acoramidis [Ligand Id: 13628] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3940890 (Acoramidis, AG-10, AG10)
  • retinol binding protein 4/Plasma retinol-binding protein in Human [ChEMBL: CHEMBL3100] [GtoPdb: 2549] [UniProtKB: P02753]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
retinol binding protein 4/Plasma retinol-binding protein 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 Binding affinity to human plasma wild type TTR assessed as dissociation constants for first binding site of TTR by isothermal titration calorimetric method B 6.5 pKd 314 nM Kd Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL Binding affinity to human TTR incubated for 20 mins by fluorescence polarization assay B 8.14 pKd 7.3 nM Kd J Med Chem (2022) 65: 15473-15486 [PMID:36327103]
ChEMBL Binding affinity to human plasma wild type TTR assessed as dissociation constants for second binding site of TTR by isothermal titration calorimetric method B 8.32 pKd 4.8 nM Kd Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL Binding affinity to transthyretin (unknown origin) by ITC method B 8.32 pKd 4.8 nM Kd J Med Chem (2018) 61: 7862-7876 [PMID:30133284]
GtoPdb Protein stabiliser - 8.32 pKd 4.8 nM Kd Proc Natl Acad Sci USA (2013) 110: 9992-7 [PMID:23716704]
ChEMBL Binding affinity to human plasma TTR tetramer assessed as displacement of diclofenac-coupled FITC by fluorescence polarization assay B 6.8 pIC50 160 nM IC50 J Med Chem (2021) 64: 9010-9041 [PMID:34138572]

ChEMBL data shown on this page come from version 34:

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]