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Assay Detail

CHEMBL5581928

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

Binding
Inhibition of G9a (unknown origin) by AlphaLISA assay
27
Total Activities
27
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

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

Publication

Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.
Yang C, Li B, Feng Z, Li H, Yang H, Yang Z, Liu L, Shi Q, Wang H, Chen ZZ, Huang X, Wang J, Wang Y.
J Med Chem (2024) 67 : 16072 -16087
PubMed 39008565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.81 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207914 1 8.07
CHEMBL5591832 1 7.50
CHEMBL5592107 1 7.44
CHEMBL5590338 1 7.35
CHEMBL5592239 1 7.32
CHEMBL5591500 1 7.27
CHEMBL5592600 1 7.19
CHEMBL5590208 1 7.18
CHEMBL5583700 1 7.07
CHEMBL5170450 1 7.00
CHEMBL1232453 1 6.80
CHEMBL5595949 1 6.78
CHEMBL5594410 1 6.70
CHEMBL5593211 1 6.70
CHEMBL5591131 1 6.62
CHEMBL5591835 1 6.51
CHEMBL5595912 1 6.48
CHEMBL5593275 1 6.46
CHEMBL5592280 1 6.05
CHEMBL5592452 1 5.95
CHEMBL5592412 1 5.89
CHEMBL5592774 1 5.54
CHEMBL5593832 1 -
CHEMBL5589842 1 -
CHEMBL2441082 1 -
CHEMBL5589782 1 -
CHEMBL5396252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207914 IC50 = 8.5 nM 8.07
CHEMBL5591832 IC50 = 31.5 nM 7.50
CHEMBL5592107 IC50 = 36.5 nM 7.44
CHEMBL5590338 IC50 = 45.0 nM 7.35
CHEMBL5592239 IC50 = 48.0 nM 7.32
CHEMBL5591500 IC50 = 53.5 nM 7.27
CHEMBL5592600 IC50 = 65.0 nM 7.19
CHEMBL5590208 IC50 = 66.0 nM 7.18
CHEMBL5583700 IC50 = 85.0 nM 7.07
CHEMBL5170450 IC50 = 100.0 nM 7.00
CHEMBL1232453 IC50 = 160.0 nM 6.80
CHEMBL5595949 IC50 = 166.0 nM 6.78
CHEMBL5594410 IC50 = 202.0 nM 6.70
CHEMBL5593211 IC50 = 200.0 nM 6.70
CHEMBL5591131 IC50 = 241.0 nM 6.62
CHEMBL5591835 IC50 = 310.0 nM 6.51
CHEMBL5595912 IC50 = 334.0 nM 6.48
CHEMBL5593275 IC50 = 344.0 nM 6.46
CHEMBL5592280 IC50 = 887.0 nM 6.05
CHEMBL5592452 IC50 = 1131.0 nM 5.95
CHEMBL5592412 IC50 = 1290.0 nM 5.89
CHEMBL5592774 IC50 = 2849.0 nM 5.54
CHEMBL5593832 IC50 > 10000.0 nM -
CHEMBL5589842 IC50 > 10000.0 nM -
CHEMBL2441082 IC50 < 2.5 nM -
CHEMBL5589782 IC50 > 10000.0 nM -
CHEMBL5396252 IC50 < 100.0 nM -