Page last updated: 2024-10-15

cct 241533

Cross-References

ID SourceID
PubMed CID135564841
CHEMBL ID1236782
SCHEMBL ID9967090
MeSH IDM0555291

Synonyms (29)

Synonym
HY-14715
CHEMBL1236782 ,
4-fluoro-2-(4-((3s,4r)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-ylamino)-6,7-dimethoxyquinazolin-2-yl)phenol
bdbm50335684
xbj ,
4-fluoro-2-(4-{[(3s,4r)-4-(1-hydroxy-1-methylethyl)pyrrolidin-3-yl]amino}-6,7-dimethoxyquinazolin-2-yl)phenol
cct-241533
CCT241533 ,
CS-0738
1262849-73-9
gtpl8044
(6z)-4-fluoro-6-[4-[[(3s,4r)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl]amino]-6,7-dimethoxy-1h-quinazolin-2-ylidene]cyclohexa-2,4-dien-1-one
79d8pwx59x ,
3-pyrrolidinemethanol, 4-((2-(5-fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl)amino)-alpha,alpha-dimethyl-, (3r,4s)-
unii-79d8pwx59x
3-pyrrolidinemethanol, 4-((2-(5-fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl)amino)-.alpha.,.alpha.-dimethyl-, (3r,4s)-
SCHEMBL9967090
AKOS025149516
4-fluoro-2-(4-(((3s,4r)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl)amino)-6,7-dimethoxyquinazolin-2-yl)phenol
(6e)-4-fluoro-6-[4-[[(3s,4r)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl]amino]-6,7-dimethoxy-1h-quinazolin-2-ylidene]cyclohexa-2,4-dien-1-one
NCGC00346436-02
Q27075789
4-fluoro-2-[4-[[(3s,4r)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl]amino]-6,7-dimethoxyquinazolin-2-yl]phenol
Q27266745
A922008
cct-241533, dihydrochloride
nsc-776821
nsc776821
PD118154

Bioavailability

ExcerptReference
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency3.70260.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency11.98770.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency18.99910.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency3.70260.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase Chk1Homo sapiens (human)IC50 (µMol)0.19000.00010.45308.8300AID566344
Serine/threonine-protein kinase Chk2Homo sapiens (human)IC50 (µMol)0.00300.00300.34823.5000AID566343
[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)
Serine/threonine-protein kinase Chk2Homo sapiens (human)MEC1.00001.00001.00001.0000AID566340
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Processvia Protein(s)Taxonomy
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
inner cell mass cell proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA replicationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA repairSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatin remodelingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleus organizationSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationSerine/threonine-protein kinase Chk1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of cell population proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2/M transition checkpointSerine/threonine-protein kinase Chk1Homo sapiens (human)
positive regulation of cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of gene expression, epigeneticSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of mitotic nuclear divisionSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of mitotic centrosome separationSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of G0 to G1 transitionSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to mechanical stimulusSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to caffeineSerine/threonine-protein kinase Chk1Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic process involved in developmentSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of DNA biosynthetic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk2Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk2Homo sapiens (human)
double-strand break repairSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of DNA-templated transcriptionSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein catabolic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic intra-S DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of protein catabolic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
positive regulation of DNA-templated transcriptionSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein stabilizationSerine/threonine-protein kinase Chk2Homo sapiens (human)
cell divisionSerine/threonine-protein kinase Chk2Homo sapiens (human)
thymocyte apoptotic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
cellular response to gamma radiationSerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic spindle assemblySerine/threonine-protein kinase Chk2Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of autophagosome assemblySerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
protein kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein domain specific bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
histone H3T11 kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein kinase bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
ubiquitin protein ligase bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein homodimerization activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
chromosome, telomeric regionSerine/threonine-protein kinase Chk1Homo sapiens (human)
condensed nuclear chromosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
extracellular spaceSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
replication forkSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
centrosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytosolSerine/threonine-protein kinase Chk1Homo sapiens (human)
intracellular membrane-bounded organelleSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatinSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein-containing complexSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromosome, telomeric regionSerine/threonine-protein kinase Chk2Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk2Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase Chk2Homo sapiens (human)
PML bodySerine/threonine-protein kinase Chk2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk2Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (103)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID566338Metabolic stability in mouse microsomes assessed as decrease in parent compound level after 30 mins by LC/MS2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566340Inhibition of etoposide-induced CHK2 bandshift in human HT-29 cells by gel electrophoresis2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566495Inhibition of SRPK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566474Inhibition of CHK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566458Inhibition of S6K1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566489Inhibition of NEK2a at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566448Inhibition of p38beta MAPK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566471Inhibition of CAMK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566512Inhibition of VEGFR at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566457Inhibition of SGK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566482Inhibition of BRSK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566456Inhibition of PKBbeta at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566444Inhibition of ERK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566476Inhibition of GSK3b at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566516Inhibition of TBK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566511Inhibition of IGF-1R at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566505Inhibition of FGF-R1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566451Inhibition of ERK8 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566506Inhibition of IRR at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566459Inhibition of PKA at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566460Inhibition of ROCK 2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566492Inhibition of PIM1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566483Inhibition of MELK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566524Inhibition of LKB1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566450Inhibition of p38delta MAPK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566449Inhibition of p38-gamma MAPK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566503Inhibition of Lck at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566509Inhibition of SYK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566469Inhibition of PRAK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566526Inhibition of TTK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566488Inhibition of DYRK3 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566468Inhibition of MAPKAP-K2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566481Inhibition of MARK3 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566463Inhibition of PKCzeta at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566462Inhibition of PKCalpha at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566473Inhibition of PHK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566502Inhibition of Src at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566344Inhibition of CHK1 by DELFIA assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566446Inhibition of JNK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566466Inhibition of MNK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566498Inhibition of HIPK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566472Inhibition of SmMLCK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566486Inhibition of DYRK1A at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566461Inhibition of PRK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566339Cytotoxicity against human HT-29 cells by SRB colorimetric assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566523Inhibition of MLK3 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566479Inhibition of Aurora B at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566515Inhibition of EPH-B3 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566453Inhibition of RSK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566496Inhibition of MST2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566465Inhibition of MSK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566500Inhibition of PAK5 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566507Inhibition of EPHA2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566464Inhibition of PKD1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566452Inhibition of RSK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566497Inhibition of EF2K at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566517Inhibition of IKKepsilon at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566520Inhibition of NUAK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566510Inhibition of YES1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566521Inhibition of MLK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566519Inhibition of IRAK4 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566345Selectivity ratio of IC50 for CHK2 to IC50 for CHK12011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566508Inhibition of MST4 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566467Inhibition of MNK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566487Inhibition of DYRK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566494Inhibition of PIM3 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566501Inhibition of PAK6 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566447Inhibition of p38alpha MAPK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566480Inhibition of AMPK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566522Inhibition of MINK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566342Inhibition of CHK2 phosphorylation at Ser516 in human HT-29 cells at 1 uM by gel electrophoresis2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566343Inhibition of CHK2 by DELFIA assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566518Inhibition of GCK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566346Inhibition of human ERG at 10 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566484Inhibition of CK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566491Inhibition of IKKb at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566443Inhibition of ERK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566455Inhibition of PKBalpha at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566470Inhibition of CAMKKbeta at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566454Inhibition of PDK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566477Inhibition of CDK2/CyclinA at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566485Inhibition of CK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566478Inhibition of PLK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566504Inhibition of CSK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566513Inhibition of BTK at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566341Inhibition of CHK2 phosphorylation at Thr68 in human HT-29 cells at 1 uM by gel electrophoresis2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566499Inhibition of PAK4 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566493Inhibition of PIM2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566514Inhibition of IR-HIS at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566347Inhibition of MKK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566475Inhibition of CHK2 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566525Inhibition of HER4 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566490Inhibition of NEK6 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID566445Inhibition of JNK1 at 1 uM2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1345650Human checkpoint kinase 1 (CHK1 subfamily)2011Cancer research, Jan-15, Volume: 71, Issue:2
CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.
AID1345648Human checkpoint kinase 2 (RAD53 family)2011Cancer research, Jan-15, Volume: 71, Issue:2
CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.
[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's0 (0.00)29.6817
2010's3 (50.00)24.3611
2020's3 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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]