Page last updated: 2024-11-13
etp-46321
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Description
ETP-46321: inhibits PI3K alpha and PI3K delta; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 46927938 |
CHEMBL ID | 2087474 |
SCHEMBL ID | 10100315 |
MeSH ID | M0576940 |
Synonyms (19)
Synonym |
---|
CHEMBL2087474 , |
bdbm50420714 |
CS-3350 |
HY-12340 |
etp-46321 |
SCHEMBL10100315 |
EX-A1284 |
1252594-99-2 |
5-(2-((4-(methylsulfonyl)piperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine |
5-[2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-yl-imidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine |
BCP19935 |
etp46321 |
5-[2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine |
5-(2-((4-(methyl sulfonyl)piperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine |
F85058 |
MS-28782 |
A926380 |
CAC59499 |
AC-36139 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (6)
Inhibition Measurements
Biological Processes (224)
Molecular Functions (36)
Ceullar Components (30)
Bioassays (139)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1365771 | Inhibition of CYP3A4 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685268 | Inhibition of CYP2D6 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685269 | Inhibition of CYP3A4 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685441 | Inhibition of JAK2 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365773 | Permeability of the compound at 300 uL after 5 hrs by PAMPA | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685447 | Inhibition of PAK1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450119 | Inhibition of CYP2C19 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685436 | Inhibition of FGFR1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685429 | Inhibition of AKT1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450092 | Inhibition of human AKT1 at 1 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685288 | Inhibition of INSR at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450103 | Inhibition of wild-type human MEK1 (M1 to V393 residues) expressed in Sf9 insect cells at 1 uM using ERK2-K54R as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450100 | Inhibition of recombinant human N-terminal GST-tagged INSR (G989 to S1382 residues) expressed in baculovirus infected Sf9 cells at 1 uM using Poly(Ala,Glu,Lys,Tyr)6:2:5:1 as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685450 | Inhibition of PIM2 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450104 | Inhibition of recombinant human N-terminal GST/His6-tagged PLK1 (M1 to S603 residues) expressed in Sf9 insect cells at 1 uM using RBER-CDC25tide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685457 | Antitumor activity in tamoxifen-induced mouse tumor model assessed as reduction in lung [18F]FDG uptake at 50 mg/kg/day, po for 3 weeks by PET-CT method | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450097 | Inhibition of DYRK1A (unknown origin) at 1 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685278 | Inhibition of ARK5 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685275 | Inhibition of human PI3Kalpha E545K mutant by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685426 | Inhibition of PIM2 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450111 | Inhibition of human SRC at 1 uM using poly(Glu,Tyr)4:1 as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685439 | Inhibition of IKKbeta at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450114 | Stability in human liver microsomes assessed as compound remaining at 1 uM measured after 15 mins | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685427 | Inhibition of RPS6KA1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365769 | Inhibition of CYP2C19 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365776 | Clearance in BALB-C mouse at 8 mg/kg, iv by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365811 | Clearance in BALB-C mouse at 8 mg/kg, iv by LC-MS/MS analysis relative to hepatic blood flow | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1450080 | Inhibition of human FAK at 1 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685290 | Inhibition of JNK1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450081 | Inhibition of recombinant human N-terminal GST/His6-tagged FGFR1 (G400 to R820 residues) expressed in Sf9 insect cells at 1 uM using poly(Glu,Tyr)4:1 as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450087 | Inhibition of PI3K p110gamma (unknown origin) using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450105 | Inhibition of recombinant human N-terminal His6-tagged PDK1 (M1 to M460 residues) expressed in Sf9 insect cells at 1 uM using LRRWSLG as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685442 | Inhibition of JNK1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450102 | Inhibition of recombinant human N-terminal GST/His6-tagged KIT (T544 to V976 residues) expressed in Sf9 insect cells at 1 uM using TRK-C-derived peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450109 | Inhibition of RPS6KA1 (unknown origin) at 1 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685444 | Inhibition of MEK1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450093 | Inhibition of recombinant human N-terminal GST/His6-tagged B-RAF V600E mutant (Q417 to H766 residues) expressed in baculovirus infected Sf9 cells at 1 uM using MEK1 as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685282 | Inhibition of EGFR at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685453 | Clearance in BALB-C mouse | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685291 | Inhibition of KIT at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685264 | Stability in mouse liver microsomes at 1 uM incubated for 15 mins | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450121 | Inhibition of CYP3A4 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365777 | Volume of distribution in BALB-C mouse at 8 mg/kg, iv by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685455 | In-vivo inhibition of PI3Kalpha-mediated AKT Ser 473 phosphorylation in lung of tamoxifen-induced mouse tumor model at 50 mg/kg, po measured 2 to 4 hrs post dose | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450115 | Stability in mouse liver microsomes assessed as compound remaining at 1 uM measured after 15 mins | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685423 | Inhibition of PAK1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685459 | Selectivity ratio of Kiapp for human PI3Kbeta to Kiapp for human PI3Kalpha (p110alpha/p85alpha) | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685277 | Inhibition of AKT1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365734 | Inhibition of recombinant human full-length N-terminal His6-tagged p110delta/human full-length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685428 | Inhibition of SGK1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685267 | Inhibition of CYP2C19 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450083 | Inhibition of full-length human p110alpha (1 to 1068 end residues)/N-terminal GST-tagged p85alpha (1 to 724 end residues) expressed in baculovirus expression system | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365765 | Stability in human liver microsomes assessed as parent compound remaining at 0.5 uM after 30 mins by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685456 | Antitumor activity in tamoxifen-induced mouse tumor model assessed as tumor growth inhibition at 50 mg/kg/day, po for 3 weeks by computed tomography | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685280 | Inhibition of CK1alpha1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365791 | Oral bioavailability in BALB-C mouse at 8 mg/kg by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685285 | Inhibition of FLT3 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685287 | Inhibition of IKKbeta at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685432 | Inhibition of CK1alpha1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685284 | Inhibition of FGFR1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365775 | Half-life in BALB-C mouse at 8 mg/kg, iv by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365741 | Inhibition of PI3K in serum-stimulated human U2OS cells assessed as decrease in AKT1 phosphorylation at S473 by C-ELISA | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685445 | Inhibition of MET at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365739 | Inhibition of recombinant human GST-tagged mTOR catalytic domain (1360 to 2549 residues) expressed in baculovirus expression system by AlexaFluor647-labeled kinase tracer 314 based LanthaScreen assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365770 | Inhibition of CYP2D6 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365737 | Selectivity ratio of Ki(app) for p110beta/85alpha (unknown origin) to Ki(app) for full-length human P110alpha (1 to 1068 residues)/N-terminal GST-fused p85alpha (1 to 724 residues) expressed in baculovirus expression system | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685435 | Inhibition of FAK at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450095 | Inhibition of full length N-terminal GST/His6-tagged human CDK8 (M1 to Y463 residues)/N-terminal His6-tagged Cyc C (M1 to S283 residues) expressed in Sf9 insect cells at 1 uM using RBER-IRStide as substrate by filter binding assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365732 | Inhibition of recombinant full-length human N-terminal His6-tagged p110gamma expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1450108 | Inhibition of recombinant human N-terminal GST/His6-tagged PDGFRalpha (Q551 to L1089 residues) expressed in Sf9 insect cells at 1 uM using TRK-C-derived peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685262 | Inhibition of human PI3Kalpha (p110alpha/p85alpha) by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685430 | Inhibition of ARK5 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685431 | Inhibition of BRAF V600E mutant at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685438 | Inhibition of IGF1R at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685446 | Inhibition of MST1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365789 | AUC (infinity) in BALB-C mouse at 8 mg/kg, po by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1450118 | Inhibition of CYP2C9 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450116 | Stability in rat liver microsomes assessed as compound remaining at 1 uM measured after 15 mins | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365768 | Inhibition of CYP2C9 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685422 | Inhibition of MST1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685281 | Inhibition of DYRK1A at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685273 | Inhibition of human PI3Kgamma by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685271 | Inhibition of human PI3Kdelta (p110delta/p85alpha) by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450110 | Inhibition of recombinant human N-terminal GST-tagged SGK1 (M1 to L431 residues) expressed in baculovirus infected Sf9 cells at 1 uM using GSK3-derived peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685437 | Inhibition of FLT3 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685274 | Inhibition of human PI3Kalpha E542K mutant by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450094 | Inhibition of recombinant human N-terminal GST/His6-tagged CK1alpha1 (M1 to F365 residues) expressed in Sf9 insect cells at 1 uM using casein as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365738 | Selectivity ratio of Ki(app) for recombinant full-length human N-terminal His6-tagged p110gamma expressed in baculovirus infected Sf21 insect cells to Ki(app) for full-length human P110alpha (1 to 1068 residues)/N-terminal GST-fused p85alpha (1 to 724 res | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1450084 | Inhibition of PI3K in serum-stimulated human U2OS cells assessed as decrease in AKT1 phosphorylation at S473 by C-ELISA | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685270 | Inhibition of human PI3Kbeta (p110beta/p85alpha) by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365790 | Half-life in BALB-C mouse at 8 mg/kg, po by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685276 | Inhibition of human PI3Kalpha H1047R mutant by ADP accumulation based HTRF assay | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365766 | Stability in mouse liver microsomes assessed as parent compound remaining at 0.5 uM after 30 mins by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365787 | Tmax in BALB-C mouse at 8 mg/kg, po by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365736 | Inhibition of p110beta/85alpha (unknown origin) using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685420 | Inhibition of MEK1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685424 | Inhibition of PDGFR at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685452 | Inhibition of SGK1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685443 | Inhibition of KIT at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685454 | Oral bioavailability in BALB-C mouse | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365772 | Kinetic solubility of the compound in phosphate buffered saline at pH 7.4 at 1 to 2 mg measured after 24 hrs by HPLC analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365735 | Selectivity ratio of Ki(app) for recombinant human full-length N-terminal His6-tagged p110delta/human full-length p85alpha expressed in baculovirus infected Sf21 insect cells to Ki(app) for full-length human P110alpha (1 to 1068 residues)/N-terminal GST-f | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365778 | AUC (infinity) in BALB-C mouse at 8 mg/kg, iv by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1450088 | Inhibition of p110delta/p85alpha (unknown origin) using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450106 | Inhibition of recombinant human N-terminal GST/His6-tagged MET (K956 to S1390 residues) expressed in Sf9 insect cells at 1 uM using TRK-C-derived peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450096 | Inhibition of recombinant human N-terminal GST/His6-tagged CHK1 (M1 to T476 residues) expressed in baculovirus infected Sf9 cells at 1 uM using S6-peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365788 | Cmax in BALB-C mouse at 8 mg/kg, po by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1365740 | Selectivity ratio of Ki(app) for recombinant human GST-tagged mTOR catalytic domain (1360 to 2549 residues) expressed in baculovirus expression system to Ki(app) for full-length human P110alpha (1 to 1068 residues)/N-terminal GST-fused p85alpha (1 to 724 | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID1450107 | Inhibition of recombinant human N-terminal GST/His6-tagged PAK1 (M1 to H545 residues) expressed in Sf9 insect cells at 1 uM using LRRWSLG as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450112 | Inhibition of recombinant human N-terminal GST-tagged VEGFR2 (D807 to V1356 residues) expressed in Sf9 insect cells at 1 uM using Poly(Glu:Tyr)4:1 as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685421 | Inhibition of MET at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685266 | Inhibition of CYP2C9 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450082 | Inhibition of recombinant human N-terminal GST/His6-tagged IKKbeta (M1 to S756 residues) expressed in baculovirus infected Sf9 cells at 1 uM by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450099 | Inhibition of recombinant human N-terminal GST/His6-tagged IGF1R (M954 to C1367 residues) expressed in Sf9 insect cells at 1 uM using poly(Glu,Tyr)4:1 as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685425 | Inhibition of PIM1 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450120 | Inhibition of CYP2D6 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685451 | Inhibition of RPS6KA1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685279 | Inhibition of BRAF V600E mutant at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365807 | Plasma concentration in BALB-C mouse at 8 mg/kg, po by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685289 | Inhibition of JAK2 at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450085 | Inhibition of recombinant human N-terminal His-tagged p110alpha/p85alpha expressed in Spodoptera frugiperda insect cells using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685283 | Inhibition of FAK at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685434 | Inhibition of EGFR at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685448 | Inhibition of PDGFR at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1365733 | Inhibition of full-length human P110alpha (1 to 1068 residues)/N-terminal GST-fused p85alpha (1 to 724 residues) expressed in baculovirus expression system by ADP Hunter assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685449 | Inhibition of PIM1 at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685458 | Antitumor activity in tamoxifen-induced mouse tumor model assessed as reduction in lung metabolic activity at 50 mg/kg/day, po for 3 weeks by [18F]FDG uptake based PET-CT method | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685261 | Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450086 | Inhibition of recombinant human N-terminal His6-tagged p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate by HTRF assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450117 | Inhibition of CYP1A2 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1450101 | Inhibition of recombinant human N-terminal GST/His6-tagged JAK2 (P717 to G1132 residues) expressed in Sf9 insect cells at 1 uM using TRK-C-derived peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID1365767 | Inhibition of CYP1A2 (unknown origin) at 10 uM relative to control | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Identification of novel PI3K inhibitors through a scaffold hopping strategy. |
AID685433 | Inhibition of DYRK1A at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685265 | Inhibition of CYP1A2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685272 | Inhibition of mTOR | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685263 | Stability in human liver microsomes at 1 uM incubated for 15 mins | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID685286 | Inhibition of IGF1R at 1 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
AID1450098 | Inhibition of recombinant human N-terminal GST/His6-tagged EGFR (H672 to A1210 residues) expressed in Sf9 insect cells at 1 uM using TRK-C-derived peptide as substrate by filter binding method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy. |
AID685440 | Inhibition of INSR at 5 uM | 2012 | Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10 | Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (5)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 5 (100.00) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 17.90
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.90) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |