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Assay Detail

CHEMBL5107240

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

Binding
Inhibition of Menin/fluorescein labeled MLL(4 to 43 residues) (unknown origin) protein protein interaction incubated for 1 hr by fluorescence polarization-based competitive binding assay
38
Total Activities
38
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

Discovery of Novel, Potent, and Selective Small-Molecule Menin-Mixed Lineage Leukemia Interaction Inhibitors through Attempting Introduction of Hydrophilic Groups.
Lei H, Zhang SQ, Bai H, Zhao HY, Sun J, Chuai H, Xin M.
J Med Chem (2022) 65 : 13413 -13435
PubMed 36173787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.76 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5192780 1 8.15
CHEMBL5182826 1 8.00
CHEMBL5184080 1 7.52
CHEMBL5194018 1 7.22
CHEMBL5201656 1 7.22
CHEMBL5204727 1 7.22
CHEMBL5195611 1 7.16
CHEMBL5201049 1 7.05
CHEMBL5172930 1 6.92
CHEMBL5187553 1 6.89
CHEMBL5188417 1 6.75
CHEMBL5183465 1 6.72
CHEMBL5201608 1 6.58
CHEMBL5206167 1 6.54
CHEMBL5189910 1 6.28
CHEMBL5207604 1 6.23
CHEMBL3586089 1 6.22
CHEMBL5176172 1 6.17
CHEMBL5190068 1 6.16
CHEMBL5200814 1 6.09
CHEMBL5173912 1 6.01
CHEMBL5172411 1 5.71
CHEMBL5176450 1 -
CHEMBL5180808 1 -
CHEMBL5194989 1 -
CHEMBL5188240 1 -
CHEMBL5202295 1 -
CHEMBL5194316 1 -
CHEMBL5191951 1 -
CHEMBL5202282 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5192780 IC50 = 7.0 nM 8.15
CHEMBL5182826 IC50 = 10.0 nM 8.00
CHEMBL5184080 IC50 = 30.0 nM 7.52
CHEMBL5194018 IC50 = 60.0 nM 7.22
CHEMBL5201656 IC50 = 60.0 nM 7.22
CHEMBL5204727 IC50 = 60.0 nM 7.22
CHEMBL5195611 IC50 = 70.0 nM 7.16
CHEMBL5201049 IC50 = 90.0 nM 7.05
CHEMBL5172930 IC50 = 120.0 nM 6.92
CHEMBL5187553 IC50 = 130.0 nM 6.89
CHEMBL5188417 IC50 = 180.0 nM 6.75
CHEMBL5183465 IC50 = 190.0 nM 6.72
CHEMBL5201608 IC50 = 260.0 nM 6.58
CHEMBL5206167 IC50 = 290.0 nM 6.54
CHEMBL5189910 IC50 = 530.0 nM 6.28
CHEMBL5207604 IC50 = 590.0 nM 6.23
CHEMBL3586089 IC50 = 600.0 nM 6.22
CHEMBL5176172 IC50 = 680.0 nM 6.17
CHEMBL5190068 IC50 = 690.0 nM 6.16
CHEMBL5200814 IC50 = 820.0 nM 6.09
CHEMBL5173912 IC50 = 970.0 nM 6.01
CHEMBL5172411 IC50 = 1970.0 nM 5.71
CHEMBL5207278 IC50 > 10000.0 nM -
CHEMBL5198558 IC50 > 10000.0 nM -
CHEMBL5208035 IC50 > 10000.0 nM -
CHEMBL5205955 IC50 > 10000.0 nM -
CHEMBL5201801 IC50 > 10000.0 nM -
CHEMBL5200144 IC50 > 10000.0 nM -
CHEMBL5175946 IC50 > 10000.0 nM -
CHEMBL5177194 IC50 > 10000.0 nM -
CHEMBL5202282 IC50 > 10000.0 nM -
CHEMBL5191951 IC50 > 10000.0 nM -
CHEMBL5194316 IC50 > 10000.0 nM -
CHEMBL5202295 IC50 > 10000.0 nM -
CHEMBL5188240 IC50 > 10000.0 nM -
CHEMBL5194989 IC50 > 10000.0 nM -
CHEMBL5180808 IC50 > 10000.0 nM -
CHEMBL5176450 IC50 > 10000.0 nM -