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Assay Detail

CHEMBL3224088

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

Binding
Antagonist activity at N-terminal His6-tagged L3MBTL1 (unknown origin) expressed in Escherichia coli BL21 Codon Plus RIL cells assessed as inhibition of L3MBTL1/biotinylated H4K20Me1 peptide interaction after 30 mins by AlphaScreen assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lethal(3)malignant brain tumor-like protein 1 (CHEMBL1287622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structureactivity relationships of methyl-lysine reader antagonists
Herold JM, James LI, Korboukh VK, Gao C, Coil KE, Bua DJ, Norris JL, Kireev DB, Brown PJ, Jin J, Janzen WP, Gozani O, Frye SV
Medchemcomm (2012) 3 : 45 -51
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.85 5.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426369 1 5.41
CHEMBL1235119 1 5.10
CHEMBL3220197 1 5.07
CHEMBL3220190 1 4.88
CHEMBL3219947 1 4.83
CHEMBL3219949 1 4.75
CHEMBL3220204 1 4.69
CHEMBL3219948 1 4.64
CHEMBL2426371 1 4.63
CHEMBL3220201 1 4.54
CHEMBL3220189 1 -
CHEMBL3220191 1 -
CHEMBL3220192 1 -
CHEMBL3220193 1 -
CHEMBL3220194 1 -
CHEMBL3220195 1 -
CHEMBL3220196 1 -
CHEMBL2426372 1 -
CHEMBL3220198 1 -
CHEMBL3220199 1 -
CHEMBL3220200 1 -
CHEMBL3220202 1 -
CHEMBL3217781 1 -
CHEMBL3220203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426369 IC50 = 3900.0 nM 5.41
CHEMBL1235119 IC50 = 7900.0 nM 5.10
CHEMBL3220197 IC50 = 8600.0 nM 5.07
CHEMBL3220190 IC50 = 13300.0 nM 4.88
CHEMBL3219947 IC50 = 14700.0 nM 4.83
CHEMBL3219949 IC50 = 17800.0 nM 4.75
CHEMBL3220204 IC50 = 20300.0 nM 4.69
CHEMBL3219948 IC50 = 22700.0 nM 4.64
CHEMBL2426371 IC50 = 23600.0 nM 4.63
CHEMBL3220201 IC50 = 28900.0 nM 4.54
CHEMBL3220189 IC50 > 30000.0 nM -
CHEMBL3220191 IC50 > 30000.0 nM -
CHEMBL3220192 IC50 > 30000.0 nM -
CHEMBL3220193 IC50 > 30000.0 nM -
CHEMBL3220194 IC50 > 30000.0 nM -
CHEMBL3220195 IC50 > 30000.0 nM -
CHEMBL3220196 IC50 > 30000.0 nM -
CHEMBL2426372 IC50 > 30000.0 nM -
CHEMBL3220198 IC50 > 30000.0 nM -
CHEMBL3220199 IC50 > 30000.0 nM -
CHEMBL3220200 IC50 > 30000.0 nM -
CHEMBL3220202 IC50 > 30000.0 nM -
CHEMBL3217781 IC50 > 30000.0 nM -
CHEMBL3220203 IC50 > 30000.0 nM -