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Assay Detail

CHEMBL5717040

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Binding
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
5
Total Activities
5
Compounds Tested
1
Activity Types
2
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

BTZO-1, a cardioprotective agent, reveals that macrophage migration inhibitory factor regulates ARE-mediated gene expression.
Kimura H, Sato Y, Tajima Y, Suzuki H, Yukitake H, Imaeda T, Kajino M, Oki H, Takizawa M, Tanida S.
Chem Biol (2010) 17 : 1282 -1294
PubMed 21168764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.79 7.15

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0003777
EFO_TERM EFO_TERM - heart disease

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4516611 BTZO-1 1 7.15
CHEMBL242080 E319 1 5.96
CHEMBL482477 1 5.44
CHEMBL1627201 L-SULFORAPHANE 2.0 1 4.60
CHEMBL210858 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4516611 BTZO-1 IC50 = 71.0 nM 7.15
CHEMBL242080 E319 IC50 = 1100.0 nM 5.96
CHEMBL482477 IC50 = 3600.0 nM 5.44
CHEMBL1627201 L-SULFORAPHANE IC50 = 25000.0 nM 4.60
CHEMBL210858 IC50 > 100000.0 nM -