AZD1981 [Ligand Id: 7680] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1914489 (Azd 1981, AZD-1981)
  • aldo-keto reductase family 1 member B/Aldose reductase in Human [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
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  • DP2 receptor/G protein-coupled receptor 44 in Human [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aldo-keto reductase family 1 member B/Aldose reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
ChEMBL Inhibition of human recombinant aldose reductase 1 after 15 mins by spectrophotometry analysis B 6.1 pIC50 794 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6288-6292 [PMID:21944852]
DP2 receptor/G protein-coupled receptor 44 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5071] [GtoPdb: 339] [UniProtKB: Q9Y5Y4]
ChEMBL Antagonist activity against human CRTh2 receptor in human eosinophils assessed as inhibition of DK-PGD2-induced CD11b expression F 8 pIC50 10 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6288-6292 [PMID:21944852]
ChEMBL Displacement of [3H]PGD2 from human CRTH2 receptor B 8.37 pIC50 4.3 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6288-6292 [PMID:21944852]
ChEMBL Displacement of [3H]PGD2 from recombinant human CRTH2 expressed in HEK293 cells after 2 hrs by microbeta scintillation counting B 8.37 pIC50 4.3 nM IC50 J. Med. Chem. (2012) 55: 2915-2931 [PMID:22224640]
GtoPdb Displacement of [3H]PGD2 from human DP2 receptor - 8.37 pIC50 4.3 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6288-92 [PMID:21944852]

ChEMBL data shown on this page come from version 27:

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]