Compounds > dpc 963
Page last updated: 2024-11-08

dpc 963

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

Description

DPC 963: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID474121
CHEMBL ID62039
SCHEMBL ID4576238
MeSH IDM0372712

Synonyms (17)

Synonym
214287-90-8
dpc 963
2(1h)-quinazolinone, 4-(cyclopropylethynyl)-5,6-difluoro-3,4-dihydro-4-(trifluoromethyl)-, (4s)-
(4s)-4-cyclopropylethynyl-5,6-difluoro-4-trifluoromethyl-3,4-dihydro-1h-quinazolin-2-one
(4s)-4-(2-cyclopropylethynyl)-5,6-difluoro-4-(trifluoromethyl)-1,3-dihydroquinazolin-2-one
dmp-963
dpc-963
CHEMBL62039
(4s)-4-(cyclopropylethynyl)-5,6-difluoro-4-(trifluoromethyl)-3,4-dihydroquinazolin-2(1h)-one
xew2aag1is ,
unii-xew2aag1is
SCHEMBL4576238
DTXSID80175700
AKOS030532151
qcnjqjjfxfjvcx-zdusscgksa-n
(s)-5,6-difluoro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-3,4-dihydro-2(1h)-quinazolinone
(s)-4-(cyclopropylethynyl)-5,6-difluoro-4-(trifluoromethyl)-3,4-dihydroquinazolin-2(1h)-one

Research Excerpts

Overview

DPC 963 is a non-nucleoside reverse transcriptase inhibitor with low aqueous solubility.

ExcerptReferenceRelevance
"DPC 963 is a non-nucleoside reverse transcriptase inhibitor with low aqueous solubility. "( Effect of drug substance particle size on the characteristics of granulation manufactured in a high-shear mixer.
Badawy, SI; Lee, TJ; Menning, MM, 2000)		1.75

Dosage Studied

ExcerptRelevanceReference
" The stability of the DPC 961 and 963 in the dosing formulation was followed over a 24-h period using a stability indicating HPLC method."( In-use testing of extemporaneously prepared suspensions of second generation non-nucleoside reversed transcriptase inhibitors in support of phase I clinical studies.
Aubry, AF; Gray, V; Hobson, T; Rabel, S; Sebastian, D; Xie, M; Xu, JQ, 2000)		0.31
" Electrospray ionization-liquid chromatography/mass spectrometry analyses of urine from subjects dosed with DPC 963 also revealed the presence of other minor metabolites including glucuronide conjugate of 6-OH DPC 963 (M7)."( Metabolism of (S)-5,6-difluoro-4-cyclopropylethynyl-4-trifluoromethyl-3, 4-dihydro-2(1H)-quinazolinone, a non-nucleoside reverse transcriptase inhibitor, in human liver microsomes. Metabolic activation and enzyme kinetics.
Chen, H; Chen, W; Gan, LS; Mutlib, AE, 2003)		0.53
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.07400.00011.076810.0000AID197782
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC90 (µMol)0.01800.00170.03850.3100AID198574
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID96289Calculated Potency against Mutant HIV-1 sL100I2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID198574Compound was evaluated for the inhibition of HIV-1 Reverse transcriptase2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID106729Protein Binding was evaluated by PB shift in MT-2 by RNA assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID93784percentage of the free compound in human serum2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID96291Plasma Potency against Mutant HIV-1 sL100I2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID106726Antiviral activity against HIV-2 in MT-2 cells by yield assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID141357Potency against Mutant HIV-1 sV179D/L100I/Y181C2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID96290In vitro antiviral activity against HIV-1 (L100I).2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID94442Potency against Mutant HIV-1 K103N2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID94312Calculated Potency against Mutant HIV-1 K103N2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID197782Inhibition of HIV-1 reverse transcriptase.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID222294Effect of human plasma protein binding on antiviral efficacy.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID152945Antiviral activity against A018C, Zidovudine resistant clinical strain of HIV in PBMC by P24 assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID152946Antiviral activity against Thai 9466, a wild-type clinical strain of HIV in PBMC by P24 assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID229259Antiviral activity was evaluated for the inhibition of wild-type RF strain of HIV-1 in an in vitro enzyme assay.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID93785percentage of the free compound in tissue culture medium2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID106728Antiviral activity against RF strain of HIV in MT-2 cells by yield assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID106727Antiviral activity against RF strain of HIV in MT-2 cells by RNA assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID94314Antiviral activity against HIV-1 K103N mutant virus.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID166687Plasma antiviral activity was evaluated for RF strain of HIV-12000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID141355Calculated Potency against Mutant HIV-1 sV179D/L100I/Y181C2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID94441Plasma Potency against Mutant HIV-1 K103N2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID106725Antiviral activity against E, Zidovudine resistant clinical strain of HIV in MT-2 cells by yield assay2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID166685Compound was evaluated for the inhibition of wide-type RF strain of HIV-12000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID94313Antiviral activity toward K103N mutant HIV-1 virus as protein binding adjusted (PB adj).2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID141356Plasma Potency against Mutant HIV-1 sV179D/L100I/Y181C2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID96292Potency against Mutant HIV-1 sL100I2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (100.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.23

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 Index12.23 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.23)

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%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		210cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
delavirdine
Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		210aminopyridine;
indolecarboxamide;
N-acylpiperazine;
sulfonamide		antiviral drug;
HIV-1 reverse transcriptase inhibitor
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		3.2660monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		210azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		210acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
oxirene
oxirene: structure		7.0110mancude organic heteromonocyclic parent;
monocyclic heteroarene;
oxacycle
dpc 961
[no description available]		2.4120
dpc 083
[no description available]		210
ConditionIndicatedRelationship StrengthStudiesTrials
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		02.0110