its pharmacokinetic profile is limited.

ExcerptReferenceRelevance
" The mean absorption half-life was approximately 7 min and the mean bioavailability was slightly in excess of 100%."( Pharmacokinetics of quinacrine after intrapleural instillation in rabbits and man.
Björkman, S; Elisson, LO; Gabrielsson, J, 1989
)
0.6
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" The aim of the study was to investigate possible pharmacokinetic and/or pharmacodynamic explanations for the discrepancy between the proven action of quinacrine in vitro and its lack of clinical efficacy."( A possible pharmacological explanation for quinacrine failure to treat prion diseases: pharmacokinetic investigations in a ovine model of scrapie.
Andréoletti, O; Gayrard, V; Laroute, V; Picard-Hagen, N; Toutain, PL; Viguié, C, 2005
)
0.79
" We identify compounds with significantly improved bioactivity (approximately 40-fold) against replication of the infectious prion isoform (PrPSc) and suitable pharmacokinetic profiles to warrant evaluation in animal models of prion disease."( Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
Cohen, FE; Legname, G; May, BC; Prusiner, SB; Sherrill, J; Wallace, AC; Witkop, J; Zorn, JA, 2007
)
0.34
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"The lipophilic cationic compound quinacrine has been used as an antimalarial drug for over 75 years but its pharmacokinetic profile is limited."( Pharmacokinetics of quinacrine efflux from mouse brain via the P-glycoprotein efflux transporter.
Ahn, M; DeArmond, SJ; Ghaemmaghami, S; Giles, K; Huang, Y; May, BC; Phuan, PW; Prusiner, SB, 2012
)
0.98

Compound-Compound Interactions

ExcerptReferenceRelevance
"We studied the in vitro and in vivo antimicrobial activities of picolinic acid (PA) in combination with the antiprotozoal drug quinacrine against intramacrophage Mycobacterium avium complex (MAC)."( Activity of picolinic acid in combination with the antiprotozoal drug quinacrine against Mycobacterium avium complex.
Shimizu, T; Tomioka, H, 2006
)
0.77

Bioavailability

ExcerptReferenceRelevance
" The mean absorption half-life was approximately 7 min and the mean bioavailability was slightly in excess of 100%."( Pharmacokinetics of quinacrine after intrapleural instillation in rabbits and man.
Björkman, S; Elisson, LO; Gabrielsson, J, 1989
)
0.6
" Enhanced oxidative stress in hypertension and diabetes is linked to decreased nitric oxide (NO) bioavailability because of its interaction with vascular superoxide (O(2)(*-)), derived predominantly from NAD(P)H-dependent oxidases."( Increased superoxide production in hypertensive patients with diabetes mellitus: role of nitric oxide synthase.
Devine, A; Dixon, LJ; Henry, W; Hughes, SM; Johnston, GD; Leahey, W; Madden, A; McVeigh, GE; Rooney, K, 2005
)
0.33
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
" The compound was orally bioavailable and displayed good plasma and brain exposure in mice."( Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
Brun, R; Buckner, FS; Chatterjee, AK; Creason, SA; Duster, NA; Gelb, MH; Gillespie, JR; Glynne, R; Hulverson, MA; McQueen, J; Molteni, V; Nagendar, P; Nagle, A; Norcross, NR; Ranade, RM; Supek, F; Tatipaka, HB; Wenzler, T, 2014
)
0.4
"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 aim of this work was to prepare liposome nano-carriers to enhance the bioavailability of Quinacrine and to improve passive targeting in A549 cells."( Sensitization of A-549 lung cancer cells to Cisplatin by Quinacrine-loaded lipidic nanoparticles via suppressing Nrf2 mediated defense mechanism.
Ahmadian, S; Bijanpour, H; Ghorbani, M; Mahmoudi, S; Maroufi, NF; Mohammadi, M; Mohammadian, J; Pirouzpanah, M; Ramezani, F; Rashidi, M; Sabzichi, M, 2021
)
1.09

Dosage Studied

Drug-induced psychosis resulted from the administration of quinacrine hydrochloride at a dosage of 100 mg twice daily for the treatment of discoid lupus. There was no dose-response effect between the one- and two-insertion groups, suggesting the possibility of recall bias.

ExcerptRelevanceReference
" A dosage of 15-25 mg/kg a day for 5 days is recommended."( Giardiasis in infancy and childhood: a prospective study of 160 cases with comparison of quinacrine (Atabrine) and metronidazole (Flagyl).
Kavousi, S, 1979
)
0.48
" In permeabilized acini, mepacrine shifted the dose-response curve for calcium to the right by a factor 2 and inhibited the release of amylase stimulated by GTPrS."( Inhibition by mepacrine and amylase secretion from intact and permeabilized rat pancreatic acini.
Dehaye, JP; Gomez, F; Grosfils, K, 1992
)
0.28
" (d) Yohimbine, but not prazosin, suppressed the noradrenaline dose-response curve for prostaglandin production."( Noradrenaline-induced prostaglandin production by sympathetic postganglionic neurons is mediated by alpha 2-adrenergic receptors.
Goldyne, ME; Gonzales, R; Levine, JD; Sherbourne, CD, 1991
)
0.28
" The dose-response curve was steep between 25 microM and 250 microM calcium and tended to flatten with higher concentrations."( Histamine secretion from permeabilized mast cells by calcium.
Chakravarty, N, 1986
)
0.27
" A dose-response relationship for quinacrine (0."( Functional and electrophysiological effects of quinacrine on the response of ventricular tissues to hypoxia and reoxygenation.
Moffat, MP; Tsushima, RG, 1989
)
0.81
" Previous treatment with 1 microM indomethacin (IND) or 10 microM quinacrine (QUIN) markedly displaced the dose-response curves for Ach on OAS preparations to the left, whereas the EC50 of His was only increased by QUIN."( Tracheal responsiveness to histamine, PAF-acether and acetylcholine in normal and actively ovalbumin-sensitized guinea pigs.
Calixto, JB; Medeiros, YS; Torres, RC, 1989
)
0.51
" Dose-response studies indicate the beta-adrenergic component of cyclic AMP stimulation is enhanced and the alpha 1-adrenergic component of cyclic GMP stimulation is diminished in LL pinealocytes."( See-saw signal processing in pinealocytes involves reciprocal changes in the alpha 1-adrenergic component of the cyclic GMP response and the beta-adrenergic component of the cyclic AMP response.
Klein, DC; Sugden, D; Vanecek, J; Weller, JL, 1986
)
0.27
"Oral mepacrine dihydrochloride, 200 mg (158 mg of the base) six-hourly for five doses followed by 100 mg (79 mg of the base) eight-hourly for six days (half dosage for those less than or equal to 50 kg) was given to 21 patients with high-grade chloroquine-resistant falciparum malaria in eastern Thailand."( Mepacrine accumulation during treatment of chloroquine-resistant falciparum malaria.
Chanthavanich, P; Edwards, G; Looareesuwan, S; Phillips, RE; Rodick, CL; Supanaranond, W; Warrell, DA, 1988
)
0.27
" Dose-response curves comparing 45Ca efflux and insulin secretion suggested that AA also stimulates hormone release by at least one other mechanism in addition to Ca2+ mobilization."( Exogenous arachidonic acid promotes insulin release from intact or permeabilized rat islets by dual mechanisms. Putative activation of Ca2+ mobilization and protein kinase C.
Metz, SA, 1988
)
0.27
"Cumulative dose-response curves for histamine induced responses in mesometrial (ME) and antimesometrial (AME) regions of uterine horns isolated from rats at 7th, 16th and 22nd days of pregnancy, were constructed."( Is there a prostaglandin involvement in the positive inotropic action of histamine in isolated pregnant rat uterus, apparently mediated via H1-receptors activation?
Dveksler, G; Franchi, AM; Gimeno, AL; Gimeno, MF; Viggiano, M, 1987
)
0.27
"This study lends support to others indicating the apparent safety and effectiveness of multiple transcervical insertions of quinacrine hydrochloride as pellets in 240 mg dosage to achieve permanent sterilization."( Clinico-pathological study of fallopian tubes after transcervical insertion of quinacrine hydrochloride pellets.
Doctor, VM; Jhaveri, CL; Kessel, E; Merchant, RN; Mumford, SD; Sinha, M; Thaku, SS, 1986
)
0.71
" A dose-response study related to the effect of increasing concentrations of mepacrine (7."( Effects of mepacrine on uterine contractile responses.
Bade, SC; Gardner, RM, 1985
)
0.27
" By using an IUD vector to deliver the quinacrine, tubal occlusion can be achieved with a reduction in total dosage and with one insertion instead of the three necessary with the solution and pellet methods."( Nonsurgical female sterilization.
Cole, LP; Laufe, LE, 1980
)
0.53
" The dose-response curve was steep, nearly all incorporation being inhibited by 2 x IC50."( Inhibition of lymphocyte transformation by mepacrine and chloroquine.
Trist, DG; Weatherall, M, 1981
)
0.26
" PAF release precedes permeability changes and both show a parallel dose-response pattern plateauing for doses higher than 1 mg."( Platelet-activating factor: an effector substance of the vasopermeability changes induced by the infusion of immune aggregates in the mouse.
Alonso, F; Iñarrea, P; Sanchez-Crespo, M, 1983
)
0.27
" The trials suffered from unclear methods, variability in study populations and total dosage of medication used, inaccuracy in determining outcomes, and inadequate sample sizes."( Issues in clinical parasitology: the treatment of giardiasis.
Davidson, RA, 1984
)
0.27
" No evidence was found for toxicity of tetracycline or its analogues for the dosage given."( Effect of intrauterine administration of tetracyclines on cynomolgus monkeys.
Dubin, NH; Ghodgaonkar, RB; King, TM; Parmley, TH; Rosenshein, NB; Strandberg, JD, 1984
)
0.27
"Drug-induced psychosis resulted from the administration of quinacrine hydrochloride at a dosage of 100 mg twice daily for the treatment of discoid lupus."( Antimalarial psychosis revisited.
Evans, RL; Khalid, S; Kinney, JL, 1984
)
0.51
" These phospholipase A2 inhibitors also inhibited the cellular uptake of 45Ca2+ evoked by carbamylcholine with similar dose-response curves to those for inhibition of catecholamine secretion."( Suppression by phospholipase A2 inhibitors of secretion of catecholamines from isolated adrenal medullary cells by suppression of cellular calcium uptake.
Izumi, F; Kobayashi, H; Sakurai, S; Wada, A; Yanagihara, N, 1983
)
0.27
" Inhibition of 45Ca2+ uptake and catecholamine secretion exhibited identical dose-response curves."( Phospholipase A2 inhibitors block catecholamine secretion and calcium uptake in cultured bovine adrenal medullary cells.
Frye, RA; Holz, RW, 1983
)
0.27
" Many of these reviews, while generally excellent, have propagated some apparent misconceptions by disregarding or de-emphasizing data suggesting that irreversible retinal toxicity due to antimalarials can be easily avoided by judicious daily dosage and regular ophthalmologic follow-up."( Antimalarials and ophthalmologic safety.
Olansky, AJ, 1982
)
0.26
" Tinidazole is a very promising drug, being effective in single dosage with infrequent side effects."( The treatment of giardiasis.
Mendelson, RM, 1980
)
0.26
" cAMP shifted the dose-response curve for calcium-induced secretion leftwards and elevated the peak value of secretion."( Inhibition by somatostatin of amylase secretion induced by calcium and cyclic AMP in rat pancreatic acini.
Kojima, I; Mine, T; Ohnishi, H, 1994
)
0.29
" Optimal time and dosage of ricin were established by determining the maximal achievable inhibition of [35S]methionine into DRG protein."( Selective inhibition of neuronal protein synthesis by retrogradely transported ricin.
Hammerschlag, R; Tang, HZ; Tsai, A, 1994
)
0.29
" In both tests KT had a poor analgesic effect without dose-response relationships."( Ketorolac tromethamine: an experimental study of its analgesic effects in the rat.
Bustamante, D; Paeile, C, 1993
)
0.29
" The number of administrations as well as the dosage are important to prevent morbidity and recurrence."( Intrapleural quinacrine instillation for recurrent pneumothorax or persistent air leak.
Derom, A; Derom, E; Derom, F; Eeckhout, C; Janzing, HM; Rosseel, MT, 1993
)
0.66
" Such a complex dose-response effect may have significant impact in explaining the pathologic effects of NO2."( Dual effect of nitrogen dioxide on rat alveolar macrophage arachidonate metabolism.
Forman, HJ; Robison, TW,
)
0.13
" Dose-response studies showed that expression of wild-type pfmdr1 causes cellular resistance to quinine, quinacrine, mefloquine, and halofantrine in yeast cells."( The pfmdr1 gene of Plasmodium falciparum confers cellular resistance to antimalarial drugs in yeast cells.
Brault, M; Delling, U; Gros, P; Ruetz, S; Schurr, E, 1996
)
0.51
" Dose-response curves were performed for each drug."( Postcardioplegic myocardial recovery: effects of halothane, nifedipine, HOE 694, and quinacrine.
Genade, S; Lochner, A; Theron, S; Trollip, G; Tromp, E, 1998
)
0.52
" Dose-response curves to noradrenaline-induced vasoconstriction were performed before and after continuous infusions of two different PAF-receptor antagonists (WEB 2086 and yangambin) and of the phospholipase A2 inhibitor mepacrine."( Involvement of platelet-activating factor in the modulation of vascular tone in the isolated perfused rabbit kidney.
Aimbire, F; Cailleaux, S; Cordeiro, RS; Lopes-Martins, RA; Tibiriçá, E, 1999
)
0.3
" However, after correcting for information bias, there was no dose-response effect between the one- and two-insertion quinacrine groups, suggesting the possibility of recall bias or differing baseline health status."( Long-term follow-up after quinacrine sterilization in Vietnam. Part II: interim safety analysis.
Hanenberg, R; Hieu, DT; Huu Vach, T; Sokal, D; Vinh, DQ; Weiner, DH, 2000
)
0.82
" With prudent dosage and monitoring, these agents can be used safely and effectively in the treatment and management of dermatologic disease."( Antimalarials.
Piette, WW; Van Beek, MJ, 2001
)
0.31
" With the hope of reducing the total dosage and making it a 1-insertion technique, quinacrine has been mixed with polyethylene oxide and place on the arms of various IUDs."( Chemical sterilization with an IUD.
Laufe, LE, 1981
)
0.49
"Determine the efficacy of two different dosage regimens of quinacrine placed at each cornual angle, employing a curved inserter, and for fundal placement of doses from 252 mg to 360 mg of quinacrine, depending on the age of the woman."( Quinacrine sterilization of 1997 women in Daharpur, Midnapore, West Bengal, India: a comparison of 3 protocols.
Pal, SK, 2003
)
2
" The total brain tissue concentrations (3556 nM) obtained after a repeated therapeutic dosage regimen were within the range of the intracellular neuroblastoma quinacrine concentrations."( A possible pharmacological explanation for quinacrine failure to treat prion diseases: pharmacokinetic investigations in a ovine model of scrapie.
Andréoletti, O; Gayrard, V; Laroute, V; Picard-Hagen, N; Toutain, PL; Viguié, C, 2005
)
0.79
" Dose-response curves for transport and the ratio of dye concentration in the secreted fluid to that in the bathing medium (S/M) were determined for Texas Red as well as for P-gp substrates (rhodamine 123, daunorubicin), the organic anion fluorescein and the organic cation quinacrine."( Transepithelial transport of fluorescent p-glycoprotein and MRP2 substrates by insect Malpighian tubules: confocal microscopic analysis of secreted fluid droplets.
Leader, JP; O'Donnell, MJ, 2005
)
0.51
" Neonatal Crl: CD-1 mice of each sex were randomly allocated into four treatment groups (0, 10, 50, and 150 mg/kg), dosed twice with quinacrine suspended in carboxymethylcellulose, observed for 52 weeks post dose, and then euthanized, necropsied, and subjected to a full histopathological examination."( A one-year neonatal mouse carcinogenesis study of quinacrine dihydrochloride.
Cancel, AM; Dillberger, JE; McClain, RM; Rehkemper, U; Smith, T; Sokal, D,
)
0.59
" However, animals dosed with human equivalent doses of quinacrine were not protected against respiratory spore challenge."( Evaluation of the protective effects of quinacrine against Bacillus anthracis Ames.
Chatuev, BM; Chopra, AK; Comer, JE; McHenry, DJ; Noffsinger, DM; Peterson, JW; Weisbaum, DM, 2006
)
0.85
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" Acute quinacrine toxicity was evident during the dosing period but did not affect long-term survival."( A lifetime cancer bioassay of quinacrine administered into the uterine horns of female rats.
Bolte, HF; Cancel, AM; Creasy, DM; Dillberger, JE; Kelly, CM; Sokal, DC, 2010
)
1.1
" Cumulative levobupivacaine dose-response curves over a range of 10(-6) to 3 x 10(-4) M were constructed in 1) aortic rings with no drug pretreatment; 2) endothelium-denuded rings pretreated with quinacrine dihydrochloride (nonspecific phospholipase A(2) inhibitor: 2 x 10(-5), 4 x 10(-5) M), nordihydroguaiaretic acid (NDGA) (lipoxygenase inhibitor: 10(-5), 3 x 10(-5) M), indomethacin (nonspecific cyclooxygenase inhibitor: 10(-5) M), AA-861 (5-lipoxygenase inhibitor: 10(-5), 5 x 10(-5) M), fluconazole (cytochrome P450 epoxygenase inhibitor: 10(-5) M), verapamil (10(-5) M), or calcium-free solution; and 3) endothelium-intact rings pretreated with N(omega)-nitro-L-arginine methyl ester (L-NAME) (nitric oxide synthase inhibitor: 5 x 10(-5) M), indomethacin, or fluconazole."( The direct effect of levobupivacaine in isolated rat aorta involves lipoxygenase pathway activation and endothelial nitric oxide release.
Choi, YS; Hah, YS; Hwang, EM; Jeong, YS; Lee, SH; Ok, SH; Park, JY; Shin, IW; Sohn, JT, 2010
)
0.55
" In order to assess extensive dose-response relationships, we selected expected weak (diazepam, phenolphthalein, quinacrine dihydrochloride dihydrate) and strong (cytosine arabinoside, mitomycin C, vinblastine sulphate) inducers of micronuclei with a variety of different mechanisms of action for testing."( Evaluation of phenolphthalein, diazepam and quinacrine dihydrochloride in the in vitro mammalian cell micronucleus test in Chinese hamster ovary (CHO) and TK6 cells.
Cheung, J; Colman, M; Dickinson, D; Engel, M; Gudi, R; Kumar, S; Maduka, N; Schuler, M; Sherman, J; Szkudlinska, A; Thiffeault, C, 2010
)
0.83
" After a 2-month course of treatment with hydroxychloroquine dosage of 200 mg per day and a break of 3 months between courses, we observed a complete remission."( Unilateral unique Lupus tumidus: pathogenetic mystery and diagnostic problem.
Bakardzhiev, I; Chokoeva, AA; Krasnaliev, I; Lotti, T; Tana, C; Tchernev, G; Wollina, U, 2016
)
0.43
" Dose-response measurements were used to generate multiparameter drug sensitivity scores using R-statistical language."( Comprehensive Drug Testing of Patient-derived Conditionally Reprogrammed Cells from Castration-resistant Prostate Cancer.
Af Hällström, TM; Aittokallio, T; Bychkov, D; Eldfors, S; Heckman, C; Horvath, P; Kallioniemi, O; Mirtti, T; Mpindi, JP; Östling, P; Paavolainen, L; Peehl, DM; Rahkama, V; Rannikko, A; Saeed, K; Wennerberg, K; Yadav, B, 2017
)
0.46
" The first 2 quinacrine dosing levels were well tolerated."( First-in-Human Phase 1b Trial of Quinacrine Plus Capecitabine in Patients With Refractory Metastatic Colorectal Cancer.
Astaturov, I; Cohen, SJ; Cooper, HS; Denlinger, CS; Dotan, E; El-Deiry, WS; Gallant, JN; Harvey, HA; Korzekwa, K; Kunkel, M; Lim, B; Ross, EA; Ruth, K; Sivik, J; Vijayvergia, N; Wang, EW; White, K; Winer, A; Zhou, L, 2021
)
1.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antimalarialA drug used in the treatment of malaria. Antimalarials are usually classified on the basis of their action against Plasmodia at different stages in their life cycle in the human.
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitorAn EC 1.8.1.* (oxidoreductase acting on sulfur group of donors, NAD+ or NADP+ as acceptor) inhibitor that interferes with the action of trypanothione-disulfide reductase (EC 1.8.1.12).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
acridines
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (72)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency16.36010.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency6.61020.100020.879379.4328AID588453; AID588456
ATAD5 protein, partialHomo sapiens (human)Potency2.21330.004110.890331.5287AID493106; AID493107
Fumarate hydrataseHomo sapiens (human)Potency35.48130.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency50.20120.031637.5844354.8130AID504865; AID540327
TDP1 proteinHomo sapiens (human)Potency5.04510.000811.382244.6684AID686978; AID686979
regulator of G-protein signaling 4Homo sapiens (human)Potency21.19230.531815.435837.6858AID504845
polyproteinZika virusPotency35.48130.00308.794948.0869AID1347053
67.9K proteinVaccinia virusPotency28.18380.00018.4406100.0000AID720580
arylsulfatase AHomo sapiens (human)Potency10.69101.069113.955137.9330AID720538
IDH1Homo sapiens (human)Potency15.84890.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.14280.035520.977089.1251AID504332; AID588346
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency18.49270.016525.307841.3999AID602332
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency58.04790.01262.451825.0177AID485313
D(1A) dopamine receptorHomo sapiens (human)Potency11.22020.02245.944922.3872AID488981; AID488983
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
flap endonuclease 1Homo sapiens (human)Potency12.73790.133725.412989.1251AID488816; AID588795
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency14.68920.65619.452025.1189AID463106
ras-related protein Rab-9AHomo sapiens (human)Potency46.10910.00022.621531.4954AID485297
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency18.94630.00378.618923.2809AID2660; AID2666; AID2667; AID2668
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency26.85450.425612.059128.1838AID504536
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency50.11870.129810.833132.6090AID485342
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency19.95260.050127.073689.1251AID588590
DNA polymerase kappa isoform 1Homo sapiens (human)Potency43.90220.031622.3146100.0000AID588579
M-phase phosphoprotein 8Homo sapiens (human)Potency23.77810.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.18380.251215.843239.8107AID504327
D(1A) dopamine receptorSus scrofa (pig)Potency14.68920.00378.108123.2809AID2667
Ataxin-2Homo sapiens (human)Potency12.58930.011912.222168.7989AID588378
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency5.35827.568615.230621.3313AID504548
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cystic fibrosis transmembrane conductance regulatorHomo sapiens (human)IC50 (µMol)19.88000.140016.625050.0000AID1224863
Bile salt export pumpHomo sapiens (human)IC50 (µMol)101.10000.11007.190310.0000AID1449628
Glutathione reductase, mitochondrialHomo sapiens (human)IC50 (µMol)1,000.00001.00004.55008.1000AID75303
Riboflavin-binding proteinGallus gallus (chicken)Ki6.70000.35003.52506.7000AID642883
Major prion proteinMus musculus (house mouse)IC50 (µMol)0.09510.09510.09510.0951AID1893058
Histidine-rich protein PFHRP-IIPlasmodium falciparum (malaria parasite P. falciparum)IC50 (µMol)292.00000.07651.12552.9000AID278900
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)2.89600.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki2.87200.00322.28879.3160AID625207
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)0.96400.00001.23267.7930AID625152
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.34300.00000.690210.0000AID625152
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC50 (µMol)1.98300.00001.15467.5858AID625154
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.27700.00000.79519.1201AID625154
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)4.50000.00052.773925.1700AID600984
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)4.50000.00052.891925.1700AID600984
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)4.50000.00052.747825.1700AID600984
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)4.50000.00052.780225.1700AID600984
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC50 (µMol)3.73600.00010.99178.0000AID625155
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki2.68400.00000.72926.9183AID625155
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)2.28000.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.85500.00010.807410.0000AID625201
DNA-directed RNA polymerase subunit betaEscherichia coli K-12IC50 (µMol)20.00000.02000.02500.0300AID1145960
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)50.00000.00022.45859.9600AID1804171
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)4.50000.00053.314249.5000AID600984
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)1.48900.00001.403910.0000AID625151
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.35900.00000.59729.1201AID625151
Phospholipase A2, membrane associatedRattus norvegicus (Norway rat)IC50 (µMol)320,000.00000.12000.12000.1200AID159104
Phospholipase A2, membrane associatedHomo sapiens (human)IC50 (µMol)76,000.00000.00301.08118.0000AID158938
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)1.82500.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.83300.00020.725710.0000AID625202
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)3.85700.00001.47257.8980AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.56000.00030.483410.0000AID625203
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50 (µMol)1.25500.00011.01049.9280AID625153
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.26600.00000.54057.7600AID625153
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)2.66700.00000.933210.0000AID625193
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)2.89600.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki2.87200.00031.465610.0000AID625207
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)3.53500.02202.298710.0000AID625270
Histamine H2 receptorHomo sapiens (human)Ki3.47600.00062.197310.0000AID625270
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)2.06500.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki1.01500.00000.360910.0000AID625200
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)2.66300.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.76100.00000.385510.0000AID625192
Trypanothione reductaseTrypanosoma cruziIC50 (µMol)133.00005.80005.80005.8000AID214493
Trypanothione reductaseTrypanosoma cruziKi19.00000.07605.15297.6000AID214657; AID419687
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)1.31800.00011.01788.7960AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.44800.00000.602010.0000AID625254
Aldehyde oxidase 1Oryctolagus cuniculus (rabbit)IC50 (µMol)10.00000.00804.002710.0000AID547842
CholinesteraseEquus caballus (horse)IC50 (µMol)4.50000.00002.22149.4000AID600984
Aldehyde oxidaseHomo sapiens (human)IC50 (µMol)3.30000.00230.63203.3000AID547838
Cyclic GMP-AMP synthaseHomo sapiens (human)IC50 (µMol)7.00000.00403.51607.0000AID1854201; AID1854214
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NPYLR7BAedes aegypti (yellow fever mosquito)EC50 (µMol)3.15000.03902.289918.3000AID1259426
Riboflavin-binding proteinGallus gallus (chicken)Kd0.26400.00500.35952.1000AID642884
Major prion proteinHomo sapiens (human)EC50 (µMol)0.30000.30004.900010.0000AID161627
ATP-dependent translocase ABCB1Homo sapiens (human)EC50 (µMol)14.40000.01600.67863.1000AID678838
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (308)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cellular oxidant detoxificationGlutathione reductase, mitochondrialHomo sapiens (human)
cellular response to oxidative stressGlutathione reductase, mitochondrialHomo sapiens (human)
glutathione metabolic processGlutathione reductase, mitochondrialHomo sapiens (human)
cell redox homeostasisGlutathione reductase, mitochondrialHomo sapiens (human)
riboflavin transportRiboflavin-binding proteinGallus gallus (chicken)
negative regulation of sensory perception of sweet tasteRiboflavin-binding proteinGallus gallus (chicken)
negative regulation of sensory perception of bitter tasteRiboflavin-binding proteinGallus gallus (chicken)
cellular response to copper ionMajor prion proteinHomo sapiens (human)
negative regulation of protein phosphorylationMajor prion proteinHomo sapiens (human)
intracellular copper ion homeostasisMajor prion proteinHomo sapiens (human)
response to oxidative stressMajor prion proteinHomo sapiens (human)
learning or memoryMajor prion proteinHomo sapiens (human)
long-term memoryMajor prion proteinHomo sapiens (human)
negative regulation of protein processingMajor prion proteinHomo sapiens (human)
protein destabilizationMajor prion proteinHomo sapiens (human)
negative regulation of type II interferon productionMajor prion proteinHomo sapiens (human)
negative regulation of interleukin-17 productionMajor prion proteinHomo sapiens (human)
negative regulation of interleukin-2 productionMajor prion proteinHomo sapiens (human)
negative regulation of apoptotic processMajor prion proteinHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityMajor prion proteinHomo sapiens (human)
positive regulation of neuron apoptotic processMajor prion proteinHomo sapiens (human)
negative regulation of activated T cell proliferationMajor prion proteinHomo sapiens (human)
response to cadmium ionMajor prion proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationMajor prion proteinHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationMajor prion proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingMajor prion proteinHomo sapiens (human)
negative regulation of T cell receptor signaling pathwayMajor prion proteinHomo sapiens (human)
protein homooligomerizationMajor prion proteinHomo sapiens (human)
regulation of cell cycleMajor prion proteinHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeMajor prion proteinHomo sapiens (human)
cellular response to xenobiotic stimulusMajor prion proteinHomo sapiens (human)
positive regulation of protein targeting to membraneMajor prion proteinHomo sapiens (human)
dendritic spine maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationMajor prion proteinHomo sapiens (human)
regulation of glutamate receptor signaling pathwayMajor prion proteinHomo sapiens (human)
positive regulation of glutamate receptor signaling pathwayMajor prion proteinHomo sapiens (human)
regulation of potassium ion transmembrane transportMajor prion proteinHomo sapiens (human)
negative regulation of amyloid-beta formationMajor prion proteinHomo sapiens (human)
negative regulation of dendritic spine maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of amyloid precursor protein catabolic processMajor prion proteinHomo sapiens (human)
positive regulation of protein localization to plasma membraneMajor prion proteinHomo sapiens (human)
response to amyloid-betaMajor prion proteinHomo sapiens (human)
cellular response to amyloid-betaMajor prion proteinHomo sapiens (human)
regulation of calcium ion import across plasma membraneMajor prion proteinHomo sapiens (human)
neuron projection maintenanceMajor prion proteinHomo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
DNA-templated transcriptionDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
DNA-templated transcription initiationDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
intracellular iron ion homeostasisDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
response to heatDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
transcription antiterminationDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
regulation of DNA-templated transcription elongationDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
cellular response to cell envelope stressDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
nitrate assimilationDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
bacterial-type flagellum assemblyDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
cell motilityDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
bacterial-type flagellum-dependent cell motilityDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
submerged biofilm formationDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
regulation of DNA-templated transcription initiationDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
protein-containing complex assemblyDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
DNA-templated transcriptionDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
DNA-templated transcription initiationDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
intracellular iron ion homeostasisDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
response to heatDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
transcription antiterminationDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
regulation of DNA-templated transcription elongationDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
cellular response to cell envelope stressDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
nitrate assimilationDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
bacterial-type flagellum assemblyDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
cell motilityDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
bacterial-type flagellum-dependent cell motilityDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
submerged biofilm formationDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
regulation of DNA-templated transcription initiationDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
DNA-templated transcriptionDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA-templated transcription initiationDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
intracellular iron ion homeostasisDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
response to heatDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
transcription antiterminationDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
regulation of DNA-templated transcription elongationDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
cellular response to cell envelope stressDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
nitrate assimilationDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
bacterial-type flagellum assemblyDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
response to antibioticDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
cell motilityDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
bacterial-type flagellum-dependent cell motilityDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
submerged biofilm formationDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
regulation of DNA-templated transcription initiationDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA-templated transcriptionDNA-directed RNA polymerase subunit betaEscherichia coli K-12
DNA-templated transcription initiationDNA-directed RNA polymerase subunit betaEscherichia coli K-12
intracellular iron ion homeostasisDNA-directed RNA polymerase subunit betaEscherichia coli K-12
response to heatDNA-directed RNA polymerase subunit betaEscherichia coli K-12
transcription antiterminationDNA-directed RNA polymerase subunit betaEscherichia coli K-12
regulation of DNA-templated transcription elongationDNA-directed RNA polymerase subunit betaEscherichia coli K-12
cellular response to cell envelope stressDNA-directed RNA polymerase subunit betaEscherichia coli K-12
nitrate assimilationDNA-directed RNA polymerase subunit betaEscherichia coli K-12
bacterial-type flagellum assemblyDNA-directed RNA polymerase subunit betaEscherichia coli K-12
response to antibioticDNA-directed RNA polymerase subunit betaEscherichia coli K-12
cell motilityDNA-directed RNA polymerase subunit betaEscherichia coli K-12
bacterial-type flagellum-dependent cell motilityDNA-directed RNA polymerase subunit betaEscherichia coli K-12
submerged biofilm formationDNA-directed RNA polymerase subunit betaEscherichia coli K-12
regulation of DNA-templated transcription initiationDNA-directed RNA polymerase subunit betaEscherichia coli K-12
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipid metabolic processPhospholipase A2, membrane associatedHomo sapiens (human)
inflammatory responsePhospholipase A2, membrane associatedHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPhospholipase A2, membrane associatedHomo sapiens (human)
lipid catabolic processPhospholipase A2, membrane associatedHomo sapiens (human)
killing of cells of another organismPhospholipase A2, membrane associatedHomo sapiens (human)
low-density lipoprotein particle remodelingPhospholipase A2, membrane associatedHomo sapiens (human)
intestinal stem cell homeostasisPhospholipase A2, membrane associatedHomo sapiens (human)
phosphatidylethanolamine metabolic processPhospholipase A2, membrane associatedHomo sapiens (human)
phosphatidylcholine metabolic processPhospholipase A2, membrane associatedHomo sapiens (human)
phosphatidic acid metabolic processPhospholipase A2, membrane associatedHomo sapiens (human)
arachidonic acid secretionPhospholipase A2, membrane associatedHomo sapiens (human)
positive regulation of inflammatory responsePhospholipase A2, membrane associatedHomo sapiens (human)
defense response to Gram-positive bacteriumPhospholipase A2, membrane associatedHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePhospholipase A2, membrane associatedHomo sapiens (human)
regulation of neutrophil activationPhospholipase A2, membrane associatedHomo sapiens (human)
negative regulation of T cell proliferationPhospholipase A2, membrane associatedHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
lipid metabolic processAldehyde oxidaseHomo sapiens (human)
xenobiotic metabolic processAldehyde oxidaseHomo sapiens (human)
activation of innate immune responseCyclic GMP-AMP synthaseHomo sapiens (human)
pattern recognition receptor signaling pathwayCyclic GMP-AMP synthaseHomo sapiens (human)
positive regulation of defense response to virus by hostCyclic GMP-AMP synthaseHomo sapiens (human)
regulation of immunoglobulin productionCyclic GMP-AMP synthaseHomo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathwayCyclic GMP-AMP synthaseHomo sapiens (human)
DNA repairCyclic GMP-AMP synthaseHomo sapiens (human)
DNA damage responseCyclic GMP-AMP synthaseHomo sapiens (human)
determination of adult lifespanCyclic GMP-AMP synthaseHomo sapiens (human)
cAMP-mediated signalingCyclic GMP-AMP synthaseHomo sapiens (human)
cGMP-mediated signalingCyclic GMP-AMP synthaseHomo sapiens (human)
positive regulation of type I interferon productionCyclic GMP-AMP synthaseHomo sapiens (human)
paracrine signalingCyclic GMP-AMP synthaseHomo sapiens (human)
innate immune responseCyclic GMP-AMP synthaseHomo sapiens (human)
regulation of T cell activationCyclic GMP-AMP synthaseHomo sapiens (human)
defense response to virusCyclic GMP-AMP synthaseHomo sapiens (human)
cGAS/STING signaling pathwayCyclic GMP-AMP synthaseHomo sapiens (human)
negative regulation of cGAS/STING signaling pathwayCyclic GMP-AMP synthaseHomo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationCyclic GMP-AMP synthaseHomo sapiens (human)
positive regulation of cellular senescenceCyclic GMP-AMP synthaseHomo sapiens (human)
cellular response to exogenous dsRNACyclic GMP-AMP synthaseHomo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (126)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
electron transfer activityGlutathione reductase, mitochondrialHomo sapiens (human)
NADP bindingGlutathione reductase, mitochondrialHomo sapiens (human)
glutathione-disulfide reductase (NADPH) activityGlutathione reductase, mitochondrialHomo sapiens (human)
flavin adenine dinucleotide bindingGlutathione reductase, mitochondrialHomo sapiens (human)
riboflavin transmembrane transporter activityRiboflavin-binding proteinGallus gallus (chicken)
riboflavin bindingRiboflavin-binding proteinGallus gallus (chicken)
signaling receptor activityRiboflavin-binding proteinGallus gallus (chicken)
type 8 metabotropic glutamate receptor bindingMajor prion proteinHomo sapiens (human)
amyloid-beta bindingMajor prion proteinHomo sapiens (human)
protease bindingMajor prion proteinHomo sapiens (human)
copper ion bindingMajor prion proteinHomo sapiens (human)
protein bindingMajor prion proteinHomo sapiens (human)
lamin bindingMajor prion proteinHomo sapiens (human)
glycosaminoglycan bindingMajor prion proteinHomo sapiens (human)
microtubule bindingMajor prion proteinHomo sapiens (human)
tubulin bindingMajor prion proteinHomo sapiens (human)
aspartic-type endopeptidase inhibitor activityMajor prion proteinHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingMajor prion proteinHomo sapiens (human)
signaling receptor activityMajor prion proteinHomo sapiens (human)
identical protein bindingMajor prion proteinHomo sapiens (human)
ATP-dependent protein bindingMajor prion proteinHomo sapiens (human)
transmembrane transporter bindingMajor prion proteinHomo sapiens (human)
protein-containing complex bindingMajor prion proteinHomo sapiens (human)
protein-folding chaperone bindingMajor prion proteinHomo sapiens (human)
molecular adaptor activityMajor prion proteinHomo sapiens (human)
molecular function activator activityMajor prion proteinHomo sapiens (human)
molecular condensate scaffold activityMajor prion proteinHomo sapiens (human)
cupric ion bindingMajor prion proteinHomo sapiens (human)
cuprous ion bindingMajor prion proteinHomo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
DNA bindingDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
DNA-directed 5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
protein bindingDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
nucleotidyltransferase activityDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
protein dimerization activityDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
bacterial-type RNA polymerase core enzyme bindingDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
DNA bindingDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
DNA-directed 5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
nucleotidyltransferase activityDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
magnesium ion bindingDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA bindingDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA-directed 5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
protein bindingDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
zinc ion bindingDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
nucleotidyltransferase activityDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
metal ion bindingDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA-directed 5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA bindingDNA-directed RNA polymerase subunit betaEscherichia coli K-12
DNA-directed 5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit betaEscherichia coli K-12
protein bindingDNA-directed RNA polymerase subunit betaEscherichia coli K-12
nucleotidyltransferase activityDNA-directed RNA polymerase subunit betaEscherichia coli K-12
ribonucleoside bindingDNA-directed RNA polymerase subunit betaEscherichia coli K-12
5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit betaEscherichia coli K-12
DNA-directed 5'-3' RNA polymerase activityDNA-directed RNA polymerase subunit betaEscherichia coli K-12
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase A2 activityPhospholipase A2, membrane associatedHomo sapiens (human)
phospholipid bindingPhospholipase A2, membrane associatedHomo sapiens (human)
calcium-dependent phospholipase A2 activityPhospholipase A2, membrane associatedHomo sapiens (human)
calcium ion bindingPhospholipase A2, membrane associatedHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
aldehyde oxidase activityAldehyde oxidaseHomo sapiens (human)
iron ion bindingAldehyde oxidaseHomo sapiens (human)
identical protein bindingAldehyde oxidaseHomo sapiens (human)
protein homodimerization activityAldehyde oxidaseHomo sapiens (human)
molybdopterin cofactor bindingAldehyde oxidaseHomo sapiens (human)
flavin adenine dinucleotide bindingAldehyde oxidaseHomo sapiens (human)
NAD bindingAldehyde oxidaseHomo sapiens (human)
2 iron, 2 sulfur cluster bindingAldehyde oxidaseHomo sapiens (human)
FAD bindingAldehyde oxidaseHomo sapiens (human)
DNA bindingCyclic GMP-AMP synthaseHomo sapiens (human)
chromatin bindingCyclic GMP-AMP synthaseHomo sapiens (human)
double-stranded DNA bindingCyclic GMP-AMP synthaseHomo sapiens (human)
protein bindingCyclic GMP-AMP synthaseHomo sapiens (human)
ATP bindingCyclic GMP-AMP synthaseHomo sapiens (human)
GTP bindingCyclic GMP-AMP synthaseHomo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingCyclic GMP-AMP synthaseHomo sapiens (human)
nucleosome bindingCyclic GMP-AMP synthaseHomo sapiens (human)
protein homodimerization activityCyclic GMP-AMP synthaseHomo sapiens (human)
metal ion bindingCyclic GMP-AMP synthaseHomo sapiens (human)
2',3'-cyclic GMP-AMP synthase activityCyclic GMP-AMP synthaseHomo sapiens (human)
molecular condensate scaffold activityCyclic GMP-AMP synthaseHomo sapiens (human)
poly-ADP-D-ribose modification-dependent protein bindingCyclic GMP-AMP synthaseHomo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (75)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
mitochondrial matrixGlutathione reductase, mitochondrialHomo sapiens (human)
cytosolGlutathione reductase, mitochondrialHomo sapiens (human)
external side of plasma membraneGlutathione reductase, mitochondrialHomo sapiens (human)
extracellular exosomeGlutathione reductase, mitochondrialHomo sapiens (human)
cytosolGlutathione reductase, mitochondrialHomo sapiens (human)
mitochondrionGlutathione reductase, mitochondrialHomo sapiens (human)
external side of plasma membraneRiboflavin-binding proteinGallus gallus (chicken)
dendriteMajor prion proteinHomo sapiens (human)
cytoplasmMajor prion proteinHomo sapiens (human)
endoplasmic reticulumMajor prion proteinHomo sapiens (human)
Golgi apparatusMajor prion proteinHomo sapiens (human)
cytosolMajor prion proteinHomo sapiens (human)
plasma membraneMajor prion proteinHomo sapiens (human)
external side of plasma membraneMajor prion proteinHomo sapiens (human)
cell surfaceMajor prion proteinHomo sapiens (human)
postsynaptic densityMajor prion proteinHomo sapiens (human)
inclusion bodyMajor prion proteinHomo sapiens (human)
extrinsic component of membraneMajor prion proteinHomo sapiens (human)
nuclear membraneMajor prion proteinHomo sapiens (human)
terminal boutonMajor prion proteinHomo sapiens (human)
intracellular membrane-bounded organelleMajor prion proteinHomo sapiens (human)
membrane raftMajor prion proteinHomo sapiens (human)
extracellular exosomeMajor prion proteinHomo sapiens (human)
postsynapseMajor prion proteinHomo sapiens (human)
plasma membraneMajor prion proteinMus musculus (house mouse)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytoplasmDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
cytosolDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
membraneDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
cytosolic DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
cytoplasmDNA-directed RNA polymerase subunit alphaEscherichia coli K-12
cytosolDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
cytosolic DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
RNA polymerase complexDNA-directed RNA polymerase subunit omegaEscherichia coli K-12
cytoplasmDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
cytosolDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
membraneDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
cytosolic DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit beta'Escherichia coli K-12
cytoplasmDNA-directed RNA polymerase subunit betaEscherichia coli K-12
cytosolDNA-directed RNA polymerase subunit betaEscherichia coli K-12
membraneDNA-directed RNA polymerase subunit betaEscherichia coli K-12
cytosolic DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit betaEscherichia coli K-12
DNA-directed RNA polymerase complexDNA-directed RNA polymerase subunit betaEscherichia coli K-12
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
extracellular regionPhospholipase A2, membrane associatedHomo sapiens (human)
extracellular spacePhospholipase A2, membrane associatedHomo sapiens (human)
mitochondrial outer membranePhospholipase A2, membrane associatedHomo sapiens (human)
endoplasmic reticulumPhospholipase A2, membrane associatedHomo sapiens (human)
endoplasmic reticulum membranePhospholipase A2, membrane associatedHomo sapiens (human)
plasma membranePhospholipase A2, membrane associatedHomo sapiens (human)
secretory granulePhospholipase A2, membrane associatedHomo sapiens (human)
perinuclear region of cytoplasmPhospholipase A2, membrane associatedHomo sapiens (human)
extracellular exosomePhospholipase A2, membrane associatedHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
cytosolAldehyde oxidaseHomo sapiens (human)
extracellular exosomeAldehyde oxidaseHomo sapiens (human)
cytoplasmCyclic GMP-AMP synthaseHomo sapiens (human)
cytosolCyclic GMP-AMP synthaseHomo sapiens (human)
nucleusCyclic GMP-AMP synthaseHomo sapiens (human)
nucleoplasmCyclic GMP-AMP synthaseHomo sapiens (human)
cytosolCyclic GMP-AMP synthaseHomo sapiens (human)
plasma membraneCyclic GMP-AMP synthaseHomo sapiens (human)
nuclear bodyCyclic GMP-AMP synthaseHomo sapiens (human)
site of double-strand breakCyclic GMP-AMP synthaseHomo sapiens (human)
nucleusCyclic GMP-AMP synthaseHomo sapiens (human)
site of double-strand breakCyclic GMP-AMP synthaseHomo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (287)

Assay IDTitleYearJournalArticle
AID1426326Cytotoxicity against human CRL8155 cells assessed as growth inhibition after 48 hrs by Alamar blue assay2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.
AID1854201Inhibition of cGAS (unknown origin) incubated for 1 hr by Typhoon imaging system analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Small molecules targeting cGAS-STING pathway for autoimmune disease.
AID270493Displacement of cy3B-GM from Hsp90-alpha at 30 uM2006Bioorganic & medicinal chemistry letters, Sep-01, Volume: 16, Issue:17
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.
AID693223Antiprion activity against human prion protein Fukuoka-1 infected mouse F3 cells assessed as drug level required for more than 99 percent reduction of PrPSc level by Western blot method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID547838Inhibition of human aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID23975logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID693222Antiprion activity against human prion protein Fukuoka-1 infected mouse F3 cells assessed as reduction of PrPSc level by Western blot method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID212743Inhibition of telomerase after assembly using recombinant Tetraymena thermophilia TR and TERT at 50 uM2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Nucleic acid-binding ligands identify new mechanisms to inhibit telomerase.
AID692039Permeability from basolateral to apical side of in wild type MDCK cells assessed as cell retention at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID334029Inhibition of Naja Naja PLA21997Journal of natural products, Nov, Volume: 60, Issue:11
Zanhasaponins A and B, antiphospholipase A2 saponins from an antiinflammatory extract of Zanha africana root bark.
AID275284Reduction of PrPSC accumulation in ScN2a cells2007Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
AID1349122Anticlonogenic activity against human MCF7 cells at 0.39 to 1.5 uM after 12 hrs by crystal violet staining based assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
AID1719207Antibiofilm activity against Candida albicans at 256 ug/ml relative to control2021Bioorganic & medicinal chemistry letters, 03-01, Volume: 35A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance.
AID158945Inhibitory activity against synovial human recombinant phospholipase (hr-PLA2) at 1 mM concentration1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Synthesis and pharmacological evaluation of 2'-hydroxychalcones and flavones as inhibitors of inflammatory mediators generation.
AID185798Compound was tested for the % inhibition rate of infarct size (myoglobin depleted area) on sc administration 15 min prior to the ligation at a dose of 75.0 mg/kg.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.
AID1338368Cytotoxicity against human HepG2 cells assessed as cell viability after 48 hrs by alamar blue assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.
AID272289Viability of human HepG2 cells at 20 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID330911Binding affinity to human serum albumin on sepharose column by affinity chromatography2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein.
AID1593290Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID692044Permeability from apical to basolateral side in MDCK cells overexpressing human MDR1 assessed as adsorption on transwell at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID159104In vitro inhibition of rat secretory Phospholipase A2 (group II).1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis and phospholipase A2 inhibitory activity of thielocin B3 derivatives.
AID602119NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID513176Displacement of [3H]astemizole from free heme crystal at 15 uM after 16 hrs by scintillation counting2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID161627Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein.
AID275286Solubility in phosphate buffer at pH 6.5 at 500 uM2007Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
AID521209Antiproliferative activity against mouse astrocyte cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID519607Cytotoxicity against Hepatocyte cells assessed as cell viability by MTT assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
New active drugs against liver stages of Plasmodium predicted by molecular topology.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID26296Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1814040Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at pH 6 in presence of glucose measured after 48 hrs by visual analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1593288Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I/A138T double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID693224Cytotoxicity against mouse N2A cells assessed as maximal tolerant concentration2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID23964logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID214657The competitive inhibitory activity against trypanothione reductase was evaluated from Lineweaver Burk plots1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships.
AID271095Therapeutic index, LD50 for ScN2a cells/EC50 for PrPSc accumulation in ScN2a cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells.
AID329525Activity at androgen receptor ligand binding domain assessed as inhibition of SRC2-3 interaction at 50 uM after 2 hrs by fluorescence polarization assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-09, Volume: 104, Issue:41
A surface on the androgen receptor that allosterically regulates coactivator binding.
AID1917909Anticancer activity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Multiple approaches to repurposing drugs for neuroblastoma.
AID322074Antimicrobial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hrs2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
AID445586Antiprion activity against Scrapie prion protein-mediated scrapie in mouse SMB cells assessed as remaining PrP-Sc level after 5 days by Bradford assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, and structure-activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease.
AID602118NOVARTIS: Antimalarial liver stage activity measured as a greater than 50% reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells at 10uM compound concentration, determined by immuno-fluorescence.2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID693232Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in MDCK cells overexpressing human MDR1 at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID233595Ratio of Inhibitory activity against glutathione reductase and inhibitory activity against trypanothione reductase was determined2001Bioorganic & medicinal chemistry letters, Oct-08, Volume: 11, Issue:19
Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine.
AID1814046Inhibition of actin polarization in Saccharomyces cerevisiae BY4741 at pH 7.5 incubated for 30 mins in presence of 8% glucose by rhodamine phalloidin staining based confocal microscopic analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1814055Inhibition HXT2 in Saccharomyces cerevisiae using 2DG as substrate assessed as reduction in 2DG uptake by measuring decrease in Vmax at 0.6 mM at pH 7.5 by Michaelis-Menten analysis (Rvb= 208 +/- 7 nmol/min)2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1814042Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at pH 8 in presence of glucose measured after 48 hrs by visual analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID344299Antiprion activity against scrapie prion protein 22L infected mouse N167 cells assessed as reduction of scrapie prion protein accumulation2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID214493Inhibitory concentration against trypanothione reductase was determined2001Bioorganic & medicinal chemistry letters, Oct-08, Volume: 11, Issue:19
Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID692045Permeability from basolateral to apical side in MDCK cells overexpressing human MDR1 assessed as adsorption on transwell at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID75303Inhibitory concentration against human Glutathione reductase was determined2001Bioorganic & medicinal chemistry letters, Oct-08, Volume: 11, Issue:19
Antiprotozoal and cytotoxicity evaluation of sulfonamide and urea analogues of quinacrine.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID693225Binding affinity to truncated human PrP 121-231 at 50 uM by surface plasmon resonance method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID357351Inhibition of secretagogue-induced beta-glucuronidase release in Sprague-Dawley rat peritoneal mast cells at 30 uM treated 30 mins before secretagogue challenge measured after 15 mins2001Journal of natural products, Aug, Volume: 64, Issue:8
Two phenanthraquinones from Dendrobium moniliforme.
AID693233Permeability from apical to basolateral side of in wild type MDCK cells assessed as mass balance at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1814059Inhibition of endocytosis in Saccharomyces cerevisiae BY4741 from plasma to vacuoles assessed as formation of discrete granules at 25 mM incubated for 2 hrs by FM4-64 staining based analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1129473Antioxidant activity assessed as trolox equivalent of ABTS radical scavenging activity up to 20 uM2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species.
AID9652In vitro cytotoxicity against transformed chinese hamster fibroblast line AA81990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID241212Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry.
AID445590Antiprion activity against Scrapie prion protein-mediated scrapie in RML mouse ScN2a cells assessed as reduction of PrP-Sc level after 6 days by immunoblotting2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Design, synthesis, and structure-activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease.
AID275285Cytotoxicity against ScN2a cells2007Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
AID1814060Ratio of antimicrobial activity against Saccharomyces cerevisiae BY4741 at pH 6 to antimicrobial activity against Saccharomyces cerevisiae BY4741 at pH 82021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID693227Apparent permeability of the compound from apical to basolateral side in wild type MDCK cells at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1814048Induction of membrane disruption in Saccharomyces cerevisiae BY4741 assessed as cell lysis by measuring increase in extracellular ATP level at pH 7.5 in presence of 8% glucose incubated for 30 mins2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID23970logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1814054Inhibition HXT2 in Saccharomyces cerevisiae using 2DG as substrate assessed as reduction in 2DG uptake by measuring Km at 0.6 mM at pH 7.5 by Michaelis-Menten analysis (Rvb= 0.76 +/- 0.08 mM)2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1377007Cytotoxicity against human 184B5 cells assessed as growth inhibition after 48 hrs by SRB assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and characterization of novel quinacrine analogs that preferentially kill cancer over non-cancer cells through the down-regulation of Bcl-2 and up-regulation of Bax and Bad.
AID355103Inhibition of snake venom phospholipase A2 assessed as oxygen consumption for 3 mins1996Journal of natural products, Oct, Volume: 59, Issue:10
Two fungal lanostane derivatives as phospholipase A2 inhibitors.
AID678838TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-CEM cells1996Anti-cancer drugs, Jul, Volume: 7, Issue:5
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.
AID344301Antiprion activity against scrapie prion protein RML infected mouse Ch2 cells assessed as reduction of scrapie prion protein accumulation2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID75454In vitro inhibition against human glutathione reductase; IA denotes inactive2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Quinoxaline N,N'-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi. Structure-activity relationships.
AID278900Inhibition of Tween 20-induced beta-hematin formation by colorimetric assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Simple colorimetric inhibition assay of heme crystallization for high-throughput screening of antimalarial compounds.
AID1129465Neuroprotective activity in mouse HT22 cells assessed as protection against glutamate-induced oxidative damage at less than cytotoxic EC50 after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species.
AID693221Antiprion activity against mouse prion protein 22L infected mouse N167 cells assessed as drug level required for more than 99 percent reduction of PrPSc level by Western blot method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1377006Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and characterization of novel quinacrine analogs that preferentially kill cancer over non-cancer cells through the down-regulation of Bcl-2 and up-regulation of Bax and Bad.
AID158833Percent inhibition of hypoxanthine uptake by Plasmodium berghei1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Syntheses of 9-acridine- and 2-phenanthridinemethanols as potential antimalarials.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1814045Inhibition of actin polarization in Saccharomyces cerevisiae BY4741 at pH 7.5 incubated for 30 mins in presence of 2% glucose by rhodamine phalloidin staining based confocal microscopic analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1888115Inhibition of recombinant His-tagged Leishmania infantum TryR oxidoreductase activity expressed in Escherichia coli BL21 (DE3) using TS2 and NADPH as substrate by DTNB-reagent based spectrophotometric method2022European journal of medicinal chemistry, Jan-05, Volume: 227Pyridazino-pyrrolo-quinoxalinium salts as highly potent and selective leishmanicidal agents targeting trypanothione reductase.
AID344297Cytotoxicity against mouse ScN2a cells assessed as maximal tolerant concentration2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID692040Permeability from apical to basolateral side of in P-glycoprotein-mediated MDCK cells over expressing human MDR1 assessed as cell retention at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID717844Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation at 20 uM after 45 mins by spectrophotometric analysis relative to control2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Identification of selective inhibitors of indoleamine 2,3-dioxygenase 2.
AID1814050Inhibition HXT2 in Saccharomyces cerevisiae using 2DG as substrate assessed as reduction in 2DG uptake at pH 7.5 preincubated for 10 min followed by substrate addition and measured after 10 min by glucose uptake-Glo assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID693234Permeability from basolateral to apical side of in wild type MDCK cells assessed as mass balance at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID519608Selectivity index, ratio of TC50 for hepatocytes to IC50 for Plasmodium yoelii 2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
New active drugs against liver stages of Plasmodium predicted by molecular topology.
AID1426323Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by Alamar blue assay2017Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1593296Inhibition of Plasmodium falciparum cytochrome b-c12019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID519606Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
New active drugs against liver stages of Plasmodium predicted by molecular topology.
AID521208Antiproliferative activity against mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1623305Antiproliferative activity against human U251 cells by MTT assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Recent advances in the discovery of small molecules targeting glioblastoma.
AID693226Effective permeability of the compound at pH 7.4 at 30 to 50 uM by PAMPA assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID396379Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by [G-3H]hypoxanthine uptake2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Pharmacophore based discovery of potential antimalarial agent targeting haem detoxification pathway.
AID344296Antiprion activity against scrapie prion protein RML infected mouse ScN2a cells assessed as drug level required for more than 99 percent reduction of scrapie prion protein by immunoblot analysis2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID275287Permeability across DOPC lipid membrane by PAMPA2007Journal of medicinal chemistry, Jan-11, Volume: 50, Issue:1
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
AID212741Inhibition of purified telomerase of Euplotes aediculatus at 50 uM2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Nucleic acid-binding ligands identify new mechanisms to inhibit telomerase.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1814065Induction of membrane disruption in Saccharomyces cerevisiae BY4741 at 50 mM incubated for 2 hrs by FM4-64 staining based analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1765968Inhibition of Leishmania Trypanothione reductase
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID212902Inhibition of human telomerase after assembly using recombinant hTR and hTERT at 50 uM2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Nucleic acid-binding ligands identify new mechanisms to inhibit telomerase.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID271092Cytotoxicity against mouse ScN2a cell line relative to control2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells.
AID1814043Antimicrobial activity against saccharomyces cerevisiae BY4741 assessed as inhibition of translation initiation by measuring polysme/monosome ratio at 1.5 mM at pH 7.5 incubated for 30 mins in presence of 2% glucose by polysome analysis (Rvb= 1.74 No_unit2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID272307Transfection of CDP/plasmid pGL3-CV in HepG2 cells at 20 uM after 48 hrs by luciferase assay2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Structure-function correlation of chloroquine and analogues as transgene expression enhancers in nonviral gene delivery.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1854214Inhibition of cGAS in human THP-1 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Small molecules targeting cGAS-STING pathway for autoimmune disease.
AID1349120Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
AID1661954Binding affinity to Ebola virus glycoprotein assessed as dissociation constant incubated for 20 to 30 mins by microscale thermophoresis2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Toward the Target: Tilorone, Quinacrine, and Pyronaridine Bind to Ebola Virus Glycoprotein.
AID1349118Antiproliferative activity against human MDA-MB-468 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
AID108138Inhibitory activity against mast cell degranulation by measuring the content of beta-glucuronidase in the supernatant2002Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21
Synthesis and antiinflammatory evaluation of 9-anilinoacridine and 9-phenoxyacridine derivatives.
AID1695254Cytotoxicity against human WIL2-NS cells assessed as reduction in cell viability after 48 hrs by alamar blue dye based assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against
AID23976logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID725519Antiprion activity against scrapie prion protein (unknown origin) infected in mouse ScGT1 cells assessed as inhibition of PrPSc replication by ELISA2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer's and Prion Diseases.
AID344302Antiprion activity against scrapie prion protein RML infected mouse Ch2 cells assessed as drug level required for more than 99 percent reduction of scrapie prion protein2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID26309Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID271644Inhibition of protease-resistant scrapie prion protein activity in ScN2a cells2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A chimeric ligand approach leading to potent antiprion active acridine derivatives: design, synthesis, and biological investigations.
AID540237Phospholipidosis-positive literature compound observed in rat
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID229940Hypersensitivity factor(HF) was determined from the ratio of IC50(AA8) / IC50(UV4)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID83578Concentration required to inhibit colony formation by 50% in human colon carcinoma HT-29 cells1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
Synthesis and DNA-sequence selectivity of a series of mono- and difunctional 9-aminoacridine nitrogen mustards.
AID1814047Induction of membrane disruption in Saccharomyces cerevisiae BY4741 assessed as cell lysis by measuring increase in extracellular ATP level at pH 7.5 in presence of 2% glucose incubated for 30 mins2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1558341Antiviral activity against Zika virus MR766 infected in African green monkey Vero cells by plaque assay2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID693237Permeability from apical to basolateral side of in wild type MDCK cells assessed as cell retention at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1593287Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring V259L mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID355106Inhibition of snake venom phospholipase A2 at 5.800 mM assessed as oxygen consumption for 3 mins1996Journal of natural products, Oct, Volume: 59, Issue:10
Two fungal lanostane derivatives as phospholipase A2 inhibitors.
AID625294Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1893058Synergistic anti-prion activity of mouse ScN2a cells infected with RML prion assessed as reduction of RML accumulation by isobologram analysis
AID642883Competitive inhibition of chicken riboflavin binding protein by surface plasmon resonance assay2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study.
AID246157Effective concentration for Plasmodium falciparum 3D72005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID23962logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1587049Cytotoxicity against human CRL8155 cells after 48 hrs by alamar blue assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID23959logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID419687Inhibition of Trypanosoma cruzi trypanothione reductase2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase.
AID600983Inhibition of bovine erythrocyte AChE using acetylthiocholine iodide as a substrate at 10 uM after 20 mins by Ellman's assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
AID692043Permeability from basolateral to apical side of in wild type MDCK cells assessed as adsorption on transwell at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID547842Inhibition of rabbit aldehyde oxidase2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.
AID1814041Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at pH 7 in presence of glucose measured after 48 hrs by visual analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID26310Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1695255Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by alamar blue dye based assay2020RSC medicinal chemistry, Aug-01, Volume: 11, Issue:8
Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against
AID577834Antiprion activity in human transmissible spongiform encephalopathies agent Fukuoka-1 prion infected GT1-7 cells assessed as proteinase K-resistant proteins after 3 days Western blotting analysis2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Synthesis of GN8 derivatives and evaluation of their antiprion activity in TSE-infected cells.
AID692041Permeability from basolateral to apical side of in P-glycoprotein-mediated MDCK cells over expressing human MDR1 assessed as cell retention at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID692042Permeability from apical to basolateral side of in wild type MDCK cells assessed as adsorption on transwell at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1721836Inhibition of trypanothione reductase (unknown origin)2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
Pre-clinical evidences of the antileishmanial effects of diselenides and selenocyanates.
AID1207663Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID159101Compound was tested for the percent inhibition of phospholipase A2 (PLA2) in rabbit heart membranes at a concentration of 100 uM.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.
AID693231Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in wild type MDCK cells at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID26294Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID158832Percent inhibition of adenosine uptake by Plasmodium berghei1981Journal of medicinal chemistry, Aug, Volume: 24, Issue:8
Syntheses of 9-acridine- and 2-phenanthridinemethanols as potential antimalarials.
AID212744Inhibition of telomerase before assembly using recombinant Tetraymena thermophilia TR and TERT at 50 uM2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Nucleic acid-binding ligands identify new mechanisms to inhibit telomerase.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1593291Antimalarial activity against drug-resistant Plasmodium falciparum 3D7 harboring A82T/V259L double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID1814044Antimicrobial activity against saccharomyces cerevisiae BY4741 assessed as inhibition of translation initiation by measuring polysme/monosome ratio at 1.5 mM at pH 7.5 incubated for 30 mins in presence of 8% glucose by polysome analysis (Rvb= 1.94 No_unit2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID246115Effective concentration against Plasmodium falciparum W22005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities.
AID1520338Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay2019European journal of medicinal chemistry, Mar-15, Volume: 166All that glitters is not gold: Panning cytotoxic natural products and derivatives with a fused tricyclic backbone by the estimation of their leadlikeness for cancer treatment.
AID1349121Antiproliferative activity against human 184B5 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
AID600984Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
AID1814049Inhibition HXT2 in Saccharomyces cerevisiae using 2DG as substrate assessed as inhibition of 2DG uptake at pH 6 preincubated for 10 min followed by substrate addition and measured after 10 min by glucose uptake-Glo assay2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1814061Ratio of antimicrobial activity against Saccharomyces cerevisiae BY4741 at pH 7 to antimicrobial activity against Saccharomyces cerevisiae BY4741 at pH 82021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1512701Inhibition of autophagy in human U2OS cells stably expressing tfLC32018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.
AID23972logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID643383Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets.
AID271091Inhibition of PrPSc accumulation in mouse ScN2a cell line relative to control2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID214665In vitro inhibition against Trypanosoma cruzi trypanothione reductase; active2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Quinoxaline N,N'-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi. Structure-activity relationships.
AID1349119Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.
AID1512702Cytotoxicity in human U2OS cells incubated for 24 to 48 hrs by CellTiter Glo assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.
AID344298Selectivity index, ratio of maximal tolerant concentration for mouse ScN2a cells to EC50 for scrapie prion protein RML infected mouse ScN2a cells2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID1558342Cytotoxicity against BHK21 cells after 24 to 48 hrs by CCK8 assay2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Drugs for the Treatment of Zika Virus Infection.
AID693235Permeability from apical to basolateral side in MDCK cells overexpressing human MDR1 assessed as mass balance at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID215309In vitro cytotoxicity against transformed chinese hamster fibroblast line UV4.1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID271093Cytotoxicity against HEK293 cells relative to control2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells.
AID725517Cytotoxicity against mouse ScGT1 cells assessed as cell viability at EC50 concentration after 5 days by fluorescence plate reader analysis2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer's and Prion Diseases.
AID26295Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1377005Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by SRB assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and characterization of novel quinacrine analogs that preferentially kill cancer over non-cancer cells through the down-regulation of Bcl-2 and up-regulation of Bax and Bad.
AID322073Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
AID1593289Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID271645Antiprion activity in ScN2a cells assessed as complete reduction of protease-resistant scrapie prion protein2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
A chimeric ligand approach leading to potent antiprion active acridine derivatives: design, synthesis, and biological investigations.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID693218Antiprion activity against mouse prion protein RML infected mouse ScN2a cells assessed as reduction of PrPSc level by Western blot method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID103232Anti MDR activity was expressed as MDR ratio or MDR fold reversal in doxorubicin resistant human breast carcinoma tumor cell line MCF-7/DOX1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
Molecular modeling of phenothiazines and related drugs as multidrug resistance modifiers: a comparative molecular field analysis study.
AID693229Apparent permeability from apical to basolateral side in MDCK cells overexpressing human MDR1 at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID693230Apparent permeability of the compound from basolateral to apical side in MDCK cells overexpressing human MDR1 at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1605383Binding affinity to immobilized mouse C-terminal Rhinovirus 3C cleavage site-fused 6xHis-tagged Frizzled-8 CRD (Q33 to G173 resideus) transfected with pDisplay_BirA-ER plasmid in HEK293T cells for biotinylation assessed as protein-compound complex formati2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID344303Antiprion activity against human prion Fukuoka-1 infected mouse F3 cells assessed as reduction of scrapie prion protein accumulation2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID681635TP_TRANSPORTER: inhibition of TEA uptake (apical to cell)(TEA: 100 uM, Quinacrine: 200 uM) in OCT2-expressing MDCK cells1999The American journal of physiology, 12, Volume: 277, Issue:6
rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger.
AID693228Apparent permeability of the compound from basolateral to apical side in MDCK cells at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID1145960Inhibition of Escherichia coli DNA-primed RNA polymerase activity using [8-14C]ATP by scintillation counting1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Synthesis and biological properties of some spin-labeled 9-aminoacridines.
AID1661953Antiviral activity against Ebolavirus infected in human HeLa cells assessed as reduction in viral replication incubated for 48 hrs by luminescence based assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Toward the Target: Tilorone, Quinacrine, and Pyronaridine Bind to Ebola Virus Glycoprotein.
AID1599414Antiviral activity against DENV2 infected in BHK cells assessed as reduction in viral yield after 24 ro 48 hrs by luciferase reporter gene assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1338367Cytotoxicity against human CRL-1855 cells assessed as cell viability after 48 hrs by alamar blue assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.
AID1814051Inhibition HXT2 in Saccharomyces cerevisiae using 2DG as substrate assessed as reduction in 2DG uptake by measuring Km at 0.2 mM at pH 7.5 by Michaelis-Menten analysis (Rvb=0.76 +/- 0.08 mM)2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID1814062Antimicrobial activity against Saccharomyces cerevisiae BY4741 assessed as inhibition of microbial growth at 50 mM at pH 5 in presence of glucose measured after 48 hrs by visual analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID644953Binding affinity to human pre-hsa-mir-155 miRNA assessed as inhibition of dicer-catalysed (33P)-labelled pre-miRNA processing at 1 mM after 1 hr by PAGE analysis2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Pre-microRNA binding aminoglycosides and antitumor drugs as inhibitors of Dicer catalyzed microRNA processing.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID23968logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID642884Binding affinity to chicken riboflavin binding protein assessed as dissociation constant at pH 7.4 in phosphate buffer by isothermal titration calorimetric assay2011ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5
Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study.
AID333452Inhibition of compound 48/80-stimulated histamine release in rat mast cell2004Journal of natural products, Nov, Volume: 67, Issue:11
Anti-inflammatory phloroglucinols and terpenoids from Garcinia subelliptica.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID693220Antiprion activity against mouse prion protein 22L infected mouse N167 cells assessed as reduction of PrPSc level by Western blot method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID344295Antiprion activity against scrapie prion protein RML infected mouse ScN2a cells assessed as reduction of scrapie prion protein accumulation by immunoblot analysis2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Antiprion activity of functionalized 9-aminoacridines related to quinacrine.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1587050Cytotoxicity against human HepG2 cells after 48 hrs by alamar blue assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID26756DNA binding dissociation constant as KD1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics.
AID693219Antiprion activity against mouse prion protein RML infected mouse ScN2a cells assessed as drug level required for more than 99 percent reduction of PrPSc level by Western blot method2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID158938In vitro inhibition of human recombinant secretory Phospholipase A2 (group II).1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Synthesis and phospholipase A2 inhibitory activity of thielocin B3 derivatives.
AID271094Cytotoxicity against HepG2 cells relative to control2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells.
AID1454610Cytotoxicity against human HepG2 cells after 48 hrs by Alamar Blue-based assay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
New Class of Antitrypanosomal Agents Based on Imidazopyridines.
AID1814052Inhibition HXT2 in Saccharomyces cerevisiae using 2DG as substrate assessed as reduction in 2DG uptake by measuring decrease in Vmax at 0.2 mM at pH 7.5 by Michaelis-Menten analysis (Rvb= 208 +/- 7 nmol/min)2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID333450Inhibition of compound 48/80-stimulated beta-glucuronidase release in rat peritoneal mast cell2004Journal of natural products, Nov, Volume: 67, Issue:11
Anti-inflammatory phloroglucinols and terpenoids from Garcinia subelliptica.
AID1917907Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Multiple approaches to repurposing drugs for neuroblastoma.
AID1593253Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes by SYBR green 1-based fluorescence assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
AID693236Permeability from basolateral to apical side of in MDCK cells overexpressing human MDR1 assessed as mass balance at 10 uM after 2 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Anti-prion activities and drug-like potential of functionalized quinacrine analogs with basic phenyl residues at the 9-amino position.
AID357350Inhibition of secretagogue-induced histamine release in Sprague-Dawley rat peritoneal mast cells at 30 uM treated 30 mins before secretagogue challenge measured after 15 mins2001Journal of natural products, Aug, Volume: 64, Issue:8
Two phenanthraquinones from Dendrobium moniliforme.
AID1917908Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Multiple approaches to repurposing drugs for neuroblastoma.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1379464Cytotoxicity against human CRL8155 cells assessed as growth inhibition after 48 hrs by Alamar blue assay2017ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8
1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti-
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1377004Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and characterization of novel quinacrine analogs that preferentially kill cancer over non-cancer cells through the down-regulation of Bcl-2 and up-regulation of Bax and Bad.
AID108139Inhibitory activity against mast cell degranulation by measuring the content of histamine in the supernatant2002Journal of medicinal chemistry, Oct-10, Volume: 45, Issue:21
Synthesis and antiinflammatory evaluation of 9-anilinoacridine and 9-phenoxyacridine derivatives.
AID1129462Cytotoxicity against mouse HT22 cells after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species.
AID214649Natural log of the value in (uM) of inhibition constant was tested against Trypanothione Reductase1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
A virtual screening approach applied to the search for trypanothione reductase inhibitors.
AID513158Inhibition of heme crystallization after 16 hrs2006Nature chemical biology, Aug, Volume: 2, Issue:8
A clinical drug library screen identifies astemizole as an antimalarial agent.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1067816Cytotoxicity against human CRL8155 cells after 48 hrs by Alamar Blue assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
AID23966logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1814064Inhibition of actin polarization in Saccharomyces cerevisiae BY4741 at pH 6 incubated for 30 mins in presence of 2% glucose by rhodamine phalloidin staining based confocal microscopic analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1067814Cytotoxicity against human HepG2 cells after 48 hrs by Alamar Blue assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
AID681644TP_TRANSPORTER: TEA uptake (TEA: 200 uM, Quinacrine: 200 uM) in Xenopus laevis oocytes1999The American journal of physiology, 12, Volume: 277, Issue:6
rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger.
AID212903Inhibition of human telomerase before assembly using recombinant hTR and hTERT at 50 uM2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Nucleic acid-binding ligands identify new mechanisms to inhibit telomerase.
AID1454609Cytotoxicity against human CRL8155 cells after 48 hrs by Alamar Blue-based assay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
New Class of Antitrypanosomal Agents Based on Imidazopyridines.
AID23973Partition coefficient (logD, measured by HPLC, log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The 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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
AID1804171DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\2020Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7
Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,793)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902554 (67.33)18.7374
1990's548 (14.45)18.2507
2000's374 (9.86)29.6817
2010's237 (6.25)24.3611
2020's80 (2.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 49.25

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.

MetricThis Compound (vs All)
Research Demand Index49.25 (24.57)
Research Supply Index8.32 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index84.80 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (49.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials65 (1.60%)5.53%
Reviews150 (3.70%)6.00%
Case Studies131 (3.23%)4.05%
Observational3 (0.07%)0.25%
Other3,702 (91.38%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open-label, Fixed-dose, Clinical Study of Quinacrine Safety and Efficacy in the Treatment of Advanced Renal Cell Carcinoma [NCT00574483]Phase 20 participants (Actual)Interventional2007-11-30Withdrawn(stopped due to reevaluation of compound development)
Quinacrine-Capecitabine Combinatorial Therapy for Advanced Stage Colorectal Adenocarcinoma:A Phase I/II Investigator-Initiated Clinical Trial [NCT01844076]Phase 1/Phase 219 participants (Actual)Interventional2016-01-14Terminated(stopped due to The single Quinacrine manufacture facility in the US was shut down by the FDA)
PRION-1: Quinacrine for Human Prion Disease. A Partially Randomized Patient Preference Trial to Evaluate the Activity and Safety of Quinacrine in Human Prion Disease [NCT00104663]160 participants Interventional2004-06-30Completed
A Phase I Study of Erlotinib in Combination With Quinacrine in Patients With Advanced Non-Small-Cell Lung Cancer [NCT01839955]Phase 112 participants (Actual)Interventional2013-09-30Completed
Novel Therapeutics For Prion Diseases: A Randomized, Double-blinded, Placebo-controlled Study of the Efficacy of Quinacrine in the Treatment of Sporadic Creutzfeldt-Jakob Disease [NCT00183092]Phase 269 participants (Actual)Interventional2005-04-30Completed
An Open-Label, Phase II Safety, Tolerability, Drug Level and Efficacy Trial of Quinacrine in Patients With Androgen-Independent Metastatic Prostate Cancer [NCT00417274]Phase 231 participants (Actual)Interventional2006-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00183092 (8) [back to overview]"Change in Phonemic Fluency (Words Beginning With Letter D)"
NCT00183092 (8) [back to overview]ADAS-Cog Change After 2 Months Among Survivors
NCT00183092 (8) [back to overview]Barthel Score Change After 2 Months
NCT00183092 (8) [back to overview]Change in Clinical Dementia Rating Scale Sum of Boxes (CDRS-SB) After 2 Months
NCT00183092 (8) [back to overview]Change in Mini-Mental State Examination (MMSE) After 2 Months
NCT00183092 (8) [back to overview]Change in Rankin Score After 2 Months
NCT00183092 (8) [back to overview]Change in Semantic Verbal Fluency (Naming Animals)
NCT00183092 (8) [back to overview]Primary Survival
NCT00417274 (1) [back to overview]Efficacy of Quinacrine, Based on Prostate Specific Antigen (PSA) Response in Patients With Androgen-independent Metastatic Prostate Cancer
NCT01844076 (3) [back to overview]Phase I - Number of Participants Who Experienced Dose Limiting Toxicities and Adverse Reactions
NCT01844076 (3) [back to overview]Phase II - Rate of Response
NCT01844076 (3) [back to overview]Phase II - Time to Progression (TTP)

"Change in Phonemic Fluency (Words Beginning With Letter D)"

"Verbal fluency tests are a kind of psychological test in which participants have to say as many words as possible from a category in 60 seconds. This category (words beginning with letter D) is phonemic. Higher scores indicate better cognition." (NCT00183092)
Timeframe: Baseline, 2 months

Interventionnumber of words generated (Mean)
Placebo-2.4
Quinacrine-2.2

[back to top]

ADAS-Cog Change After 2 Months Among Survivors

ADAS-cog measures cognitive performance by combining ratings of 11 components (word recall, word recognition, constructional praxis, orientation, naming objects and fingers, commands, ideational praxis, remembering instruction, spoken language, word finding, comprehension) representing six areas of cognition: memory; language; orientation to time, place and person; construction of simple designs and planning; and performing simple behaviors in pursuit of a basic, predefined goal. Seven components are scored as the 'number incorrect'. For example, in the commands component, the number of five commands performed incorrectly (range: 0-5). Four components are scored from 0 (no limitations) to 5 (max limitations) as the examiner's perception of remembering instructions, spoken language ability, word finding and comprehension. Component scores are summed into a total ADAS-cog score ranging from 0-75, with low scores indicating better cognitive performance. (NCT00183092)
Timeframe: Baseline, 2 months

Interventionunits on a scale (Mean)
Placebo13.0
Quinacrine12.6

[back to top]

Barthel Score Change After 2 Months

An ordinal scale used to measure performance in activities of daily living. Scores range from 0 (worst, fully dependent) to 100 (best, independent); higher score associated with a greater likelihood of being able to live at home with a degree of independence following discharge from hospital. 10 individual items are scored and summed to derive the overall Barthel index score. Each item may be scored 0, 5, 10 or 15; not all items use the full range of 4 possible values. The amount of time and physical assistance required to perform each item are considered in scoring each item. For subjects unable to return for month-2 visit, Barthel Index was performed via telephone. (NCT00183092)
Timeframe: baseline, 2 months

Interventionunits on a scale (Mean)
Placebo-23.2
Quinacrine-13.2

[back to top]

Change in Clinical Dementia Rating Scale Sum of Boxes (CDRS-SB) After 2 Months

Clinical Dementia Rating Scale Sum of Boxes (CDRS-SB). The CDR is obtained through semistructured interviews of patients and informants, and cognitive functioning is rated in 6 domains of functioning: memory, orientation, judgment and problem solving, community affairs, home and hobbies, and personal care. Each domain is rated on a 5-point scale of functioning: 0, no impairment; 0.5, questionable impairment; 1, mild impairment; 2, moderate impairment; and 3, severe impairment (personal care is scored on a 4-point scale without a 0.5 rating available). The global CDR score is computed via an algorithm. The CDR-SB score is obtained by summing each of the domain box scores, with scores ranging from 0 to 18. A higher value and/or positive change is worse. For subjects unable to return for month-2 visit, CDRS-SB was performed via telephone. (NCT00183092)
Timeframe: Baseline, 2 months

Interventionunits on a scale (Mean)
Placebo3.2
Quinacrine0.3

[back to top]

Change in Mini-Mental State Examination (MMSE) After 2 Months

The mini-mental state examination (MMSE) is a brief 30-point questionnaire that is used to screen for cognitive impairment. In about 10 minutes it samples functions including arithmetic, memory and orientation. A score greater than or equal to 25 points (out of 30) indicates a normal cognition. Lower scores can indicate severe (≤9 points), moderate (10-18 points) or mild (19-24 points) cognitive impairment. Low to very low scores correlate closely with the presence of dementia, although other mental disorders can also lead to abnormal findings on MMSE testing. (NCT00183092)
Timeframe: Baseline to Month-2

Interventionunits on a scale (Mean)
Placebo-6.9
Quinacrine-3.9

[back to top]

Change in Rankin Score After 2 Months

"The scale runs from 0-6, running from perfect health without symptoms to death. 0 - No symptoms.~- No significant disability. Able to carry out all usual activities, despite some symptoms.~- Slight disability. Able to look after own affairs without assistance, but unable to carry out all previous activities.~- Moderate disability. Requires some help, but able to walk unassisted.~- Moderately severe disability. Unable to attend to own bodily needs without assistance, and unable to walk unassisted.~- Severe disability. Requires constant nursing care and attention, bedridden, incontinent.~- Dead. For subjects unable to return for the 2-month visit, Rankin score was assessed via telephone." (NCT00183092)
Timeframe: Baseline, 2 months

Interventionunits on a scale (Mean)
Placebo0.8
Quinacrine0.3

[back to top]

Change in Semantic Verbal Fluency (Naming Animals)

Verbal fluency tests are a kind of psychological test in which participants have to say as many words as possible from a category in 60 seconds. This category (naming animals) is semantic. Higher scores indicate better cognition. (NCT00183092)
Timeframe: Baseline, 2 months

Interventionnumber of words generated (Mean)
Placebo-3.2
Quinacrine-2.2

[back to top]

Primary Survival

Participants alive after 2 months on study treatment (NCT00183092)
Timeframe: Randomization to Month-2

Interventionparticipants (Number)
Placebo19
Quinacrine13

[back to top]

Efficacy of Quinacrine, Based on Prostate Specific Antigen (PSA) Response in Patients With Androgen-independent Metastatic Prostate Cancer

Patients who achieved a complete response (CR) or a partial response (PR) to therapy were allowed to continue to receive treatment until disease progression or unacceptable toxicity occurred, until the patient discontinued treatment for another reason, or for a total of 6 months. Patients who continued to show a CR or PR or who maintained stable disease (SD) after 6 months of therapy were to be allowed to continue therapy at the investigator's discretion. (NCT00417274)
Timeframe: End of treatment

InterventionParticipants (Number)
Quinacrine Treatment1

[back to top]

Phase I - Number of Participants Who Experienced Dose Limiting Toxicities and Adverse Reactions

Establish the tolerability of both agents in combination when used at established clinical doses. The objective is to determine toxicities and adverse reactions of patients in each group with different dose levels to find the maximum tolerated dose (MTD). (NCT01844076)
Timeframe: One year

InterventionParticipants (Count of Participants)
Phase I Level -20
Phase I Level -10
Phase I Level 03

[back to top]

Phase II - Rate of Response

Determine rate of response in patients receiving quinacrine in combination with capecitabine. Using Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1) complete response (CR) is a disappearance of all target lesions, partial response (PR) is at least 30% decrease in the sum of diameters of target lesions, and overall response is the number of patients who experience a complete response or partial response. (NCT01844076)
Timeframe: 2-3 years

InterventionParticipants (Count of Participants)
Phase I Level -20
Phase I Level -10
Phase I Level 00
Phase II1

[back to top]

Phase II - Time to Progression (TTP)

Determine time to progression from start of treatment in patients receiving quinacrine in combination with capecitabine. Using Response Evaluation Criteria in Solid Tumors (RECIST) guideline (version 1.1), progression is defined as a 20% increase in sum of target lesions, with at least a 5 mm absolute increase. (NCT01844076)
Timeframe: 2-3 years

Interventionmonths (Median)
Phase II2.12

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