Page last updated: 2024-11-13

kys 05090

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID23661603
CHEMBL ID394956
CHEMBL ID1269457
SCHEMBL ID10019253
MeSH IDM0546220

Synonyms (8)

Synonym
kys-05090
CHEMBL394956 ,
n-benzyl-2-{3-biphenyl-4-yl-2-[(5-dimethylamino-pentyl)-methyl-amino]-3,4-dihydro-quinazolin-4-yl}-acetamide
n-benzyl-2-(3-(biphenyl-4-yl)-2-((5-(dimethylamino)pentyl)(methyl)amino)-3,4-dihydroquinazolin-4-yl)acetamide
bdbm50222222
chembl1269457
SCHEMBL10019253
n-benzyl-2-[2-[5-(dimethylamino)pentyl-methylamino]-3-(4-phenylphenyl)-4h-quinazolin-4-yl]acetamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Moreover, compound 1ยท2HCl has an oral bioavailability of 98% with LD(50) values of 693 mg/kg (p."( Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
Chang, SK; Choo, DJ; Jung, SY; Kang, HB; Kim, J; Kim, YD; Lee, JY; Lee, KT; Lee, SH; Oh, CR; Park, HA; Seo, JH, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)IC50 (µMol)0.12870.03700.89152.5000AID1058669; AID1662453; AID301834; AID340327; AID452446
Voltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)IC50 (µMol)3.60000.03201.04793.6000AID1662454
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.04100.00031.38338.4000AID301834
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
sinoatrial node developmentVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
response to nickel cationVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
regulation of membrane potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
calcium ion importVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
SA node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
AV node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
SA node cell to atrial cardiac muscle cell signalingVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
AV node cell to bundle of His cell signalingVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
muscle contractionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
muscle organ developmentVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
myoblast fusionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
regulation of heart contractionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
aldosterone biosynthetic processVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cellular response to hormone stimulusVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cortisol biosynthetic processVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cellular response to potassium ionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
regulation of membrane potentialVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
calcium ion importVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
inorganic cation transmembrane transportVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
positive regulation of acrosome reactionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
low voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
scaffold protein bindingVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated monoatomic ion channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
protein bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
low voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
metal ion bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
scaffold protein bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
cytoplasmVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
synapseVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
AID301835Selectivity for alpha-1B N-type calcium channel over alpha1G T-type calcium channel expressed in HEK293 cells2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Discovery of potent T-type calcium channel blocker.
AID301834Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current by patch-clamp assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Discovery of potent T-type calcium channel blocker.
AID1058667Cytotoxicity against human A2780 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID340030Growth inhibition of human HT29 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID1662450Inhibition of human Cav3.3 expressed in tsA-201 cells at 10uM by patch clamp electrophysiology2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID1058652Ratio of IC50 for mibefradil to compound IC50 for human paclitaxel-resistant A2780T cells2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID1058662Cell cycle arrest in human A2780 cells assessed as accumulation at S phase at 6 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID1058658Cell cycle arrest in human A2780 cells assessed as accumulation at sub-G1 phase at 2 to 4 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID340028Growth inhibition of human A549 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID1662448Inhibition of human Cav3.1 expressed in tsA-201 cells at 10uM by patch clamp electrophysiology2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID527106Cytotoxicity against human MDA-MB-231 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID1058661Cell cycle arrest in human A2780 cells assessed as accumulation at sub-G1 phase at 8 uM after 24 hrs by FACS analysis (Rvb = 3.1%)2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID340029Growth inhibition of human DU145 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID340031Growth inhibition of human SK-MEL-2 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID527103Cytotoxicity against human LNCAP cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID527104Cytotoxicity against human SKOV3 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID527102Cytotoxicity against human HeLa cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID340032Growth inhibition of human SKOV3 cells after 72 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID301831Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current at 10 uM by high throughput screening2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Discovery of potent T-type calcium channel blocker.
AID452446Inhibition of human T-type calcium channel alpha1G in HEK293 cells2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
3D QSAR studies on 3,4-dihydroquinazolines as T-type calcium channel blocker by comparative molecular similarity indices analysis (CoMSIA).
AID1058659Cell cycle arrest in human paclitaxel-resistant A2780T cells assessed as accumulation at sub-G1 phase at 2 to 4 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID301833Selectivity for Alpha-1B N-type calcium channel over alpha-1G T-type calcium channel expressed in HEK293 cells at 10 uM2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Discovery of potent T-type calcium channel blocker.
AID1058670Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current at 1 uM by whole cell patch-clamp method relative to control2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID1058657Cell cycle arrest in human paclitaxel-resistant A2780T cells assessed as accumulation at sub-G1 phase at 8 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID340033Acute toxicity in ICR CD1 mouse assessed as mortality at 1000 mg/kg, po after 5 days2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID1058664Cell cycle arrest in human A2780 cells assessed as accumulation at G0/G1 phase at 6 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID1662454Inhibition of human Cav3.2 expressed in tsA-201 cells by patch clamp electrophysiology2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID1058669Inhibition of t-type Cav3.1 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of 50 ms depolarizing voltage step-induced current by whole cell patch-clamp method2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID527107Cytotoxicity against human SKBR3 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID527105Cytotoxicity against human A172 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID1662453Inhibition of human Cav3.1 expressed in tsA-201 cells by patch clamp electrophysiology2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID301832Inhibition of N-type calcium channel Cav3.1 alpha-1B subunit expressed in HEK293 cells assessed as calcium current at 10 uM by patch-clamp assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Discovery of potent T-type calcium channel blocker.
AID340327Inhibition of T-type calcium channel Cav3.1 alpha1G expressed in HEK293 cells by whole cell patch-clamp method2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
AID1058668Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID527101Cytotoxicity against human A549 cells by MTT assay2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
AID1662449Inhibition of human Cav3.2 expressed in tsA-201 cells at 10uM by patch clamp electrophysiology2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID1058663Cell cycle arrest in human A2780 cells assessed as accumulation at sub-G1 phase at 6 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID1662451Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID1662452Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID1058660Cell cycle arrest in human A2780 cells assessed as accumulation at G2/M phase at 6 uM after 24 hrs by FACS analysis2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
AID1662455Inhibition of human Cav3.3 expressed in tsA-201 cells by patch clamp electrophysiology2020Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.
AID301830Inhibition of T-type calcium channel Cav3.1 alpha-1G subunit expressed in HEK293 cells assessed as calcium current at 10 uM by patch-clamp assay2007Bioorganic & medicinal chemistry letters, Nov-01, Volume: 17, Issue:21
Discovery of potent T-type calcium channel blocker.
AID1058666Cytotoxicity against human paclitaxel-resistant A2780T cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
In vitro cytotoxicity on human ovarian cancer cells by T-type calcium channel blockers.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (33.33)29.6817
2010's3 (50.00)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.43

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 Index12.43 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.43)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]