1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid profile

**1-(4-Methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid**, also known as **(4-Methoxybenzyl)-quinolone-3-carboxylic acid** or **(4-Methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid** (abbreviated as **(4-MeOBz)-QCA**), is a synthetic organic compound with a quinolone scaffold.

**Importance in Research:**

**(4-MeOBz)-QCA** is an interesting molecule for research due to its potential therapeutic applications, particularly in the fields of:

* **Anti-cancer Research:**
* Studies have shown that (4-MeOBz)-QCA exhibits significant anticancer activity against various cancer cell lines, including leukemia, breast cancer, and colon cancer.
* The compound's mechanism of action may involve inhibiting the growth and proliferation of cancer cells.
* Researchers are investigating (4-MeOBz)-QCA as a potential new drug candidate for cancer treatment.

* **Anti-inflammatory Research:**
* (4-MeOBz)-QCA has demonstrated anti-inflammatory properties, potentially by suppressing the production of inflammatory mediators.
* Its anti-inflammatory potential is being explored for the treatment of various inflammatory conditions, such as rheumatoid arthritis.

* **Anti-microbial Research:**
* The compound has also shown antibacterial activity against certain bacterial strains.
* Researchers are investigating its potential for developing new antibiotics.

* **Other Therapeutic Potential:**
* Studies have suggested that (4-MeOBz)-QCA may have other therapeutic benefits, such as anti-diabetic and anti-obesity effects.

**Research Focus:**

Current research on (4-MeOBz)-QCA focuses on:

* Elucidating its precise mechanism of action.
* Optimizing its pharmacological properties, such as bioavailability and potency.
* Exploring its therapeutic potential in clinical trials.
* Developing safe and effective drug delivery systems.

**Overall, (4-MeOBz)-QCA is a promising compound with significant potential for various therapeutic applications. Its anti-cancer, anti-inflammatory, and anti-microbial activities make it a valuable target for further research and drug development.**

1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid: has been shown to exhibit unprecedented positive allosteric activity for ACh binding as well as inherent agonist activity at the M1 muscarinic receptor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	1476756
CHEMBL ID	608112
SCHEMBL ID	1549479
MeSH ID	M0587378

Synonym
HMS2641J10
1-(4-methoxybenzyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
MLS000755157
smr000338032
OPREA1_185678
CHEMBL608112 ,
AKOS005090242
bdbm50313638
1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
1-[(4-methoxyphenyl)methyl]-4-oxoquinoline-3-carboxylic acid
338747-41-4
bqca ,
S5931
BZBBTGCKPRSPGF-UHFFFAOYSA-N ,
1-(4-methoxy-benzyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid
4M-309S
SCHEMBL1549479
mfcd01315710
DTXSID20363104
HY-101858
CS-6880
bqca, >=98% (hplc)
J-019354
FT-0730708
BCP20645
1,4-dihydro-1-[(4-methoxyphenyl)methyl]-4-oxo-3-quinolinecarboxylic acid
HMS3886P07
EX-A4230
A875168

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
TDP1 protein	Homo sapiens (human)	Potency	26.1011	0.0008	11.3822	44.6684	AID686978; AID686979
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cholinesterase	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0000	1.5599	10.0000	AID1384004
Aldo-keto reductase family 1 member B1	Rattus norvegicus (Norway rat)	IC50 (µMol)	12.0310	0.0004	1.8773	10.0000	AID1659473
Acetylcholinesterase	Homo sapiens (human)	IC50 (µMol)	1,000.0000	0.0000	0.9332	10.0000	AID1384003
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	EC50 (µMol)	1.4218	0.0016	1.3043	10.0000	AID1154128; AID1199331; AID1390852; AID1496167; AID463611; AID675654; AID755901
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	Kd	54.9541	0.0009	0.9829	2.6915	AID1199333
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	Activity	0.6600	0.0012	0.4953	0.6600	AID1075683; AID458267; AID474925
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	IP	0.7235	0.6600	0.7235	0.8450	AID1171997; AID1224322; AID1384930; AID452752; AID453937; AID475746; AID579779; AID712838
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	Kb	26.5000	0.0004	0.0052	0.0100	AID1154127; AID1273856
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	Cholinesterase	Homo sapiens (human)
learning	Cholinesterase	Homo sapiens (human)
negative regulation of cell population proliferation	Cholinesterase	Homo sapiens (human)
neuroblast differentiation	Cholinesterase	Homo sapiens (human)
peptide hormone processing	Cholinesterase	Homo sapiens (human)
response to alkaloid	Cholinesterase	Homo sapiens (human)
cocaine metabolic process	Cholinesterase	Homo sapiens (human)
negative regulation of synaptic transmission	Cholinesterase	Homo sapiens (human)
response to glucocorticoid	Cholinesterase	Homo sapiens (human)
response to folic acid	Cholinesterase	Homo sapiens (human)
choline metabolic process	Cholinesterase	Homo sapiens (human)
acetylcholine catabolic process	Cholinesterase	Homo sapiens (human)
positive regulation of monoatomic ion transport	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
signal transduction	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
neuromuscular synaptic transmission	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
nervous system development	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
regulation of locomotion	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
saliva secretion	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
cognition	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
regulation of postsynaptic membrane potential	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
regulation of glial cell proliferation	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
positive regulation of intracellular protein transport	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmission	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
chemical synaptic transmission	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
acetylcholine catabolic process in synaptic cleft	Acetylcholinesterase	Homo sapiens (human)
regulation of receptor recycling	Acetylcholinesterase	Homo sapiens (human)
osteoblast development	Acetylcholinesterase	Homo sapiens (human)
acetylcholine catabolic process	Acetylcholinesterase	Homo sapiens (human)
cell adhesion	Acetylcholinesterase	Homo sapiens (human)
nervous system development	Acetylcholinesterase	Homo sapiens (human)
synapse assembly	Acetylcholinesterase	Homo sapiens (human)
receptor internalization	Acetylcholinesterase	Homo sapiens (human)
negative regulation of synaptic transmission, cholinergic	Acetylcholinesterase	Homo sapiens (human)
amyloid precursor protein metabolic process	Acetylcholinesterase	Homo sapiens (human)
positive regulation of protein secretion	Acetylcholinesterase	Homo sapiens (human)
retina development in camera-type eye	Acetylcholinesterase	Homo sapiens (human)
acetylcholine receptor signaling pathway	Acetylcholinesterase	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Acetylcholinesterase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
amyloid-beta binding	Cholinesterase	Homo sapiens (human)
catalytic activity	Cholinesterase	Homo sapiens (human)
acetylcholinesterase activity	Cholinesterase	Homo sapiens (human)
cholinesterase activity	Cholinesterase	Homo sapiens (human)
protein binding	Cholinesterase	Homo sapiens (human)
hydrolase activity, acting on ester bonds	Cholinesterase	Homo sapiens (human)
enzyme binding	Cholinesterase	Homo sapiens (human)
choline binding	Cholinesterase	Homo sapiens (human)
identical protein binding	Cholinesterase	Homo sapiens (human)
phosphatidylinositol phospholipase C activity	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
protein binding	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
amyloid-beta binding	Acetylcholinesterase	Homo sapiens (human)
acetylcholinesterase activity	Acetylcholinesterase	Homo sapiens (human)
cholinesterase activity	Acetylcholinesterase	Homo sapiens (human)
protein binding	Acetylcholinesterase	Homo sapiens (human)
collagen binding	Acetylcholinesterase	Homo sapiens (human)
hydrolase activity	Acetylcholinesterase	Homo sapiens (human)
serine hydrolase activity	Acetylcholinesterase	Homo sapiens (human)
acetylcholine binding	Acetylcholinesterase	Homo sapiens (human)
protein homodimerization activity	Acetylcholinesterase	Homo sapiens (human)
laminin binding	Acetylcholinesterase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular region	Cholinesterase	Homo sapiens (human)
nuclear envelope lumen	Cholinesterase	Homo sapiens (human)
endoplasmic reticulum lumen	Cholinesterase	Homo sapiens (human)
blood microparticle	Cholinesterase	Homo sapiens (human)
plasma membrane	Cholinesterase	Homo sapiens (human)
extracellular space	Cholinesterase	Homo sapiens (human)
plasma membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
presynaptic membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
axon terminus	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
postsynaptic density membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
glutamatergic synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
cholinergic synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
synapse	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
dendrite	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
plasma membrane	Muscarinic acetylcholine receptor M1	Homo sapiens (human)
extracellular region	Acetylcholinesterase	Homo sapiens (human)
basement membrane	Acetylcholinesterase	Homo sapiens (human)
extracellular space	Acetylcholinesterase	Homo sapiens (human)
nucleus	Acetylcholinesterase	Homo sapiens (human)
Golgi apparatus	Acetylcholinesterase	Homo sapiens (human)
plasma membrane	Acetylcholinesterase	Homo sapiens (human)
cell surface	Acetylcholinesterase	Homo sapiens (human)
membrane	Acetylcholinesterase	Homo sapiens (human)
neuromuscular junction	Acetylcholinesterase	Homo sapiens (human)
synaptic cleft	Acetylcholinesterase	Homo sapiens (human)
synapse	Acetylcholinesterase	Homo sapiens (human)
perinuclear region of cytoplasm	Acetylcholinesterase	Homo sapiens (human)
side of membrane	Acetylcholinesterase	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (83)

Assay ID	Title	Year	Journal	Article
AID1513631	Selectivity ratio of compound effect for positive allosteric modulation of human M1 AchR expressed in CHO cells to compound effect for positive allosteric modulation of human M2 AchR expressed in CHO cells	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID1513632	Selectivity ratio of compound effect for positive allosteric modulation of human M1 AchR expressed in CHO cells to compound effect for positive allosteric modulation of human M3 AchR expressed in CHO cells	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID463621	Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization at 100 uM after 1 hr by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6	Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.
AID1199333	Displacement of [3H]NMS from human muscarinic M1 acetylcholine receptor expressed in CHO cell membranes by radioligand binding assay	2015	Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2	Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
AID755903	Displacement of [3H]-NMS from human muscarinic M1 acetylcholine receptor expressed CHO cells after 4 hrs by scintillation counting	2013	Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12	Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.
AID1273859	Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO Flp-In cells up to 10 uM after 1 hr by microbeta liquid scintillation counting-based radioligand binding assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID1273858	Allosteric agonist activity at human muscarinic M1 receptor expressed in CHO Flp-In cells assessed as intrinsic activity measured as IP1 accumulation after 1 hr by HTRF method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID453945	Half life in dog	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID1659477	Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM relative to control	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID1390852	Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO-NFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 4 mins followed by acetylcholine addition measured after 4 min	2018	Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7	Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M
AID474925	Agonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inflection point for increase of EC20 of acetylcholine-induced calcium mobilization by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.
AID1273862	Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO Flp-In cells up to 10 uM after 1 hr by microbeta liquid scintillation counting-based radioligand binding assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID1513634	Selectivity ratio of compound effect for positive allosteric modulation of human M1 AchR expressed in CHO cells to compound effect for positive allosteric modulation of human M5 AchR expressed in CHO cells	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID458276	Plasma concentration in ip dosed mouse after 24 hrs	2010	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4	N-heterocyclic derived M1 positive allosteric modulators.
AID453943	Clearance in dog	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID1154135	Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 30 mins prior to [3H]NMS addition measured 4 hrs after compound washout by whole cell radioligand displacement analysis relative to vehicle-t	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID453938	Plasma protein binding in human serum by equilibrium dialysis method	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID463612	Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay relative to acetylcholine	2010	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6	Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.
AID1224322	Positive allosteric modulation of human mAChR1 expressed in CHONFAT cells assessed as potention of acetylcholine-induced effect incubated for 4 mins prior to acetylcholine addition measured after 4 mins by FLIPR assay	2014	ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5	Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators.
AID453937	Allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced calcium mobilization by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID1384007	Positive allosteric modulation of human M1 mAChR expressed in CHO cells assessed as increase in oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1384004	Inhibition of human plasmatic BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1513630	Positive allosteric modulation of human M1 AchR expressed in CHO cells harboring NFAT assessed as increase in acteylcholine-induced calcium mobilization at 100 uM by Fluo-4-AM dye based FLIPR assay relative to control	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID1659474	Inhibition of AKR1A1 in rat kidney at 10 uM relative to control	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID1273860	Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO Flp-In cells up to 10 uM after 1 hr by microbeta liquid scintillation counting-based radioligand binding assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID675654	Positive allosteric modulation activity at muscarinic M1 receptor	2012	Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4	Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
AID475741	Plasma protein binding in rat serum by equilibrium dialysis method	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.
AID1273857	Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO Flp-In cells assessed as functional cooperativity with acetylcholine measured as IP1 accumulation after 1 hr by HTRF method	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID1513633	Selectivity ratio of compound effect for positive allosteric modulation of human M1 AchR expressed in CHO cells to compound effect for positive allosteric modulation of human M4 AchR expressed in CHO cells	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID1154128	Activation of human M1 mAChR expressed in FlpIn-CHO cells assessed as FBS-induced ERK1/2 phosphorylation incubated for 5 mins by Alphascreen assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1384006	Antagonist activity at human M1 mAChR expressed in CHO cells assessed as inhibition of oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1273856	Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO Flp-In cells after 1 hr by microbeta liquid scintillation counting-based radioligand binding assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID1154127	Displacement of [3H]NMS from human M1 mAChR expressed in FlpIn-CHO cells after 4 hrs by microplate counting analysis	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1390854	Allosteric agonist at human muscarinic acetylcholine receptor M1 expressed in CHO-NFAT cells assessed as induction of calcium mobilization after 4 mins by Fluo-4AM-based FLIPR assay	2018	Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7	Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M
AID453941	Half life in rat	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID1075683	Positive allosteric modulation of human muscarinic M1 receptor expressed CHO cells assessed as intrinsic potency of acetylcholine-induced calcium mobilization by FLIPR assay	2014	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5	Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.
AID1199344	Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation at 10 uM incubated for 30 mins by FRET based HTRF assay	2015	Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2	Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
AID1384003	Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1513636	Protein binding in rat plasma	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID1659475	Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM relative to control	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID579779	Positive allosteric modulation at human muscarinic M1 receptor expressing CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization by FLIPR assay	2011	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6	Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series.
AID1171997	Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay	2015	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2	Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.
AID453944	Oral bioavailability in dog	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID1384005	Selectivity ratio of IC50 for human plasmatic BuChE to IC50 for human erythrocyte AChE	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1659476	Antioxidant activity assessed as DPPH radical scavenging activity at 50 uM relative to control	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID1154134	Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cell membrane assessed as receptor alkylation incubated for 30 mins prior to [3H]NMS addition measured after 4 hrs by radioligand displacement analysis (Rvb = 100%)	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1199331	Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay	2015	Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2	Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
AID607310	Antiamnesic activity against scopolamine-induced dementia in ip dosed B6SJL mouse assessed as increase in freezing behavior at 33 uM plasma concentration	2011	Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13	Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold.
AID755901	Allosteric modulation of human muscarinic M1 acetylcholine receptor expressed CHO cells assessed as intracellular calcium mobilization after 1 hr by Fluo-4-AM based fluorescence assay	2013	Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12	Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.
AID453940	Clearance in rat	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID1659473	Inhibition of AKR1B1 in rat lenses	2020	Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9	Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.
AID668740	Inhibition of scopolamine-induced memory deficit in ip dosed contextual fear conditioning memory model of mouse by measuring freezing behavior at 33 uM of plasma concentration after 24 hrs by novel object recognition test relative to control	2010	ACS medicinal chemistry letters, Sep-09, Volume: 1, Issue:6	Quinolizidinone carboxylic acids as CNS penetrant, selective m1 allosteric muscarinic receptor modulators.
AID453942	Oral bioavailability in rat	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID453939	Plasma protein binding in rat serum by equilibrium dialysis method	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
AID463611	Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6	Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.
AID1496167	Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO-NFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization after 4 hrs by CCF4-AM dye-based assay	2018	Bioorganic & medicinal chemistry letters, 07-01, Volume: 28, Issue:12	The discovery of VU0486846: steep SAR from a series of M
AID1384011	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease.
AID1474760	Displacement of [3H]NMS from recombinant human mAChR1 expressed in Flp-In-CHO cells after 1 hr by microbeta scintillation counting analysis	2017	Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11	Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID458267	Allosteric modulator activity at human muscarinic M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4	N-heterocyclic derived M1 positive allosteric modulators.
AID712838	Positive allosteric modulation of human muscarinic M1 receptor expressing in CHONFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 4 mins and measured 4 mins after acetylcholine stimulation by FLIPR assay	2012	ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12	Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.
AID595200	Ratio of AUC in brain to plasma in Sprague-Dawley rat	2011	Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9	Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.
AID452752	Allosteric modulation of human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced calcium mobilization by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2	Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding.
AID1390848	Displacement of [3H]-NMS from human muscarinic acetylcholine receptor M1 expressed in flpIn-CHO cell membranes after 5 hrs by liquid scintillation counting	2018	Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7	Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M
AID475746	Positive allosteric modulator activity at human muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization by FLIPR assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.
AID1199342	Agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation at 1 uM incubated for 30 mins by FRET based HTRF assay	2015	Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2	Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
AID1384930	Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 4 mins followed by acetylcholine addition and measured after 4 mins by Fl	2018	ACS medicinal chemistry letters, Jul-12, Volume: 9, Issue:7	MK-7622: A First-in-Class M
AID1154133	Irreversible binding to human M1 mAChR expressed in FlpIn-CHO cells assessed as receptor alkylation incubated for 30 mins prior to [3H]NMS addition measured after 4 hrs by whole cell radioligand displacement analysis relative to vehicle-treated control	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.
AID1273861	Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO Flp-In cells up to 10 uM after 1 hr by microbeta liquid scintillation counting-based radioligand binding assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.
AID1199332	Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay relative to 100 uM acetylcholine	2015	Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2	Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.
AID1513635	Protein binding in human plasma	2019	Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1	Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810	Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812	Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	1 (2.50)	29.6817
2010's	37 (92.50)	24.3611
2020's	2 (5.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (5.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	38 (95.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
tacrine Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.	2.17	1	acridines; aromatic amine	EC 3.1.1.7 (acetylcholinesterase) inhibitor
atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.	2.17	1	ethanolamines; monocarboxylic acid amide; propanolamine	anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic
chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.	2.17	1	organochlorine compound; phenothiazines; tertiary amine	anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug
desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.	2.17	1	dibenzoazepine; secondary amino compound	adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor
donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.	3.47	2	aromatic ether; indanones; piperidines; racemate	EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent
imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.	2.17	1	dibenzoazepine	adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.	2.21	1	aromatic amine
pirenzepine Pirenzepine: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.	2.13	1	pyridobenzodiazepine	anti-ulcer drug; antispasmodic drug; muscarinic antagonist
promazine Promazine: A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.. promazine : A phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.	2.17	1	phenothiazines; tertiary amine	antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; muscarinic antagonist; phenothiazine antipsychotic drug; serotonergic antagonist
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.21	1	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.	2.11	1	pilocarpine	antiglaucoma drug
galantamine Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils.	2.21	1	benzazepine alkaloid fundamental parent; benzazepine alkaloid; organic heterotetracyclic compound; tertiary amino compound	antidote to curare poisoning; cholinergic drug; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; plant metabolite
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid [no description available]	2.25	1	chromanol; monocarboxylic acid; phenols	antioxidant; ferroptosis inhibitor; neuroprotective agent; radical scavenger; Wnt signalling inhibitor
aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.	3.25	1	aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone	drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist
n-methylscopolamine N-Methylscopolamine: A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.	2.13	1
acetylcholine mustard acetylcholine mustard: structure	2.1	1
7-methoxytacrine [no description available]	2.17	1
bifeprunox bifeprunox: an antipsychotic agent	3.25	1	biphenyls
2-amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophene 2-amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophene: an allosteric adenosine modulator	2.07	1
epalrestat epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.	2.25	1	monocarboxylic acid; thiazolidines	EC 1.1.1.21 (aldehyde reductase) inhibitor
2-[[1-[(3-fluorophenyl)methyl]-3-indolyl]sulfonyl]-N-(5-methyl-3-isoxazolyl)acetamide [no description available]	2.06	1	indoles
dizocilpine maleate Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.	2.13	1	maleate salt; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
n,n'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: structure in first source	3.25	1	aryl sulfide
iperoxo iperoxo: a muscarinic M2 receptor agonist; structure in first source	2.11	1
6-chlorotacrine 6-chlorotacrine: structure given in first source	2.17	1
cariprazine cariprazine: Structure in first source. cariprazine : An N-alkylpiperazine that is N,N-dimethyl-N'-{trans-4-[2-(piperazin-1-yl)ethyl]cyclohexyl}urea substituted at position 4 on the piperazine ring by a 2,3-dichlorophenyl group. Used (as the hydrochloride salt) for treatment of schizophrenia and bipolar disorder.	3.25	1
ly2033298 [no description available]	4.19	2
1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione [no description available]	2.07	1
2-[[1-[(3-chlorophenyl)methyl]-3-indolyl]sulfonyl]-N-(5-methyl-3-isoxazolyl)acetamide [no description available]	2.06	1	indoles
piperidines Piperidines: A family of hexahydropyridines.	3.48	2
N-(5-methyl-3-isoxazolyl)-2-[[1-[[3-(trifluoromethyl)phenyl]methyl]-3-indolyl]sulfonyl]acetamide [no description available]	2.06	1	(trifluoromethyl)benzenes
2-[[1-[(3-bromophenyl)methyl]-3-indolyl]sulfonyl]-N-(5-methyl-3-isoxazolyl)acetamide [no description available]	2.06	1	indoles
ml 137 [no description available]	2.99	4
piroxicam [no description available]	2.17	1	benzothiazine; monocarboxylic acid amide; pyridines	analgesic; antirheumatic drug; cyclooxygenase 1 inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug
vu0364572 VU0364572: muscarinic agonist; structure in first source	3.04	1

Condition	Relationship Strength	Studies
Innate Inflammatory Response [description not available]	2.51	2
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2.51	2
Acute Confusional Senile Dementia [description not available]	2.84	3
Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.	2.13	1
Dementia Praecox [description not available]	2.53	2
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	2.84	3
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	2.53	2
Complications of Diabetes Mellitus [description not available]	2.25	1
Brain Contusion A bruise of the brain from an impact of the skull.	2.21	1
Endotoxemia A condition characterized by the presence of ENDOTOXINS in the blood. On lysis, the outer cell wall of gram-negative bacteria enters the systemic circulation and initiates a pathophysiologic cascade of pro-inflammatory mediators.	2.21	1
Age-Related Memory Disorders [description not available]	2.15	1
Dementias, Transmissible [description not available]	2.15	1
Memory Disorders Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.	2.15	1

1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Description

Cross-References

Synonyms (29)

Protein Targets (5)

Potency Measurements

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (43)

Molecular Functions (18)

Ceullar Components (23)

Bioassays (83)

Research

Studies (40)

Market Indicators

Research Demand Index: 11.13

Study Types

1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Description

Cross-References

Synonyms (29)

Protein Targets (5)

Potency Measurements

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (43)

Molecular Functions (18)

Ceullar Components (23)

Bioassays (83)

Research

Studies (40)

Market Indicators

Research Demand Index: 11.13

Study Types

Related Drugs (35)

Related Conditions (13)