| Assay ID | Title | Year | Journal | Article |
|---|
| AID753428 | Inhibition of rat VAP-1 expressed in CHO cells using [14C]-benzylamine as substrate preincubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Novel 1H-imidazol-2-amine derivatives as potent and orally active vascular adhesion protein-1 (VAP-1) inhibitors for diabetic macular edema treatment. |
| AID1265731 | Inhibition of recombinant human tPA using H-D-Ile-Pro-L-Arg-pNA-2HCl as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID213433 | Acid dissociation constant (pKa) of the compound | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Identification of novel inhibitors of urokinase via NMR-based screening. |
| AID19834 | Partition coefficient in an aqueous 1-octanol buffer system by the shake-flask method | 2003 | Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6
| Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG). |
| AID1265730 | Inhibition of human plasma thrombin using pyroGlu-Pro-Arg-pNA-HCl as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID210841 | Inhibition against human plasma thrombin at 1.0 mM | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID753430 | Inhibition of human VAP-1 expressed in CHO cells using [14C]-benzylamine as substrate preincubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrometric analysis | 2013 | Bioorganic & medicinal chemistry, Jul-01, Volume: 21, Issue:13
| Novel 1H-imidazol-2-amine derivatives as potent and orally active vascular adhesion protein-1 (VAP-1) inhibitors for diabetic macular edema treatment. |
| AID447915 | Ionization constant for the compound (pKa) | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists. |
| AID1303292 | Dissociation constant, pKa of the compound | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Isouronium and N-hydroxyguanidinium derivatives as Cell growth inhibitors: A comparative study. |
| AID1265735 | Inhibition of bovine pancreatic trypsin using Na-benzoyl-D,L-Arg-pNA-HCl as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID157989 | Inhibition against human plasmin was determined at 0.5 mM | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID95039 | Inhibition against human plasma Kallikrein at 2 mM | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID1265733 | Inhibition of human plasma plasmin using pyroGlu-Pro-Arg-pNA-HCl as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID1463537 | Selectivity ratio of IC50 for human OCT2 expressed in HEK293 cells to IC50 for human OCT3 expressed in HEK293 cells | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3). |
| AID215985 | Inhibitory activity against Urokinase-type plasminogen activator | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Identification of novel inhibitors of urokinase via NMR-based screening. |
| AID1463536 | Inhibition of human OCT3 expressed in HEK293 cells assessed as decrease in uptake of substrate [3H]MPP+ after 1 min by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3). |
| AID215213 | Inhibition against Trypsin | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID210580 | The compound was tested for its inhibition against Tissue plasminogen activator at 1 mM when assayed against 0.3 mM S-2288 (Km = 0.673 mM) | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID6343 | Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
| Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors. |
| AID1265732 | Inhibition of purified human factor 10a using Suc-Ile-Glu(yPip)-GlyArg-pNa-HCl as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID1412985 | Basic dissociation constant, pKa of the compound in water at 0.1 mM by UV-spectrophotometric method | | | |
| AID6339 | Binding affinity to 5-HT3 serotonin receptor in NG 108-15 neuroblastoma glioma cells using [3H]GR-65630 radioligand. | 2001 | Bioorganic & medicinal chemistry letters, Jun-18, Volume: 11, Issue:12
| The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation. |
| AID1463535 | Inhibition of human OCT2 expressed in HEK293 cells assessed as decrease in uptake of substrate [3H]MPP+ after 1 min by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3). |
| AID1265729 | Inhibition of purified human factor 7a using MeSO2-Cha-Abu-Arg-pNA as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID215237 | log1/Ki value was calculated against Trypsin | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID26313 | pKa value determined | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24
| Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers. |
| AID1463539 | Selectivity ratio of IC50 for human OCT1 expressed in HEK293 cells to IC50 for human OCT3 expressed in HEK293 cells | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3). |
| AID215841 | Inhibition against Urokinase-type plasminogen activator | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID1265734 | Inhibition of human plasma kallikrein using D-Pro-Phe-Arg-pNA-2HCl as substrate at 100 uM measured for 5 mins by spectrophotometric assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold. |
| AID1463534 | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of substrate [3H]MPP+ after 1 min by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
| A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3). |
| AID215976 | log1/Ki value was calculated against Urokinase-type plasminogen activator | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
| AID1799881 | Enzymatic Assay from Article 10.1021/bi00839a042: \\Nature of the active site of a subunit of the first component of human complement.\\ | 1969 | Biochemistry, Nov, Volume: 8, Issue:11
| Nature of the active site of a subunit of the first component of human complement. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |