| Assay ID | Title | Year | Journal | Article |
|---|
| AID384243 | Inhibition of glucose-induced insulin secretion in Wistar rat pancreatic beta islets assessed as residual insulin secretion relative to control | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
| New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers. |
| AID249972 | Percent residual insulin release in rat pancreatic islets upon incubation with the compound (10 uM) at 37 degree C for 90 mins | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity. |
| AID195741 | Percent inhibition of residual insulin release from rat pancreatic islets in the presence of 16.7mM glucose at 0.1 uM concentration | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID643191 | Drug metabolism in rat liver microsomes assessed as biotransformation into enantiomers of 7-chloro-3-(1-hydroxy-2-propyl)amino-4H-1,2,4-benzothiadiazine 1,1-dioxide by capillary electrophoresis | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Hydroxylated analogues of ATP-sensitive potassium channel openers belonging to the group of 6- and/or 7-substituted 3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides: toward an improvement in sulfonylurea receptor 1 selectivity and metabolism stabil |
| AID246913 | Concentration giving 50% relaxation of the 30 mM KCl-induced contraction of rat aortic rings (n=6) | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID195744 | Percent inhibition of residual insulin release from rat pancreatic islets in the presence of 16.7 mM glucose at 50 uM concentration | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID444898 | Inhibition of glucose-induced insulin secretion in rat pancreatic islets assessed as residual insulin release at 1 uM | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity. |
| AID444897 | Inhibition of glucose-induced insulin secretion in rat pancreatic islets assessed as residual insulin release at 10 uM | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity. |
| AID286541 | Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as repolarization of tolbutamide-induced membrane depolarization | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
| Virtual screening for novel openers of pancreatic K(ATP) channels. |
| AID596291 | Myorelaxant effect in Wistar rat uterus smooth muscle assessed as inhibition of contractions induced by bolus of oxytocin injected in superfusion system at 50 uM | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels. |
| AID195743 | Percent inhibition of residual insulin release from rat pancreatic islets in the presence of 16.7 mM glucose at 10 uM concentration | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID251164 | Percent efficacy for inhibition of glucose stimulated insulin release from beta TC6 cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels. |
| AID444896 | Inhibition of glucose-induced insulin secretion in rat pancreatic islets assessed as residual insulin release at 50 uM | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity. |
| AID444903 | Dissociation constant, pKa of the compound | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity. |
| AID384241 | Inhibition of glucose-induced insulin secretion in Wistar rat pancreatic beta islets assessed as residual insulin secretion at 10 uM relative to control | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
| New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers. |
| AID195359 | Effective dose required for relaxation of the 30 mM KCl-induced contraction of rat aortic rings | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID252258 | Ratio of EC50 required to relax KCl induced rat aorta ring contractions to that of IC50 required to inhibit insulin release in rat pancreatic islets | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity. |
| AID596288 | Inhibition of glucose induced insulin secretion from rat Pancreatic islet assessed as percentage of residual insulin release | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels. |
| AID444899 | Inhibition of glucose-induced insulin secretion in rat pancreatic islets assessed as residual insulin release at 0.1 uM | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity. |
| AID384245 | Ratio of IC50 for glucose-induced insulin secretion in Wistar rat pancreatic beta islets to EC50 for myorelaxant activity in Wistar rat aorta rings | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
| New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers. |
| AID249971 | Percent residual insulin release in rat pancreatic islets upon incubation with the compound (1 uM) at 37 degree C for 90 mins | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity. |
| AID643190 | Selectivity index, ratio of EC50 for activation of KATP channel in rat aortic rings assessed as relaxation of KCl-induced contraction to IC50 for activation of SUR1 in rat pancreatic islets assessed as inhibition of glucose-induced insulin secretion | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Hydroxylated analogues of ATP-sensitive potassium channel openers belonging to the group of 6- and/or 7-substituted 3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides: toward an improvement in sulfonylurea receptor 1 selectivity and metabolism stabil |
| AID195742 | Percent inhibition of residual insulin release from rat pancreatic islets in the presence of 16.7 mM glucose at 1 uM concentration | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID248864 | Concentration required to inhibit insulin release in rat pancreatic islets by 50% upon incubation with the compound at 37 degree C for 90 mins | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity. |
| AID247947 | Concentration required for 50% inhibition of insulin release in rat pancreatic B-cells | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID286542 | Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as activation of K+ currents | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
| Virtual screening for novel openers of pancreatic K(ATP) channels. |
| AID384244 | Myorelaxant activity in potassium depolarized Wistar rat aorta rings assessed as relaxation of KCl-induced contraction | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
| New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers. |
| AID643188 | Activation of SUR1 in rat pancreatic islets assessed as inhibition of glucose-induced insulin secretion | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Hydroxylated analogues of ATP-sensitive potassium channel openers belonging to the group of 6- and/or 7-substituted 3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides: toward an improvement in sulfonylurea receptor 1 selectivity and metabolism stabil |
| AID596290 | Myorelaxant effect in Wistar rat uterus smooth muscle assessed as inhibition of contractions induced by bolus of oxytocin injected in superfusion system at 100 uM | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels. |
| AID29349 | pKa value determined at pH 7.4 | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID249397 | ED50/IC50 ratio was determined | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID236597 | Ionization constant was determined | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID248152 | Potency by glucose stimulated insulin release from HEK 293 cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels. |
| AID253201 | Effect on insulin secretion from rat pancreatic islets at 10 uM concentration (n=32) | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID248136 | Concentration required for inhibition of glucose stimulated insulin release from beta TC6 cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels. |
| AID253213 | Effect on insulin secretion from rat pancreatic islets at 50 uM concentration (n=35) | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID728946 | Activation of ATP-sensitive potassium channel opening in albino rat pancreatic islets assessed as inhibition of glucose-induced insulin release measured as residual insulin release at 10 uM after 90 mins by radioimmunoassay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| 1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action. |
| AID246525 | Concentration required to relax KCl induced rat aorta ring contractions by 50% upon incubation with the compound at 37 degree C for 90 mins | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity. |
| AID233236 | Estimated selectivity ratio of ED50 and IC50 in rat was calculated | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID643193 | Hydrosolubility of the compound by HPLC analysis | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
| Hydroxylated analogues of ATP-sensitive potassium channel openers belonging to the group of 6- and/or 7-substituted 3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides: toward an improvement in sulfonylurea receptor 1 selectivity and metabolism stabil |
| AID248509 | inhibitory concentration required for repolarization of beta cell membrane potential in presence of 10 mM glucose | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 2-(4-Methoxyphenoxy)-5-nitro-N-(4-sulfamoylphenyl)benzamide activates Kir6.2/SUR1 K(ATP) channels. |
| AID253190 | Effect on insulin secretion from rat pancreatic islets at 1 uM concentration (n=31) | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID596292 | Myorelaxant effect in Wistar rat uterus smooth muscle assessed as inhibition of contractions induced by bolus of oxytocin injected in superfusion system at 10 uM | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels. |
| AID286545 | Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as repolarization of tolbutamide-induced membrane depolarization relative to BPDZ73 | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
| Virtual screening for novel openers of pancreatic K(ATP) channels. |
| AID179405 | Concentration required to inhibit insulin release in rat | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. |
| AID728947 | Activation of ATP-sensitive potassium channel opening in albino rat aorta rings assessed as relaxation of KCl-induced contraction of aorta rings | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| 1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action. |
| AID249975 | Percent residual insulin release in rat pancreatic islets upon incubation with the compound (0.1 uM) at 37 degree C for 90 mins | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
| 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity. |
| AID286544 | Inhibition of insulin release from rat INS-1E cells | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
| Virtual screening for novel openers of pancreatic K(ATP) channels. |
| AID444900 | Myorelaxant activity in rat aortic ring assessed as inhibition of KCL-induced contraction | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Chloro-substituted 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel activators: impact of the position of the chlorine atom on the aromatic ring on activity and tissue selectivity. |
| AID384242 | Inhibition of glucose-induced insulin secretion in Wistar rat pancreatic beta islets assessed as residual insulin secretion at 1 uM relative to control | 2008 | Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
| New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers. |
| AID596282 | Dissociation constant, pKa of the compound | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
| Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |