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

CHEMBL3782136

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

Binding
Inhibition of recombinant MTH1 (unknown origin) assessed as hydrolysis of 8-oxodGTP to 8-oxodGMP and pyrophosphate by PPiLight assay
19
Total Activities
19
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

Oxidized purine nucleoside triphosphate hydrolase (CHEMBL3708265)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of potent and selective MTH1 inhibitors.
Petrocchi A, Leo E, Reyna NJ, Hamilton MM, Shi X, Parker CA, Mseeh F, Bardenhagen JP, Leonard P, Cross JB, Huang S, Jiang Y, Cardozo M, Draetta G, Marszalek JR, Toniatti C, Jones P, Lewis RT.
Bioorg Med Chem Lett (2016) 26 : 1503 -1507
PubMed 26898335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.00 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3780962 1 9.70
CHEMBL3781661 1 9.70
CHEMBL3780613 1 9.30
CHEMBL3780596 1 9.30
CHEMBL3780032 1 9.22
CHEMBL3781316 1 8.80
CHEMBL3780321 1 8.74
CHEMBL3781917 1 8.51
CHEMBL3781015 1 8.35
CHEMBL3782004 1 8.00
CHEMBL3780307 1 8.00
CHEMBL3781296 1 7.66
CHEMBL3781387 1 7.28
CHEMBL3781861 1 7.08
CHEMBL3781493 1 6.95
CHEMBL3781662 1 6.92
CHEMBL3780652 1 6.52
CHEMBL3781282 1 6.48
CHEMBL3781267 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3780962 IC50 = 0.2 nM 9.70
CHEMBL3781661 IC50 = 0.2 nM 9.70
CHEMBL3780613 IC50 = 0.5 nM 9.30
CHEMBL3780596 IC50 = 0.5 nM 9.30
CHEMBL3780032 IC50 = 0.6 nM 9.22
CHEMBL3781316 IC50 = 1.6 nM 8.80
CHEMBL3780321 IC50 = 1.8 nM 8.74
CHEMBL3781917 IC50 = 3.1 nM 8.51
CHEMBL3781015 IC50 = 4.5 nM 8.35
CHEMBL3782004 IC50 = 10.0 nM 8.00
CHEMBL3780307 IC50 = 10.0 nM 8.00
CHEMBL3781296 IC50 = 22.0 nM 7.66
CHEMBL3781387 IC50 = 53.0 nM 7.28
CHEMBL3781861 IC50 = 84.0 nM 7.08
CHEMBL3781493 IC50 = 112.0 nM 6.95
CHEMBL3781662 IC50 = 120.0 nM 6.92
CHEMBL3780652 IC50 = 302.0 nM 6.52
CHEMBL3781282 IC50 = 332.0 nM 6.48
CHEMBL3781267 IC50 = 2980.0 nM 5.53