cambritaxestat [Ligand Id: 13506] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3917975
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
autotaxin/Autotaxin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3691] [GtoPdb: 2901] [UniProtKB: Q13822]
ChEMBL Inhibition of ATX in human plasma assessed as decrease in LPA C18:1 levels after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay B 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639]
ChEMBL Inhibition of ATX in human plasma assessed as decrease in hydrolysis of lysophosphatidylcholine by measuring choline release after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639]
GtoPdb Inhibition of human recombinant ATX in vitro - 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639]
ChEMBL Inhibition of human recombinant ATX using Rac-1-Palmitoyl-glycero-3-phosphocholine as substrate incubated for 2 hrs using ADHP fluorogenic peroxidase substrate by horseradish peroxidase/choline oxidase-coupled assay B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639]
ChEMBL Inhibition of human recombinant ATX/LPC 18:1-mediated mouse 4T1 cell migration after overnight incubation by Transwell assay B 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639]

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]