| Assay ID | Title | Year | Journal | Article |
|---|
| AID349617 | Inhibition of CP-55940-induced hypothermia in NSA mouse at 1 mg/kg, ip dosed 30 mins before CP-55940 challenge measured 60 mins post dose | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID328662 | Binding affinity to CB2 receptor | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
| Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model. |
| AID255682 | Antagonism of CP-55940 induced hypotension in rat expressed as effective dose upon peroral administration | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID464993 | Inhibition of CP-55940-induced hypotension in po dosed rat | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists. |
| AID349613 | Metabolic stability in human microsomes assessed as intrinsic clearance | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID428190 | Displacement of [3H]rimonabant from human CB2 receptor expressed in HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Discovery and functional evaluation of diverse novel human CB(1) receptor ligands. |
| AID349610 | Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID464992 | Selectivity ratio of Ki for human cannabinoid CB1 receptor to Ki for human cannabinoid CB2 receptor | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists. |
| AID464989 | Displacement of [3H]CP-55940 from human cannabinoid CB1 receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists. |
| AID349616 | Inhibition of CP-55940-induced hypothermia in NSA mouse at 3 mg/kg, ip dosed 30 mins before CP-55940 challenge measured 60 mins post dose | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID349609 | Inverse agonist activity at CB1 receptor assessed as repression of basal receptor activity by mammalian cell-based receptor selection and amplification technology method | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID15431 | Mean percentage of compound transport through P-glycoprotein; expressed as p-glycoprotein affinity | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID464991 | Displacement of [3H]CP-55940 from human cannabinoid CB2 receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists. |
| AID254403 | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2 | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID319062 | Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity. |
| AID49475 | In vivo effective dose to antagonise cannabinoid receptor 1 agonist (CP-55940) induced hypotension in rat upon peroral administration | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID254404 | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1 | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID317745 | Displacement of radioligand from human CB1 receptor expressed in HEK293 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Discovery of a novel class of selective human CB1 inverse agonists. |
| AID321306 | Inhibition of 5% sucrose solution intake in Zucker fa/fa rat at 10 mg/kg, po on day 7 after 1 hr | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole. |
| AID19206 | Partition coefficient (logP) | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID255585 | Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID253843 | Partition coefficient (logP) (HPLC) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID49471 | In vivo least effective dose required to antagonise cannabinoid receptor 1 agonist (WIN-55212) induced hypothermia in mouse upon peroral administration | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID255466 | Antagonism of WIN-55212-2 induced hypothermia in mice expressed as least effective dose upon peroral administration | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID328661 | Binding affinity to CB1 receptor | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
| Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model. |
| AID15432 | Mean percentage of compound transport through membrane; expressed as membrane transport | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID49329 | Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID349618 | Inhibition of food intake in 18 hrs fasted Sprague-Dawley rat at 10 mg/kg, po after 2.5 hrs relative to control | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID349614 | Metabolic stability in rat microsomes assessed as intrinsic clearance | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID1177620 | Receptor occupancy at CB1 receptor in rat frontal cortex at 10 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
| Peripherally restricted CB1 receptor blockers. |
| AID274572 | Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity. |
| AID625578 | Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies. |
| AID317748 | Selectivity ratio, Ki for human CB2 receptor to Ki for human CB1 receptor | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Discovery of a novel class of selective human CB1 inverse agonists. |
| AID321303 | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation per ug of protein at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole. |
| AID428189 | Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Discovery and functional evaluation of diverse novel human CB(1) receptor ligands. |
| AID255178 | P-glycoprotein-based membrane transport factor, expressed as the ratio of the bottom to top transport and top to bottom transport | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
| Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. |
| AID49833 | Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID49305 | Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID349611 | Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
| Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. |
| AID464990 | Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists. |
| AID274573 | Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity. |
| AID1346728 | Human CB2 receptor (Cannabinoid receptors) | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| AID1346701 | Human CB1 receptor (Cannabinoid receptors) | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. |
| 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. |
| 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. |
| 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. |
| 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] |