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Assay Detail

CHEMBL3614558

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

Binding
Inhibition of N-terminal thioredoxin His6-tagged full-length human menin expressed in Escherichia coli Rosetta (DE3) cells assessed as reduction in menin interaction with FITC-MBM1 peptide of MLL (4 to 15 residues) by fluorescence polarization assay
9
Total Activities
9
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

Menin (CHEMBL1615381)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein-Ligand Complexes.
Pollock J, Borkin D, Lund G, Purohit T, Dyguda-Kazimierowicz E, Grembecka J, Cierpicki T.
J Med Chem (2015) 58 : 7465 -7474
PubMed 26288158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.58 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586090 1 7.34
CHEMBL3613789 1 7.19
CHEMBL3613786 1 7.09
CHEMBL3613784 1 7.04
CHEMBL3613788 1 6.58
CHEMBL3613790 1 6.17
CHEMBL3612085 1 6.11
CHEMBL3613787 1 5.92
CHEMBL3613785 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586090 IC50 = 46.0 nM 7.34
CHEMBL3613789 IC50 = 65.0 nM 7.19
CHEMBL3613786 IC50 = 82.0 nM 7.09
CHEMBL3613784 IC50 = 92.0 nM 7.04
CHEMBL3613788 IC50 = 260.0 nM 6.58
CHEMBL3613790 IC50 = 674.0 nM 6.17
CHEMBL3612085 IC50 = 779.0 nM 6.11
CHEMBL3613787 IC50 = 1200.0 nM 5.92
CHEMBL3613785 IC50 = 1653.0 nM 5.78