Page last updated: 2024-11-13

a 867744

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Description

4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide: positive modulator of alpha7 nicotinic acetylcholine receptor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23642319
CHEMBL ID490153
SCHEMBL ID1459705
MeSH IDM0537466

Synonyms (29)

Synonym
HY-12149
bdbm50250187
4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1h-pyrrol-1-yl)-benzenesulfonamide
a-867744
CHEMBL490153 ,
SCHEMBL1459705
CS-0271
4-[5-(4-chlorophenyl)-2-methyl-3-propanoyl-1h-pyrrol-1-yl]benzene-1-sulfonamide
gtpl3986
a 867744
4-[5-(4-chloro-phenyl)-2-methyl-3-propionyl-pyrrol-1-yl]-benzenesulfonamide
ABACVOXFUHDKNZ-UHFFFAOYSA-N ,
o6nw23a765 ,
1000279-69-5
benzenesulfonamide, 4-(5-(4-chlorophenyl)-2-methyl-3-(1-oxopropyl)-1h-pyrrol-1-yl)-
unii-o6nw23a765
4-(5-(4-chlorophenyl)-2-methyl-3-propionylpyrrol-1-yl)benzenesulfonamide
AKOS016363413
4-[5-(4-chlorophenyl)-2-methyl-3-(1-oxopropyl)-1h-pyrrol-1-yl]benzenesulfonamide
DTXSID20142875
4-[5-(4-chlorophenyl)-2-methyl-3-propionylpyrrol-1-yl]benzenesulfonamide
AS-73954
NCGC00371047-02
benzenesulfonamide, 4-[5-(4-chlorophenyl)-2-methyl-3-(1-oxopropyl)-1h-pyrrol-1-yl]-
4-[5-(4-chlorophenyl)-2-methyl-3-propanoylpyrrol-1-yl]benzenesulfonamide
Q27074090
F83439
A921547
4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1h-pyrrol-1-yl)benzenesulfonamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.39190.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency6.74120.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency2.13170.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency6.74120.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency6.74120.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency6.74120.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency6.74120.01238.964839.8107AID1645842
[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)
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)10.00000.00011.753610.0000AID350620
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)2.00000.00002.015110.0000AID350622
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)10.00000.00002.800510.0000AID350621
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)20.00000.00091.901410.0000AID350624
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki10.00000.00211.840710.0000AID350623
[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)
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)EC50 (µMol)0.72800.12802.80188.9000AID1164738; AID1559307; AID1731320; AID350591
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (135)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein phosphorylationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
intracellular calcium ion homeostasisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
learning or memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
short-term memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of cell population proliferationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of MAPK cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of angiogenesisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapse organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
sensory processingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein metabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendritic spine organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
modulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendrite arborizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of long-term synaptic potentiationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid precursor protein catabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to amyloid-betaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid fibril formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of CoA-transferase activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (66)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
amyloid-beta bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
toxic substance bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chloride channel regulator activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein homodimerization activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (95)

Assay IDTitleYearJournalArticle
AID350596Modulator activity at alpha7 nAChR in Xenopus laevis oocytes cells assessed as decay of acetylcholine-evoked electric current response at -60 mV by two-electrode voltage clamp technique2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350609Oral bioavailability in dog at 1 umol/kg2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559192Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 3 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 16.33 sec)
AID1559292Drug level in Wistar rat brain at 3 mg/kg, po after 2 hrs by LC-MS/MS analysis
AID350611Volume of distribution at steady state in monkey at 0.5 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559219Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for novel object at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 12.81 sec)
AID1559213Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in novel object discrimination index at 0.05 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 0.21 No_unit
AID1731328Efflux ratio of apparent permeability in vinblastine-treated human Caco2 cells at 1 uM after 180 mins by HPLC or UHPLC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID1559202Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 0.15 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 15.63 se
AID350615Improvement in gating deficits in DBA/2 mouse model of sensory gating deficits assessed as reduction in ratio of response to test stimulus relative to preceding response to conditioning stimulus at 0.1 to 10 umol/kg, ip by paired auditory stimulus paradig2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350592Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of agonist-induced intracellular calcium level by FLIPR assay relative to 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559259Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 0.3
AID350617Drug level in brain of DBA/2 mouse model of sensory gating deficits at 1 umol/kg, ip2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731317Kinetic solubility of compound in in PBS buffer at pH 7.4 by HPLC analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID350612Plasma clearance in monkey at 0.5 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559191Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 3 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 13.95 sec)
AID350602Plasma clearance in rat at 2 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731354Cognitive enhancing effect in scopolamine-induced NMRI mouse model of amnesia assessed as increase in recognition index at 3 mg/kg, ip by Y maze test2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID1559203Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 0.15 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 8.
AID350598Activity at human recombinant alpha4beta2 nAChR expressed in HEK293 cells assessed as potentiation of nicotine-evoked calcium transients up to 30 uM2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559265Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 0.9 No_unit)
AID350594Modulator activity at alpha7 nAChR in Xenopus laevis oocytes cells assessed as activation of electric currents at 0.1 nM to 10 uM at -60 mV by two-electrode voltage clamp technique2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731324Intrinsic clearance in mouse liver microsome at 1 to 2.5 uM up to 40 mins2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID350597Modulator activity at alpha7 nAChR in rat neonatal cortical neurons assessed as enhancement of (R)-4-chloro-N-(quinuclidin-8-yl)benzamide-induced calcium flux response at 5 uM by FLIPR assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559244Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 16.11 sec)
AID1559228Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 10.20 sec)
AID350616Drug level in brain of DBA/2 mouse model of sensory gating deficits at 0.1 umol/kg, ip2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350618Drug level in brain of DBA/2 mouse model of sensory gating deficits at 10 umol/kg, ip2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559263Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 9.
AID350604Oral bioavailability in rat at 2 umol/kg2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350608Cmax in dog at 1 umol/kg, po2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559270Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index at 0.15 mg/kg, po for 7 days and measured on day 9 (Rvb = 1.05 No_unit)
AID350607Plasma clearance in dog at 0.5 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350624Inhibition of human ERG channel2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350623Displacement of [3H]dofetilide from human ERG channel2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559294Ratio of drug level in brain to plasma in Wistar rat at 3 mg/kg, po after 2 hrs by LC-MS/MS analysis
AID350603Cmax in rat at 2 umol/kg, po2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559199Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in novel object discrimination index at 3 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 0.03 No_unit)
AID350625Plasma concentration Sprague-Dawley rat at 3 mg/kg2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559229Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for novel object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 15.37 sec)
AID1164738Positive allosteric modulation at human alpha7 nACHR expressed in Xenopus oocyte assessed as potentiation of 200 uM ACh-induced current at holding potential of -80 mV by electrophysiology2014European journal of medicinal chemistry, Oct-30, Volume: 86Chalcones as positive allosteric modulators of α7 nicotinic acetylcholine receptors: a new target for a privileged structure.
AID350595Modulator activity at alpha7 nAChR in Xenopus laevis oocytes cells assessed as enhancement of acetylcholine-evoked electric currents at -60 mV by two-electrode voltage clamp technique2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559307Positive allosteric modulatory activity against alpha7 nAChR in human IMR-32 cells assessed as potentiation of PNU-282987-induced Ca2+ efflux at by FLIPR assay
AID1559247Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for novel object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 12.09 sec)
AID1559218Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for familiar object at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 10.6 sec)
AID350613Cmax in monkey at 1 umol/kg, po2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731320Agonist activity at recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in intra cellular calcium level after 10 mins by fluorescence relative to control2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID350599Activity at human recombinant alpha3beta4 nAChR expressed in HEK293 cells assessed as potentiation of nicotine-evoked calcium transients up to 30 uM2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350593Metabolic stability in rat liver microsomes assessed as compound remaining after 30 mins2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350601Volume of distribution at steady state in rat at 2 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559217Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object2 at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 21.07 sec)
AID1559279Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index at 0.15 mg/kg, po for 7 days measured after 24 hrs (Rvb = 0.93 No_unit)
AID1559256Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in discrimination index at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 0.21 No_unit)
AID1559224Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in novel object discrimination at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 0.08 No_unit)
AID1559267Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 0.15 mg/kg, po for 7 days and measured on day 9 (Rvb = -0.5%)
AID350620Inhibition of CYP3A42009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350619Improvement in gating deficits in DBA/2 mouse model of sensory gating deficits assessed as reduction in ratio of response to test stimulus relative to preceding response to conditioning stimulus at 0.1 umol/kg, ip by paired auditory stimulus paradigm assa2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559246Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 8.59 sec)
AID1731326Apparent permeability across apical to basolateral side in vinblastine-treated human Caco2 cells at 1 uM after 180 mins by HPLC or UHPLC-MS/MS analysis2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID350610Half life in monkey at 0.5 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559204Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in exploration time for novel object in retention trial at 0.15 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test
AID1559261Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 1 No_unit)
AID350626Plasma concentration Sprague-Dawley rat at 10 mg/kg2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559226Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 13.73 sec)
AID350591Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of agonist-induced intracellular calcium level by FLIPR assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350614Oral bioavailability in monkey at 1 umol/kg2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731325Intrinsic clearance in rat liver microsome at 1 to 2.5 uM up to 40 mins2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID1731318Agonist activity at recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in intra cellular calcium level at 10 uM after 10 mins by fluorescence relative to control2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID350844Plasma concentration Sprague-Dawley rat at 30 mg/kg2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559216Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object1 at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 19.09 sec)
AID350600Half life in rat at 2 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731337Lipophilicity, logP of compound2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID1559276Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 0.15 mg/kg, po for 7 days measured after 24 hrs (Rvb =6.59%)
AID350605Half life in dog at 0.5 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350622Inhibition of CYP2D62009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559238Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in discrimination index at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 0.12 No_unit)
AID1731321Positive allosteric modulation of recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in choline-induced inward current at 10 uM after 6 to 10 mins by whole-cell patch clamp method2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID350621Inhibition of CYP2C92009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID350606Volume of distribution at steady state in dog at 0.5 umol/kg, iv2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1559193Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 3 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 13.05
AID1559201Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 0.15 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 16.11 se
AID350590Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of intracellular calcium level up to 100 uM by FLIPR assay2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
AID1731323Intrinsic clearance in human liver microsome at 1 to 2.5 uM up to 40 mins2021European journal of medicinal chemistry, Mar-15, Volume: 214Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach.
AID1559293Drug concentration in Wistar rat plasma at 3 mg/kg, po after 2 hrs by LC-MS/MS analysis
AID1559227Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 11.76 sec)
AID1559194Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in exploration time for novel object in retention trial at 3 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb
AID1559245Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 15.63 sec)
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.
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.
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.
AID1346547Human nicotinic acetylcholine receptor alpha4 subunit (Nicotinic acetylcholine receptors)2009The Journal of pharmacology and experimental therapeutics, Jul, Volume: 330, Issue:1
In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
AID1346583Human nicotinic acetylcholine receptor alpha7 subunit (Nicotinic acetylcholine receptors)2009The Journal of pharmacology and experimental therapeutics, Jul, Volume: 330, Issue:1
In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
AID1346570Human nicotinic acetylcholine receptor alpha3 subunit (Nicotinic acetylcholine receptors)2009The Journal of pharmacology and experimental therapeutics, Jul, Volume: 330, Issue:1
In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (25.00)29.6817
2010's5 (41.67)24.3611
2020's4 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.01

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.01 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.01)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]