| Assay ID | Title | Year | Journal | Article |
|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| 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. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| AID354273 | Steady-state unbound ratio of drug level in brain to plasma in rat | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID673846 | Apparent intrinsic clearance in human liver microsomes | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID354267 | Binding affinity to CB2 receptor | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354269 | Bioavailability in rat at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354293 | Antiobesity activity in diet-induced obese mouse assessed as reduction in weight gain at 1 mg/kg, po for 7 days | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354291 | Antiobesity activity in diet-induced obese mouse assessed as reduction in food intake at 1 mg/kg, po for 7 days | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354297 | AUC in rat plasma at 500 mg/kg, po | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID673844 | Efflux ratio of apparent permeability from basal to apical to apical to basal side of MDCK cells expressing MDR1 | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID354301 | Toxicity in rat assessed as incidence of clinical signs or histological changes at 500 mg/kg, po after 4 days | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354268 | Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354287 | Inhibition of CP-55940-induced hypothermia in ICR mouse at >=1 mg/kg, sc administered 15 mins before CP-55940 challenge measured after 65 mins | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354289 | Antiobesity activity in fast-induced refeeding Sprague-Dawley rat model assessed as reduction in food intake at 1 mg/kg, po administered 30 mins prior to food intake measured every 10 mins for 2 hrs | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354272 | Steady-state ratio of drug level in brain to plasma in rat | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354270 | Half life in rat at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354296 | Oral bioavailability in rat up to 50 mg/kg | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354266 | Binding affinity to CB1 receptor | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354288 | Inhibition of CP-55940-induced analgesia in ICR mouse at >=1 mg/kg, sc administered 15 mins before CP-55940 challenge measured after 45 mins by hot plate method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354285 | Inhibition of CP-55940-induced locomotor activity in ICR mouse at >=1 mg/kg, sc administered 15 mins before CP-55940 challenge measured after 25 mins | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354286 | Inhibition of CP-55940-induced catalepsy in ICR mouse at >=1 mg/kg, sc administered 15 mins before CP-55940 challenge measured after 90 mins | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354300 | Toxicity in rat assessed as incidence of clinical signs or histological changes at 50 mg/kg, po after 4 days | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354271 | Volume of distribution at steady state in rat at 1 mg/kg, iv and 5 mg/kg, po | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354299 | Therapeutic index, ratio of toxicity to plasma concentration of compound required for reduction in food intake in Sprague-Dawley rat | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID354295 | Toxicity in rat assessed as incidence of clinical signs or histological changes at 5 mg/kg, po after 4 days | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| AID673843 | Apparent permeability from apical to basal side of MDCK cells expressing MDR1 | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID673839 | Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID673842 | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID673840 | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID673845 | 1-Octanol-sodium phosphate buffer partition coefficient, log D of the compound at pH 7.4 after 24 hrs by shake flask method | 2012 | ACS medicinal chemistry letters, May-10, Volume: 3, Issue:5
| Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents. |
| AID1798959 | CB1 Radioligand Binding Assay (Ki) and GTP-gamma-[35S] Binding Assay (EC50) from Article 10.1021/jm900255t: \\Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a nov | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |