Assay ID | Title | Year | Journal | Article |
AID1386004 | Potency index, ratio of Kd for diflunisal to Kd for test compound for binding affinity to transthyretin (unknown origin) by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1615478 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at A25 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1755167 | Aqueous solubility of the compound in pH 6.8 JP2 fluid measured after 4 hrs by HPLC-UV analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1615449 | Binding affinity to His6-tagged wild-type TTR (unknown origin) expressed in Escherichia coli BL21 star (DE3) at 0.5:1 ratio of test compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1755181 | Cmax in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1755183 | AUC infinity in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1452015 | Inhibition human wild type TTR expressed in Escherichia coli BL-21 assessed as fibril formation at 14.4 uM incubated for 30 mins after 96 hrs by light scattering method relative to control | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation. |
AID1696717 | Stabilization of human His-tagged TTR (Gly21 to Glu147) expressed in HEK293 cells assessed as reduction in acid-induced protein aggregation by measuring reduction in high molecular aggregates at 50 uM incubated for 72 hrs at pH 4 by Western blot analysis | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities. |
AID1898642 | Displacement of [125I]-T4 from human recombinant TTR expressed in Escherichia coli BL21(DE3) Star by gamma spectrometric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease. |
AID1725432 | Inhibition of amyloid beta aggregation in mouse N2a695 cells measured for 4 hrs by fluorescence correlation spectroscopic analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1486518 | Inhibition of acid-induced wild type transthyretin (unknown origin) aggregation expressed in Escherichia coli pre-incubated for 30 mins before acid addition and further incubated for 72 hrs at 37 degC under dark conditions by UV-Vis spectrophotometry | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
| Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors. |
AID1848637 | Binding affinity to first binding site of wild type TTR (unknown origin) assessed as change in enthalpy by ITC analysis | | | |
AID1486520 | Displacement of [125I]-triiodothyronine from thyroid hormone receptor in rat liver membrane homogenates incubated for 18 hrs by scintillation counting method | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
| Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors. |
AID1322957 | Binding affinity to recombinant human wild type TTR expressed in Escherichia coli BL21 (DE3) assessed as dissociation constants for second binding site of TTR by isothermal titration calorimetric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1896522 | Binding affinity to human serum TTR assessed as target occupancy incubated for 6 hrs by fluorescence polarization assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
| Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand. |
AID1615490 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at protein dimer-dimer interface at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1705464 | Binding affinity to wild type TTR (unknown origin) assessed as Kd2 by isothermal titration calorimetry | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments. |
AID1615473 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of confirmational change at L55 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1774080 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1386007 | Binding affinity to transthyretin (unknown origin) assessed as free TdeltaS changes by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1386032 | Binding affinity to purified human transthyretin assessed as protein occupancy at 10 uM incubated for 6 hrs in pH 7.4 PBS buffer in presence of 70 uM IgG by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1331734 | Inhibition of TTR V30M mutant (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs relative to | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1615479 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at I26 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615493 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at BEF strands of outer beta sheet at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615505 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at K9 residue at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615469 | Binding affinity to wild-type TTR (unknown origin) assessed as increase in bound resonance at L55 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1810857 | Stabilization of human plasma TTR assessed as inhibition of formation of high molecular weight forms of TTR with acetate buffer at pH 4 by measured at 50 uM after 72 hrs by acid-induced aggregation assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th |
AID1452016 | Inhibition of human TTR V30M mutant expressed in Escherichia coli BL-21 assessed as fibril formation at 7.2 uM incubated for 30 mins measured after 96 hrs by light scattering method relative to control | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation. |
AID1615488 | Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as association rate at binding site-2 by surface plasmon resonance | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1755170 | Protein binding in Sprague-Dawley rat plasma assessed as unbound fraction at 1 uM measured after 4 hrs by equilibrium dialysis assay | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1386029 | Binding affinity to purified human transthyretin assessed as protein occupancy at 10 uM incubated for 6 hrs in pH 7.4 PBS buffer in presence of 600 uM albumin by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1725430 | Inhibition of gamma secretase in mouse N2a695 cells using Sb4 substrate incubated for 3 hrs by ELISA | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1755166 | Aqueous solubility of the compound in pH 1.2 JP1 fluid measured after 4 hrs ny HPLC-UV analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1755168 | Permeability of the compound at 10 uM measured after 4 hrs by PAMPA based LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1810858 | Stabilization of human plasma TTR assessed as fold reduction in amount of aggregate formation at 50 uM measured after 72 hrs by Western blotting analysis relative to control | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th |
AID1615507 | Binding affinity to wild-type TTR (unknown origin) assessed as stabilization of hydrogen bond between A120 and Y114 by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1848652 | Binding affinity to second binding site of wild type TTR (unknown origin) assessed as dissociation constant by ITC assay | | | |
AID1848655 | Binding affinity to second binding site of wild type TTR (unknown origin) assessed as change in enthalpy by ITC analysis | | | |
AID1725427 | Increase in APP fragmentation in mouse N2a695 cells at 10 uM incubated for 6 hrs by Western blot analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1755164 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as residual rate at 1 uM preincubated for 5 mins followed by NADPH addition and measured after 30 mins by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1386015 | Dissociation constant, pKa of the compound | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1386024 | Binding affinity to human serum albumin assessed as compound level bound to protein at 30 uM measured immediately after gel filtration | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1615486 | Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as association rate at binding site-1 by surface plasmon resonance | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1774082 | Stabilization of TTR V3OM mutant (unknown origin) assessed as suppression of TTR tetramer dissociation at 3 uM incubated for 9 days by glutaraldehyde cross-linking assay based SDS-PAGE analysis relative to control | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1615484 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at V122 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1810837 | Binding affinity to human plasma TTR tetramer assessed as displacement of diclofenac-coupled FITC by fluorescence polarization assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th |
AID1615450 | Binding affinity to His6-tagged wild-type TTR (unknown origin) expressed in Escherichia coli BL21 star (DE3) at 2:1 ratio of test compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1386019 | Binding affinity to transthyretin (unknown origin) in human serum assessed as protein stabilization at 10 uM in pH 7.4 urea buffer by Western blot | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1386002 | Binding affinity to human serum albumin | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1386001 | Binding affinity to human serum albumin by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1452014 | Inhibition of human wild type TTR expressed in Escherichia coli BL-21 assessed as fibril formation at 7.2 uM incubated for 30 mins measured after 96 hrs by light scattering method relative to control | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation. |
AID1774081 | Stabilization of TTR V3OM mutant (unknown origin) assessed as suppression of TTR tetramer dissociation at 1 to 10 uM incubated for 9 days by glutaraldehyde cross-linking assay based SDS-PAGE analysis | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1385999 | Binding affinity to transthyretin in dog serum assessed as protein stabilization at 10 uM by by Western blot | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1486519 | Binding affinity to transthyretin in human blood plasma assessed as plasma binding selectivity by measuring stoichiometry of small molecule bound to TTR incubated for 24 hrs at 37 degC by RP-HPLC | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
| Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors. |
AID1386030 | Binding affinity to purified human transthyretin assessed as protein occupancy at 10 uM incubated for 6 hrs in pH 7.4 PBS buffer in presence of 25 uM transferrin by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1725441 | Stabilization of recombinant dual FLAG-tagged wild type TTR (unknown origin) in plasma blood at < 30 uM incubated for 48 hrs by ion exchange chromatographic method | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1615492 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at V121 residue at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1452013 | Competitive binding affinity to human wild type TTR expressed in Escherichia coli BL-21 assessed as equilibrium dissociation constant of second site in presence of ANS by spectrofluorometer | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation. |
AID1725431 | Effect on TTR-induced amyloid beta aggregation inhibition in mouse N2a695 cells measured for 4 hrs by fluorescence correlation spectroscopic analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1386006 | Binding affinity to transthyretin (unknown origin) assessed as free enthalpy changes by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1807499 | Binding affinity to human TTR in human serum assessed as target occupancy at 10 uM measured every 15 mins for 6 hrs by fluorescent probe exclusion selectivity assay | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Enhancing the Pharmacokinetic Profile of Interleukin 2 through Site-Specific Conjugation to a Selective Small-Molecule Transthyretin Ligand. |
AID1755185 | Volume of distribution at steady state in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1696718 | Stabilization of human His-tagged TTR (Gly21 to Glu147) expressed in HEK293 cells assessed as reduction in acid-induced protein aggregation by measuring increase in TTR monomer level at 50 uM incubated for 72 hrs at pH 4 by Western blot | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities. |
AID1848657 | Binding affinity to second binding site of wild type TTR (unknown origin) assessed as change in entropy by ITC analysis | | | |
AID1322953 | Stabilization of wild type TTR tetramer in human plasma assessed as tetramer to total protein ratio preincubated overnight at 4 degC followed by further incubation at room temperature for 1 hr in presence of 4M urea by isoelectric focusing densitometric a | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1331733 | Inhibition of TTR V30M mutant (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation at 3.6 uM preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs re | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1755182 | Elimination half life in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1386008 | Binding affinity to transthyretin (unknown origin) in pH 7.4 PBS buffer assessed as protein occupancy at 1:1 compound to TTR ratio by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1615485 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at W79 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615502 | Binding affinity to wild-type TTR (unknown origin) assessed as formation of hydrogen bond between K76 and E89 at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615470 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at L55 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1755162 | Inhibition of acid-mediated aggregation of TTR V30M mutant (unknown origin) expressed in Escherichia coli pretreated for 30 mins at pH 7 followed by protein dilution in acetate buffer and further incubated for 96 hrs at pH 4.6 by thioflavin-T fluorescence | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1615477 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at R104 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1774086 | Binding affinity to TTR V30M mutant (unknown origin) by isothermal titration calorimetry | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1322954 | Stabilization of recombinant human wild type TTR expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid beta formation by measuring turbidity preincubated for 30 mins followed by lowering pH from 7.2 to 4.4 measured after 72 hrs by mic | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1331731 | Inhibition of wild type TTR (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs relative to co | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1452019 | Binding affinity to wild type TTR (unknown origin) assessed as equilibrium dissociation constant of second site by isothermal titration calorimetry | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation. |
AID1725428 | Increase in APP-CTF fragmentation in mouse N2a695 cells at 10 uM incubated for 6 hrs by Western blot analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1755163 | Binding affinity to TTR V30M mutant (unknown origin) expressed in Escherichia coli by isothermal titration calorimetry | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1888715 | Inhibition of Transthyretin V30M mutant (unknown origin) assessed as acid mediated fibril formation at 1.8 uM measured after 72 hrs by UV-vis spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors. |
AID1331729 | Inhibition of wild type TTR (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation at 7.2 uM preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs rela | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1615501 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at E89 residue at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1605605 | Stabilization of wild type human transthyretin expressed in Escherichia coli BL21(DE3) Star assessed as reduction in fibril formation by measuring round particles and pre-fibrillar species levels at 50 uM pre-incubated with transthyretin for 1 hr before a | | | |
AID1486521 | Displacement of [125I]-triiodothyronine from thyroid hormone receptor in rat liver membrane homogenates assessed as relative T3 displacement incubated for 18 hrs by scintillation counting method relative to control | 2017 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
| Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors. |
AID1888712 | Inhibition of wild-type Transthyretin (unknown origin) expressed in Escherichia coli expression system assessed as acid mediated fibril formation at 7.2 uM measured after 72 hrs by UV-vis spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors. |
AID1386010 | Binding affinity to transthyretin in human serum assessed as protein stabilization at 2:1 compound to TTR ratio after 72 hrs by Western blot | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1774083 | Stabilization of wild type TTR (unknown origin) expressed in Escherichia coli assessed as reduction in methanol-induced aggregation at 50 uM incubated for 60 min by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1810836 | Disruption of retional-induced bacterially expressed MBP-tagged RBP4-TTR (unknown origin) protein-protein interaction measured by d2 dye based HTFR assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th |
AID1386003 | Potency index, ratio of Kd for tolcapone to Kd for test compound for binding affinity to transthyretin (unknown origin) by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1322964 | Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1615476 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at R103 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1386025 | Binding affinity to human serum albumin assessed as compound level bound to protein at 30 uM measured 124 hrs after dialysis | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1386033 | Binding affinity to transthyretin in dog serum assessed as protein occupancy at 10 uM by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1615474 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at K15 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1386028 | Binding affinity to purified human transthyretin assessed as protein occupancy at 10 uM incubated for 6 hrs in pH 7.4 PBS buffer by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1331732 | Inhibition of TTR V30M mutant (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation at 7.2 uM preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs re | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1386000 | Binding affinity to transthyretin (unknown origin) by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1755165 | Metabolic stability in Sprague-Dawley rat liver microsomes assessed as residual rate at 1 uM measured after 30 mins by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1848635 | Binding affinity to first binding site of wild type TTR (unknown origin) assessed as dissociation constant by ITC assay | | | |
AID1386012 | Cmax in human at 80 mg qd | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1615452 | Binding affinity to wild-type TTR (unknown origin) assessed as increase in bound resonance at D99 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1322965 | Stabilization of TTR V30M mutant tetramer in human plasma assessed as tetramer to total protein ratio preincubated overnight at 4 degC followed by further incubation at room temperature for 1 hr in presence of 4M urea by isoelectric focusing densitometric | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1774078 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1774075 | Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1386018 | Binding affinity to transthyretin (unknown origin) in human serum assessed as protein occupancy at 200 uM by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1725434 | Brain concentration in 5XFAD mouse at 50 mg/kg, po measured after 15 days by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1888717 | Inhibition of urea-induced Transthyretin denaturation in human plasma preincubated for 1 hr followed by urea addition by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors. |
AID1615494 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at AB loops at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615448 | Binding affinity to His6-tagged wild-type TTR (unknown origin) expressed in Escherichia coli BL21 star (DE3) assessed as assignment of protein resonance by TROSY [1H-13C-15N] HNCA spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1605604 | Stabilization of wild type human transthyretin expressed in Escherichia coli BL21(DE3) Star assessed as dissociation constant for TTR-amyloid beta (12 to 28) complex formation at 200 uM at 25 degC pre-incubated with transthyretin before amyloid beta (12 t | | | |
AID1848656 | Binding affinity to first binding site of wild type TTR (unknown origin) assessed as change in entropy by ITC analysis | | | |
AID1322960 | Displacement of [125I]-T4 from wild type TTR in human plasma after 1 hr by PAGE analysis | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1322956 | Binding affinity to recombinant human wild type TTR expressed in Escherichia coli BL21 (DE3) assessed as dissociation constants for first binding site of TTR by isothermal titration calorimetric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition. |
AID1615487 | Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as dissociation rate at binding site-1 by surface plasmon resonance | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1774085 | Stabilization of TTR V142I mutant (unknown origin) expressed in Escherichia coli assessed as reduction in trypsin-induced aggregation incubated for 3 to 4 days by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1386009 | Binding affinity to transthyretin in human serum assessed as protein occupancy at 2:1 compound to TTR ratio after 72 hrs by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1615508 | Binding affinity to wild-type TTR (unknown origin) assessed as stabilization of hydrogen bond between V121 and T106 by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1848654 | Binding affinity to second binding site of wild type TTR (unknown origin) assessed as gibbs free energy change by ITC analysis | | | |
AID1386031 | Binding affinity to purified human transthyretin assessed as protein occupancy at 10 uM incubated for 6 hrs in pH 7.4 PBS buffer in presence of 5 uM fibrinogen by fluorescent probe exclusion assay | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1331730 | Inhibition of wild type TTR (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring fibril formation at 3.6 uM preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured after 72 hrs rela | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1615489 | Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as dissociation rate at binding site-2 by surface plasmon resonance | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615471 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of confirmational change at D99 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1605603 | Stabilization of wild type human transthyretin expressed in Escherichia coli BL21(DE3) Star assessed as fibril formation at 50 uM pre-incubated with transthyretin before amyloid beta (1 to 42) addition by ThT fluorescence assay (Rvb = 25 +/- 1%) | | | |
AID1774076 | Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1810859 | Stabilization of human plasma TTR assessed as increase in dimer band intensity at 50 uM measured after 72 hrs by Western blotting analysis | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th |
AID1888714 | Inhibition of Transthyretin V30M mutant (unknown origin) assessed as acid mediated fibril formation at 3.6 uM measured after 72 hrs by UV-vis spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors. |
AID1615480 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at S52 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1331735 | Inhibition of wild type TTR (unknown origin) assessed as inhibition of acid-mediated amyloidogenesis by measuring reduction in fibril formation at 3.6 uM preincubated with enzyme followed by amyloidogenesis stimulation by adjusting pH to 4.4 measured up t | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors. |
AID1755186 | AUC (0 to 8 hrs) in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1705463 | Binding affinity to wild type TTR (unknown origin) assessed as Kd1 by isothermal titration calorimetry | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
| Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments. |
AID1755184 | Total clearance in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1615468 | Binding affinity to wild-type TTR (unknown origin) assessed as increase in bound resonance at S117 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615481 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at H90 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1452017 | Inhibition of human TTR V30M mutant expressed in Escherichia coli BL-21 assessed as fibril formation at 14.2 uM incubated for 30 mins measured after 96 hrs by light scattering method relative to control | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
| Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation. |
AID1755187 | Bioavailability in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1848653 | Binding affinity to first binding site of wild type TTR (unknown origin) assessed as gibbs free energy change by ITC analysis | | | |
AID1755190 | AUC (0 to 8 hrs) in Sprague-Dawley rat at 0.1 mg/kg, po measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1386005 | Binding affinity to transthyretin (unknown origin) assessed as free energy changes by ITC method | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
| Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis. |
AID1725433 | Plasma concentration in 5XFAD mouse at 50 mg/kg, po measured after 15 days by LC-MS/MS analysis | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage. |
AID1755189 | Tmax in Sprague-Dawley rat at 0.1 mg/kg, po measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1755188 | Cmax in Sprague-Dawley rat at 0.1 mg/kg, po measured up to 8 hrs by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1615475 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at L17 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615483 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift perturbation at A120 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1605601 | Stabilization of wild type human transthyretin expressed in Escherichia coli BL21(DE3) Star assessed as dissociation constant for TTR-amyloid beta (1 to 42) complex formation at 200 uM at 25 degC pre-incubated with transthyretin before amyloid beta (1 to | | | |
AID1615472 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of confirmational change at S117 residue at 0.5:1 to 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615495 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at BC loops at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1615504 | Binding affinity to wild-type TTR (unknown origin) assessed as chemical shift perturbation at A91 residue at 2:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1888713 | Inhibition of wild-type Transthyretin (unknown origin) expressed in Escherichia coli expression system assessed as acid mediated fibril formation at 3.6 uM measured after 72 hrs by UV-vis spectrophotometry | 2022 | Bioorganic & medicinal chemistry, 01-01, Volume: 53 | Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors. |
AID1615482 | Binding affinity to wild-type TTR (unknown origin) assessed as induction of chemical shift at V94 residue at 1:1 ratio of compound to protein by 2D TROSY [1H-15N] spectroscopy | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| Binding of Monovalent and Bivalent Ligands by Transthyretin Causes Different Short- and Long-Distance Conformational Changes. |
AID1755169 | Intrinsic clearance in Sprague-Dawley rat liver microsomes at 1 uM preincubated for 5 mins followed by NADPH addition and measured after 30 mins by LC-MS/MS analysis | 2021 | Bioorganic & medicinal chemistry, 08-15, Volume: 44 | Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis. |
AID1774079 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
| Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
AID1810838 | Displacement of [3H]-all trans retinol from human urine biotinylated RBP4 incubated for 16 hrs measured by Scintillation Proximity Assay | 2021 | Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
| Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Th |
AID1346206 | Human transthyretin (Carrier proteins) | 2012 | Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 109, Issue:24
| Tafamidis, a potent and selective transthyretin kinetic stabilizer that inhibits the amyloid cascade. |
AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2013 | Proceedings of the National Academy of Sciences of the United States of America, Jun-11, Volume: 110, Issue:24
| AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |