MF63 [Ligand Id: 14084] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL412099 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330] | ||||||||
| ChEMBL | Inhibition of PGF synthase in IL1-beta treated human A549 cell microsome assessed as inhibition of PGF2alpha production after 1 min in presence of 50% FBS | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1488-1492 [PMID:21295979] |
| Microsomal prostaglandin E synthase-1 in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5152] [UniProtKB: Q2TJZ7] | ||||||||
| ChEMBL | Inhibition of guinea pig mPGES1 | B | 9.05 | pIC50 | 0.9 | 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 mPGES1 in LPS-stimulated human whole blood assessed as reduction in PGE2 production incubated for 24 hrs at 37 degC by enzyme immunoassay | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2012) 55: 2597-2605 [PMID:22380511] |
| ChEMBL | Inhibition of PGES-1 in human whole blood assessed as LPS-induced PGE2 formation incubated for 15 mins prior to LPS addition measured after 24 hrs by EIA | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2013) 56: 3296-3309 [PMID:23527738] |
| ChEMBL | Inhibition of purified microsomal PGES1 (unknown origin) | B | 5.8 | pIC50 | 1600 | nM | IC50 | Medchemcomm (2015) 6: 2081-2123 |
| 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 | 5.8 | pIC50 | 1590 | nM | IC50 | J Med Chem (2015) 58: 4727-4737 [PMID:25961169] |
| ChEMBL | Inhibition of mPGES1 in human whole blood assessed as inhibition of LPS-induced PGE2 production measured after 20 to 24 hrs | B | 5.87 | pIC50 | 1360 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5131-5138 [PMID:29100801] |
| ChEMBL | Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated followed by LPS stimulation for 20 to 24 hrs | B | 5.87 | pIC50 | 1360 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5977-5984 [PMID:27865703] |
| ChEMBL | Inhibition of mPGES1 in LPS-stimulated human whole blood assessed as inhibition of PGE2 production | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1488-1492 [PMID:21295979] |
| ChEMBL | Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis | B | 6.17 | pIC50 | 676 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
| ChEMBL | Inhibition of mPGES1 in IL1-beta treated human A549 cell microsome assessed as inhibition of PGE2 production after 1 min in presence of 50% FBS | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1488-1492 [PMID:21295979] |
| ChEMBL | Inhibition of mPGES1 in IL-1-beta-stimulated human A549 cells assessed as blockade of PGH2 to PGE2 conversion in presence of 50% fetal bovine serum | B | 6.38 | pIC50 | 420 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5837-5841 [PMID:19748780] |
| ChEMBL | Inhibition of mPGES1 in rhIL-1beta-stimulated human A549 cells assessed as PGE2 level treated for 18 hrs after 30 mins pre-incubation with rhIL-1beta by EIA method | B | 7.12 | pIC50 | 76 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
| ChEMBL | Inhibition of mPGES-1 in human A549 cells assessed as reduction in interleukin-1 beta-induced PGE2 production incubated for 30 mins followed by IL-1beta stimulation for 16 to 20 hrs in presence of 2% fetal bovine serum by HTRF assay | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5977-5984 [PMID:27865703] |
| ChEMBL | Inhibition of mPGES-1 in human A549 cells assessed as decrease in IL1beta induced PGE2 release preincubated for 30 mins followed by IL-1beta addition after 16 to 20 hrs by HTRF method | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2594-2601 [PMID:28400234] |
| 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 | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2015) 58: 4727-4737 [PMID:25961169] |
| ChEMBL | Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis | B | 8.28 | pIC50 | 5.3 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
| ChEMBL | Inhibition of microsomal PGES1 transfected in human HEK293 cells assessed as PGE2 production after 60 mins by HTRF assay | B | 8.37 | pIC50 | 4.3 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 285-288 [PMID:22137787] |
| ChEMBL | Inhibition of microsomal PGES-1 (unknown origin) assessed as PGH2 conversion to PGE2 after 1 min by enzyme immunoassay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2764-2767 [PMID:24794107] |
| ChEMBL | Inhibition of mPGES1 expressed in Escherichia coli Rosetta-DE3 assessed as reduction in PGE2 production by enzyme immunoassay based cell-free system assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2012) 55: 2597-2605 [PMID:22380511] |
| ChEMBL | Inhibition of full-length microsomal PGES-1 (unknown origin) expressed in Escherichia coli Rosetta(DE3) using PGH2 as substrate assessed as inhibition of PGH2 conversion to PGE2 incubated 15 mins prior to substrate addition measured after 1 min by EIA | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2013) 56: 3296-3309 [PMID:23527738] |
| ChEMBL | Inhibition of human recombinant mPGES-1 expressed in CHO cells assessed as reduction in conversion of PGH2 to PGE2 incubated for 10 mins followed by substrate addition measured after 1 min in presence of GSH | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5977-5984 [PMID:27865703] |
| ChEMBL | Inhibition of recombinant human mPGES-1 expressed in CHO cells assessed as reduction in PGE2 formation using PGH2 a substrate preincubated for 10 mins followed by substrate addition measured after 1 min | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2594-2601 [PMID:28400234] |
| GtoPdb | - | - | 8.89 | pIC50 | 1.3 | nM | IC50 | J Pharmacol Exp Ther (2008) 326: 754-63 [PMID:18524979] |
| ChEMBL | Displacement of [3H]PGH2 from human recombinant PGES1 expressed in CHOK1 cells | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5837-5841 [PMID:19748780] |
| ChEMBL | Inhibition of human recombinant mPGES-1 using PGH2 as substrate incubated 20 mins prior to substrate addition measured after 30 secs by EIA | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 907-911 [PMID:23266122] |
| ChEMBL | Inhibition of mPGES1 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1488-1492 [PMID:21295979] |
| ChEMBL | Inhibition of human mPGES1 assessed as PGE2 level after 41 sec by ELISA | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1604-1609 [PMID:20144869] |
| mPGES2/Prostaglandin E synthase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4411] [GtoPdb: 1378] [UniProtKB: Q9H7Z7] | ||||||||
| ChEMBL | Inhibition of human mPGES2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6816-6820 [PMID:18029174] |
| ChEMBL | Inhibition of human PGES2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5837-5841 [PMID:19748780] |
| CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
| ChEMBL | Inhibition of TX synthase in LPS-stimulated human whole blood assessed as inhibition of TXB2 production | B | 4.4 | pIC50 | >40000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1488-1492 [PMID:21295979] |
| ChEMBL | Inhibition of TX synthase | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6816-6820 [PMID:18029174] |
| ChEMBL | Inhibition of TX synthase | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5837-5841 [PMID:19748780] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of human JAK2 | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6816-6820 [PMID:18029174] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of human JAK3 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6816-6820 [PMID:18029174] |
ChEMBL data shown on this page come from version 35:
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]
