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Assay Detail

CHEMBL4822204

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

Binding
Binding affinity to human recombinant TET2 (1099 to 1936) catalytic domain assessed as dissociation constant by micro-scale thermophoresis analysis
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

Methylcytosine dioxygenase TET2 (CHEMBL4523344)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates.
Tiwari AD, Guan Y, Grabowski DR, Maciejewski JP, Jha BK, Phillips JG.
Bioorg Med Chem (2021) 39 : 116141 -116141
PubMed 33894507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.97 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4851104 1 6.52
CHEMBL4855677 1 6.21
CHEMBL4859276 1 5.69
CHEMBL4870693 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4851104 Kd = 300.0 nM 6.52
CHEMBL4855677 Kd = 610.0 nM 6.21
CHEMBL4859276 Kd = 2050.0 nM 5.69
CHEMBL4870693 Kd = 3420.0 nM 5.47