| Assay ID | Title | Year | Journal | Article |
|---|
| AID1409331 | Inhibition of human PI3Kdelta (108 to 1044 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1409333 | Inhibition of human PI4Kbeta (1 to 828 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230516 | Cmax in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230526 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 4 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1409337 | Selectivity ratio of Kd for human PI3Kdelta (108 to 1044 residues) to Kd for human mTOR (1382 to 2549 residues) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230518 | AUC (0 to infinity) in rat at 5 mg/kg, po | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230548 | Inhibition of CYP450 (unknown origin) up to 10 uM | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230531 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 24 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230535 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 2 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230537 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 24 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1409329 | Inhibition of human PI3Kalpha (108 to 1068 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230549 | Mutagenicity in Salmonella typhi by Ames test | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230514 | Clearance in rat at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230547 | Inhibition of cFMS (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230529 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 4 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1754883 | Inhibition of mTOR (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. |
| AID1409339 | Selectivity ratio of Kd for human human PI4Kbeta (1 to 828 residues) to Kd for human mTOR (1382 to 2549 residues) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230550 | Genotoxicity in mouse erythrocytes by micronucleus test | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230509 | Metabolic stability in rat S9 fraction assessed as compound remaining measured at 60 mins | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230521 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 2 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1409338 | Selectivity ratio of Kd for human PI3Kgamma (144 to 1102 residues) to Kd for human mTOR (1382 to 2549 residues) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230508 | Inhibition of mTOR (unknown origin) by HTR-FRET substrate phosphorylation assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230533 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 8 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230534 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 24 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230528 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 24 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1409335 | Selectivity ratio of Kd for human PI3Kalpha (108 to 1068 residues) to Kd for human mTOR (1382 to 2549 residues) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1409332 | Inhibition of human PI3Kgamma (144 to 1102 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1409336 | Selectivity ratio of Kd for human PI3Kbeta (118 to 1070 residues) to Kd for human mTOR (1382 to 2549 residues) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230539 | Antitumor activity against human PC3 cells xenografted in po dosed mouse assessed as tumor growth inhibition administered as qd for 21 days | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230520 | Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230542 | Antitumor activity against human PC3 cells xenografted in mouse assessed as tumor growth inhibition at 25 mg/kg, po qd | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230532 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 4 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230551 | Inhibition of human ERG | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1409330 | Inhibition of human PI3Kbeta (118 to 1070 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230525 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 4 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230519 | Oral bioavailability in rat at 5 mg/kg | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230546 | Inhibition of Flt4 (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230522 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 2 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230515 | Selectivity ratio of IC50 for PI3K-alpha (unknown origin) to IC50 for mTOR (unknown origin) | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1409340 | Selectivity ratio of Kd for human human VPS34 (282 to 879 residues) to Kd for human mTOR (1382 to 2549 residues) | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1409328 | Inhibition of human mTOR (1382 to 2549 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1409334 | Inhibition of human VPS34 (282 to 879 residues) expressed in mammalian expression system by KINOMEscan assay | 2018 | Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
| Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders. |
| AID1230545 | Antitumor activity against human PC3 cells xenografted in mouse assessed as tumor volume reduction at 25 mg/kg, po qd for 21 days relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230523 | Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230524 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of Akt phosphorylation at S473 at 100 mg/kg, po measured after 2 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230536 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 8 hrs to IC50 for mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230527 | In vivo inhibition of mTORC1 in human PC3 cells xenografted in mouse assessed as inhibition of S6 phosphorylation at 100 mg/kg, po measured after 8 hrs relative to control | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230530 | Ratio of drug uptake in human PC3 cells xenografted in mouse at 100 mg/kg, po measured after 8 hrs to IC50 for mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1230505 | Inhibition of PI3K-alpha (unknown origin) by mobility shift assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| 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. |
| AID1345520 | Human fms related tyrosine kinase 4 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1345726 | Human mechanistic target of rapamycin kinase (FRAP subfamily) | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| AID1345508 | Human colony stimulating factor 1 receptor (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |