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ChEMBL ligand: CHEMBL180650 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]