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

CHEMBL4387485

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

Binding
Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by SPR analysis
8
Total Activities
8
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

Identification and characterization of the first fragment hits for SETDB1 Tudor domain.
Mader P, Mendoza-Sanchez R, Iqbal A, Dong A, Dobrovetsky E, Corless VB, Liew SK, Houliston SR, De Freitas RF, Smil D, Sena CCD, Kennedy S, Diaz DB, Wu H, Dombrovski L, Allali-Hassani A, Min J, Schapira M, Vedadi M, Brown PJ, Santhakumar V, Yudin AK, Arrowsmith CH.
Bioorg Med Chem (2019) 27 : 3866 -3878
PubMed 31327677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 2.36 2.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4455427 1 2.60
CHEMBL4542222 1 2.57
CHEMBL4576037 1 2.46
CHEMBL4453131 1 2.40
CHEMBL4589361 1 2.11
CHEMBL4451286 1 2.00
CHEMBL4461772 1 -
CHEMBL4456448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4455427 Kd = 2500000.0 nM 2.60
CHEMBL4542222 Kd = 2700000.0 nM 2.57
CHEMBL4576037 Kd = 3500000.0 nM 2.46
CHEMBL4453131 Kd = 4000000.0 nM 2.40
CHEMBL4589361 Kd = 7700000.0 nM 2.11
CHEMBL4451286 Kd = 10000000.0 nM 2.00
CHEMBL4461772 Kd - -
CHEMBL4456448 Kd = 1270000.0 nM -