Assay ID | Title | Year | Journal | Article |
AID350596 | Modulator activity at alpha7 nAChR in Xenopus laevis oocytes cells assessed as decay of acetylcholine-evoked electric current response at -60 mV by two-electrode voltage clamp technique | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350609 | Oral bioavailability in dog at 1 umol/kg | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559192 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 3 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 16.33 sec) | | | |
AID1559292 | Drug level in Wistar rat brain at 3 mg/kg, po after 2 hrs by LC-MS/MS analysis | | | |
AID350611 | Volume of distribution at steady state in monkey at 0.5 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559219 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for novel object at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 12.81 sec) | | | |
AID1559213 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in novel object discrimination index at 0.05 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 0.21 No_unit | | | |
AID1731328 | Efflux ratio of apparent permeability in vinblastine-treated human Caco2 cells at 1 uM after 180 mins by HPLC or UHPLC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID1559202 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 0.15 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 15.63 se | | | |
AID350615 | Improvement in gating deficits in DBA/2 mouse model of sensory gating deficits assessed as reduction in ratio of response to test stimulus relative to preceding response to conditioning stimulus at 0.1 to 10 umol/kg, ip by paired auditory stimulus paradig | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350592 | Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of agonist-induced intracellular calcium level by FLIPR assay relative to 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559259 | Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 0.3 | | | |
AID350617 | Drug level in brain of DBA/2 mouse model of sensory gating deficits at 1 umol/kg, ip | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731317 | Kinetic solubility of compound in in PBS buffer at pH 7.4 by HPLC analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID350612 | Plasma clearance in monkey at 0.5 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559191 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 3 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 13.95 sec) | | | |
AID350602 | Plasma clearance in rat at 2 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731354 | Cognitive enhancing effect in scopolamine-induced NMRI mouse model of amnesia assessed as increase in recognition index at 3 mg/kg, ip by Y maze test | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID1559203 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 0.15 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 8. | | | |
AID350598 | Activity at human recombinant alpha4beta2 nAChR expressed in HEK293 cells assessed as potentiation of nicotine-evoked calcium transients up to 30 uM | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559265 | Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 0.9 No_unit) | | | |
AID350594 | Modulator activity at alpha7 nAChR in Xenopus laevis oocytes cells assessed as activation of electric currents at 0.1 nM to 10 uM at -60 mV by two-electrode voltage clamp technique | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731324 | Intrinsic clearance in mouse liver microsome at 1 to 2.5 uM up to 40 mins | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID350597 | Modulator activity at alpha7 nAChR in rat neonatal cortical neurons assessed as enhancement of (R)-4-chloro-N-(quinuclidin-8-yl)benzamide-induced calcium flux response at 5 uM by FLIPR assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559244 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 16.11 sec) | | | |
AID1559228 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 10.20 sec) | | | |
AID350616 | Drug level in brain of DBA/2 mouse model of sensory gating deficits at 0.1 umol/kg, ip | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350618 | Drug level in brain of DBA/2 mouse model of sensory gating deficits at 10 umol/kg, ip | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559263 | Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 9. | | | |
AID350604 | Oral bioavailability in rat at 2 umol/kg | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350608 | Cmax in dog at 1 umol/kg, po | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559270 | Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index at 0.15 mg/kg, po for 7 days and measured on day 9 (Rvb = 1.05 No_unit) | | | |
AID350607 | Plasma clearance in dog at 0.5 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350624 | Inhibition of human ERG channel | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350623 | Displacement of [3H]dofetilide from human ERG channel | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559294 | Ratio of drug level in brain to plasma in Wistar rat at 3 mg/kg, po after 2 hrs by LC-MS/MS analysis | | | |
AID350603 | Cmax in rat at 2 umol/kg, po | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559199 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in novel object discrimination index at 3 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 0.03 No_unit) | | | |
AID350625 | Plasma concentration Sprague-Dawley rat at 3 mg/kg | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559229 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for novel object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 15.37 sec) | | | |
AID1164738 | Positive allosteric modulation at human alpha7 nACHR expressed in Xenopus oocyte assessed as potentiation of 200 uM ACh-induced current at holding potential of -80 mV by electrophysiology | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Chalcones as positive allosteric modulators of α7 nicotinic acetylcholine receptors: a new target for a privileged structure. |
AID350595 | Modulator activity at alpha7 nAChR in Xenopus laevis oocytes cells assessed as enhancement of acetylcholine-evoked electric currents at -60 mV by two-electrode voltage clamp technique | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559307 | Positive allosteric modulatory activity against alpha7 nAChR in human IMR-32 cells assessed as potentiation of PNU-282987-induced Ca2+ efflux at by FLIPR assay | | | |
AID1559247 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for novel object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 12.09 sec) | | | |
AID1559218 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for familiar object at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 10.6 sec) | | | |
AID350613 | Cmax in monkey at 1 umol/kg, po | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731320 | Agonist activity at recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in intra cellular calcium level after 10 mins by fluorescence relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID350599 | Activity at human recombinant alpha3beta4 nAChR expressed in HEK293 cells assessed as potentiation of nicotine-evoked calcium transients up to 30 uM | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350593 | Metabolic stability in rat liver microsomes assessed as compound remaining after 30 mins | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350601 | Volume of distribution at steady state in rat at 2 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559217 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object2 at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 21.07 sec) | | | |
AID1559279 | Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index at 0.15 mg/kg, po for 7 days measured after 24 hrs (Rvb = 0.93 No_unit) | | | |
AID1559256 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in discrimination index at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 0.21 No_unit) | | | |
AID1559224 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in novel object discrimination at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 0.08 No_unit) | | | |
AID1559267 | Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 0.15 mg/kg, po for 7 days and measured on day 9 (Rvb = -0.5%) | | | |
AID350620 | Inhibition of CYP3A4 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350619 | Improvement in gating deficits in DBA/2 mouse model of sensory gating deficits assessed as reduction in ratio of response to test stimulus relative to preceding response to conditioning stimulus at 0.1 umol/kg, ip by paired auditory stimulus paradigm assa | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559246 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 8.59 sec) | | | |
AID1731326 | Apparent permeability across apical to basolateral side in vinblastine-treated human Caco2 cells at 1 uM after 180 mins by HPLC or UHPLC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID350610 | Half life in monkey at 0.5 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559204 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as increase in exploration time for novel object in retention trial at 0.15 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test | | | |
AID1559261 | Improvement in social recognition time delay-induced Sprague-Dawley rat model of amnesia assessed as reduction in recognition index 3 mg/kg, po administered as single dose prior to 1 hr training and measured after 30 mins (Rvb = 1 No_unit) | | | |
AID350626 | Plasma concentration Sprague-Dawley rat at 10 mg/kg | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559226 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 13.73 sec) | | | |
AID350591 | Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of agonist-induced intracellular calcium level by FLIPR assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350614 | Oral bioavailability in monkey at 1 umol/kg | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731325 | Intrinsic clearance in rat liver microsome at 1 to 2.5 uM up to 40 mins | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID1731318 | Agonist activity at recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in intra cellular calcium level at 10 uM after 10 mins by fluorescence relative to control | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID350844 | Plasma concentration Sprague-Dawley rat at 30 mg/kg | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559216 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object1 at 3 mg/kg, po administered as single dose after acquisition trial by novel object recognition test (Rvb = 19.09 sec) | | | |
AID350600 | Half life in rat at 2 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731337 | Lipophilicity, logP of compound | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID1559276 | Improvement in social recognition scopolamine-induced Sprague-Dawley rat model of amnesia assessed as increase in reduction in social investigation time at 0.15 mg/kg, po for 7 days measured after 24 hrs (Rvb =6.59%) | | | |
AID350605 | Half life in dog at 0.5 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350622 | Inhibition of CYP2D6 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559238 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in discrimination index at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 0.12 No_unit) | | | |
AID1731321 | Positive allosteric modulation of recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in choline-induced inward current at 10 uM after 6 to 10 mins by whole-cell patch clamp method | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID350621 | Inhibition of CYP2C9 | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID350606 | Volume of distribution at steady state in dog at 0.5 umol/kg, iv | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1559193 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for familiar object in retention trial at 3 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb = 13.05 | | | |
AID1559201 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object1 in acquisition trial at 0.15 mg/kg, po administered as single dose and measured on day 8 by novel object recognition test (Rvb = 16.11 se | | | |
AID350590 | Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of intracellular calcium level up to 100 uM by FLIPR assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor. |
AID1731323 | Intrinsic clearance in human liver microsome at 1 to 2.5 uM up to 40 mins | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. |
AID1559293 | Drug concentration in Wistar rat plasma at 3 mg/kg, po after 2 hrs by LC-MS/MS analysis | | | |
AID1559227 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 11.76 sec) | | | |
AID1559194 | Memory enhancement effect in time-delay induced Wistar rat model of amnesia assessed as increase in exploration time for novel object in retention trial at 3 mg/kg, po administered as single dose and measured on day 9 by novel object recognition test (Rvb | | | |
AID1559245 | Memory enhancement effect in scopolamine-induced Wistar rat model of amnesia assessed as exploration time for object2 in acquisition trial at 0.05 mg/kg, po for 7 days and measured on day 8 by novel object recognition test (Rvb = 15.63 sec) | | | |
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. |
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. |
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. |
AID1346547 | Human nicotinic acetylcholine receptor alpha4 subunit (Nicotinic acetylcholine receptors) | 2009 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 330, Issue:1
| In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. |
AID1346583 | Human nicotinic acetylcholine receptor alpha7 subunit (Nicotinic acetylcholine receptors) | 2009 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 330, Issue:1
| In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. |
AID1346570 | Human nicotinic acetylcholine receptor alpha3 subunit (Nicotinic acetylcholine receptors) | 2009 | The Journal of pharmacology and experimental therapeutics, Jul, Volume: 330, Issue:1
| In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |