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Assay Detail

CHEMBL4044676

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Binding
Inhibition of EHMT1 (unknown origin)
3
Total Activities
3
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 EHMT1 (CHEMBL6031)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
Liu Q, Cai X, Yang D, Chen Y, Wang Y, Shao L, Wang MW.
Bioorg Med Chem (2017) 25 : 4579 -4594
PubMed 28739157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.96 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231795 1 7.72
CHEMBL1214186 SINEFUNGIN 2.0 1 7.00
CHEMBL569864 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231795 IC50 = 19.0 nM 7.72
CHEMBL1214186 SINEFUNGIN IC50 = 100.0 nM 7.00
CHEMBL569864 IC50 = 700.0 nM 6.16