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Assay Detail

CHEMBL4329002

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

Binding
Inhibition of recombinant human Tdp1 using 5'-biotin-GATCTAAAAGACTT-pY-3' as substrate measured after 20 mins by AlphaScreen assay
1
Total Activities
1
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

Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
Zakharenko AL, Luzina OA, Sokolov DN, Kaledin VI, Nikolin VP, Popova NA, Patel J, Zakharova OD, Chepanova AA, Zafar A, Reynisson J, Leung E, Leung IKH, Volcho KP, Salakhutdinov NF, Lavrik OI.
Eur J Med Chem (2019) 161 : 581 -593
PubMed 30396105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.44 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1256623 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1256623 IC50 = 360.0 nM 6.44