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Assay Detail

CHEMBL5111562

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

Binding
Inhibition of human DNA polymerase theta using 5'-CACTGACTGTATGATG as primer and DNA 16/19 as substrate by FRET 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

DNA polymerase theta (CHEMBL6025)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of <b>RP-6685</b>, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.
Bubenik M, Mader P, Mochirian P, Vallée F, Clark J, Truchon JF, Perryman AL, Pau V, Kurinov I, Zahn KE, Leclaire ME, Papp R, Mathieu MC, Hamel M, Duffy NM, Godbout C, Casas-Selves M, Falgueyret JP, Baruah PS, Nicolas O, Stocco R, Poirier H, Martino G, Fortin AB, Roulston A, Chefson A, Dorich S, St-Onge M, Patel P, Pellerin C, Ciblat S, Pinter T, Barabé F, El Bakkouri M, Parikh P, Gervais C, Sfeir A, Mamane Y, Morris SJ, Black WC, Sicheri F, Gallant M.
J Med Chem (2022) 65 : 13198 -13215
PubMed 36126059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5195920 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5195920 IC50 = 10.0 nM 8.00