Page last updated: 2024-11-12

tafamidis

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

tafamidis: may be effective in treating transthyretin amyloid polyneuropathy [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tafamidis : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazole-6-carboxylic acid in which the hydrogen at position 2 is replaced by a 3,5-dichlorophenyl group. Used (as its meglumine salt) for the amelioration of transthyretin-related hereditary amyloidosis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID11001318
CHEMBL ID2103837
CHEBI ID78538
SCHEMBL ID442508
MeSH IDM0543569

Synonyms (60)

Synonym
2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid
3mi ,
tafamidis (jan/usan/inn)
D09673
594839-88-0
vyndamax (tn)
8fg9h9d31j ,
6-benzoxazolecarboxylic acid, 2-(3,5-dichlorophenyl)-
unii-8fg9h9d31j
vyndamax
tafamidis [usan:inn]
tafamidis
2-(3,5-dichlorophenyl)benzoxazole-6-carboxylic acid
fx-1006
137464-18-7
FT-0674793
4HIS
fx-1005
CHEMBL2103837
fx1006
chebi:78538 ,
S6465
tafamidis [usan]
tafamidis [jan]
tafamidis [mart.]
tafamidis [inn]
tafamidis [orange book]
tafamidis [who-dd]
tafamidis [mi]
HY-14852
SCHEMBL442508
AKOS017550076
tafamidisum
2-(3,5-dichlorophenyl)-6-benzoxazole carboxylic acid
c14h7cl2no3
gtpl8378
DTXSID00208185 ,
pf-06291826(tafamidis)
C75776
bdbm50197883
A869196
DB11644
BCP29089
Q519447
594839-88-0 (free acid)
Z1443584665
discontinued until pfizer approves it for our agreement
mfcd16621109
VS-0125
tafamidis-meglumine
HMS3741E09
NCGC00390731-01
2-(3,5-dichlorophenyl)benzo[d]oxazole-6-carboxylic acid
EN300-307185
EX-A3575
SY217402
tafamidis (mart.)
dtxcid20130676
2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid
n07xx08

Research Excerpts

Overview

Tafamidis is a first-in-class, disease-modifying transthyretin (TTR) kinetic stabilizer. It is orally administered and, by interfering with amyloid fibril formation and deposition, is capable of slowing progression of TTR polyneuropathy and of early-stage cardiomyopathy.

ExcerptReferenceRelevance
"Tafamidis is an effective treatment for patients with ATTR-CM, however its long-term effects on cardiac remodeling and cardiac amyloid deposition are unknown."( Tafamidis decreased cardiac amyloidosis deposition in patients with Ala97Ser hereditary transthyretin cardiomyopathy: a 12-month follow-up cohort study.
Chao, CC; Cheng, MF; Chou, CH; Hsieh, ST; Hsueh, HW; Jyh-Ming Juang, J; Lee, MJ; Lin, YH; Shun, CT; Su, MY; Tsai, CH; Tseng, PH; Wu, YA; Yu, AL, 2023
)
3.07
"Tafamidis is an effective treatment for transthyretin amyloid cardiomyopathy (ATTR-CM) in the Tafamidis in Transthyretin Cardiomyopathy Clinical Trial (ATTR-ACT). "( Efficacy and safety of tafamidis doses in the Tafamidis in Transthyretin Cardiomyopathy Clinical Trial (ATTR-ACT) and long-term extension study.
Damy, T; Garcia-Pavia, P; Gundapaneni, B; Hanna, M; Judge, DP; Merlini, G; Patterson, TA; Riley, S; Schwartz, JH; Sultan, MB; Witteles, R, 2021
)
2.37
"Tafamidis is an effective treatment for transthyretin amyloid cardiomyopathy (ATTR-CM), this study aimed to determine whether there is a differential effect between variant transthyretin amyloidosis (ATTRv) and wild-type transthyretin (ATTRwt)."( Efficacy of Tafamidis in Patients With Hereditary and Wild-Type Transthyretin Amyloid Cardiomyopathy: Further Analyses From ATTR-ACT.
Berk, JL; Boman, K; Damy, T; Elliott, P; Gundapaneni, B; Maurer, MS; Nativi-Nicolau, J; Patterson, TA; Rapezzi, C; Schwartz, JH; Sultan, MB; Velazquez, EJ, 2021
)
2.44
"Tafamidis is a first-in-class, disease-modifying transthyretin (TTR) kinetic stabilizer that represents a major breakthrough in the treatment of transthyretin amyloidosis (ATTR amyloidosis)."( Drug Discovery and Development in Rare Diseases: Taking a Closer Look at the Tafamidis Story.
Bruno, M; Burton, A; Castaño, A; Judge, DP; Kelly, JW; Patel, JK; Riley, S; Schumacher, J; See Tai, S; Sultan, MB, 2021
)
1.57
"tafamidis) is a treatment option."( Diagnosis and management of transthyretin familial amyloid polyneuropathy in Japan: red-flag symptom clusters and treatment algorithm.
Ando, Y; Ishii, T; Koike, H; Misawa, S; Sekijima, Y; Ueda, M, 2018
)
1.2
"Tafamidis is a TTR stabilizer that is orally administered and, by interfering with amyloid fibril formation and deposition, is capable of slowing progression of TTR polyneuropathy and of early-stage cardiomyopathy."( Failure of Tafamidis to Halt Progression of Ala36Pro TTR Oculomeningovascular Amyloidosis.
Bianchi, A; Mascalchi, M; Pastorelli, F; Rapezzi, C; Salvi, F; Vella, A; Volpe, R, 2018
)
1.59
"Tafamidis is a transthyretin (TTR) stabilizer able to prevent TTR tetramer dissociation. "( Monitoring effectiveness and safety of Tafamidis in transthyretin amyloidosis in Italy: a longitudinal multicenter study in a non-endemic area.
Bisogni, G; Calabrese, D; Cavallaro, T; Cortese, A; Fabrizi, GM; Gemelli, C; Gentile, L; Grandis, M; Lozza, A; Luigetti, M; Manganelli, F; Mauro, A; Mazzeo, A; Obici, L; Pareyson, D; Perlini, S; Piscosquito, G; Pradotto, LG; Russo, M; Sabatelli, M; Santoro, L; Schenone, A; Stancanelli, C; Vita, G, 2016
)
2.15
"Tafamidis is a transthyretin (TTR) stabilizer recently approved to slow the neurologic impairment in TTR familial amyloid polyneuropathy (TTR-FAP). "( Long-term treatment of transthyretin familial amyloid polyneuropathy with tafamidis: a clinical and neurophysiological study.
Ayache, SS; Azoulay, D; Damy, T; Feray, C; Gorram, F; Le Corvoisier, P; Lefaucheur, JP; Nordine, T; Planté-Bordeneuve, V; Salhi, H, 2017
)
2.13
"Tafamidis is a first-in-class inhibitor of transthyretin amyloid fibril formation. "( Development and validation of a liquid chromatography-tandem mass spectrometry method for the assay of tafamidis in rat plasma: Application to a pharmacokinetic study in rats.
Choi, S; Hyun, HC; Jeong, JW; Kim, HR; Kim, YS; Koo, TS; Lee, JH; Oh, JH, 2017
)
2.11
"Tafamidis meglumine is a novel medicine that has been shown to slow the progression of peripheral neurological impairment in patients with hereditary transthyretin amyloidosis (ATTR). "( Tafamidis for the Treatment of Hereditary Transthyretin Amyloid Cardiomyopathy: A Case Report.
Ako, J; Fujita, T; Iida, Y; Ikeda, Y; Inomata, T; Ishii, S; Kaida, T; Kitamura, E; Koitabashi, T; Maekawa, E; Nabeta, T; Naruke, T; Sekijima, Y,
)
3.02
"Tafamidis is a TTR stabilizer able to prevent TTR tetramer dissociation, and several studies have demonstrated its safety and efficacy at slowing the progression of neuropathy in FAP caused by the TTR Val30Met mutation."( Treatment of transthyretin familial amyloid polyneuropathy with tafamidis: a case report.
Miyazaki, Y, 2017
)
1.42
"Tafamidis is a small-molecule inhibitor that binds selectively to TTR in human plasma and kinetically stabilizes the tetrameric structure of both wild-type TTR and a number of different mutants."( Tafamidis for transthyretin amyloidosis.
de Lartigue, J, 2012
)
2.54

Effects

Tafamidis has been used for treatment of transthyretin cardiac amyloidosis (ATTR-CA) The drug has been unsuccessful for cardiac or nerve involvement after the first seven months.

ExcerptReferenceRelevance
"Tafamidis has been used for treatment of transthyretin cardiac amyloidosis (ATTR-CA). "( Follow-up Tc-99 m pyrophosphate cardiac scan for patients with transthyretin cardiac amyloidosis treated with tafamidis.
Chang, CY; Hu, LH; Huang, WS; Lee, TH; Peng, NJ; Wang, YF, 2023
)
2.56
"Tafamidis has been unsuccessful for cardiac or nerve involvement after the first seven months."( Coronary ectasia in amyloid cardiomyopathy and neuropathy due to the transthyretin mutation c.323A>G.
Finsterer, J; Gatterer, E; Rauschka, H; Stöllberger, C,
)
0.85
"Tafamidis has been granted marketing authorization by the European Commission for the treatment of TTR-FAP and the U.S."( Tafamidis for transthyretin amyloidosis.
de Lartigue, J, 2012
)
2.54

Actions

ExcerptReferenceRelevance
"Tafamidis reduced all-cause mortality and cardiovascular-related hospitalizations and minimized patient-reported health status deterioration at 30 months in patients with transthyretin (ATTR) amyloidosis. "( Association of Tafamidis With Health Status in Patients With ATTR Cardiac Amyloidosis: A Post Hoc Analysis of the ATTR-ACT Randomized Clinical Trial.
Barsdorf, AI; Floden, L; Hanna, M; Kapadia, H; Maurer, MS; Nativi-Nicolau, J; Sperry, BW; Spertus, JA; Stewart, M; Wyrwich, KW, 2023
)
2.71

Treatment

Treatment with tafamidis free acid 61 mg in ATTR-CM patients delays the deterioration of LA and LV longitudinal function, resulting in significant clinical benefits compared with natural history. Tafamidi treatment positively affects left ventricular (LV) structure and function and improves outcomes in patients with transthyretin amyloid cardiomyopathy.

ExcerptReferenceRelevance
"Tafamidis treatment was introduced for approximately half of the study patients with ATTRwt CA in real-world practice. "( Early Experience of Tafamidis Treatment in Japanese Patients With Wild-Type Transthyretin Cardiac Amyloidosis From the Kochi Amyloidosis Cohort.
Baba, Y; Hamada, T; Hirota, T; Kitaoka, H; Kubo, T; Miyagawa, K; Noguchi, T; Ochi, Y; Sugiura, K; Yamasaki, N, 2022
)
2.49
"Tafamidis treatment positively affects left ventricular (LV) structure and function and improves outcomes in patients with transthyretin amyloid cardiomyopathy (ATTR-CM). "( Monitoring tafamidis treatment with quantitative SPECT/CT in transthyretin amyloid cardiomyopathy.
Badr Eslam, R; Beitzke, D; Binder, C; Bonderman, D; Camuz Ligios, L; Cherouny, B; Dachs, TM; Dalos, D; Duca, F; Hacker, M; Kastner, J; Loewe, C; Rettl, R; Schrutka, L; Wollenweber, T, 2023
)
2.74
"tafamidis) is a treatment option."( Diagnosis and management of transthyretin familial amyloid polyneuropathy in Japan: red-flag symptom clusters and treatment algorithm.
Ando, Y; Ishii, T; Koike, H; Misawa, S; Sekijima, Y; Ueda, M, 2018
)
1.2
"Tafamidis treatment was generally well tolerated although 7 of 31 patients had bouts of diarrhea."( Tafamidis in transthyretin amyloid cardiomyopathy: effects on transthyretin stabilization and clinical outcomes.
Aarts, J; Falk, RH; Grogan, DR; Judge, DP; Lombardo, I; Maurer, MS; Mundayat, R; Packman, J; Quyyumi, AA, 2015
)
2.58
"Tafamidis treatment effectively achieved and maintained TTR stabilization and was well tolerated. "( Tafamidis in transthyretin amyloid cardiomyopathy: effects on transthyretin stabilization and clinical outcomes.
Aarts, J; Falk, RH; Grogan, DR; Judge, DP; Lombardo, I; Maurer, MS; Mundayat, R; Packman, J; Quyyumi, AA, 2015
)
3.3
"Treatment with tafamidis free acid 61 mg in ATTR-CM patients delays the deterioration of LA and LV longitudinal function, resulting in significant clinical benefits compared with natural history. "( Impact of tafamidis on myocardial strain in transthyretin amyloid cardiomyopathy.
Badr Eslam, R; Binder, C; Bonderman, D; Camuz Ligios, L; Charwat-Resl, S; Cherouny, B; Dachs, TM; Dalos, D; Duca, F; Kastner, J; Mann, C; Rettl, R; Schrutka, L, 2023
)
1.67
"Treatment with tafamidis in ATTR-CM patients results in a significant reduction in SUV retention index, associated with significant benefits for LV and RV function and cardiac biomarkers. "( Monitoring tafamidis treatment with quantitative SPECT/CT in transthyretin amyloid cardiomyopathy.
Badr Eslam, R; Beitzke, D; Binder, C; Bonderman, D; Camuz Ligios, L; Cherouny, B; Dachs, TM; Dalos, D; Duca, F; Hacker, M; Kastner, J; Loewe, C; Rettl, R; Schrutka, L; Wollenweber, T, 2023
)
1.65
"Treatment with tafamidis is projected to produce substantial clinical benefit but would greatly exceed conventional cost-effectiveness thresholds at the current US list price. "( Cost-Effectiveness of Tafamidis Therapy for Transthyretin Amyloid Cardiomyopathy.
Arnold, SV; Baron, SJ; Bellows, BK; Cohen, DJ; Kazi, DS; Maurer, MS; Shah, SJ; Shen, C; Sperry, BW; Spertus, JA; Yeh, RW, 2020
)
1.23
"Treatment with tafamidis meglumine was started."( Failure of Tafamidis to Halt Progression of Ala36Pro TTR Oculomeningovascular Amyloidosis.
Bianchi, A; Mascalchi, M; Pastorelli, F; Rapezzi, C; Salvi, F; Vella, A; Volpe, R, 2018
)
1.21

Toxicity

Long-term tafamidis was associated with a favourable safety/tolerability profile, without any unexpected adverse events. Incidence of adverse events in both taf amidis doses were comparable to placebo.

ExcerptReferenceRelevance
"The misassembly of soluble proteins into toxic aggregates, including amyloid fibrils, underlies a large number of human degenerative diseases."( AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin.
Alhamadsheh, MM; Baranczak, A; Chan, WK; Connelly, S; Graef, IA; Kelly, JW; Liedtke, M; Park, MS; Penchala, SC; Powers, ET; Rappley, I; Reixach, N; Vogel, H; Wang, Y; Wilson, IA; Witteles, RM; Zhao, L, 2013
)
0.39
" Seven patients (19%) were withdrawn for adverse effects."( Effect on disability and safety of Tafamidis in late onset of Met30 transthyretin familial amyloid polyneuropathy.
Adams, D; Ducot, B; Lacroix, C; Lozeron, P; Mincheva, Z; Théaudin, M, 2013
)
0.67
" There were a total of 19 adverse events, including four febrile urinary tract infections and three severe diarrhoeas, with faecal incontinence in two."( Effect on disability and safety of Tafamidis in late onset of Met30 transthyretin familial amyloid polyneuropathy.
Adams, D; Ducot, B; Lacroix, C; Lozeron, P; Mincheva, Z; Théaudin, M, 2013
)
0.67
" Most adverse events (AEs) were mild/moderate, with no discontinuations due to AEs."( Effects of tafamidis treatment on transthyretin (TTR) stabilization, efficacy, and safety in Japanese patients with familial amyloid polyneuropathy (TTR-FAP) with Val30Met and non-Val30Met: A phase III, open-label study.
Ando, Y; Ikeda, S; Machii, K; Misumi, Y; Morita, H; Obayashi, K; Ohta, M; Sekijima, Y; Takata, A; Ueda, M; Yamashita, T, 2016
)
0.82
" Tafamidis proved safe and well-tolerated."( Monitoring effectiveness and safety of Tafamidis in transthyretin amyloidosis in Italy: a longitudinal multicenter study in a non-endemic area.
Bisogni, G; Calabrese, D; Cavallaro, T; Cortese, A; Fabrizi, GM; Gemelli, C; Gentile, L; Grandis, M; Lozza, A; Luigetti, M; Manganelli, F; Mauro, A; Mazzeo, A; Obici, L; Pareyson, D; Perlini, S; Piscosquito, G; Pradotto, LG; Russo, M; Sabatelli, M; Santoro, L; Schenone, A; Stancanelli, C; Vita, G, 2016
)
1.61
"Long-term tafamidis was associated with a favourable safety/tolerability profile, without any unexpected adverse events."( Long-term safety and efficacy of tafamidis for the treatment of hereditary transthyretin amyloid polyneuropathy: results up to 6 years.
Amass, L; Barroso, FA; Ebede, B; Judge, DP; Li, H; Stewart, M; Sultan, MB, 2017
)
1.14
" Data on patient demographic and clinical characteristics and adverse drug reactions (ADRs) were captured using case-report forms."( Characteristics of Patients with Hereditary Transthyretin Amyloidosis and an Evaluation of the Safety of Tafamidis Meglumine in Japan: An Interim Analysis of an All-case Postmarketing Surveillance.
Ando, Y; Hirano, Y; Ishii, T; Matsumoto, N; Sekijima, Y; Takata, A; Ueda, M, 2020
)
0.77
" Incidence of adverse events in both tafamidis doses were comparable to placebo."( Efficacy and safety of tafamidis doses in the Tafamidis in Transthyretin Cardiomyopathy Clinical Trial (ATTR-ACT) and long-term extension study.
Damy, T; Garcia-Pavia, P; Gundapaneni, B; Hanna, M; Judge, DP; Merlini, G; Patterson, TA; Riley, S; Schwartz, JH; Sultan, MB; Witteles, R, 2021
)
1.2

Pharmacokinetics

ExcerptReferenceRelevance
" The method was also assessed for its applicability to pharmacokinetic studies in rats."( Development and validation of a liquid chromatography-tandem mass spectrometry method for the assay of tafamidis in rat plasma: Application to a pharmacokinetic study in rats.
Choi, S; Hyun, HC; Jeong, JW; Kim, HR; Kim, YS; Koo, TS; Lee, JH; Oh, JH, 2017
)
0.67
" The objective of this analysis was to develop a unified population pharmacokinetic (PK) model of tafamidis, which can describe the PK of various different formulations in healthy subjects as well as patients with TTR amyloidosis, and to understand effects of intrinsic and extrinsic factors on the PK variability."( Population pharmacokinetic modelling and simulation of tafamidis in healthy subjects and patients with transthyretin amyloidosis.
Harnisch, L; Huh, Y; Nicholas, T; Riley, S, 2021
)
1.09
" Several protein conjugation strategies have been developed for half-life extension."( Enhancing the Pharmacokinetic Profile of Interleukin 2 through Site-Specific Conjugation to a Selective Small-Molecule Transthyretin Ligand.
Alhamadsheh, MM; Liang, D; Liu, F; Park, MS; Ul Amin, T, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
" The oral bioavailability of AG10, combined with additional desirable drug-like features, makes it a very promising candidate to treat TTR amyloid cardiomyopathy."( AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretin.
Alhamadsheh, MM; Baranczak, A; Chan, WK; Connelly, S; Graef, IA; Kelly, JW; Liedtke, M; Park, MS; Penchala, SC; Powers, ET; Rappley, I; Reixach, N; Vogel, H; Wang, Y; Wilson, IA; Witteles, RM; Zhao, L, 2013
)
0.39

Dosage Studied

Tafamidis meglumine (Vyndaqel) can be dosed at 20 or 80 mg QD. An alternative single solid oral dosage formulation was developed for patient convenience.

ExcerptRelevanceReference
" Oral dosing in each of the three treatment periods was separated by a washout period of  ≥ 14 days."( The effect of tafamidis on the QTc interval in healthy subjects.
Klamerus, KJ; Moller, R; Riley, S; Wang, R; Watsky, E, 2015
)
0.78
" An alternative single solid oral dosage formulation (tafamidis 61-mg free acid capsules) was developed and introduced for patient convenience (approved in the United States, United Arab Emirates, and European Union)."( The Bioequivalence of Tafamidis 61-mg Free Acid Capsules and Tafamidis Meglumine 4 × 20-mg Capsules in Healthy Volunteers.
Le, VH; Lockwood, PA; O'Gorman, MT; Patterson, TA; Riley, S; Sultan, MB; Tankisheva, E; Wang, Q, 2020
)
1.12
"Tafamidis meglumine (Vyndaqel) can be dosed at 20 or 80 mg QD."( Tafamidis concentration required for transthyretin stabilisation in cerebrospinal fluid.
Coelho, T; Jaeger, M; Kelly, JW; Powers, ET; Tsai, FJ, 2023
)
3.8
"Tafamidis stabilises TTR in CSF to what is likely a clinically meaningful extent at CSF concentrations achieved by the normal tafamidis dosing regimen."( Tafamidis concentration required for transthyretin stabilisation in cerebrospinal fluid.
Coelho, T; Jaeger, M; Kelly, JW; Powers, ET; Tsai, FJ, 2023
)
3.8
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
central nervous system drugA class of drugs producing both physiological and psychological effects through a variety of mechanisms involving the central nervous system.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
1,3-benzoxazolesCompounds based on a fused 1,3-oxazole and benzene bicyclic ring skeleton.
monocarboxylic acidAn oxoacid containing a single carboxy group.
dichlorobenzeneAny member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TransthyretinHomo sapiens (human)IC50 (µMol)3.37130.16004.292110.0000AID1322954; AID1331731; AID1331734; AID1755162; AID1774080; AID1810837; AID1888717
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TransthyretinHomo sapiens (human)Kd0.42660.00301.348210.0000AID1322956; AID1322957; AID1386000; AID1452013; AID1452019; AID1605601; AID1605604; AID1705463; AID1705464; AID1774086; AID1848635; AID1848652
AlbuminHomo sapiens (human)Kd2.40000.08933.31358.0000AID1386001; AID1386002
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AlbuminHomo sapiens (human)PB21.45007.80007.80007.8000AID1386024; AID1386025
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
eye developmentRetinol-binding protein 4Homo sapiens (human)
positive regulation of immunoglobulin productionRetinol-binding protein 4Homo sapiens (human)
gluconeogenesisRetinol-binding protein 4Homo sapiens (human)
heart developmentRetinol-binding protein 4Homo sapiens (human)
visual perceptionRetinol-binding protein 4Homo sapiens (human)
maintenance of gastrointestinal epitheliumRetinol-binding protein 4Homo sapiens (human)
lung developmentRetinol-binding protein 4Homo sapiens (human)
positive regulation of insulin secretionRetinol-binding protein 4Homo sapiens (human)
response to retinoic acidRetinol-binding protein 4Homo sapiens (human)
retinol transportRetinol-binding protein 4Homo sapiens (human)
retinol metabolic processRetinol-binding protein 4Homo sapiens (human)
glucose homeostasisRetinol-binding protein 4Homo sapiens (human)
embryonic organ morphogenesisRetinol-binding protein 4Homo sapiens (human)
embryonic skeletal system developmentRetinol-binding protein 4Homo sapiens (human)
cardiac muscle tissue developmentRetinol-binding protein 4Homo sapiens (human)
female genitalia morphogenesisRetinol-binding protein 4Homo sapiens (human)
negative regulation of cardiac muscle cell proliferationRetinol-binding protein 4Homo sapiens (human)
embryonic retina morphogenesis in camera-type eyeRetinol-binding protein 4Homo sapiens (human)
uterus developmentRetinol-binding protein 4Homo sapiens (human)
vagina developmentRetinol-binding protein 4Homo sapiens (human)
urinary bladder developmentRetinol-binding protein 4Homo sapiens (human)
heart trabecula formationRetinol-binding protein 4Homo sapiens (human)
signal transductionTransthyretinHomo sapiens (human)
purine nucleobase metabolic processTransthyretinHomo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
protein bindingRetinol-binding protein 4Homo sapiens (human)
retinal bindingRetinol-binding protein 4Homo sapiens (human)
retinol bindingRetinol-binding protein 4Homo sapiens (human)
retinol transmembrane transporter activityRetinol-binding protein 4Homo sapiens (human)
hormone activityTransthyretinHomo sapiens (human)
protein bindingTransthyretinHomo sapiens (human)
identical protein bindingTransthyretinHomo sapiens (human)
thyroid hormone bindingTransthyretinHomo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
extracellular regionRetinol-binding protein 4Homo sapiens (human)
extracellular spaceRetinol-binding protein 4Homo sapiens (human)
extracellular exosomeRetinol-binding protein 4Homo sapiens (human)
extracellular spaceRetinol-binding protein 4Homo sapiens (human)
extracellular regionTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
azurophil granule lumenTransthyretinHomo sapiens (human)
extracellular exosomeTransthyretinHomo sapiens (human)
extracellular spaceTransthyretinHomo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (154)

Assay IDTitleYearJournalArticle
AID1386004Potency index, ratio of Kd for diflunisal to Kd for test compound for binding affinity to transthyretin (unknown origin) by ITC method2018Journal 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.
AID1615478Binding 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] spectroscopy2019Journal 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.
AID1755167Aqueous solubility of the compound in pH 6.8 JP2 fluid measured after 4 hrs by HPLC-UV analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1615449Binding 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] spectroscopy2019Journal 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.
AID1755181Cmax in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1755183AUC infinity in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1452015Inhibition 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 control2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
AID1696717Stabilization 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 2020Journal 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.
AID1898642Displacement of [125I]-T4 from human recombinant TTR expressed in Escherichia coli BL21(DE3) Star by gamma spectrometric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Targeting transthyretin in Alzheimer's disease: Drug discovery of small-molecule chaperones as disease-modifying drug candidates for Alzheimer's disease.
AID1725432Inhibition of amyloid beta aggregation in mouse N2a695 cells measured for 4 hrs by fluorescence correlation spectroscopic analysis2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1486518Inhibition 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 spectrophotometry2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors.
AID1848637Binding affinity to first binding site of wild type TTR (unknown origin) assessed as change in enthalpy by ITC analysis
AID1486520Displacement of [125I]-triiodothyronine from thyroid hormone receptor in rat liver membrane homogenates incubated for 18 hrs by scintillation counting method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors.
AID1322957Binding 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 method2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1896522Binding affinity to human serum TTR assessed as target occupancy incubated for 6 hrs by fluorescence polarization assay2022Journal 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.
AID1615490Binding 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] spectroscopy2019Journal 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.
AID1705464Binding affinity to wild type TTR (unknown origin) assessed as Kd2 by isothermal titration calorimetry2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.
AID1615473Binding 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] spectroscopy2019Journal 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.
AID1774080Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1386007Binding affinity to transthyretin (unknown origin) assessed as free TdeltaS changes by ITC method2018Journal 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.
AID1386032Binding 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 assay2018Journal 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.
AID1331734Inhibition 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 2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1615479Binding 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] spectroscopy2019Journal 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.
AID1615493Binding 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] spectroscopy2019Journal 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.
AID1615505Binding 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] spectroscopy2019Journal 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.
AID1615469Binding 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] spectroscopy2019Journal 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.
AID1810857Stabilization 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 assay2021Journal 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
AID1452016Inhibition 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 control2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
AID1615488Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as association rate at binding site-2 by surface plasmon resonance2019Journal 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.
AID1755170Protein binding in Sprague-Dawley rat plasma assessed as unbound fraction at 1 uM measured after 4 hrs by equilibrium dialysis assay2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1386029Binding 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 assay2018Journal 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.
AID1725430Inhibition of gamma secretase in mouse N2a695 cells using Sb4 substrate incubated for 3 hrs by ELISA2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1755166Aqueous solubility of the compound in pH 1.2 JP1 fluid measured after 4 hrs ny HPLC-UV analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1755168Permeability of the compound at 10 uM measured after 4 hrs by PAMPA based LC-MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1810858Stabilization 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 control2021Journal 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
AID1615507Binding affinity to wild-type TTR (unknown origin) assessed as stabilization of hydrogen bond between A120 and Y114 by 2D TROSY [1H-15N] spectroscopy2019Journal 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.
AID1848652Binding affinity to second binding site of wild type TTR (unknown origin) assessed as dissociation constant by ITC assay
AID1848655Binding affinity to second binding site of wild type TTR (unknown origin) assessed as change in enthalpy by ITC analysis
AID1725427Increase in APP fragmentation in mouse N2a695 cells at 10 uM incubated for 6 hrs by Western blot analysis2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1755164Metabolic 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 analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1386015Dissociation constant, pKa of the compound2018Journal 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.
AID1386024Binding affinity to human serum albumin assessed as compound level bound to protein at 30 uM measured immediately after gel filtration2018Journal 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.
AID1615486Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as association rate at binding site-1 by surface plasmon resonance2019Journal 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.
AID1774082Stabilization 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 control2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1615484Binding 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] spectroscopy2019Journal 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.
AID1810837Binding affinity to human plasma TTR tetramer assessed as displacement of diclofenac-coupled FITC by fluorescence polarization assay2021Journal 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
AID1615450Binding 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] spectroscopy2019Journal 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.
AID1386019Binding affinity to transthyretin (unknown origin) in human serum assessed as protein stabilization at 10 uM in pH 7.4 urea buffer by Western blot2018Journal 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.
AID1386002Binding affinity to human serum albumin2018Journal 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.
AID1386001Binding affinity to human serum albumin by ITC method2018Journal 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.
AID1452014Inhibition 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 control2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
AID1774081Stabilization 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 analysis2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1385999Binding affinity to transthyretin in dog serum assessed as protein stabilization at 10 uM by by Western blot2018Journal 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.
AID1486519Binding 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-HPLC2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors.
AID1386030Binding 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 assay2018Journal 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.
AID1725441Stabilization of recombinant dual FLAG-tagged wild type TTR (unknown origin) in plasma blood at < 30 uM incubated for 48 hrs by ion exchange chromatographic method2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1615492Binding 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] spectroscopy2019Journal 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.
AID1452013Competitive 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 spectrofluorometer2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
AID1725431Effect on TTR-induced amyloid beta aggregation inhibition in mouse N2a695 cells measured for 4 hrs by fluorescence correlation spectroscopic analysis2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1386006Binding affinity to transthyretin (unknown origin) assessed as free enthalpy changes by ITC method2018Journal 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.
AID1807499Binding 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 assay2021Journal 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.
AID1755185Volume of distribution at steady state in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1696718Stabilization 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 blot2020Journal 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.
AID1848657Binding affinity to second binding site of wild type TTR (unknown origin) assessed as change in entropy by ITC analysis
AID1322953Stabilization 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 a2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1331733Inhibition 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 re2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1755182Elimination half life in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1386008Binding 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 assay2018Journal 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.
AID1615485Binding 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] spectroscopy2019Journal 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.
AID1615502Binding 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] spectroscopy2019Journal 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.
AID1615470Binding 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] spectroscopy2019Journal 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.
AID1755162Inhibition 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 fluorescence2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1615477Binding 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] spectroscopy2019Journal 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.
AID1774086Binding affinity to TTR V30M mutant (unknown origin) by isothermal titration calorimetry2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1322954Stabilization 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 mic2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1331731Inhibition 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 co2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1452019Binding affinity to wild type TTR (unknown origin) assessed as equilibrium dissociation constant of second site by isothermal titration calorimetry2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
AID1725428Increase in APP-CTF fragmentation in mouse N2a695 cells at 10 uM incubated for 6 hrs by Western blot analysis2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1755163Binding affinity to TTR V30M mutant (unknown origin) expressed in Escherichia coli by isothermal titration calorimetry2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1888715Inhibition of Transthyretin V30M mutant (unknown origin) assessed as acid mediated fibril formation at 1.8 uM measured after 72 hrs by UV-vis spectrophotometry2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors.
AID1331729Inhibition 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 rela2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1615501Binding 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] spectroscopy2019Journal 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.
AID1605605Stabilization 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
AID1486521Displacement 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 control2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors.
AID1888712Inhibition 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 spectrophotometry2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors.
AID1386010Binding affinity to transthyretin in human serum assessed as protein stabilization at 2:1 compound to TTR ratio after 72 hrs by Western blot2018Journal 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.
AID1774083Stabilization 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 method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1810836Disruption of retional-induced bacterially expressed MBP-tagged RBP4-TTR (unknown origin) protein-protein interaction measured by d2 dye based HTFR assay2021Journal 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
AID1386003Potency index, ratio of Kd for tolcapone to Kd for test compound for binding affinity to transthyretin (unknown origin) by ITC method2018Journal 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.
AID1322964Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1615476Binding 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] spectroscopy2019Journal 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.
AID1386025Binding affinity to human serum albumin assessed as compound level bound to protein at 30 uM measured 124 hrs after dialysis2018Journal 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.
AID1386033Binding affinity to transthyretin in dog serum assessed as protein occupancy at 10 uM by fluorescent probe exclusion assay2018Journal 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.
AID1615474Binding 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] spectroscopy2019Journal 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.
AID1386028Binding 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 assay2018Journal 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.
AID1331732Inhibition 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 re2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1386000Binding affinity to transthyretin (unknown origin) by ITC method2018Journal 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.
AID1755165Metabolic stability in Sprague-Dawley rat liver microsomes assessed as residual rate at 1 uM measured after 30 mins by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1848635Binding affinity to first binding site of wild type TTR (unknown origin) assessed as dissociation constant by ITC assay
AID1386012Cmax in human at 80 mg qd2018Journal 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.
AID1615452Binding 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] spectroscopy2019Journal 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.
AID1322965Stabilization 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 densitometric2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1774075Inhibition 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%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1386018Binding affinity to transthyretin (unknown origin) in human serum assessed as protein occupancy at 200 uM by fluorescent probe exclusion assay2018Journal 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.
AID1725434Brain concentration in 5XFAD mouse at 50 mg/kg, po measured after 15 days by LC-MS/MS analysis2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1888717Inhibition of urea-induced Transthyretin denaturation in human plasma preincubated for 1 hr followed by urea addition by Western blot analysis2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors.
AID1615494Binding 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] spectroscopy2019Journal 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.
AID1615448Binding 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 spectroscopy2019Journal 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.
AID1605604Stabilization 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
AID1848656Binding affinity to first binding site of wild type TTR (unknown origin) assessed as change in entropy by ITC analysis
AID1322960Displacement of [125I]-T4 from wild type TTR in human plasma after 1 hr by PAGE analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1322956Binding 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 method2016European journal of medicinal chemistry, Oct-04, Volume: 121A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.
AID1615487Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as dissociation rate at binding site-1 by surface plasmon resonance2019Journal 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.
AID1774085Stabilization 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 method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1386009Binding affinity to transthyretin in human serum assessed as protein occupancy at 2:1 compound to TTR ratio after 72 hrs by fluorescent probe exclusion assay2018Journal 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.
AID1615508Binding affinity to wild-type TTR (unknown origin) assessed as stabilization of hydrogen bond between V121 and T106 by 2D TROSY [1H-15N] spectroscopy2019Journal 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.
AID1848654Binding affinity to second binding site of wild type TTR (unknown origin) assessed as gibbs free energy change by ITC analysis
AID1386031Binding 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 assay2018Journal 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.
AID1331730Inhibition 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 rela2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1615489Negative cooperative binding affinity to wild-type biotinylated human TTR assessed as dissociation rate at binding site-2 by surface plasmon resonance2019Journal 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.
AID1615471Binding 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] spectroscopy2019Journal 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.
AID1605603Stabilization 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%)
AID1774076Inhibition 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%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1810859Stabilization of human plasma TTR assessed as increase in dimer band intensity at 50 uM measured after 72 hrs by Western blotting analysis2021Journal 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
AID1888714Inhibition of Transthyretin V30M mutant (unknown origin) assessed as acid mediated fibril formation at 3.6 uM measured after 72 hrs by UV-vis spectrophotometry2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors.
AID1615480Binding 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] spectroscopy2019Journal 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.
AID1331735Inhibition 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 t2016European journal of medicinal chemistry, Nov-10, Volume: 123Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.
AID1755186AUC (0 to 8 hrs) in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1705463Binding affinity to wild type TTR (unknown origin) assessed as Kd1 by isothermal titration calorimetry2020Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.
AID1755184Total clearance in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1615468Binding 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] spectroscopy2019Journal 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.
AID1615481Binding 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] spectroscopy2019Journal 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.
AID1452017Inhibition 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 control2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
AID1755187Bioavailability in Sprague-Dawley rat at 0.1 mg/kg, iv measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1848653Binding affinity to first binding site of wild type TTR (unknown origin) assessed as gibbs free energy change by ITC analysis
AID1755190AUC (0 to 8 hrs) in Sprague-Dawley rat at 0.1 mg/kg, po measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1386005Binding affinity to transthyretin (unknown origin) assessed as free energy changes by ITC method2018Journal 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.
AID1725433Plasma concentration in 5XFAD mouse at 50 mg/kg, po measured after 15 days by LC-MS/MS analysis2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Brain Permeable Tafamidis Amide Analogs for Stabilizing TTR and Reducing APP Cleavage.
AID1755189Tmax in Sprague-Dawley rat at 0.1 mg/kg, po measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1755188Cmax in Sprague-Dawley rat at 0.1 mg/kg, po measured up to 8 hrs by LC-MS/MS analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1615475Binding 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] spectroscopy2019Journal 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.
AID1615483Binding 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] spectroscopy2019Journal 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.
AID1605601Stabilization 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
AID1615472Binding 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] spectroscopy2019Journal 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.
AID1615495Binding 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] spectroscopy2019Journal 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.
AID1615504Binding 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] spectroscopy2019Journal 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.
AID1888713Inhibition 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 spectrophotometry2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors.
AID1615482Binding 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] spectroscopy2019Journal 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.
AID1755169Intrinsic 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 analysis2021Bioorganic & medicinal chemistry, 08-15, Volume: 44Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1810838Displacement of [3H]-all trans retinol from human urine biotinylated RBP4 incubated for 16 hrs measured by Scintillation Proximity Assay2021Journal 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
AID1346206Human transthyretin (Carrier proteins)2012Proceedings 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.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2013Proceedings 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]

Research

Studies (212)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (0.47)29.6817
2010's101 (47.64)24.3611
2020's110 (51.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 77.46

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index77.46 (24.57)
Research Supply Index5.51 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index130.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (77.46)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials25 (11.26%)5.53%
Reviews45 (20.27%)6.00%
Case Studies19 (8.56%)4.05%
Observational4 (1.80%)0.25%
Other129 (58.11%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]