Assay ID | Title | Year | Journal | Article |
AID265288 | Toxicity in po dosed Beagle dog | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID443824 | Inhibition of alphavbeta3 integrin-mediated cell adhesion in HUVEC on vitronectin coated plate after 30 mins | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics. |
AID709958 | Selectivity ratio of IC50 for integrin alphaVbeta5 receptor to IC50 for integrin alphaVbeta3 receptor | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrin αVβ3. |
AID265273 | Binding affinity to opioid receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265246 | Inhibition of human recombinant cytochrome P450 2C19 | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265947 | Inhibition of adhesion of K562 cells expressing alphaVbeta3 integrin receptor to vitronectin | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior. |
AID265286 | Decrease in basal rectal temperature in stress-induced hyperthermic 129S6/SvEvTac mouse at 20 mg/kg, po | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265280 | Binding affinity to potassium channel by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265231 | Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265236 | Binding affinity to bovine 5HT1D receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265281 | Binding affinity to chloride channel by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686204 | Antagonist activity at alpha2bbeta3 in human HEL cells assessed as reduction in cell adhesion to fibrinogen pre-incubated for 30 mins before fibrinogen and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265234 | Binding affinity to 5HT1A receptor in rat cerebral cortex by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265221 | Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1576814 | Inhibition of human vitronectin binding to human integrin alphavbeta3 receptor after 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID265274 | Binding affinity to somatostatin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265267 | Binding affinity to chemokine receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID589567 | Displacement of [125I]echistatin from human integrin alpha5beta3 expressed in human A549 cells by binding assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
| Exploring new near-infrared fluorescent disulfide-based cyclic RGD peptide analogs for potential integrin-targeted optical imaging. |
AID265279 | Binding affinity to sodium channel by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID91596 | Dissociation constant for human integrin alphaIIb-beta3 | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
| Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR: RGD peptide ligands binding to integrin alphaIIbbeta3. |
AID1686187 | Toxicity in human SK-MEL-24 cells assessed as induction of cell necrosis and/or apoptosis incubated for 3 hrs by annexin V-PE and 7-AAD staining based by flow cytometry | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID217315 | Inhibition of alphaV-beta3 interaction with vitronectin | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
| Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor. |
AID265270 | Binding affinity to neurokinin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID276738 | Inhibition of integrin alphavbeta3 mediated cell adhesion of human M21 cells to vitronectin | 2006 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
| Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening. |
AID1686197 | Antagonist activity at alphaVbeta5 in human MCF7 cells assessed as reduction in cell adhesion to fibrinogen pre-incubated for 30 mins before fibrinogen and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID709959 | Competitive inhibition of biotinylated vitronectin to integrin alphaVbeta5 receptor after 3 hrs by microplate reader analysis | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrin αVβ3. |
AID265269 | Binding affinity to muscarinic receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265226 | Displacement of [3H]RX 821002 from Adrenergic alpha-2a receptor in rat cerebral cortex cells at 1 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686206 | Agonist activity at alphaLbeta2 in human Jurkat E6.1 cells assessed as increase in cell adhesion to ICAM1 pre-incubated for 30 mins before ICAM1 and further incubated for 30 mins by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic ass | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265263 | Binding affinity to endothelin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265245 | Inhibition of human recombinant cytochrome P450 2C9 | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265222 | Half life in Sprague-Dawley rat at 3 mg/kg, po | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265219 | Elimination half life in human | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265266 | Binding affinity to cholecystokinin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265257 | Binding affinity to beta adrenergic receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686211 | Inhibition of fibronectin binding to alpha4bbeta1 isolated from human Jurkat E6.1 cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265254 | Ratio of drug level in brain against serum in Sprague-Dawley rat at 3 mg/kg, po or 1 mg/kg, iv after 1 hr | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686209 | Inhibition of fibrinogen binding to alphaVbeta5 isolated form human mCf7 cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID1686188 | Toxicity in human MCF7 cells assessed as induction of cell necrosis and/or apoptosis incubated for 3 hrs by annexin V-PE and 7-AAD staining based by flow cytometry | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265251 | Half life in Beagle dog at 3 mg/kg, po | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID328215 | Displacement of [125I]echistatin from human placental integrin alphaVbeta3 receptor | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands. |
AID265262 | Binding affinity to bradykinin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686190 | Toxicity in human K562 cells assessed as induction of cell necrosis and/or apoptosis incubated for 3 hrs by annexin V-PE and 7-AAD staining based by flow cytometry | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265249 | Displacement of [3H]prazosin from Adrenergic alpha-1 receptor in rat cerebral cortex cells at 10 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265252 | Oral bioavailability in Beagle dog at 3 mg/kg, po and 1 mg/kg, iv | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265278 | Binding affinity to neuropeptide receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686207 | Antagonist activity at alphaLbeta2 in human Jurkat E6.1 cells assessed as reduction in cell adhesion to ICAM1 pre-incubated for 30 mins before ICAM1 and further incubated for 30 mins by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID1686208 | Inhibition of fibronectin binding to human recombinant alphaVbeta3 expressed in HEK293 cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID1686193 | Antagonist activity at alphaVbeta3 in human SK-MEL-24 cells assessed as reduction in cell adhesion to fibronectin pre-incubated for 30 mins before fibronectin and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chro | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265214 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor in HEK293 cells | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265290 | Transient increase in prolactin level in human serum at greater than 30 mg | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1433902 | Displacement of biotinylated vitronectin from human integrin alphaVbeta3 measured after 3 hrs by solid-phase receptor binding assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
AID265228 | Binding affinity to 5HT2A receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265225 | Displacement of [3H]RX 821002 from Adrenergic alpha-2a receptor in rat cerebral cortex cells | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1355340 | Allosteric activation of integrin alphaVbeta3 receptor in human MSR3 cell membranes assessed as increase in anti-beta3 LIBS integrin antibody AP5 binding at 500 uM incubated for 90 mins by flow cytometry | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to α |
AID265239 | Binding affinity to human 5HT4e receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265248 | Inhibition of human recombinant cytochrome P450 3A4 | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID443823 | Inhibition of alphavbeta3 integrin-mediated cell adhesion in human SK-MEL-24 cells on fibronectin coated plate after 30 mins | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics. |
AID265287 | Toxicity in po dosed Sprague-Dawley rat | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265224 | Displacement of [3H]prazosin from Adrenergic alpha-1 receptor in rat cerebral cortex cells at 1 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686210 | Inhibition of fibronectin binding to alphaVbeta6 isolated form human HT-29 cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265259 | Binding affinity to histamine receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID392384 | Inhibition of VEGF-induced HUVEC proliferation after 48 hrs | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
| Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5). |
AID265215 | Displacement of [3H]prazosin from adrenergic alpha-1 receptor in rat cerebral cortex cells | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265255 | Protein binding in human serum at 10 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID443825 | Inhibition of alpha5beta1 integrin-mediated cell adhesion in human K562 cells on fibronectin coated plate after 30 mins | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics. |
AID265260 | Binding affinity to angiotensin2 receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1576813 | Binding affinity to integrin alphavbeta3 receptor in human WM115 cells assessed as inhibition of cell adhesion to vitronectin after 0.5 hr by fluorescence assay | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID265265 | Binding affinity to galanin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265272 | Binding affinity to orphanin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265284 | Binding affinity to guinea pig sigma receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265285 | Decrease in stress-induced hyperthermia in 129S6/SvEvTac mouse at 20 mg/kg, po | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265241 | Binding affinity to human 5HT6 receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265227 | Binding affinity to 5HT7 receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686205 | Antagonist activity at alpha4beta1 in human Jurkat E6.1 cells assessed as reduction in cell adhesion to VCAM1 pre-incubated for 30 mins before VCAM1 and further incubated for 30 mins by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID1686189 | Toxicity in human HT-29 cells assessed as induction of cell necrosis and/or apoptosis incubated for 3 hrs by annexin V-PE and 7-AAD staining based by flow cytometry | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265242 | Half life in human liver S9 fraction at 5 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID709960 | Competitive inhibition of biotinylated vitronectin to integrin alphaVbeta3 receptor after 3 hrs by microplate reader analysis | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrin αVβ3. |
AID1686200 | Agonist activity at alpha5beta1 in human K562 cells assessed as increase in cell adhesion to fibronectin pre-incubated for 30 mins before fibronectin and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic a | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265283 | Binding affinity to dopamine transporter by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265247 | Inhibition of human recombinant cytochrome P450 2D6 | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265276 | Binding affinity to vasoactive intestinal peptide receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265218 | Selectivity for D2 receptor over 5HT1A receptor | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265250 | Cmax in Sprague-Dawley rat at 3 mg/kg, po | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265264 | Binding affinity to GABA receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265237 | Binding affinity to human 5HT2C receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265277 | Binding affinity to vasopressin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686185 | Inhibition of fibrinogen binding to alpha2bbeta3 isolated from human HEL cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265240 | Binding affinity to human 5HT5A receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID93130 | Inhibition of human platelet aggregation mediated by alpha llb/beta3 interaction with fibrinogen | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
| Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor. |
AID265216 | Selectivity for adrenergic alpha-1 receptor over 5HT1A receptor | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265261 | Binding affinity to benzodiazepine receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265223 | Oral bioavailability in Sprague-Dawley rat at 3 mg/kg, po and 1 mg/kg, iv | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1686203 | Agonist activity at alpha2bbeta3 in human HEL cells assessed as increase in cell adhesion to fibrinogen pre-incubated for 30 mins before fibrinogen and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic ass | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID277076 | Inhibition of human alpha-v-beta-3 integrin receptor by ELISA | 2006 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
| Natural inhibitors targeting osteoclast-mediated bone resorption. |
AID1686186 | Inhibition of fibronectin binding to alpha5beta1 isolated from human K562 cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID1349626 | Inhibition of vitronectin binding to human integrin alphaVbeta3 measured after 4 hrs by ELISA | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
| Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application. |
AID265233 | Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay at 1 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265253 | Cmax in Beagle dog at 3 mg/kg, po | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1156786 | Antagonist activity at alpha5beta1 integrin in human K562 cells assessed as inhibition of fibronectin-mediated cell adhesion after 30 mins by fluorescence assay | 2014 | European journal of medicinal chemistry, Aug-18, Volume: 83 | Targeting integrins αvβ3 and α5β1 with new β-lactam derivatives. |
AID328216 | Displacement of [125I]Echistatin from human placental integrin alpha-V-beta-5 receptor | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands. |
AID265275 | Binding affinity to sigma receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265289 | Terminal half life in human | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265229 | Binding affinity to 5HT2B receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1576815 | Inhibition of human fibronectin binding to human integrin alpha5beta1 incubated for 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID1686201 | Antagonist activity at alpha5beta1 in human K562 cells assessed as reduction in cell adhesion to fibronectin pre-incubated for 30 mins before fibronectin and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogen | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID726201 | Binding affinity to integrin in human WM-115 cells after 30 mins by immobilized vitronectin-based competitive cell adhesion assay | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
| Conjugates of modified cryptophycins and RGD-peptides enter target cells by endocytosis. |
AID261127 | Displacement of [125I]echistatin from AlphaV-beta-3 integrin receptor | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
| Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior. |
AID265282 | Binding affinity to norepinephrine transporter by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265238 | Binding affinity to mouse 5HT3 receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID1349625 | Inhibition of vitronectin binding to integrin alphaVbeta3 in HDF pretreated for 20 mins followed by vitronectin addition measured after 40 mins by crystal violet staining based assay | 2018 | ACS medicinal chemistry letters, Jan-11, Volume: 9, Issue:1
| Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application. |
AID265271 | Binding affinity to neurotensin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID91595 | Inhibition of integrin alphaIIb-beta3 binding | 2001 | Journal of medicinal chemistry, Sep-13, Volume: 44, Issue:19
| Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR: RGD peptide ligands binding to integrin alphaIIbbeta3. |
AID392386 | Apparent permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
| Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5). |
AID1576816 | Inhibition of human fibronectin binding to human Integrin alpha2b beta3 receptor incubated for 1 hr by ELISA | 2019 | Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
| Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
AID256968 | Displacement of [125I]-echistatin from alphavbeta3 integrin receptor | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
| Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders. |
AID265230 | Binding affinity to 5HT transporter by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID256969 | Displacement of [125I]-echistatin from alpha-v-beta-5 integrin receptor | 2005 | Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
| Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders. |
AID1686191 | Toxicity in human HEL cells assessed as induction of cell necrosis and/or apoptosis incubated for 3 hrs by annexin V-PE and 7-AAD staining based by flow cytometry | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID392385 | Inhibition of HUVEC migration after 4 hrs | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
| Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5). |
AID265220 | Activity against 5HT1A receptor relative to 5-HT by Gi-[35S]GTP-gamma-S binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID392383 | Inhibition of FGF-induced HUVEC proliferation after 48 hrs | 2009 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
| Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5). |
AID261128 | Displacement of [125I]echistatin from AlphaV-beta-5 integrin receptor | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
| Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior. |
AID1686202 | Agonist activity at alpha4beta1 in human Jurkat E6.1 cells assessed as increase in cell adhesion to VCAM1 pre-incubated for 30 mins before VCAM1 and further incubated for 30 mins by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic ass | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID1686199 | Antagonist activity at alphaVbeta6 in human HT-29 cells assessed as reduction in cell adhesion to fibronectin pre-incubated for 30 mins before fibronectin and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromoge | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21
| New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. |
AID265232 | Half life in human liver microsome at 5 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265243 | Protein binding in human serum at 2 uM | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265217 | Binding affinity to D2 receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265244 | Inhibition of human recombinant cytochrome P450 1A2 | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265256 | Binding affinity to adrenergic alpha receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265258 | Binding affinity to dopamine receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265235 | Binding affinity to 5HT1B receptor in rat cerebral cortex by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
AID265268 | Binding affinity to melanocortin receptor by radioligand binding assay | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
| An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |