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Assay Detail

CHEMBL4722622

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Macrophage migration inhibitory factor (CHEMBL2085)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF).
Xiao Z,Fokkens M,Chen D,Kok T,Proietti G,van Merkerk R,Poelarends GJ,Dekker FJ
Eur J Med Chem (2020) 186 : 111849 -111849
PubMed 31767137 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 4.93 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3953102 1 6.36
CHEMBL4741927 1 6.02
CHEMBL4745151 1 5.48
CHEMBL4751935 1 5.30
CHEMBL4749241 1 5.19
CHEMBL4754122 1 5.16
CHEMBL4763772 1 5.16
CHEMBL4755471 1 4.77
CHEMBL4800056 1 4.72
CHEMBL4782511 1 4.64
CHEMBL4752116 1 4.64
CHEMBL4756250 1 4.58
CHEMBL4756731 1 4.55
CHEMBL4742375 1 4.52
CHEMBL4795431 1 4.50
CHEMBL4743992 1 4.44
CHEMBL4745143 1 4.37
CHEMBL210858 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3953102 Ki = 440.0 nM 6.36
CHEMBL4741927 Ki = 960.0 nM 6.02
CHEMBL4745151 Ki = 3300.0 nM 5.48
CHEMBL4751935 Ki = 5000.0 nM 5.30
CHEMBL4749241 Ki = 6500.0 nM 5.19
CHEMBL4754122 Ki = 6900.0 nM 5.16
CHEMBL4763772 Ki = 6900.0 nM 5.16
CHEMBL4755471 Ki = 17000.0 nM 4.77
CHEMBL4800056 Ki = 19000.0 nM 4.72
CHEMBL4782511 Ki = 23000.0 nM 4.64
CHEMBL4752116 Ki = 23000.0 nM 4.64
CHEMBL4756250 Ki = 26000.0 nM 4.58
CHEMBL4756731 Ki = 28000.0 nM 4.55
CHEMBL4742375 Ki = 30000.0 nM 4.52
CHEMBL4795431 Ki = 32000.0 nM 4.50
CHEMBL4743992 Ki = 36000.0 nM 4.44
CHEMBL4745143 Ki = 43000.0 nM 4.37
CHEMBL210858 Ki = 44000.0 nM 4.36