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Assay Detail

CHEMBL4345253

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Binding
Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia coli BL21 (DE3) using dGTP as substrate measured after 30 mins by malachite green dye based inorganic phosphatase coupled absorbance assay
2
Total Activities
2
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

Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Farand J, Kropf JE, Blomgren P, Xu J, Schmitt AC, Newby ZE, Wang T, Murakami E, Barauskas O, Sudhamsu J, Feng JY, Niedziela-Majka A, Schultz BE, Schwartz K, Viatchenko-Karpinski S, Kornyeyev D, Kashishian A, Fan P, Chen X, Lansdon EB, Ports MO, Currie KS, Watkins WJ, Notte GT.
ACS Med Chem Lett (2020) 11 : 358 -364
PubMed 32184970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.70 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3781316 1 9.10
CHEMBL3782004 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3781316 IC50 = 0.8 nM 9.10
CHEMBL3782004 IC50 = 5.0 nM 8.30