15-deoxy-Δ-12,14-prostaglandin J2 [Ligand Id: 2692] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL482477
  • Macrophage migration inhibitory factor in Human [ChEMBL: CHEMBL2085] [UniProtKB: P14174]
  • Macrophage migration inhibitory factor in Rat [ChEMBL: CHEMBL4524037] [UniProtKB: P30904]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Transient receptor potential cation channel subfamily A member 1 in Rhesus macaque [ChEMBL: CHEMBL6066835] [UniProtKB: A0A1D5QMT1]
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Macrophage migration inhibitory factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2085] [UniProtKB: P14174]
ChEMBL Inhibition of [3H]-BTZO-1 binding to recombinant human C-terminal His-tagged MIF expressed in Escherichia coli BL21 (DE3) measured after 3 hrs by SPA B 5.44 pIC50 3600 nM IC50 Chem Biol (2010) 17: 1282-1294 [PMID:21168764]
Macrophage migration inhibitory factor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4524037] [UniProtKB: P30904]
ChEMBL Inhibition of recombinant rat MIF expressed in Escherichia coli BL21 (DE3) assessed as reduction in tautomerase activity using L-dopachrome carboxy-methyl ester as substrate by spectrophotometry B 5.43 pIC50 3700 nM IC50 Chem Biol (2010) 17: 1282-1294 [PMID:21168764]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Binding affinity to PPARgamma B 5.7 pKd 2000 nM Kd J Med Chem (2012) 55: 4027-4061 [PMID:22260081]
GtoPdb - - 6.3 pIC50 - - - Proc Natl Acad Sci USA (1997) 94: 4318-23 [PMID:9113987];
Cell (1995) 83: 813-9 [PMID:8521498];
Anal Biochem (1998) 257: 112-9 [PMID:9514791];
Cell Signal (2002) 14: 573-83 [PMID:11955950];
Biochem Biophys Res Commun (2005) 337: 521-5 [PMID:16198309]
Transient receptor potential cation channel subfamily A member 1 in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6066835] [UniProtKB: A0A1D5QMT1]
ChEMBL Agonist activity at rhesus monkey TRPA1 transfected in HEK293F cells assessed as increase in Ca2+ influx by FLIPR calcium assay B 4 pEC50 >100000 nM EC50 J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL Agonist activity at full length human TRPA1 transfected in HEK293F cells assessed as increase in Ca2+ influx by FLIPR calcium assay B 4.39 pEC50 40400 nM EC50 J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
ChEMBL Activation of TRPA1 channel B 5.25 pEC50 5600 nM EC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
ChEMBL Agonist activity at full length mouse TRPA1 transfected in HEK293F cells assessed as increase in Ca2+ influx by FLIPR calcium assay B 4.25 pEC50 56400 nM EC50 J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
ChEMBL Agonist activity at full length rat TRPA1 transfected in HEK293F cells assessed as increase in Ca2+ influx by FLIPR calcium assay B 4.7 pEC50 19900 nM EC50 J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]

ChEMBL data shown on this page come from version 36:

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]