Compounds > cgp 77675
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cgp 77675

Description

CGP 77675: belongs to class of substituted 5,7-diphenyl-pyrrolo(2,3-d)pyrimidines; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID5311381
CHEMBL ID475584
SCHEMBL ID6250604
MeSH IDM0306918

Synonyms (27)

Synonym
cgp77675
CHEMBL475584 ,
1-[2-[4-[4-amino-5-(3-methoxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]phenyl]ethyl]piperidin-4-ol
234772-64-6
AKOS016013805
bdbm50413999
cgp-77675
4-piperidinol, 1-(2-(4-(4-amino-5-(3-methoxyphenyl)-7h-pyrrolo(2,3-d)pyrimidin-7-yl)phenyl)ethyl)-
cgp 77675
1-(2-(4-(4-amino-5-(3-methoxyphenyl)-7h-pyrrolo(2,3-d)pyrimidin-7-yl)phenyl)ethyl)-4-piperidinol(c119957 - m000636242)
unii-eqh27e0wrv
eqh27e0wrv ,
SCHEMBL6250604
1-(4-(4-amino-5-(3-methoxyphenyl)-7h-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol
1-(amino-5-(3-methoxyphenyl)-7h-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol
DTXSID20178033
cgp77675, >=98% (hplc)
NCGC00386693-01
CS-0054689
mfcd20039929
EX-A7643
SB20029
4-piperidinol, 1-[2-[4-[4-amino-5-(3-methoxyphenyl)-7h-pyrrolo[2,3-d]pyrimidin-7-yl]phenyl]ethyl]-
HMS3740G21
Q27277307
HY-W062835
P12687

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.9083AID1645841
GVesicular stomatitis virusPotency37.9083AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency16.9330AID1645840
Interferon betaHomo sapiens (human)Potency37.9083AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency37.9083AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency37.9083AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency37.9083AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Tyrosine-protein kinase FynHomo sapiens (human)IC500.0004AID1803322
Tyrosine-protein kinase LynHomo sapiens (human)IC500.0004AID1407823; AID1803322
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC500.0102AID1803322; AID352998

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560		Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
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
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		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
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1803322In Vitor Src Tyrosine Kinase Activity Assay from Article 10.3109/14756366.2012.715288: \\Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.\\2013Journal of enzyme inhibition and medicinal chemistry, Oct, Volume: 28, Issue:5
ISSN: 1475-6374		Synthesis, biological evaluation and docking studies of new pyrrolo[2,3-d] pyrimidine derivatives as Src family-selective tyrosine kinase inhibitors.
AID1407823Inhibition of Lyn (unknown origin) using Src-family kinase bisamide rhodamine 110 peptide substrate after 1 hr by fluorescence assay2018European journal of medicinal chemistry, Sep-05, Volume: 157ISSN: 1768-3254Pyrrolopyrimidines: An update on recent advancements in their medicinal attributes.
AID352998Inhibition of c-Src2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
ISSN: 1768-3254		Docking, 3D-QSAR studies and in silico ADME prediction on c-Src tyrosine kinase inhibitors.

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (5.00)18.2507
2000's14 (70.00)29.6817
2010's3 (15.00)24.3611
2020's2 (10.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (95.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
glimepiride
1
sulfonamide201820186.0low000010
ag 1879
2
aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine		beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector		201320188.5low000020
cytarabine
1
beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent		201820186.0low000010
ribavirin
1
1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor		201820186.0low000010
a 419259
2
201320188.5medium000020
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
phosphoserine
1
non-proteinogenic alpha-amino acid;
O-phosphoamino acid;
serine derivative		human metabolite2003200321.0low000100
1,10-phenanthroline
1
phenanthrolineEC 2.7.1.1 (hexokinase) inhibitor;
EC 3.4.19.3 (pyroglutamyl-peptidase I) inhibitor		2006200618.0low000100
pd 98059
1
aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector		2006200618.0low000100
ag 1879
1
aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine		beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector		2006200618.0low000100
tyrosine
2
amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical		2002200222.0low000200
pyrroles
14
pyrrole;
secondary amine		1999200920.9high0021200
alpha-naphthoflavone
1
extended flavonoid;
naphtho-gamma-pyrone;
organic heterotricyclic compound		aryl hydrocarbon receptor agonist;
aryl hydrocarbon receptor antagonist;
EC 1.14.14.14 (aromatase) inhibitor		2006200618.0low000100
fluorine
1
diatomic fluorine;
gas molecular entity		NMR chemical shift reference compound2002200222.0low000100
phosphotyrosine
1
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid;
O(4)-phosphotyrosine		Escherichia coli metabolite;
immunogen		2003200321.0low000100
1,7-phenanthroline
1
phenanthroline2006200618.0low000100
u 73122
1
aromatic ether;
aza-steroid;
maleimides		EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor2004200420.0low000100
paxilline
1
diterpene alkaloid;
enone;
organic heterohexacyclic compound;
terpenoid indole alkaloid;
tertiary alcohol		anticonvulsant;
Aspergillus metabolite;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
genotoxin;
geroprotector;
mycotoxin;
Penicillium metabolite;
potassium channel blocker		1999199925.0low001000
cilengitide
1
oligopeptide2009200915.0low000100
purvalanol a
1
purvalanol2005200519.0low000100
u 0126
1
aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent		2006200618.0low000100
aluminum
1
boron group element atom;
elemental aluminium;
metal atom		2002200222.0low000100
epidermal growth factor
5
2001200621.4medium000500
s-nitroglutathione
1
2006200618.0low000100
ferric ammonium citrate
1
2006200618.0low000100
transforming growth factor alpha
2
2003200619.5low000200
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Adenocarcinoma, Clear Cell0
1
2004200420.0low000100
Bone Diseases, Metabolic0
1
1999199925.0low001000
Bone Loss, Osteoclastic0
2
1999200422.5medium001100
Cancer of Prostate0
2
2003201813.5medium000110
Congenital Zika Syndrome0
1
202020204.0low000010
Disease Models, Animal0
2
1999202014.5medium001010
HIV Coinfection0
1
201820186.0low000010
HIV Infections0
1
201820186.0low000010
Invasiveness, Neoplasm0
1
2003200321.0low000100
Low Bone Density0
1
1999199925.0low001000
Pregnancy0
1
1999199925.0low001000
Prostatic Neoplasms0
2
2003201813.5medium000110
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (1)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019