Compounds > tgx 221
Page last updated: 2024-08-02 11:46:24

tgx 221

Description

TGX 221: a platelet aggregation inhibitor [MeSH]

9-(1-anilinoethyl)-7-methyl-2-(4-morpholinyl)-4-pyrido[1,2-a]pyrimidinone : no description available [CHeBI]

Cross-References

ID SourceID
PubMed CID9907093
CHEMBL ID1972466
SCHEMBL ID902952
CHEBI ID91428
MeSH IDM0490761

Synonyms (52)

Synonym
tgx 221
HY-10114
tgx-221 ,
HMS3229L09
KINOME_3610
7-methyl-2-morpholino-9-(1-(phenylamino)ethyl)-4h-pyrido[1,2-a]pyrimidin-4-one
A19415
tgx221
663619-89-4
CHEMBL1972466 ,
CCG-101299
HMS3244E16
HMS3244F15
HMS3244E15
BCPP000046
NCGC00346495-01
7-methyl-2-(morpholin-4-yl)-9-[1-(phenylamino)ethyl]pyrido[1,2-a]pyrimidin-4-one
CS-0110
S1169
bdbm50447094
BRD-A41692738-001-01-9
7-methyl-2-morpholin-4-yl-9-[1-(phenylamino)ethyl]pyrido[2,1-b]pyrimidin-4-one
gtpl8244
AKOS022177036
MLS006010987
smr004702789
6l28aw98th ,
7-methyl-2-(morpholin-4-yl)-9-(1-(phenylamino)ethyl)pyrido(1,2-a)pyrimidin-4-one
unii-6l28aw98th
4h-pyrido(1,2-a)pyrimidin-4-one, 7-methyl-2-(4-morpholinyl)-9-(1-(phenylamino)ethyl)-
7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4h-pyrido[1,2-a]pyrimidin-4-one
SCHEMBL902952
7-methyl-2-morpholin-4-yl-9-(1-phenylaminoethyl)-pyrido[1,2-a]-pyrimidin-4-one
AC-33159
9-(1-anilinoethyl)-7-methyl-2-morpholin-4-ylpyrido[1,2-a]pyrimidin-4-one
J-519312
EX-A1105
CHEBI:91428
HMS3654K14
mfcd11113209
NCGC00346495-12
SW218249-2
FT-0767048
pi 3-kbeta inhibitor vi, tgx-221 - cas 663619-89-4
Q27088979
AS-16240
BCP01971
SB19244
HMS3295M19
HMS3744G09
pi 3-k beta inhibitor vi, tgx-221
DTXSID101025688

Drug Classes (1)

ClassDescription
pyridopyrimidineAny organic heterobicyclic compound consisting of a pyridine ring ortho-fused at any position to a pyrimidine ring.

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency9.5221AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency30.3531AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency1.0684AID1645842
Interferon betaHomo sapiens (human)Potency1.0684AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.0684AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.0684AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.0684AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformHomo sapiens (human)IC500.5188AID1068549; AID1231393; AID1658512; AID676029; AID676252
Phosphatidylinositol 3-kinase regulatory subunit alphaHomo sapiens (human)IC502.7210AID1658510; AID1658511; AID1658512
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC505.2625AID1068551; AID1184419; AID1189519; AID1231391; AID1658511; AID676027; AID676250; AID695153
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoformHomo sapiens (human)IC500.1713AID1068547; AID1068550; AID1182053; AID1184418; AID1189520; AID1231392; AID1326858; AID1658510; AID1861742; AID676028; AID676242; AID676251; AID676293; AID695152
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Homo sapiens (human)IC507.7500AID1068548; AID1658513; AID676030; AID676253

Bioassays (82)

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.
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.
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.
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.
AID493040Navigating the Kinome2011Nature chemical biology, Apr, Volume: 7, Issue:4
ISSN: 1552-4469		Navigating the kinome.
AID676030Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID676241Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1068551Inhibition of N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804		Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
AID1231393Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
ISSN: 1464-3391		Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
AID1326869Inhibition of PI3Kbeta in human washed platelets assessed as suppression of ADP-induced platelet aggregation at 0.5 uM preincubated for 5 mins followed by 25 uM ADP stimulation after 10 mins by light transmission aggregometric analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122ISSN: 1768-3254Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).
AID1658513Inhibition of human full length p110gamma using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID676250Inhibition of human PI3Kalpha-mediated Akt phosphorylation at Ser473 residue expressed in human H460 cells after 0.5 to 2 hrs by Western blot analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID676293Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1231394Inhibition of cell proliferation of human NZB5 cells containing wild-type p110alpha gene incubated for 5 days by [3H]thymidine incorporation assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
ISSN: 1464-3391		Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
AID676252Inhibition of human PI3Kdelta-mediated Akt phosphorylation at Ser473 residue expressed in mouse MEF-3T3 cells after 0.5 to 2 hrs by Western blot analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1189519Inhibition of PI3K p110alpha (unknown origin)2015Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
ISSN: 1520-4804		Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.
AID1326875Antiplatelet activity against human washed platelets assessed as reduction in shear-induced stationary platelet adhesionto vWF matrix at 2 uM preincubated for 5 mins followed by blood perfusion after 4 mins2016European journal of medicinal chemistry, Oct-21, Volume: 122ISSN: 1768-3254Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).
AID1231391Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
ISSN: 1464-3391		Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
AID1231395Inhibition of cell proliferation of human NZOV9 cells containing wild-type p53 protein and p110alpha Y1021C mutant incubated for 5 days by [3H]thymidine incorporation assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
ISSN: 1464-3391		Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
AID695152Inhibition of human recombinant His6-tagged PI3K p110beta expressed in baculovirus using DiC8-PI(4,5)P2 as substrate after 20 mins by AlphaScreen assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
ISSN: 1464-3405		Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation.
AID1068550Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804		Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
AID1658515Selectivity index, ratio of IC50 for human p110delta catalytic subunit/p85alpha to IC50 for recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID1068547Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804		Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
AID676251Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in mouse MEF-3T3 cells after 0.5 to 2 hrs by Western blot analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1068548Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804		Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
AID676028Inhibition of N-terminus poly-His tagged human PI3Kbeta expressed in baculovirus infected insect S21 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1184418Inhibition of human recombinant PI3Kbeta assessed as PIP3 production by AlphaScreen assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
ISSN: 1464-3405		Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
AID1326858Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay2016European journal of medicinal chemistry, Oct-21, Volume: 122ISSN: 1768-3254Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).
AID1658516Selectivity index, ratio of IC50 for human full length p110gamma to IC50 for recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID676027Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1861742Inhibition of PI3Kbeta (unknown origin) incubated for 60 mins in the presence of ATP by Kinase-Glo luminescence assay2022Bioorganic & medicinal chemistry, 09-01, Volume: 69ISSN: 1464-3391Synthesis and biological evaluation of 4H-benzo[e][1,3]oxazin-4-ones analogues of TGX-221 as inhibitors of PI3Kβ.
AID676242Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1326886Drug level in iv dosed rat serum after 5 mins by LC-MS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122ISSN: 1768-3254Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).
AID676243Selectivity ratio of IC50 for human PI3Kbeta-mediated Akt phosphorylation at T308 residue to IC50 for human mTOR-mediated Akt phosphorylation at Ser473 residue2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1184422Lipophilicity, log D of the compound at pH 7.4 by HPLC method2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
ISSN: 1464-3405		Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
AID1184419Inhibition of human recombinant PI3Kalpha assessed as PIP3 production by AlphaScreen assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
ISSN: 1464-3405		Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
AID695153Inhibition of human recombinant His6-tagged PI3K p110alpha expressed in baculovirus using DiC8-PI(4,5)P2 as substrate after 20 mins by AlphaScreen assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
ISSN: 1464-3405		Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation.
AID1189520Inhibition of PI3K p110beta (unknown origin)2015Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
ISSN: 1520-4804		Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.
AID695154Lipophilicity, log D of the compound by HPLC analysis at pH 7.42012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
ISSN: 1464-3405		Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one-containing Phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation.
AID1231396Selectivity index, ratio of IC50 for N-terminal His-tagged human p110alpha to IC50 for N-terminal His-tagged human p110beta2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
ISSN: 1464-3391		Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
AID1182053Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
ISSN: 1464-3405		Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
AID1326887Drug level in iv dosed rat serum after 60 mins by LC-MS analysis2016European journal of medicinal chemistry, Oct-21, Volume: 122ISSN: 1768-3254Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922).
AID1068549Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
ISSN: 1520-4804		Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
AID1231392Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
ISSN: 1464-3391		Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
AID1658512Inhibition of human p110delta catalytic subunit/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID1658510Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration 2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID676253Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1184420Apparent permeability across apical to basolateral side of human Caco2 cells at 10 uM at pH 6.5 by LC-tandem MS analysis2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
ISSN: 1464-3405		Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
AID1658514Selectivity index, ratio of IC50 for human full length p110alpha/p85alpha to IC50 for recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID1658511Inhibition of human full length p110alpha/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
ISSN: 1948-5875		Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
AID1184421Intrinsic clearance in human hepatocytes at 2 uM by LCMS analysis2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
ISSN: 1464-3405		Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
AID676029Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
ISSN: 1520-4804		Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression2022The Journal of biological chemistry, 08, Volume: 298, Issue:8
ISSN: 1083-351X
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
ISSN: 2211-1247		A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173ISSN: 1872-9096A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
ISSN: 1949-2553		Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1345748Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta (Phosphatidylinositol kinases)2005Nature medicine, May, Volume: 11, Issue:5
ISSN: 1078-8956		PI 3-kinase p110beta: a new target for antithrombotic therapy.
AID1345778Human phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta (Phosphatidylinositol kinases)2005Nature medicine, May, Volume: 11, Issue:5
ISSN: 1078-8956		PI 3-kinase p110beta: a new target for antithrombotic therapy.

Research

Studies (54)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (7.41)29.6817
2010's40 (74.07)24.3611
2020's10 (18.52)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%
Other54 (100.00%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
pd 173074
0
aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist		00low000000
pd 158780
0
aromatic amine;
bromobenzenes;
diamine;
pyridopyrimidine;
secondary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		00low000000
pipemidic acid
0
amino acid;
monocarboxylic acid;
N-arylpiperazine;
pyridopyrimidine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor		00low000000
piromidic acid
0
monocarboxylic acid;
pyridopyrimidine;
pyrrolidines;
quinolone antibiotic;
tertiary amino compound		antibacterial drug;
DNA synthesis inhibitor		00low000000
risperidone
0
1,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist		00low000000
trequinsin
0
pyridopyrimidine00low000000
pemirolast
0
pyridopyrimidine00low000000
ocaperidone
0
pyridopyrimidine00low000000
probon
0
pyridopyrimidine00low000000
8-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
paliperidone
0
1,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine;
secondary alcohol		00low000000
pd 173955
0
aryl sulfide;
dichlorobenzene;
methyl sulfide;
pyridopyrimidine		tyrosine kinase inhibitor00low000000
2-imino-N,8-dimethyl-5-oxo-1-propan-2-yl-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
3-(benzenesulfonyl)-2-imino-1-(2-oxolanylmethyl)-5-dipyrido[1,2-d-3',4'-f]pyrimidinone
0
pyridopyrimidine00low000000
N-ethyl-2-imino-10-methyl-1-[(4-methylphenyl)methyl]-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
9,10-dimethoxy-2-(2-pyridinylmethylamino)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
0
pyridopyrimidine00low000000
LSM-33283
0
pyridopyrimidine00low000000
LSM-20487
0
pyridopyrimidine00low000000
LSM-31933
0
pyridopyrimidine00low000000
N-cyclopentyl-2-imino-1-[3-(4-morpholinyl)propyl]-5-oxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
LSM-28559
0
pyridopyrimidine00low000000
N-(2-furanylmethyl)-2-imino-5-oxo-1-(2-phenylethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
2-imino-10-methyl-N-[2-(4-morpholinyl)ethyl]-5-oxo-1-(3-pyridinylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
3-(benzenesulfonyl)-2-imino-1-propyl-5-dipyrido[1,2-d-3',4'-f]pyrimidinone
0
pyridopyrimidine00low000000
7-methyl-4-oxo-2-[(phenylmethyl)amino]-3-pyrido[1,2-a]pyrimidinecarboxaldehyde
0
pyridopyrimidine00low000000
6-propan-2-yl-2-sulfanylidene-1,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-one
0
pyridopyrimidine00low000000
2-[[3-(2-chloro-6-fluorophenyl)-5-methyl-4-isoxazolyl]-oxomethyl]imino-1-(2-methylpropyl)-5-oxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
LSM-26967
0
pyridopyrimidine00low000000
2-[2-furanyl(oxo)methyl]imino-5-oxo-1-propan-2-yl-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
1-(2-methoxyethyl)-7-thiophen-2-yl-5-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione
0
pyridopyrimidine00low000000
1-butyl-2,4-dioxo-7-thiophen-2-yl-5-pyrido[2,3-d]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
1-cyclopentyl-2-imino-10-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
2-methyl-1-cyclopropanecarboxylic acid (7-bromo-4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl ester
0
pyridopyrimidine00low000000
2-imino-1-[(4-methylphenyl)methyl]-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
2-(3-ethoxypropylamino)-8-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[1,2-pyrimidinecarboxamide
0
pyridopyrimidine00low000000
3-[2,4-dioxo-1-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl]-3-quinazolinyl]-N-(2-furanylmethyl)propanamide
0
pyridopyrimidine00low000000
2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-pyridinecarboxylic acid propan-2-yl ester
0
isopropyl ester;
pyridopyrimidine		00low000000
2-chloro-6-[4-morpholinyl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone
0
pyridopyrimidine00low000000
N-(2-furanylmethyl)-1-[2-(2-hydroxyethoxy)ethyl]-2-imino-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
1-(3-ethoxypropyl)-2-[2-furanyl(oxo)methyl]imino-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
1-butyl-2-[2-furanyl(oxo)methyl]imino-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
2-benzoylimino-1-(2-furanylmethyl)-10-methyl-5-oxo-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxylic acid ethyl ester
0
pyridopyrimidine00low000000
6-[4-oxo-2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-thieno[3,2-d]pyrimidinyl]hexanoic acid
0
pyridopyrimidine00low000000
3-[4-oxo-2-[(4-oxo-2-pyrido[1,2-a]pyrimidinyl)methylthio]-3-thieno[3,2-d]pyrimidinyl]propanoic acid
0
pyridopyrimidine00low000000
2-chloro-8-[4-morpholinyl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone
0
pyridopyrimidine00low000000
3-(3,4-dimethylphenyl)sulfonyl-2-imino-1-prop-2-enyl-5-dipyrido[1,2-e-4',3'-f]pyrimidinone
0
pyridopyrimidine00low000000
1-[2-(3,4-dimethoxyphenyl)ethyl]-2-imino-10-methyl-5-oxo-N-(2-oxolanylmethyl)-3-dipyrido[3,4-c-1',2'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
3-(4-fluorophenyl)sulfonyl-1-(2-furanylmethyl)-2-imino-10-methyl-5-dipyrido[3,4-c-1',2'-f]pyrimidinone
0
pyridopyrimidine00low000000
LSM-27960
0
pyridopyrimidine00low000000
1-[(7-chloro-4-oxo-2-pyrido[1,2-a]pyrimidinyl)methyl]-3-(3-fluoro-4-methylphenyl)thieno[3,2-d]pyrimidine-2,4-dione
0
pyridopyrimidine00low000000
LSM-16446
0
pyridopyrimidine00low000000
2-bromo-6-[1,4-dioxa-8-azaspiro[4.5]decan-8-yl(oxo)methyl]-11-pyrido[2,1-b]quinazolinone
0
pyridopyrimidine00low000000
LSM-16483
0
pyridopyrimidine00low000000
5-[[2-(diethylamino)-9-methyl-4-oxo-3-pyrido[1,2-a]pyrimidinyl]methylidene]-1,3-diazinane-2,4,6-trione
0
pyridopyrimidine00low000000
LSM-28172
0
pyridopyrimidine00low000000
3-ethyl-2-sulfanylidene-6,7,8,9-tetrahydro-1H-pyrimido[4,5-b]quinolin-4-one
0
pyridopyrimidine00low000000
8-(1-piperidinylsulfonyl)-6-pyrido[1,2-a]quinazolinone
0
pyridopyrimidine00low000000
pd 166866
0
biaryl;
dimethoxybenzene;
primary arylamine;
pyridopyrimidine;
ureas		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		00low000000
palbociclib
0
aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor		00low000000
5-deazaflavin
0
pyridopyrimidine00low000000
gw2974
0
pyridopyrimidine00low000000
1-(3,4-dimethylphenyl)-2,5-dioxo-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarbonitrile
0
pyridopyrimidine00low000000
paliperidone palmitate
0
1,2-benzoxazoles;
fatty acid ester;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		00low000000
ssr 69071
0
pyridopyrimidine00low000000
trametinib
0
acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector		00low000000
pamapimod
0
aromatic amine;
aromatic ether;
difluorobenzene;
diol;
primary alcohol;
pyridopyrimidine;
secondary amino compound		antirheumatic drug;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor		00low000000
2-imino-8-methyl-5-oxo-1-(2-oxolanylmethyl)-N-(2-phenylethyl)-3-dipyrido[1,2-d-3',4'-f]pyrimidinecarboxamide
0
pyridopyrimidine00low000000
ku 0063794
0
benzyl alcohols;
monomethoxybenzene;
morpholines;
pyridopyrimidine;
tertiary amino compound		antineoplastic agent;
mTOR inhibitor		00low000000
3-[(3-chlorophenyl)methyl]-5-ethoxy-1,6-dimethylpyrido[2,3-d]pyrimidine-2,4-dione
0
pyridopyrimidine00low000000
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol
0
benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
mTOR inhibitor		00low000000
kin-193
0
pyridopyrimidine00low000000
ly3009120
0
aminotoluene;
aromatic amine;
biaryl;
monofluorobenzenes;
phenylureas;
pyridopyrimidine;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
B-Raf inhibitor;
necroptosis inhibitor		00low000000
sotorasib
0
acrylamides;
methylpyridines;
monofluorobenzenes;
N-acylpiperazine;
phenols;
pyridopyrimidine;
tertiary amino compound;
tertiary carboxamide		antineoplastic agent00low000000
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
1
indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor2011201113.0low000010
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
3
chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector		2011201610.0low000030
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
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
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
n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea
1
2011201113.0low000010
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
1
N-arylpiperazine2011201113.0low000010
cyc 116
1
2011201113.0low000010
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
2011201113.0low000010
gw843682x
1
(trifluoromethyl)benzenes2011201113.0low000010
ic 86621
1
aromatic ketone201520159.0medium000010
nu 7026
1
organic heterotricyclic compound;
organooxygen compound		201520159.0low000010
sb 242235
1
2011201113.0low000010
pi103
2
aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor		2011201511.0low000020
PI3-Kinase alpha Inhibitor 2
1
organic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound		201520159.0high000010
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
nu 7441
1
dibenzothiophenes201520159.0low000010
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
zstk474
2
benzimidazoles;
morpholines;
organofluorine compound;
triamino-1,3,5-triazine		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor		201520168.5low000020
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
ku 60019
1
201520159.0low000010
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
kin-193
2
pyridopyrimidine2014201410.0medium000020
pki 402
1
201520159.0low000010
pki 587
1
201520159.0low000010
abt-348
1
2011201113.0medium000010
vs-5584
1
201520159.0low000010
azd8186
1
202020204.0low000010
chir 258
1
2011201113.0low000010
r 1530
1
2011201113.0medium000010
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
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
adenine
4
6-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite		2010201910.2low000130
dalteparin
1
2008200816.0low000100
palmitic acid
1
long-chain fatty acid;
straight-chain saturated fatty acid		algal metabolite;
Daphnia magna metabolite;
EC 1.1.1.189 (prostaglandin-E2 9-reductase) inhibitor;
plant metabolite		201920195.0low000010
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
6
chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector		201220198.2low000060
adenosine diphosphate
2
adenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		fundamental metabolite;
human metabolite		2010201213.0low000110
phenylephrine
1
phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent		201620168.0low000010
tyrosine
1
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		2008200816.0low000100
quinazolines
4
azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines		2010201910.2low000130
indazoles
2
indazole201420178.5low000020
thiazoles
2
1,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		201720205.5low000020
alpha-aminopyridine
1
2011201113.0low000010
fura-2
1
2012201212.0low000010
tirofiban
1
L-tyrosine derivative;
piperidines;
sulfonamide		anticoagulant;
fibrin modulating drug;
platelet glycoprotein-IIb/IIIa receptor antagonist		2008200816.0low000100
fibrinogen
1
iditolfungal metabolite2008200816.0low000100
erlotinib hydrochloride
1
hydrochloride;
terminal acetylenic compound		antineoplastic agent;
protein kinase inhibitor		201520159.0low000010
wortmannin
1
acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent		201620168.0low000010
oleic acid
1
octadec-9-enoic acidantioxidant;
Daphnia galeata metabolite;
EC 3.1.1.1 (carboxylesterase) inhibitor;
Escherichia coli metabolite;
mouse metabolite;
plant metabolite;
solvent		201920195.0low000010
thromboxane a2
1
epoxy monocarboxylic acid;
thromboxanes A		mouse metabolite2010201014.0low000100
lysophosphatidic acid
1
1-acyl-sn-glycerol 3-phosphate201720177.0low000010
su 11248
1
monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist		202020204.0low000010
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		201620168.0low000010
ic 87114
4
6-aminopurines;
biaryl;
quinazolines		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor2010201910.2low000130
azd 6244
1
benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor		201720177.0low000010
pik 75
3
2011201910.0medium000030
crenolanib
1
aminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor		201720177.0low000010
5-(2,2-difluorobenzo(1,3)dioxol-5-ylmethylene)thiazolidine-2,4-dione
1
2010201014.0low000100
idelalisib
2
aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor		201520178.0low000020
as 252424
3
201220199.3medium000030
zstk474
1
benzimidazoles;
morpholines;
organofluorine compound;
triamino-1,3,5-triazine		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor		201520159.0low000010
mdv 3100
1
(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent		201720177.0low000010
cardiovascular agents
1
2008200816.0low000100
neurotensin
1
peptide hormonehuman metabolite;
mitogen;
neurotransmitter;
vulnerary		2012201212.0low000010
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol
1
benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
mTOR inhibitor		201720177.0low000010
piperidines
1
201720177.0low000010
pf-4708671
1
202120213.0low000001
3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-(4-(4-ethylpiperazin-1-yl)-phenylamino)pyrimidin-4-yl)-1-methylurea
1
aminopyrimidine;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
phenylureas		antineoplastic agent;
fibroblast growth factor receptor antagonist		201720177.0low000010
byl719
2
proline derivative201720205.5low000020
transforming growth factor beta
1
2011201113.0low000010
pyrimidinones
36
200520229.8medium0005292
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Adenocarcinoma Of Kidney0
2
201520206.5low000020
Androgen-Independent Prostatic Cancer0
1
201720177.0low000010
Angiogenesis, Pathologic0
2
201620206.0low000020
Asthma0
1
2012201212.0low000010
Asthma, Bronchial0
1
2012201212.0low000010
Astrocytoma, Grade IV0
1
201720177.0low000010
B16 Melanoma0
1
202020204.0low000010
Benign Neoplasms0
3
2010201610.7low000120
Benign Neoplasms, Brain0
2
201720196.0low000020
Bleeding0
1
2011201113.0low000010
Blood Clot0
2
2005200519.0low000200
Brain Neoplasms0
2
201720196.0low000020
Breast Cancer0
1
2011201113.0low000010
Breast Neoplasms0
1
2011201113.0low000010
Cancer of Endometrium0
1
201720177.0low000010
Cancer of Kidney0
2
201520206.5low000020
Cancer of Lung0
1
201520159.0low000010
Cancer of Pancreas0
1
201720177.0low000010
Cancer of Prostate0
4
2011201710.2low000040
Carcinoma, Ductal, Pancreatic0
1
201720177.0low000010
Carcinoma, Non-Small Cell Lung0
2
201520168.5low000020
Carcinoma, Non-Small-Cell Lung0
2
201520168.5low000020
Carcinoma, Pancreatic Ductal0
1
201720177.0low000010
Carcinoma, Renal Cell0
2
201520206.5low000020
Carotid Artery Thrombosis0
1
2011201113.0low000010
Cell Transformation, Neoplastic0
3
2010201610.3low000120
Congenital Zika Syndrome0
1
202020204.0low000010
Diffuse Lymphocytic Lymphoma, Poorly-Differentiated0
1
2014201410.0low000010
Disease Models, Animal0
2
201120208.5low000020
Endometrial Neoplasms0
1
201720177.0low000010
Experimental Neoplasms0
2
2012201411.0low000020
Fra(X) Syndrome0
1
202120213.0low000001
Fragile X Syndrome0
1
202120213.0low000001
Glial Cell Tumors0
1
201920195.0low000010
Glioblastoma0
1
201720177.0low000010
Glioma0
1
201920195.0low000010
Hemorrhage0
1
2011201113.0low000010
Kidney Neoplasms0
2
201520206.5low000020
Lung Neoplasms0
1
201520159.0low000010
Lymphoma, Mantle-Cell0
1
2014201410.0low000010
Muscle Relaxation0
1
2008200816.0low000100
Neoplasms0
3
2010201610.7low000120
Pancreatic Neoplasms0
1
201720177.0low000010
Prostatic Neoplasms0
4
2011201710.2low000040
Prostatic Neoplasms, Castration-Resistant0
1
201720177.0low000010
Thrombosis0
2
2005200519.0low000200
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (3)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16		2014
Sustained release of PI3K inhibitor from PHA nanoparticles and in vitro growth inhibition of cancer cell lines.
Applied microbiology and biotechnology, , Volume: 89, Issue:5		2011

Dosage (2)

ArticleYear
Discovery of 9-(1-phenoxyethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as oral PI3Kβ inhibitors, useful as antiplatelet agents.
Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16		2014
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16		2014