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Assay Detail

CHEMBL4431146

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

Binding
Inhibition of recombinant TDP1 (unknown origin) using 5'-32P-labeled N14Y DNA substrate incubated for 15 mins by PAGE 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

Tyrosyl-DNA phosphodiesterase 1 (CHEMBL1075138)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tyrosyl-DNA phosphodiesterase inhibitors: Progress and potential.
Laev SS, Salakhutdinov NF, Lavrik OI.
Bioorg Med Chem (2016) 24 : 5017 -5027
PubMed 27687971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.50 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464463 1 8.30
CHEMBL4571632 1 7.66
CHEMBL4465069 1 5.11
CHEMBL4457160 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464463 IC50 = 5.0 nM 8.30
CHEMBL4571632 IC50 = 22.0 nM 7.66
CHEMBL4465069 IC50 = 7700.0 nM 5.11
CHEMBL4457160 IC50 = 12100.0 nM 4.92