Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
AID1458811 | Reduction in cocaine-induced reinstatement of cocaine seeking behavior in Sprague-Dawley rat at 30 mg/kg pretreated for 10 mins followed by cocaine treatment on day following last extinction session | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1776939 | Antagonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization preincubated for 15 mins followed by agonist addition and measured every 1 sec for 90 secs | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1458809 | Half life in rat liver microsomes in presence of NADPH by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1458810 | Clearance in rat liver microsomes in presence of NADPH by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1776936 | Allosteric antagonist activity at N-terminal 3HA-tagged human CB1 receptor expressed in HEK293 cells assessed as reduction in CP55940-stimulated inhibition of forskolin-induced cAMP accumulation measured for 20 mins by BRET assay | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1458803 | Allosteric modulation of CB1 receptor in CD-1 mouse cerebellar membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding after 60 mins | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1616828 | Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as increase in specific binding of [3H]CP55,940 incubated for 90 mins by radioligand binding assay relative to control | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616819 | Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by c | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1426536 | Allosteric modulation at CB1 receptor (unknown origin) expressed in HEK293T cell membranes assessed as inhibition of CP55,940 induced [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method | | | |
AID1426535 | Positive allosteric modulation of CB1 receptor (unknown origin) expressed in HEK293T cell membranes assessed as increase in [3H]CP55,940 binding by liquid scintillation counting method | | | |
AID1776940 | Agonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as stimulation of calcium mobilization measured every 1 sec for 90 secs by Calcium-3 dye based FLIPR assay relative to Emax of CP55940 | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1161647 | Antagonist activity at human CB1 receptor stably expressed in RD-HGA16 cells assessed as inhibition of CP55,940-induced calcium mobilization after 15 mins by FLIPR assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). |
AID1458804 | Allosteric modulation of CB1 receptor in rat cerebellar membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1273373 | Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). |
AID1616825 | Allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1458805 | Allosteric modulation of CB1 receptor in HEK293 cell membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1616821 | Displacement of [3H]CP55,940 from human CB1 receptor | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1458800 | Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by calciu | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1366770 | Inhibition of FAAH in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels up to 10 uM preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1366774 | Inhibition of [ethanolamine-1-3H]AEA uptake in human U937 cell homogenate preincubated for 20 mins followed by AEA addition measured after 5 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1616820 | Allosteric antagonist activity at human CB1 receptor by Ca2+ assay | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1776934 | Allosteric antagonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization preincubated for 15 mins followed by agonist addition and measured every 1 sec f | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1616823 | Half life in rat liver microsomes | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1532934 | Agonist activity at CB1 receptor (unknown origin) relative to CP55940 | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
| Allosteric CB |
AID1776935 | Allosteric antagonist activity at human CB1 receptor expressed in HEK293 cell membrane assessed as inhibition of CP55940-stimulated [35S]GTPgammaS binding incubated for 60 mins by [35S]GTP-gammaS binding assay | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1616834 | Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding at 10 uM incubated for 60 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1458799 | Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 assessed as increase in calcium mobilization at 10 uM measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay relative to CP55,940 | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1616838 | Half life in rat liver microsomes in presence of NADPH by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616833 | Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616841 | Apparent permeability from apical to basolateral side in MDCK-MDR1 cells incubated up to 90 mins by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616830 | Agonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as increase in calcium mobilization at 10 uM measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay relative to CP55,940 | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1161648 | Agonist activity at human CB1 receptor stably expressed in RD-HGA16 cells assessed as calcium mobilization at 10000 nM after 15 mins by FLIPR assay relative to CP55,940 | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). |
AID1616843 | Efflux ratio from basolateral to apical side over apical to basolateral side in MDCK-MDR1 cells incubated up to 90 mins by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616822 | Allosteric antagonist activity at mouse CB1 receptor by GTPgammaS assay | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1161652 | Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). |
AID1161649 | Antagonist activity at human CB2 receptor stably expressed in CHO-RD-HGA16 cells assessed as inhibition of CP55,940-induced calcium mobilization after 15 mins by FLIPR assay | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). |
AID1616842 | Apparent permeability from basolateral to apical side in MDCK-MDR1 cells incubated up to 90 mins by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616826 | Allosteric modulator activity at CB1 receptor in mouse cerebellar membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1366773 | Inhibition of MAGL in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1616824 | Allosteric modulator activity at human CB1 receptor expressed in CHO-RD-HGA16 cells co-expressing Galpha16 assessed as suppression of 100 nM CP55,940-induced calcium mobilization pre-incubated for 15 mins by Calcium 5 dye based FLIPR assay | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616837 | Ratio of IC50 for allosteric modulator activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of 100 nM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method IC50 for allosteric m | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1776937 | Agonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as stimulation of calcium mobilization measured every 1 sec for 90 secs by Calcium-3 dye based FLIPR assay relative to Emax of CP55940 | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1366772 | Inhibition of FAAH in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1616836 | Allosteric modulator activity at CB1 receptor in mouse cerebellar membranes assessed as suppression of 1 uM CP55,940-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1273375 | Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). |
AID1616840 | Kinetic solubility in phosphate buffer at 400 uM incubated for 2 hrs by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616832 | Allosteric modulator activity at human CB1 receptor expressed in HEK293 cells assessed as suppression of 100 nM CP55,940-induced reduction in forskolin-stimulated cAMP production pre-incubated for 25 mins before forskolin and CP55,940 addition and measure | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1532935 | Allosteric modulation of CB1 receptor (unknown origin) assessed as inhibition of CP55940-induced [35S]GTPgammaS binding | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
| Allosteric CB |
AID1458806 | PAM antagonist activity at CB1 receptor in CD-1 mouse cerebellar membranes assessed as inhibition of CP55,940-induced [35S]GTPgammaS binding after 60 mins | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1426538 | Positive allosteric modulation of CB1 receptor (unknown origin) expressed in HEK293T cell membrane assessed as ERK1/2 phosphorylation in presence of beta-arrestin1 siRNA at 10 uM incubated for 5 mins by Western blot method | | | |
AID1273376 | Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as effect on CP55,940-induced inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by CP55,940 addition measured for 30 mins by HitHunte | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). |
AID1161653 | Displacement of [3H]CP55,940 from human CB1 receptor expressed in HEK293 cells after 1 hr by scintillation counting relative to control | 2014 | Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
| Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1). |
AID1776938 | Antagonist activity at human CB2 receptor expressed in CHO-RD-HGA16 cells overexpressing Galpha16 assessed as inhibition of CP55940-stimulated calcium mobilization at 10 uM preincubated for 15 mins followed by agonist addition and measured every 1 sec for | 2021 | Bioorganic & medicinal chemistry, 07-01, Volume: 41 | Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. |
AID1366769 | Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO-K1 cell membranes after 1.5 hrs by liquid scintillation counting assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1458801 | Agonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as increase in calcium mobilization at 10 uM measured at 1 sec interval for 90 secs by calcium-5 dye based FLIPR assay relative to CP55,940 | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1532933 | Allosteric modulation of CB1 receptor (unknown origin) assessed as inhibition of calcium mobilization by FLIPR assay | 2018 | ACS medicinal chemistry letters, Dec-13, Volume: 9, Issue:12
| Allosteric CB |
AID1366771 | Inhibition of MAGL in human U937 cell homogenate assessed as decrease in [ethanolamine-1-3H]AEA levels up to 10 uM preincubated for 30 mins followed by AEA addition measured after 15 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1458798 | Allosteric modulation of human CB1 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of CP55,940-induced calcium mobilization preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 secs by calc | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
| Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution. |
AID1366765 | Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cell membranes assessed as induction of [3H]CP55,940 binding after 1.5 hrs by liquid scintillation counting assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1616831 | Antagonist activity at human CB2 receptor expressed in CHO cells co-expressing Galpha16 assessed as inhibition of EC80 CP55,940-induced calcium mobilization at 10 uM preincubated for 15 mins followed by CP55,490 addition measured at 1 sec interval for 90 | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1366764 | Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cell membranes assessed as induction of [3H]CP55,940 binding at 0.001 to 100 uM after 1.5 hrs by liquid scintillation counting assay relative to control | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1273374 | Negative allosteric modulator activity at human CB1R expressed in CHO-K1 cells assessed as inhibition of CP55,940-induced beta-arrestin recruitment preincubated for 30 mins followed by CP55,940 addition measured for 90 mins by PathHunter assay relative to | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
| Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s). |
AID1366768 | Negative allosteric modulation of human CB1 receptor expressed in HEK293 cells assessed as inhibition of 33 nM CP55,940-induced SRE transcriptional activity after 5 hrs by luciferase reporter gene assay | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
| Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor. |
AID1616839 | Clearance in rat liver microsomes in presence of NADPH incubated up to 45 mins by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
AID1616829 | Agonist activity at human CB1 receptor expressed in CHO-RD-HGA16 cells co-expressing Galpha16 assessed as suppression stimulation of calcium mobilization incubated for 45 mins by Calcium 5 dye based FLIPR assay relative to CP55,940 | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |