| Assay ID | Title | Year | Journal | Article |
|---|
| AID708620 | Inhibition of PI3Kalpha in human PC3 cells assessed as reduction in pAKT level by immunoblotting method | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708653 | Cytotoxicity against human LN229 cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708622 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral in mouse Bcrp1 transfected MDCK2 cells at 5 uM after 2 hrs by LC-MS/MS analysis | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708640 | Ratio of drug level in brain to plasma in CD-1 mouse at 50 mg/kg, po at 6 hrs | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID704975 | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction in S6RP phosphorylation at 10 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708631 | Clearance in po dosed CD-1 mouse | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID704976 | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction in S6RP phosphorylation at 40 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708667 | Toxicity in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as loss in body weight at 50 mg/kg, po qd for 24 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708608 | Inhibition of PI3KC2beta at 1 uM | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708655 | Cytotoxicity against human SF539 cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID1304983 | Inhibition of human recombinant mTOR (1360 to 2549 residues) expressed in insect cells assessed as inhibition of GFP-labeled 4-EBP1 phosphorylation at Thr-37/46 residues incubated for 30 mins by FRET assay | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
| Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
| AID708613 | Fraction unbound in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 1 hr post dose | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708669 | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction of AKT phosphorylation at ser473 at 10 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708648 | Ratio of fraction unbound in brain to fraction unbound in plasma in CD-1 mouse at 50 mg/kg, po at 6 hrs | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID704978 | Drug uptake in healthy mouse brain at 50 mg/kg after 1 hr | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708632 | Half life in po dosed CD-1 mouse | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708659 | Inhibition of PI3K signaling in CD-1 mouse assessed as reduction in pAKT level at 50 mg/kg, po administered as single dose measured after 1 hr post dose by immunoblotting method | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708611 | Antitumor activity against PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as inhibition of tumor growth at 3 to 14 mg/kg, po qd for 24 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708661 | Toxicity in PTEN deficient human U87MG cells xenografted in NCr nude mouse at dosed orally once daily for 24 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708651 | Cytotoxicity against human A172 cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708652 | Cytotoxicity against human Hs683 cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708639 | Ratio of drug level in brain to plasma in CD-1 mouse at 50 mg/kg, po at 1 hr | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708668 | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction of AKT phosphorylation at ser473 at 3 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708647 | Ratio of fraction unbound in brain to fraction unbound in plasma in CD-1 mouse at 50 mg/kg, po at 1 hr | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708616 | Drug level in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 6 hrs post dose | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID704977 | Drug uptake in NCr nude mouse brain xenografted with PTEN deficient human U87MG cells at 40 mg/kg after 1 hr | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID1304982 | Inhibition of recombinant PI3Kalpha (unknown origin) using dioctanoylglycerol-PIP2 as substrate incubated for 30 mins in presence of TAMRA-PIP3 by fluorescence polarization assay | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
| Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
| AID708633 | Oral bioavailability in CD-1 mouse | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708656 | Cytotoxicity against human U87MG cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708654 | Cytotoxicity against human M059J cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID1304988 | Ratio of unbound fraction in CD1 mouse brain to plasma at 50 mg/kg, po after 6 hrs by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
| Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
| AID708630 | Inhibition of human recombinant mTOR (1360 to 2549 amino acids) assessed as reduction in phosphorylation of (GFP)-4-EBP1 after 30 mins by FRET assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708618 | Drug level in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 1 hr post dose | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID1304984 | Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
| Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
| AID1304985 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK1 cells expressing human MDR1 at 5 uM incubated for 2 hrs by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
| Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
| AID708671 | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction in S6RP phosphorylation at 3 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID1304986 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK2 cells expressing mouse BCRP1 at 5 uM incubated for 2 hrs by LC-MS/MS analysis | 2016 | ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
| Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. |
| AID708665 | Toxicity in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as loss in body weight at 30 mg/kg, po qd for 24 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708660 | Inhibition of PI3K signaling in CD-1 mouse assessed as reduction in pAKT level at 50 mg/kg, po administered as single dose measured after 6 hrs post dose by immunoblotting method | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708657 | Cytotoxicity against human SF268 cells incubated for 4 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708612 | Fraction unbound in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 6 hrs post dose | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708670 | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction of AKT phosphorylation at ser473 at 40 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708634 | Plasma protein binding in CD-1 mouse | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID708666 | Antitumor activity in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as loss in body weight at 40 mg/kg, po after 24 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS 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) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |