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ChEMBL ligand: CHEMBL210858 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]