Assay ID | Title | Year | Journal | Article |
AID553231 | Tmax in rat at 1 mg/kg, iv or 1 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1566259 | Inhibition of MGL in rat brain at 10 uM incubated for 30 mins followed by incubation with FP-Rh probe for 45 mins by ABPP assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
| Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology. |
AID553239 | Volume of distribution at steady state in dog at 0.5 mg/kg, iv or 0.5 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553222 | Inhibition of FAAH in human brain membrane proteomes at 10 uM by competitive activity based protein profiling | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553237 | Tmax in dog at 0.5 mg/kg, iv or 0.5 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553233 | Volume of distribution at steady state in rat at 1 mg/kg, iv or 1 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553232 | Clearance in rat at 1 mg/kg, iv or 1 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553245 | Metabolic stability in human hepatocytes assessed as glutathione conjugate formation | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553225 | Inhibition of FAAH in mouse brain membrane proteomes at 100 uM by competitive activity based protein profiling | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553217 | Inhibition of CYP2D6 | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553224 | Inhibition of FAAH in mouse brain membrane proteomes at 10 uM by competitive activity based protein profiling | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553242 | Apparent permeability from apical to basolateral side of MDCK cells | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1573817 | Inhibition of human transmembrane domain deficient FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model. |
AID553247 | Half life in human liver microsomes at 0.8 mg/mL protein concentration | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553226 | Inhibition of fluorophosphonate-reactive serine proteases in mouse liver soluble proteomes at 100 uM by competitive activity based protein profiling | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553249 | Antihyperalgesic activity in orally dosed Sprague-Dawley rat model of complete Freund's adjuvant-induced inflammatory pain model assessed as reduction in mechanical allodynia measured 4 hrs post dose | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553240 | Half life in dog at 0.5 mg/kg, iv | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1573818 | Inhibition of rat FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model. |
AID553223 | Inhibition of FAAH in human brain membrane proteomes at 100 uM by competitive activity based protein profiling | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553230 | Cmax in rat at 1 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553243 | Apparent permeability from basolateral to apical side of MDCK cells | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553244 | Ratio of apical to basolateral side over basolateral to apical side ofMDCK cells | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553248 | Protein binding in human liver microsomes at 0.8 mg/mL protein concentration | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553235 | Oral bioavailability in rat at 1 mg/kg | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553227 | Inhibition of fluorophosphonate-reactive serine proteases in human liver soluble proteomes at 100 uM by competitive activity based protein profiling | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553238 | Clearance in dog at 0.5 mg/kg, iv or 0.5 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553241 | Oral bioavailability in dog at 0.5 mg/kg, iv | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553246 | Metabolic stability in rat hepatocytes assessed as glutathione conjugate formation | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553218 | Inhibition of CYP3A4 uisng midazolam substrate | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1566258 | Inhibition of FAAH in rat brain at 10 uM incubated for 30 mins followed by incubation with FP-Rh probe for 45 mins by ABPP assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
| Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology. |
AID553221 | Irreversible inhibition of His-tagged rat FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli preincubated for 60 mins before oleamide substrate addition | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553234 | Half life in rat at 1 mg/kg, iv | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553220 | Inhibition of His-tagged human FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli preincubated for 60 mins before oleamide substrate addition | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553250 | Antihyperalgesic activity in Sprague-Dawley rat model of complete Freund's adjuvant-induced inflammatory pain model assessed as reduction in mechanical allodynia at 0.1 mg/kg, po measured 4 hrs post dose | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1573871 | Antihyperalgesic activity in Sprague-Dawley rat model of cisplatin-induced peripheral neuropathy assessed as increase in paw withdrawal latency at 10 mg/kg, po administered once daily via gavage for 7 days measured 4 hrs post last dose by plantar test | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model. |
AID553215 | Irreversible inhibition of His-tagged human FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli assessed as ratio of Kinact to Ki by GDH-coupled FAAH assay | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553216 | Irreversible inhibition of His-tagged rat FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli assessed as ratio of Kinact to Ki by GDH-coupled FAAH assay | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553236 | Cmax in dog at 0.5 mg/kg, po | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID553219 | Inhibition of CYP3A4 uisng testosterone substrate | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1566260 | Inhibition of ABHD6 in rat brain at 10 uM incubated for 30 mins followed by incubation with FP-Rh probe for 45 mins by ABPP assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
| Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology. |
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. |
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. |
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. |
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. |
AID1345299 | Human Fatty acid amide hydrolase (Hydrolases) | 2011 | ACS medicinal chemistry letters, Feb-10, Volume: 2, Issue:2
| Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
AID1345299 | Human Fatty acid amide hydrolase (Hydrolases) | 2017 | Science (New York, N.Y.), 06-09, Volume: 356, Issue:6342
| Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |