Compounds > r 1530
Page last updated: 2024-08-04 02:14:22

r 1530

Description

Cross-References

ID SourceID
PubMed CID135398512
CHEMBL ID1980391
SCHEMBL ID13751393
SCHEMBL ID3824661
MeSH IDM0553571

Synonyms (40)

Synonym
cid 11610113
KINOME_3737
unii-xqj55r5ppq
pyrazolo(3,4-b)(1,4)benzodiazepine, 5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-
5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepine
xqj55r5ppq ,
rg-1530
CHEMBL1980391 ,
bdbm50426474
r-1530
R1530 ,
HY-13737
CS-1627
882531-87-5
5-(2-chlorophenyl)-1,2-dihydro-7-fluoro-8-methoxy-3-methyl-pyrazolo[3,4-b][1,4]benzodiazepine
UOVCGJXDGOGOCZ-UHFFFAOYSA-N ,
SCHEMBL13751393
SCHEMBL3824661
5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine
r-1521
r 1530
AKOS024458398
AKOS030526962
9-(2-chlorophenyl)-12-fluoro-13-methoxy-6-methyl-2,4,5,8-tetraazatricyclo[8.4.0.0?,?]tetradeca-1(14),2,6,8,10,12-hexaene
r1530, >=98% (hplc)
F20797
FT-0768325
EX-A2311
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydrobenzo[e]pyrazolo[4,3-b][1,4]diazepine
mfcd23704870
AS-16578
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine
NCGC00390699-04
Q27293966
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-2,10-dihydropyrazolo[3,4-b][1,4]benzodiazepine
compound 2 [pmid: 24900658]
gtpl10361
nsc767953
nsc-767953
AC-36024

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency14.7403AID1347411
Interferon betaHomo sapiens (human)Potency14.7403AID1347411

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Serine/threonine-protein kinase PLK4Homo sapiens (human)IC500.0070AID1860512
Serine/threonine-protein kinase PLK4Homo sapiens (human)Ki0.0110AID762206
Aurora kinase AHomo sapiens (human)IC500.0580AID1860511; AID727965
Serine/threonine-protein kinase Chk2Homo sapiens (human)IC500.0240AID1860510; AID727964
Fibroblast growth factor receptor 1Homo sapiens (human)IC500.0280AID727967
Cyclin-dependent kinase 4Homo sapiens (human)IC5010.0000AID727966
Cyclin-dependent kinase 2Homo sapiens (human)IC501.3300AID727968
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC500.0100AID1860509; AID727969

Bioassays (59)

Assay IDTitleYearJournalArticle
AID493040Navigating the Kinome2011Nature chemical biology, Apr, Volume: 7, Issue:4
ISSN: 1552-4469		Navigating the kinome.
AID727933Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as tumor regression at 25 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727950Total clearance in monkey at 1 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727930Antitumor activity against human A549 cells xenografted in mouse assessed as tumor growth inhibition at 1.56 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727961Antiproliferative activity against human lung cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727948Volume of distribution at steady state in monkey at 1 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860512Inhibition of PLK4 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727957Antiangiogenic activity in HUVEC assessed as inhibition of PDGF-induced cell proliferation2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727929Toxicity in human MDA-MB-231 cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727940Oral bioavailability in rat at 50 mg/kg2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727926Toxicity in human A549 cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727939Tmax in monkey at 10 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727934Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as tumor regression at 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727955Terminal half life in mouse at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727943Tmax in rat at 50 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860509Inhibition of VEGFR2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727931Antitumor activity against human HCT116 cells xenografted in mouse assessed as tumor growth inhibition at 1.56 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860511Inhibition of Aurora A (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727927Toxicity in human HCT116 cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727947Tmax in mouse at 25 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727941Cmax in rat at 50 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727954Volume of distribution at steady state in mouse at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727928Toxicity in human LoVo cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727958Antiproliferative activity against human melanoma cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727935Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as tumor growth inhibition at 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727952Terminal half life in rat at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860510Inhibition of CHK2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238ISSN: 1768-3254Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727959Antiproliferative activity against human oral epidermoid cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727932Antitumor activity against human LoVo cells xenografted in mouse assessed as tumor growth inhibition at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727967Inhibition of FGFR1 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727963Antiproliferative activity against human colon cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727922Antitumor activity against human A549 cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727937Cmax in monkey at 10 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727945AUC (0 to 24 hrs) in mouse at 25 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727965Inhibition of aurora-A (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727946Cmax in mouse at 25 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727964Inhibition of CHK2 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727960Antiproliferative activity against human prostate cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727936Oral bioavailability in monkey at 10 mg/kg2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727968Inhibition of CDK2 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727970Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727923Antitumor activity against human HCT116 cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727944Oral bioavailability in mouse at 25 mg/kg2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727938AUC (0 to 24 hrs) in monkey at 10 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727971Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727951Volume of distribution at steady state in rat at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727924Antitumor activity against human LoVo cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727925Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727956Total clearance in mouse at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727962Antiproliferative activity against human breast cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727942AUC (0 to 24 hrs) in rat at 50 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727949Terminal half life in monkey at 1 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727969Inhibition of KDR (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727966Inhibition of CDK4 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID762206Inhibition of human PLK42013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
ISSN: 1520-4804		The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
AID727953Total clearance in rat at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
ISSN: 1948-5875		Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937		High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.

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's4 (66.67)24.3611
2020's2 (33.33)2.80

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
2-cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-2-propenamide
1
hydroxycinnamic acid2011201113.0medium000010
n(6),n(6)-dimethyladenine
1
tertiary amine2011201113.0low000010
go 6976
2
indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor2011201312.0low000020
gw8510
1
2011201113.0low000010
N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
1
bromobenzenes;
isoquinolines;
olefinic compound;
secondary amino compound;
sulfonamide		EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitor2011201113.0medium000010
fasudil
1
isoquinolines;
N-sulfonyldiazepane		antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent		2011201113.0low000010
nsc 664704
1
indolobenzazepine;
lactam;
organobromine compound		cardioprotective agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
geroprotector		2011201113.0low000010
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
1
chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector		2011201113.0low000010
olomoucine
1
2,6-diaminopurines;
ethanolamines		EC 2.7.11.22 (cyclin-dependent kinase) inhibitor2011201113.0low000010
3,3',4,5'-tetrahydroxystilbene
1
stilbenoid2011201113.0medium000010
ag 1879
1
aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine		beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector		2011201113.0low000010
sb 220025
1
aminopyrimidine;
imidazoles;
organofluorine compound;
piperidines		angiogenesis inhibitor;
anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor		2011201113.0low000010
sb 239063
1
imidazoles2011201113.0low000010
sb 202190
1
imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor		2011201113.0low000010
imatinib
1
aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor		2011201113.0low000010
sulfaphenazole
1
primary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor		202220222.0low000001
gatifloxacin
1
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor		2011201113.0low000010
1,3-diphenylurea
1
phenylureascytokinin;
plant metabolite		2011201113.0low000010
pyrazolanthrone
1
anthrapyrazole;
aromatic ketone;
cyclic ketone		antineoplastic agent;
c-Jun N-terminal kinase inhibitor;
geroprotector		2011201113.0low000010
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		202220222.0low000001
norharman
1
beta-carbolines;
mancude organic heterotricyclic parent		fungal metabolite;
marine metabolite		2011201113.0low000010
eupatorin
1
dihydroxyflavone;
polyphenol;
trimethoxyflavone		anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
Brassica napus metabolite;
calcium channel blocker;
P450 inhibitor;
vasodilator agent		2011201113.0low000010
gefitinib
1
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist		2011201113.0low000010
ns 1608
1
ureas2011201113.0medium000010
vatalanib
1
monochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist		2011201113.0low000010
birb 796
1
aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator		2011201113.0low000010
sb 203580
1
imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent		2011201113.0low000010
erlotinib
1
aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor		2011201113.0low000010
orantinib
1
monocarboxylic acid;
oxindoles;
pyrroles		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist		2011201113.0medium000010
lapatinib
1
furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor		2011201113.0low000010
sorafenib
1
(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor		2011201113.0low000010
quinidine
1
cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker		202220222.0low000001
n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea
1
2011201113.0low000010
ketoconazole
1
cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine202220222.0low000001
4-(4-(4-chloro-phenyl)thiazol-2-ylamino)phenol
1
substituted aniline2011201113.0low000010
3-amino-n-(4-methoxybenzyl)-4,6-dimethylthieno(2,3-b)pyridine-2-carboxamide
1
2011201113.0low000010
cct018159
1
benzodioxine;
pyrazoles;
resorcinols		antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor		2011201113.0low000010
bms 387032
1
1,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor		2011201113.0low000010
tandutinib
1
aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		2011201113.0low000010
vx-745
1
aryl sulfide;
dichlorobenzene;
difluorobenzene;
pyrimidopyridazine		anti-inflammatory drug;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor		2011201113.0low000010
dasatinib
1
1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor		2011201113.0low000010
zd 6474
1
aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor		2011201113.0low000010
N-methyl-2-[[3-[2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide
1
aryl sulfide2011201113.0medium000010
N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
1
indoles2011201113.0medium000010
ver-49009
1
aromatic amide;
monochlorobenzenes;
monomethoxybenzene;
pyrazoles;
resorcinols		Hsp90 inhibitor2011201113.0medium000010
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide
1
benzamides;
benzodioxoles;
imidazoles;
pyridines		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor2011201113.0low000010
alsterpaullone
1
C-nitro compound;
caprolactams;
organic heterotetracyclic compound		anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor		2011201113.0low000010
imd 0354
1
benzamides2011201113.0low000010
acacetin
1
dihydroxyflavone;
monomethoxyflavone		anticonvulsant;
plant metabolite		2011201113.0low000010
pd 166285
1
2011201113.0low000010
palbociclib
1
aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor		2011201113.0low000010
jnj-7706621
1
sulfonamide2011201113.0low000010
2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one
1
organic heterotetracyclic compound;
organofluorine compound		EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor2011201113.0low000010
vx680
3
N-arylpiperazine201120228.7low000021
gw-5074
1
2013201311.0low000010
cyc 116
1
2011201113.0low000010
axitinib
1
aryl sulfide;
benzamides;
indazoles;
pyridines		antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist		2013201311.0low000010
1-azakenpaullone
1
lactam;
organic heterotetracyclic compound;
organobromine compound;
organonitrogen heterocyclic compound		EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator		2011201113.0medium000010
a 419259
1
2011201113.0low000010
gdp 366
1
2011201113.0medium000010
2-[[6-[(phenylmethyl)amino]-9-propan-2-yl-2-purinyl]amino]ethanol
1
thiopurine2011201113.0medium000010
a 770041
1
aromatic amide2011201113.0medium000010
cp 547632
1
2011201113.0low000010
bms345541
1
quinoxaline derivative2011201113.0low000010
adw 742
1
2011201113.0medium000010
gw843682x
1
(trifluoromethyl)benzenes2011201113.0low000010
sb 242235
1
2011201113.0low000010
pi103
1
aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor		2011201113.0low000010
tgx 221
1
pyridopyrimidine2011201113.0low000010
zm 447439
1
aromatic ether;
benzamides;
morpholines;
polyether;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor		2011201113.0low000010
rucaparib
1
azepinoindole;
caprolactams;
organofluorine compound;
secondary amino compound		antineoplastic agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor		2011201113.0low000010
cediranib
1
aromatic ether2011201113.0low000010
tae226
1
morpholines2011201113.0low000010
tak-715
1
benzamides2011201113.0low000010
chir 99021
1
aminopyridine;
aminopyrimidine;
cyanopyridine;
diamine;
dichlorobenzene;
imidazoles;
secondary amino compound		EC 2.7.11.26 (tau-protein kinase) inhibitor2011201113.0low000010
ly2090314
1
diazepinoindole;
imidazopyridine;
maleimides;
monofluorobenzenes;
piperidinecarboxamide;
ureas		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator		2011201113.0medium000010
pazopanib
1
aminopyrimidine;
indazoles;
sulfonamide		angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist		2011201113.0low000010
bay 61-3606
1
pyrimidines2011201113.0low000010
sotrastaurin
1
indoles;
maleimides;
N-alkylpiperazine;
N-arylpiperazine;
quinazolines		anticoronaviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunosuppressive agent		2011201113.0low000010
vx 702
1
phenylpyridine2011201113.0low000010
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
1
methoxybenzenes;
substituted aniline		2011201113.0low000010
cvt-6883
1
2011201113.0low000010
r 1487
1
2011201113.0medium000010
nvp-ast487
1
2011201113.0low000010
abt 869
1
aromatic amine;
indazoles;
phenylureas		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		2011201113.0low000010
azd 1152
1
anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
Aurora kinase inhibitor;
prodrug		2011201113.0low000010
3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine
1
aminopyridine;
aromatic ether;
dichlorobenzene;
organofluorine compound;
pyrazolylpiperidine;
racemate		antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		2011201113.0high000010
gw 2580
1
2011201113.0low000010
osi 906
1
cyclobutanes;
quinolines		2011201113.0low000010
mln8054
1
benzazepine2011201113.0low000010
pf-562,271
1
indoles2011201113.0low000010
pha 767491
1
pyrrolopyridine2011201113.0low000010
gpi 15427
1
2011201113.0low000010
dactolisib
1
imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor		2011201113.0low000010
a-484954
1
2011201113.0low000010
azd 1152-hqpa
1
anilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
Aurora kinase inhibitor		2011201113.0low000010
nvp-tae684
1
piperidines2011201113.0low000010
gsk 269962a
1
2011201113.0low000010
3-[(1-methyl-3-indolyl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one
1
indoles2011201113.0medium000010
tg101209
1
N-alkylpiperazine;
N-arylpiperazine;
pyrimidines;
secondary amino compound;
sulfonamide		antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor		2011201113.0low000010
pf 04217903
1
quinolines2011201113.0low000010
3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1-pyrazolyl]propanenitrile
1
pyrrolopyrimidine2011201113.0high000010
gdc 0941
1
indazoles;
morpholines;
piperazines;
sulfonamide;
thienopyrimidine		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor2011201113.0low000010
ph 797804
1
aromatic ether;
benzamides;
organobromine compound;
organofluorine compound;
pyridone		anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor		2011201113.0low000010
mln 8237
1
benzazepine2011201113.0low000010
mk-1775
1
piperazines2011201113.0low000010
PP121
1
aromatic amine;
cyclopentanes;
pyrazolopyrimidine;
pyrrolopyridine		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
tyrosine kinase inhibitor		2011201113.0low000010
sns 314
1
ureas2011201113.0low000010
entrectinib
1
benzamides;
difluorobenzene;
indazoles;
N-methylpiperazine;
oxanes;
secondary amino compound;
secondary carboxamide		antibacterial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		2011201113.0low000010
abt-348
1
2011201113.0medium000010
cfi-400945
1
202220222.0high000001
centrinone
1
202220222.0medium000001
chir 258
1
2011201113.0low000010
2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile
1
hydroxyindoles;
morpholines;
nitrile;
pyridines;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
tau aggregation inhibitor		2011201113.0medium000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Breast Cancer0
1
202220222.0high000001
Breast Neoplasms0
1
202220222.0high000001

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