Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5144037

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

Binding
Inhibition of SMYD2 (unknown origin) using 3H-SAM as substrate incubated for 1 hr by filter binding method
37
Total Activities
37
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

N-lysine methyltransferase SMYD2 (CHEMBL2169716)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Positioning of an unprecedented 1,5-oxaza spiroquinone scaffold into SMYD2 inhibitors in epigenetic space.
Dhorma LP, Teli MK, Nangunuri BG, Venkanna A, Ragam R, Maturi A, Mirzaei A, Vo DK, Maeng HJ, Kim MH.
Eur J Med Chem (2022) 227 : 113880 -113880
PubMed 34656041 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.89 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3819011 1 8.52
CHEMBL3818083 1 7.57
CHEMBL2169920 1 6.92
CHEMBL5188628 1 6.40
CHEMBL3414623 1 6.37
CHEMBL5172262 1 6.17
CHEMBL5170181 1 6.17
CHEMBL5184091 1 5.67
CHEMBL5207034 1 5.64
CHEMBL5190397 1 5.62
CHEMBL5191647 1 5.51
CHEMBL5181874 1 5.51
CHEMBL5198917 1 5.42
CHEMBL5199015 1 5.26
CHEMBL5180712 1 5.24
CHEMBL5200671 1 5.21
CHEMBL5176478 1 5.12
CHEMBL5175819 1 4.94
CHEMBL4476753 1 4.73
CHEMBL5196609 1 -
CHEMBL5202235 1 -
CHEMBL5204697 1 -
CHEMBL5190577 1 -
CHEMBL5182950 1 -
CHEMBL5200846 1 -
CHEMBL5193070 1 -
CHEMBL5189265 1 -
CHEMBL5196302 1 -
CHEMBL5187033 1 -
CHEMBL5194340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3819011 IC50 = 3.0 nM 8.52
CHEMBL3818083 IC50 = 27.0 nM 7.57
CHEMBL2169920 IC50 = 120.0 nM 6.92
CHEMBL5188628 IC50 = 399.0 nM 6.40
CHEMBL3414623 IC50 = 425.0 nM 6.37
CHEMBL5172262 IC50 = 679.0 nM 6.17
CHEMBL5170181 IC50 = 678.0 nM 6.17
CHEMBL5184091 IC50 = 2130.0 nM 5.67
CHEMBL5207034 IC50 = 2310.0 nM 5.64
CHEMBL5190397 IC50 = 2390.0 nM 5.62
CHEMBL5191647 IC50 = 3060.0 nM 5.51
CHEMBL5181874 IC50 = 3060.0 nM 5.51
CHEMBL5198917 IC50 = 3820.0 nM 5.42
CHEMBL5199015 IC50 = 5550.0 nM 5.26
CHEMBL5180712 IC50 = 5800.0 nM 5.24
CHEMBL5200671 IC50 = 6200.0 nM 5.21
CHEMBL5176478 IC50 = 7520.0 nM 5.12
CHEMBL5175819 IC50 = 11600.0 nM 4.94
CHEMBL4476753 IC50 = 18500.0 nM 4.73
CHEMBL5187033 IC50 > 20000.0 nM -
CHEMBL5194131 IC50 > 20000.0 nM -
CHEMBL5206631 IC50 > 20000.0 nM -
CHEMBL5184109 IC50 > 20000.0 nM -
CHEMBL5206649 IC50 > 20000.0 nM -
CHEMBL5207271 IC50 > 20000.0 nM -
CHEMBL5189975 IC50 > 20000.0 nM -
CHEMBL5191667 IC50 > 20000.0 nM -
CHEMBL5194340 IC50 > 20000.0 nM -
CHEMBL5196609 IC50 > 30000.0 nM -
CHEMBL5196302 IC50 > 20000.0 nM -
CHEMBL5189265 IC50 > 20000.0 nM -
CHEMBL5193070 IC50 > 20000.0 nM -
CHEMBL5200846 IC50 > 20000.0 nM -
CHEMBL5182950 IC50 > 20000.0 nM -
CHEMBL5190577 IC50 > 20000.0 nM -
CHEMBL5204697 IC50 > 30000.0 nM -
CHEMBL5202235 IC50 > 30000.0 nM -