Compounds > protac-3
Page last updated: 2024-08-04 02:10:34

protac-3

Description

Cross-References

ID SourceID
PubMed CID135156947
CHEMBL ID4587573
SCHEMBL ID20305518
MeSH IDM0468599

Synonyms (18)

Synonym
SCHEMBL20305518
(2s,4r)-1-[(2s)-2-[3-[2-[5-[4-(3-chloro-4-fluoroanilino)-7-methoxyquinazolin-6-yl]oxypentoxy]ethoxy]propanoylamino]-3,3-dimethylbutanoyl]-4-hydroxy-n-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
ntn21277
(2s,4r)-1-((s)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-n-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
EX-A3010
gefitinib-based protac 3
2230821-27-7
CS-0087480
D80333
HY-123921
protac 3
gtpl10636
S0070
AKOS037653377
CHEMBL4587573
AC-36293
GLXC-25268
BP-28379

Protein Targets (2)

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Epidermal growth factor receptorHomo sapiens (human)DC500.0139AID1704977; AID1880578; AID1881819; AID1881821; AID1904302
von Hippel-Lindau disease tumor suppressorHomo sapiens (human)DC500.0139AID1704977; AID1880578; AID1881819; AID1881821; AID1904302

Bioassays (18)

Assay IDTitleYearJournalArticle
AID1881820Protac activity against VHL/EGFR deletion 19 mutant in human HCC827 cells relative to control2022European journal of medicinal chemistry, Jan-05, Volume: 227ISSN: 1768-3254VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.
AID1881821Protac activity against VHL/EGFR L858R mutant in human HCC827 cells2022European journal of medicinal chemistry, Jan-05, Volume: 227ISSN: 1768-3254VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.
AID1704977Protac activity at VHL/EGFR del19 mutant in human HCC827 cells assessed as induction of EGFR degradation measured after 24 hrs by Western blot analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208ISSN: 1768-3254Discovery of potent small molecule PROTACs targeting mutant EGFR.
AID1582400Protac activity at VHL/EGFR exon 19 deletion mutant in human HCC827 cells assessed as induction of EGFR degradation at 1 to 10 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1582388Protac activity at VHL/EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in EGFR autophosphorylation up to 10 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1880577PROTAC activity at VHL/wild type EGFR in human OVCAR-8 cells assessed as EGFR degradation measured after 24 hrs by Immunoblotting analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
ISSN: 1520-4804		Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.
AID1881819Protac activity against VHL/EGFR deletion 19 mutant in human HCC827 cells2022European journal of medicinal chemistry, Jan-05, Volume: 227ISSN: 1768-3254VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.
AID1582399Protac activity at VHL/EGFR L858R mutant in human H3255 cells assessed as induction of EGFR degradation up to 500 nM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1582398Protac activity at VHL/EGFR exon 19 deletion mutant in human HCC827 cells assessed as induction of EGFR degradation up to 500 nM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1880578PROTAC activity at VHL/EGFR Del19 mutant in human HCC827 cells assessed as EGFR degradation measured after 24 hrs by Immunoblotting analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
ISSN: 1520-4804		Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.
AID1881822Protac activity against VHL/EGFR L858R mutant in human HCC827 cells relative to control2022European journal of medicinal chemistry, Jan-05, Volume: 227ISSN: 1768-3254VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.
AID1582389Protac activity at VHL/EGFR L858R mutant in human H3255 cells assessed as reduction in EGFR autophosphorylation up to 10 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1582441Antiproliferative activity against human H3255 cells measured after 3 days by CCK8 assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1850524Thermodynamic solubility of the compound in phosphate buffer at pH 7 incubated for 1 hr by shake flask based HPLC-UV analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
ISSN: 1520-4804
AID1582390Protac activity at VHL/EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in AKT phosphorylation up to 10 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1582401Protac activity at VHL/EGFR L858R mutant in human H3255 cells assessed as induction of EGFR degradation at 1 to 10 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1582391Protac activity at VHL/EGFR L858R mutant in human H3255 cells assessed as reduction in AKT phosphorylation up to 10 uM treated 8 hrs post serum starvation measured after 16 hrs by Western blot analysis2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
ISSN: 1520-4804		Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
AID1904302Protac activity at VHL/EGFR deletion19 mutant in human HCC827 cells assessed as induction of EGFR degradation2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
ISSN: 1520-4804		Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's6 (100.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
gefitinib
2
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist		202020223.0high000011
gw 3965
1
diarylmethane202220222.0medium000001
mdv 3100
1
(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent		202220222.0medium000001
osimertinib
2
acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist		202020223.0high000011
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Cancer of Lung0
1
202220222.0high000001
Carcinoma, Non-Small Cell Lung0
1
202220222.0high000001
Carcinoma, Non-Small-Cell Lung0
1
202220222.0high000001
Lung Neoplasms0
1
202220222.0high000001