ChEMBL ligand: CHEMBL2103837 (FX-1005, FX-1006, FX1006, Tafamidis, Vyndamax)
retinol binding protein 4/Retinol-binding protein 4 in Human [ChEMBL: CHEMBL3100] [GtoPdb: 2549] [UniProtKB: P02753] There should be some charts here, you may need to enable JavaScript!
transthyretin/Transthyretin in Human [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766] 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
retinol binding protein 4/Retinol-binding protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3100] [GtoPdb: 2549] [UniProtKB: P02753]
ChEMBL	Displacement of [3H]-all trans retinol from human urine biotinylated RBP4 incubated for 16 hrs measured by Scintillation Proximity Assay	B	4.52	pIC50	>30000	nM	IC50	J Med Chem (2021) 64: 9010-9041 [PMID:34138572]
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 wild type TTR (unknown origin) assessed as Kd2 by isothermal titration calorimetry	B	6.56	pKd	278	nM	Kd	J Med Chem (2020) 63: 14228-14242 [PMID:32914975]
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 N-terminal hexa-histidine tagged TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as dissociation constant at 60 uM by ITC assay	B	6.59	pKd	260	nM	Kd	J Med Chem (2023) 66: 15511-15523 [PMID:37910439]
ChEMBL	Binding affinity to second binding site of wild type TTR (unknown origin) assessed as dissociation constant by ITC assay	B	6.59	pKd	260	nM	Kd	J Med Chem (2022) 65: 14673-14691 [PMID:36306808]
ChEMBL	Binding affinity to TTR V30M mutant (unknown origin) by isothermal titration calorimetry	B	6.7	pKd	200	nM	Kd	J Med Chem (2021) 64: 14344-14357 [PMID:34547896]
ChEMBL	Binding affinity to TTR V30M mutant (unknown origin) assessed as dissociation constant by ITC analysis	B	6.86	pKd	138	nM	Kd	J Med Chem (2024) 67: 6987-7005 [PMID:38670538]
ChEMBL	Binding affinity to first binding site of wild type TTR (unknown origin) assessed as dissociation constant by ITC assay	B	8	pKd	9.9	nM	Kd	J Med Chem (2022) 65: 14673-14691 [PMID:36306808]
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]
ChEMBL	Binding affinity to wild type TTR (unknown origin) assessed as Kd1 by isothermal titration calorimetry	B	8.52	pKd	3	nM	Kd	J Med Chem (2020) 63: 14228-14242 [PMID:32914975]
GtoPdb	-	-	8.7	pKd	2	nM	Kd	Proc Natl Acad Sci USA (2012) 109: 9629-34 [PMID:22645360]
ChEMBL	Inhibition of recombinant N-terminal hexa-histidine tagged TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as acid mediated amyloid-like fibril formation by measuring turbidity incubated for 1 week at 310K in presence of sodium acetate by absorbance based assay	B	5.51	pKi	3100	nM	Ki	J Med Chem (2023) 66: 15511-15523 [PMID:37910439]
ChEMBL	Inhibition of urea-induced Transthyretin denaturation in human plasma preincubated for 1 hr followed by urea addition by Western blot analysis	B	5.03	pIC50	9300	nM	IC50	Bioorg Med Chem (2022) 53: 116550-116550 [PMID:34890995]
ChEMBL	Inhibition of acid mediated TTR V30M mutant aggregation (unknown origin) expressed in Escherichia coli preincubated for 30 mins followed by acetic buffer addition at pH 4.7 and measured after 7 days by thioflavin T based fluorescence analysis	B	5.26	pIC50	5500	nM	IC50	Bioorg Med Chem (2023) 90: 117370-117370 [PMID:37311373]
ChEMBL	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 assay	B	5.28	pIC50	5300	nM	IC50	Bioorg Med Chem (2021) 44: 116292-116292 [PMID:34225167]
ChEMBL	Covalent inhibition of urea-induced Transthyretin denaturation in human plasma preincubated for 1 hr followed by urea addition by Western blot analysis	B	5.46	pIC50	3490	nM	IC50	J Med Chem (2023) 66: 2893-2903 [PMID:36749109]
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	In vitro evaluation of inhibitory activity against WT-TTR: In vitro evaluation of inhibitory activity against WT-TTR amyloid fibril formation of AT09 and reference compounds. Reference compounds (thyroxine, tafamidis and 2OH—PCB80) are represented by dash bars and AT09 compounds by solid-gray bars. All compounds were analyzed at 2×, 1× and 0.5× the molar concentration of wild-type TTR (3.6 μM). Upon assay completion at 72 hours incubation at 37° C., the percentage of amyloid fibril formation was normalized against the positive control (black bar) corresponding to 100% of amyloid formation in the absence of test compounds.	B	5.51	pIC50	3100	nM	IC50	US-10377729-B2. Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP) (2019)
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	Stabilization of TTR V30M mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio incubated for 1 week by absorbance method	B	5.59	pIC50	2600	nM	IC50	J Med Chem (2021) 64: 14344-14357 [PMID:34547896]
ChEMBL	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 control	B	5.79	pIC50	1620	nM	IC50	Eur J Med Chem (2016) 123: 777-787 [PMID:27541261]
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	Binding affinity to human plasma TTR tetramer assessed as displacement of diclofenac-coupled FITC by fluorescence polarization assay	B	6.39	pIC50	410	nM	IC50	J Med Chem (2021) 64: 9010-9041 [PMID:34138572]
ChEMBL	Binding affinity to TTR in human plasma assessed as target occupancy incubated for 6 hrs in presence of E)-S-phenyl 3-(4-hydroxy-3,5-dimethyistyryl)benzothioate by fluorescence based competitive binding assay	B	4.81	pEC50	15600	nM	EC50	J Med Chem (2024) 67: 6987-7005 [PMID:38670538]
ChEMBL	Inhibition of wild type human transthyretin extracted from Escherichia coli	B	5.57	pEC50	2700	nM	EC50	Eur J Med Chem (2024) 275: 116593-116593 [PMID:38889609]
ChEMBL	Inhibition of wild type TTR (unknown origin)	B	8.57	pEC50	2.7	nM	EC50	Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
ChEMBL	Inhibition of TTR V30M mutant (unknown origin)	B	8.57	pEC50	2.7	nM	EC50	Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]
ChEMBL	Inhibition of TTR V122I mutant (unknown origin)	B	8.57	pEC50	2.7	nM	EC50	Eur J Med Chem (2022) 243: 114742-114742 [PMID:36155354]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]