tafamidis [Ligand Id: 8378] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL2103837 (Tafamidis, Vyndamax, Vyndaqel, FX-1005, FX-1006, FX1006)
  • transthyretin/Transthyretin in Human [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
  • This target only has 0 pki data point
  • 0
1 CHEMBL2103837_lig_chart_1 Transthyretin Human
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
ChEMBL 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 to 28) addition by ITC assay (Rvb = 3 +/- 0.2 microM) B 5.55 pKd 2800 nM Kd J Med Chem (2020) 63: 3205-3214 [PMID:32124607]
ChEMBL 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 42) addition by ITC assay (Rvb = 0.94 +/- 0.04 microM) B 5.98 pKd 1050 nM Kd J Med Chem (2020) 63: 3205-3214 [PMID:32124607]
ChEMBL 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 B 6.43 pKd 370 nM Kd J Med Chem (2017) 60: 7820-7834 [PMID:28920684]
ChEMBL Binding affinity to wild type TTR (unknown origin) assessed as equilibrium dissociation constant of second site by isothermal titration calorimetry B 6.56 pKd 278 nM Kd J Med Chem (2017) 60: 7820-7834 [PMID:28920684]
ChEMBL 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 B 6.56 pKd 274 nM Kd Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL 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 B 8.03 pKd 9.3 nM Kd Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL Binding affinity to transthyretin (unknown origin) by ITC method B 8.36 pKd 4.4 nM Kd J Med Chem (2018) 61: 7862-7876 [PMID:30133284]
GtoPdb - - 8.7 pKd 2 nM Kd Proc Natl Acad Sci USA (2012) 109: 9629-34 [PMID:22645360]
ChEMBL 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 microplate spectrophotometric method B 5.51 pIC50 3100 nM IC50 Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL 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 microplate spectrophotometric method B 5.51 pIC50 3090.3 nM IC50 Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL 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 control B 5.81 pIC50 1550 nM IC50 Eur J Med Chem (2016) 123: 777-787 [PMID:27541261]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]