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Assay Detail

CHEMBL1217455

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

Binding
Activity at methyl transferase activity G9a by enzyme coupled S-adenocylehomocystein detection assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histone-lysine N-methyltransferase EHMT2 (CHEMBL6032)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
Liu F, Chen X, Allali-Hassani A, Quinn AM, Wigle TJ, Wasney GA, Dong A, Senisterra G, Chau I, Siarheyeva A, Norris JL, Kireev DB, Jadhav A, Herold JM, Janzen WP, Arrowsmith CH, Frye SV, Brown PJ, Simeonov A, Vedadi M, Jin J.
J Med Chem (2010) 53 : 5844 -5857
PubMed 20614940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.49 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1213903 1 5.10
CHEMBL1214066 1 5.05
CHEMBL1213957 1 4.60
CHEMBL576781 1 4.37
CHEMBL1213902 1 4.29
CHEMBL1213901 1 4.28
CHEMBL1214067 1 4.24
CHEMBL1213828 1 4.02
CHEMBL578227 1 -
CHEMBL1214630 1 -
CHEMBL572373 1 -
CHEMBL570120 1 -
CHEMBL571717 1 -
CHEMBL585180 1 -
CHEMBL576260 1 -
CHEMBL1213766 1 -
CHEMBL1213827 1 -
CHEMBL569864 1 -
CHEMBL1213830 1 -
CHEMBL1213958 1 -
CHEMBL1213959 1 -
CHEMBL1214015 1 -
CHEMBL1214068 1 -
CHEMBL1214145 1 -
CHEMBL1213829 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1213903 IC50 = 8000.0 nM 5.10
CHEMBL1214066 IC50 = 9000.0 nM 5.05
CHEMBL1213957 IC50 = 25000.0 nM 4.60
CHEMBL576781 IC50 = 43000.0 nM 4.37
CHEMBL1213902 IC50 = 51000.0 nM 4.29
CHEMBL1213901 IC50 = 52000.0 nM 4.28
CHEMBL1214067 IC50 = 57000.0 nM 4.24
CHEMBL1213828 IC50 = 95000.0 nM 4.02
CHEMBL578227 IC50 = 330000.0 nM -
CHEMBL1214630 IC50 = 910000.0 nM -
CHEMBL572373 IC50 = 150000.0 nM -
CHEMBL570120 IC50 = 550000.0 nM -
CHEMBL571717 IC50 = 1600000.0 nM -
CHEMBL585180 IC50 = 910000.0 nM -
CHEMBL576260 IC50 = 1100000.0 nM -
CHEMBL1213766 IC50 = 110000.0 nM -
CHEMBL1213827 IC50 = 140000.0 nM -
CHEMBL569864 IC50 = 180000.0 nM -
CHEMBL1213830 IC50 = 120000.0 nM -
CHEMBL1213958 IC50 = 880000.0 nM -
CHEMBL1213959 IC50 = 3400000.0 nM -
CHEMBL1214015 IC50 = 235000.0 nM -
CHEMBL1214068 IC50 = 345000.0 nM -
CHEMBL1214145 IC50 = 1500000.0 nM -
CHEMBL1213829 IC50 = 15100000.0 nM -