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Assay Detail

CHEMBL5536077

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Binding
Binding affinity N-terminal his tagged wild type human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry
4
Total Activities
4
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 SETDB1 (CHEMBL2321646)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SETDB1 as a cancer target: challenges and perspectives in drug design.
Hassanie H, Penteado AB, de Almeida LC, Calil RL, da Silva Emery F, Costa-Lotufo LV, Trossini GHG.
RSC Med Chem (2024) 15 : 1424 -1451
PubMed 38799223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.24 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5569118 1 7.10
CHEMBL4449143 1 6.68
CHEMBL4471748 1 5.80
CHEMBL4471746 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5569118 Kd = 80.0 nM 7.10
CHEMBL4449143 Kd = 210.0 nM 6.68
CHEMBL4471748 Kd = 1600.0 nM 5.80
CHEMBL4471746 Kd = 4400.0 nM 5.36