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Assay Detail

CHEMBL5116774

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

Binding
Inhibition of GLP (unknown origin)
18
Total Activities
18
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

Identification and in vitro characterization of a new series of potent and highly selective G9a inhibitors as novel anti-fibroadipogenic agents.
Randazzo P, Sinisi R, Gornati D, Bertuolo S, Bencheva L, De Matteo M, Nibbio M, Monteagudo E, Turcano L, Bianconi V, Peruzzi G, Summa V, Bresciani A, Mozzetta C, Di Fabio R.
Bioorg Med Chem Lett (2022) 72 : 128858 -128858
PubMed 35718104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.74 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187766 1 7.26
CHEMBL3109630 1 6.93
CHEMBL5195846 1 6.48
CHEMBL5193402 1 6.48
CHEMBL5172085 1 6.39
CHEMBL5199280 1 5.96
CHEMBL5189772 1 5.71
CHEMBL5183771 1 5.66
CHEMBL5194471 1 5.57
CHEMBL5188089 1 5.46
CHEMBL5184153 1 5.36
CHEMBL5177309 1 5.28
CHEMBL5207069 1 4.96
CHEMBL5191130 1 4.81
CHEMBL5202307 1 4.81
CHEMBL5209060 1 4.76
CHEMBL5185925 1 -
CHEMBL5191627 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187766 IC50 = 55.3 nM 7.26
CHEMBL3109630 IC50 = 118.1 nM 6.93
CHEMBL5195846 IC50 = 328.3 nM 6.48
CHEMBL5193402 IC50 = 332.3 nM 6.48
CHEMBL5172085 IC50 = 403.5 nM 6.39
CHEMBL5199280 IC50 = 1107.2 nM 5.96
CHEMBL5189772 IC50 = 1952.6 nM 5.71
CHEMBL5183771 IC50 = 2177.5 nM 5.66
CHEMBL5194471 IC50 = 2715.8 nM 5.57
CHEMBL5188089 IC50 = 3456.0 nM 5.46
CHEMBL5184153 IC50 = 4366.6 nM 5.36
CHEMBL5177309 IC50 = 5230.6 nM 5.28
CHEMBL5207069 IC50 = 11014.0 nM 4.96
CHEMBL5191130 IC50 = 15643.0 nM 4.81
CHEMBL5202307 IC50 = 15456.0 nM 4.81
CHEMBL5209060 IC50 = 17467.0 nM 4.76
CHEMBL5185925 IC50 > 5000.0 nM -
CHEMBL5191627 IC50 > 5000.0 nM -