ISO-1 [Ligand Id: 9984] 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: CHEMBL210858
  • Macrophage migration inhibitory factor in Human [ChEMBL: CHEMBL2085] [UniProtKB: P14174]
  • Macrophage migration inhibitory factor in Mouse [ChEMBL: CHEMBL1926491] [UniProtKB: P34884]
There should be some charts here, you may need to enable JavaScript!
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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
Macrophage migration inhibitory factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2085] [UniProtKB: P14174]
ChEMBL Displacement of 4'-(7-Hydroxy-2-oxo-2H-chromen-3-yl)-[1,1'-biphenyl]-4-carboxylic acid from C-terminal His-tagged recombinant human MIF expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins followed by probe addition and measured after 10 mins by fluorescence assay B 4.33 pKd 47000 nM Kd J Med Chem (2020) 63: 11920-11933 [PMID:32940040]
ChEMBL Inhibition of C-terminal His-tagged recombinant human MIF expressed in Escherichia coli BL21 (DE3) using 4-HPP as substrate preincubated for 10 mins followed by substrate addition by UV absorption spectrum analysis B 4.36 pKi 44000 nM Ki J Med Chem (2020) 63: 11920-11933 [PMID:32940040]
ChEMBL Inhibition of C-terminal His-tagged recombinant human MIF tautomerase activity expressed in Escherichia coli BL21 using 4-hydroxyphenyl pyruvic acid as substrate preincubated for 15 mins followed by substrate addition and measured for 10 mins in presence of 0.5 mM EDTA by UV absorbance based Cheng-Prusoff equation analysis B 4.36 pKi 44000 nM Ki Eur J Med Chem (2020) 186: 111849-111849 [PMID:31767137]
ChEMBL Inhibition of dopachrome tautomerase activity of human recombinant MIF B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2009) 19: 4773-4776 [PMID:19592246]
ChEMBL Inhibition of recombinant His-tagged MIF tautomerase activity (unknown origin) using 4-HPP as substrate B 4.1 pIC50 79000 nM IC50 Bioorg Med Chem (2018) 26: 999-1005 [PMID:29428527]
ChEMBL Inhibition of dopachrome tautomerase activity of MIF in human THP1 cells B 4.16 pIC50 69000 nM IC50 Bioorg Med Chem Lett (2009) 19: 4773-4776 [PMID:19592246]
ChEMBL Inhibition of C-terminal His-tagged recombinant human MIF tautomerase activity expressed in Escherichia coli BL21 using 4-hydroxyphenyl pyruvic acid as substrate preincubated for 15 mins followed by substrate addition and measured for 10 mins in presence of 0.5 mM EDTA by UV absorbance analysis B 4.19 pIC50 64000 nM IC50 Eur J Med Chem (2020) 186: 111849-111849 [PMID:31767137]
ChEMBL Inhibition of spontaneous secretion/release/recognition of MIF from freshly isolated human PBMC by ELISA B 4.6 pIC50 25000 nM IC50 Bioorg Med Chem Lett (2009) 19: 4773-4776 [PMID:19592246]
ChEMBL Inhibition of recombinant human MIF (Pro2 to Ala115 residues) expressed in Escherichia coli using dopachrome methyl ester as substrate preincubated with protein followed by substrate addition B 4.74 pIC50 18200 nM IC50 J Med Chem (2018) 61: 8104-8119 [PMID:29812929]
ChEMBL Inhibition of MIF tautomerase activity B 4.96 pIC50 11000 nM IC50 Bioorg Med Chem Lett (2006) 16: 3376-3379 [PMID:16682188]
ChEMBL Inhibition of recombinant MIF (unknown origin) tautomerase activity using dopachrome methyl ester as substrate measured for 2 to 20 secs by spectrophotometric analysis B 5.15 pIC50 7000 nM IC50 J Med Chem (2018) 61: 8104-8119 [PMID:29812929]
Macrophage migration inhibitory factor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926491] [UniProtKB: P34884]
ChEMBL Enzyme Assay: MIF tautomerase activity was measured by UV-Visible recording spectrophotometry (SHIMADZU, UV1600U). A fresh stock solution of L-dopachrome methyl ester was prepared at 2.4 mM through oxidation of L-3,4-dihydroxyphenylalanine methyl ester with sodium periodate. 1 μL of MIF solution (800-900 ng/mL) and 1 μL of a DMSO solution with various concentrations of the enzymatic inhibitor were added into a plastic cuvette (10 mm, 1.5 mL) containing 0.7 mL assay buffer (50 mM potassium phosphate, pH 7.2). Then L-dopachrome methyl ester solution (0.3 mL) was added to the assay buffer mixture. Activity was determined at room temperature and the spectrometric measurements were made at λ=475 nm for 20 seconds by monitoring the rate of decolorization of L-dopachrome methyl ester in comparison to a standard solution. B 4.96 pIC50 11000 nM IC50 US-8618147-B2. Modified macrophage migration inhibitory factor inhibitors (2013)
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in rat brain by competition binding assay B 6.99 pKi 102.3 nM Ki Medchemcomm (2015) 6: 1093-1103

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]