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Assay Detail

CHEMBL4186853

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

Binding
Displacement of FITC-MBM1 from full length human menin measured after 2 hrs by fluorescence polarization assay
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Menin (CHEMBL1615381)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting protein-protein interaction between MLL1 and reciprocal proteins for leukemia therapy.
Wang ZH, Li DD, Chen WL, You QD, Guo XK.
Bioorg Med Chem (2018) 26 : 356 -365
PubMed 29254892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.12 6.08
Ki 1 7.10 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4216333 2 7.10
CHEMBL841 LOPERAMIDE 4.0 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4216333 Ki = 80.0 nM 7.10
CHEMBL4216333 IC50 = 830.0 nM 6.08
CHEMBL841 LOPERAMIDE IC50 = 69000.0 nM 4.16