| Assay ID | Title | Year | Journal | Article |
|---|
| AID411779 | Inhibition of P-gp assessed as ATP turnover at 1.25 to 25 mM by cell-based ATPase assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411332 | Reversal of CP-55940-induced locomotor activity in ICR mouse at 10 mg/kg, sc pretreated 15 mins before CP-55940 challenge measured 25 mins post challenge | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411331 | Inhibition of human ERG | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID1392453 | Displacement of [3H]CP55940 from human CB2 expressed in CHOK1 cell membranes | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor. |
| AID425918 | Antiobesity activity in TBU8 high fat diet-induced obese C57/BL6 mouse assessed as serum LDL-cholesterol level at 30 mg/kg, po administered once daily for 14 days (Rvb=0.84+/-0.03 mmol/mL) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. |
| AID411783 | Thermodynamic solubility in USP simulated gastric fluid at pH 1.2 by reversed phase HPLC | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411333 | Reversal of CP-55940-induced catalepsy in ICR mouse at 10 mg/kg, sc pretreated 15 mins before CP-55940 challenge measured 90 mins post challenge | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411781 | Induction of P-gp-mediated efflux in mdr1a/1b knockout mouse model | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411326 | Displacement of [3H]SR141716A from CB1 receptor in rat brain | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID710519 | Permeability from apical to basolateral side in dog MDCK cells expressing MDR-1 gene | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists. |
| AID411780 | Inhibition of P-gp by cell-based calcein-acetoxymethyl ester assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411777 | Fraction unbound in Sprague-Dawley rat brain at 10 mg/kg, po after 2 hrs | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411329 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID1392454 | Selectivity ratio of Ki for human CB2 to Ki for human CB1 | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor. |
| AID411335 | Reversal of CP-55940-induced hypothermia in ICR mouse at 10 mg/kg, sc pretreated 15 mins before CP-55940 challenge measured 65 mins post challenge | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID425913 | Antiobesity activity in TBU8 high fat diet-induced obese C57/BL6 mouse assessed as body weight at 30 mg/kg, po administered once daily for 14 days (Rvb=41.90 g) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. |
| AID411327 | Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID425915 | Antiobesity activity in TBU8 high fat diet-induced obese C57/BL6 mouse assessed as serum cholesterol level at 30 mg/kg, po administered once daily for 14 days (Rvb = 5.35+/-0.12 mmol/mL) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. |
| AID660986 | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity. |
| AID411778 | Ratio of fraction unbound in Sprague-Dawley rat brain to plasma at 10 mg/kg, po after 2 hrs | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID425916 | Antiobesity activity in TBU8 high fat diet-induced obese C57/BL6 mouse assessed as serum triglyceride level at 30 mg/kg, po administered once daily for 14 days (Rvb = 1.42+/-0.04 mmol/mL) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. |
| AID411515 | Anorectic activity in Sprague-Dawley rat assessed as reduction in food intake at 10 mg/kg, po measured at 10 mins interval for 2 hrs by fast-induced refeeding assay relative to control | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID660991 | Permeability from apical to basal side of MDCK cells expressing human mdr1 gene | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity. |
| AID1392452 | Displacement of [3H]CP55940 from human CB1 expressed in CHOK1 cell membranes | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor. |
| AID411325 | Lipophilicity, log D of the compound | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411328 | Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID710523 | Antagonist activity at human CB1 receptor transfected in CHO-K1 cells co-expressing Galphaq16 assessed as intracellular calcium mobilization using Calcein-4 AM by fluorescence assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Diphenyl purine derivatives as peripherally selective cannabinoid receptor 1 antagonists. |
| AID1138123 | Elimination half life in human | 2013 | Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
| Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties. |
| AID1392478 | Suppression of CP55940-induced hypothermia in C57BL/6 mouse assessed as reduction in body temperature at 30 mg/kg, po administered via gavage pretreated for 30 mins followed by CP55940 addition measured at regular interval up to 4 hrs | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor. |
| AID425914 | Antiobesity activity in TBU8 high fat diet-induced obese C57/BL6 mouse assessed as serum glucose level at 30 mg/kg, po administered once daily for 14 days (Rvb = 9.52+/-0.38 mmol/mL) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. |
| AID411334 | Reversal of CP-55940-induced analgesia in ICR mouse at 10 mg/kg, sc pretreated 15 mins before CP-55940 challenge measured 45 mins post challenge by hot plate method | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411776 | Fraction unbound in Sprague-Dawley rat plasma at 10 mg/kg, po after 2 hrs | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID1392451 | Antagonist activity at human CB1 expressed in CHOK1 cells co-expressing Galpha-q16 assessed as reduction in CP55940-induced inositol phosphatase 3-mediated intercellular calcium mobilization by Calcein-4 AM dye-based FLIPR assay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor. |
| AID411782 | Thermodynamic solubility in 0.1 M phosphate buffered saline at pH 6.5 by reversed phase HPLC | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID411330 | Metabolic stability in human liver microsomes assessed as intrinsic clearance | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID425917 | Antiobesity activity in TBU8 high fat diet-induced obese C57/BL6 mouse assessed as serum HDL-cholesterol level at 30 mg/kg, po administered once daily for 14 days (Rvb=4.42+/-0.08 mmol/mL) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1346753 | Rat CB1 receptor (Cannabinoid receptors) | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| AID1798798 | CB Receptor Binding Assay from Article 10.1021/jm8012932: \\Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 re | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
| Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |