Assay ID | Title | Year | Journal | Article |
AID1154951 | Apparent permeability across apical to basolateral side in human Caco2 cells | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
AID25820 | PKa values of the compound | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. |
AID728958 | Lipophilicity, log D of the compound | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID71822 | Binding affinity against Gamma-aminobutyric acid A receptor in rat cerebral cortex | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. |
AID1154950 | Displacement of [3H]-muscimol from GABAA receptor in Sprague-Dawley rat brain membranes after 1 hr by microbeta scintillation counting analysis | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
AID472677 | Displacement of [3H]muscimol from GABAA in rat synaptic membrane by scintillation counting | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships. |
AID71386 | Affinity for GABA-B receptor by inhibiting GABA uptake into rat brain synaptosomes | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. |
AID239462 | Displacement of [3H]muscimol from rat brain gamma-aminobutyric-acid GABA-A receptor | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
| Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. |
AID1154948 | Binding affinity to human full length Glu-plasminogen in buffer assessed as inhibition of interaction with fibrin preincubated for 15 mins followed by thrombin addition measured every 2 mins for 15 hrs by Spectra-Max reader analysis in presence of tPA | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
AID1154949 | Binding affinity to full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin in presence of tPA | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
AID728960 | Ratio of TXA IC50 to compound IC50 for plasminogen/fibrinogen interaction in human platelet-poor plasma by microtiter plate analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID71975 | Inhibition of Gamma-aminobutyric acid A (GABA-A) receptor in vitro by whole-cell patch-clamp recording in cultured cerebral cortical neurones | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology. |
AID132660 | Electrophysiology using Whole-cell patch-clamp recordings in mouse embryos | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. |
AID196024 | Concentration inhibiting GABA uptake rat brain synaptosomes. | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. |
AID281443 | Displacement of [3H]GABA from GABAB receptor in Sprague-Dawley rat brain synaptic membrane at 100 uM | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| 4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships. |
AID72457 | Affinity for GABA-A receptor alpha by inhibiting binding of [3H]muscimol to rat brain synaptosomes | 2002 | Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
| Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. |
AID472676 | Agonist activity at human GABAA alpha-1-beta-2-gamma-2 receptor expressed in mouse tsA201 cells at < 500 uM by FMP red assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships. |
AID1154976 | Potency index, ratio of tranexamic acid IC50 to compound IC50 for full length human Glu-plasminogen in buffer assessed as inhibition of interaction with fibrin | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
AID71392 | Inhibition of Gamma-aminobutyric acid type B receptor of rat cortex | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. |
AID728963 | Dissociation constant, pKa of the compound at acidic pH by pressure-assisted capillary electrophoresis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID248086 | In vitro concentration required to inhibit peak currents in cerebral cortical neurones of rat | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
| Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. |
AID728962 | Dissociation constant, pKa of the compound at basic pH by pressure-assisted capillary electrophoresis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID72135 | In vitro inhibition of [3H]muscimol to rat brain synaptic membranes | 2000 | Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
| A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology. |
AID728961 | Apparent permeability from apical to basolateral side in human Caco2 cells at pH 6.5 by LC/MS analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID728965 | Inhibition of plasminogen/fibrinogen interaction in pooled citreated human platelet-poor plasma assessed as inhibition of lysis of CaCl2/t-PA-induced clot by microtiter plate analysis | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID728959 | Ratio of TXA IC50 to compound IC50 for human Glu-plasminogen/fibrinogen interaction by clot-lysis buffer assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID235130 | Reversal potential is determined electrophysiologically against the GABA A receptor | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol. |
AID281444 | Antagonist activity at human GABAA alpha-1-beta-3-gamma-2S expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| 4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships. |
AID728964 | Inhibition of human Glu-plasminogen/fibrinogen interaction in HEPES buffer assessed as inhibition of lysis of thrombin-induced clot preincubated for 15 mins prior to thrombin addition measured for 15 hrs by clot-lysis buffer assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
| Potent fibrinolysis inhibitor discovered by shape and electrostatic complementarity to the drug tranexamic acid. |
AID281442 | Displacement of [3H]muscimol from GABAA receptor in Sprague-Dawley rat brain synaptic membrane | 2007 | Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
| 4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships. |
AID1154977 | Potency index, ratio of tranexamic acid IC50 to compound IC50 for full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |