compound 30 [PMID: 15953724] [Ligand Id: 8812] 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: CHEMBL180650
  • 5-lipoxygenase activating protein in Human [ChEMBL: CHEMBL4550] [UniProtKB: P20292]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • mPGES2/Prostaglandin E synthase 2 in Human [ChEMBL: CHEMBL4411] [GtoPdb: 1378] [UniProtKB: Q9H7Z7]
There should be some charts here, you may need to enable JavaScript!
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
5-lipoxygenase activating protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4550] [UniProtKB: P20292]
ChEMBL In vitro binding affinity against FLAP (5-Lipoxygenase activation protein) B 6 pIC50 >1000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 3352-3355 [PMID:15953724]
ChEMBL Inhibition of FLAP B 6 pIC50 >1000 nM IC50 J. Med. Chem. (2008) 51: 4059-4067 [PMID:18459759]
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Inhibition of purified mPGES-1 (1 to 152) (unknown origin) extracted from detergent-solubilized baculovirus-infected insect Sf9 cell membranes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis B 6.02 pIC50 960 nM IC50 J. Med. Chem. (2015) 58: 4727-4737 [PMID:25961169]
ChEMBL Inhibition of recombinant human mPGES-1 expressed in human 293E cell microsomes using PGH2 as substrate assessed as PGE2 production after 2.5 mins by LC/MS analysis B 7.64 pIC50 23 nM IC50 J. Med. Chem. (2015) 58: 4727-4737 [PMID:25961169]
GtoPdb - - 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2005) 15: 3352-5 [PMID:15953724]
ChEMBL Inhibition of human microsomal PGES1 in cell-free system assessed as inhibition of conversion of PGH2 to PGE2 by HPLC assay B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2011) 54: 3163-3174 [PMID:21466167]
mPGES2/Prostaglandin E synthase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4411] [GtoPdb: 1378] [UniProtKB: Q9H7Z7]
GtoPdb - - 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3352-5 [PMID:15953724]
ChEMBL In vitro inhibition against recombinant human mPGES-2 B 6 pIC50 >1000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 3352-3355 [PMID:15953724]
ChEMBL Inhibition of human mPGES2 B 6 pIC50 >1000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6816-6820 [PMID:18029174]
ChEMBL Inhibition of mPGES2 B 6 pIC50 >1000 nM IC50 J. Med. Chem. (2008) 51: 4059-4067 [PMID:18459759]
ChEMBL Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1) B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 3352-3355 [PMID:15953724]
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL Inhibition of TX synthase B 6 pIC50 >1000 nM IC50 J. Med. Chem. (2008) 51: 4059-4067 [PMID:18459759]
ChEMBL In vitro inhibition against human Thromboxane synthase B 6.02 pIC50 950 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 3352-3355 [PMID:15953724]
ChEMBL Inhibition of TX synthase B 6.02 pIC50 950 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6816-6820 [PMID:18029174]

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]