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Assay Detail

CHEMBL3587283

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

Binding
Inhibition of menin-MLL1 interaction (unknown origin) incubated for 1 hr by fluorescein and Texas Red labeled MBM1 based fluorescence polarization assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Menin/Histone-lysine N-methyltransferase MLL (CHEMBL2093861)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility.
Senter T, Gogliotti RD, Han C, Locuson CW, Morrison R, Daniels JS, Cierpicki T, Grembecka J, Lindsley CW, Stauffer SR.
Bioorg Med Chem Lett (2015) 25 : 2720 -2725
PubMed 25987377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.40 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586086 1 7.05
CHEMBL3126199 1 6.94
CHEMBL3126188 1 6.71
CHEMBL3126190 1 6.65
CHEMBL3126192 1 6.62
CHEMBL3586088 1 6.61
CHEMBL3126191 1 6.52
CHEMBL3586087 1 6.45
CHEMBL3126185 1 6.41
CHEMBL3126189 1 6.36
CHEMBL3586085 1 6.34
CHEMBL3586084 1 5.96
CHEMBL3585356 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586086 IC50 = 90.0 nM 7.05
CHEMBL3126199 IC50 = 114.0 nM 6.94
CHEMBL3126188 IC50 = 197.0 nM 6.71
CHEMBL3126190 IC50 = 226.0 nM 6.65
CHEMBL3126192 IC50 = 242.0 nM 6.62
CHEMBL3586088 IC50 = 246.0 nM 6.61
CHEMBL3126191 IC50 = 302.0 nM 6.52
CHEMBL3586087 IC50 = 354.0 nM 6.45
CHEMBL3126185 IC50 = 390.0 nM 6.41
CHEMBL3126189 IC50 = 437.0 nM 6.36
CHEMBL3586085 IC50 = 460.0 nM 6.34
CHEMBL3586084 IC50 = 1100.0 nM 5.96
CHEMBL3585356 IC50 = 28000.0 nM 4.55