Assay ID | Title | Year | Journal | Article |
AID1167265 | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167250 | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay relative to carbachol | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167248 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein activation assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167251 | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479882 | Displacement of [3H]CGP12177 from human recombinant beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167266 | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay relative to carbachol | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167268 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479871 | Selectivity ratio of Ki for human dopamine D2 receptor to Ki for human dopamine D4 receptor | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167270 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167231 | Displacement of [3H]NMS from human M4 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167269 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by beta-arrestin engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479870 | Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167263 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479884 | Displacement of [3H](+)-pentazocine from sigma1 receptor in Hartley guinea pig brain cortex after 120 mins by scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1479886 | Displacement of [3H]-citalopram from SERT in Sprague-Dawley rat midbrain after 60 mins by scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1479888 | Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay relative to dopamine | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167262 | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay relative to carbachol | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167260 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by BRET based Gq protein engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1851864 | Selectivity ratio of pKi for displacement of [3H]N-methylspiperone from human D3R expressed in HEK293T cell membrane to pKi for displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane | | | |
AID1167261 | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein activation assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479887 | Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167230 | Displacement of [3H]NMS from human M3 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167255 | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167241 | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167240 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479889 | Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167254 | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by BRET based beta-arrestin engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167242 | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein activation assay relative to to carbachol | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479885 | Displacement of [3H]WIN 35,428 from DAT in Sprague-Dawley rat striatum after 120 mins by scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167257 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167252 | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1851860 | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method | | | |
AID1479891 | Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1479880 | Displacement of [3H]prazosin from human recombinant alpha-1B adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167229 | Displacement of [3H]NMS from human M2 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167232 | Displacement of [3H]NMS from human M5 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167228 | Displacement of [3H]NMS from human M1 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479883 | Displacement of [3H]CGP12177 from human recombinant beta2 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by beta counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1851861 | Displacement of [3H]N-methylspiperone from human D3R receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method | | | |
AID1851863 | Selectivity ratio of pKi for displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cell membrane to pKi for displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane | | | |
AID1167256 | Agonist activity at human M4 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay relative to carbachol | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167249 | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based beta-arrestin engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479868 | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167234 | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay relative carbachol | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167264 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167245 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein activation assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479881 | Displacement of [3H]prazosin from human recombinant alpha-1D adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167233 | Agonist activity at human M1 receptor expressed in HEK293T cells by BRET based Gq protein engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167253 | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by BRET based beta-arrestin engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167259 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of xanomeline-induced response by BRET based Gq protein engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167258 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479879 | Displacement of [3H]prazosin from human recombinant alpha-1A adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167237 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1851862 | Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method | | | |
AID1167267 | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479890 | Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1479869 | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167239 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein engagement assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167238 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein engagement assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1167246 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on carbachol-induced response by BRET based Gq protein activation assay relative to untreated control | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
AID1479872 | Selectivity ratio of Ki for human dopamine D3 receptor to Ki for human dopamine D4 receptor | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
AID1167247 | Positive modulatory activity at human M1 receptor expressed in HEK293T cells assessed as effect on xanomeline-induced response by BRET based Gq protein activation assay | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
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. |
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |