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Assay Detail

CHEMBL4345256

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

Functional
Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U2OS
Confidence 1 — Organism
Curated By Autocuration

Target

U2OS (CHEMBL615023)
Type CELL-LINE
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
EC50 8 5.11 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3781316 1 6.16
CHEMBL3782004 1 5.25
CHEMBL1825141 1 5.17
CHEMBL4436749 1 5.09
CHEMBL4565569 1 4.84
CHEMBL4570428 1 4.69
CHEMBL4435983 1 4.60
CHEMBL3793901 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3781316 EC50 = 700.0 nM 6.16
CHEMBL3782004 EC50 = 5600.0 nM 5.25
CHEMBL1825141 EC50 = 6800.0 nM 5.17
CHEMBL4436749 EC50 = 8048.0 nM 5.09
CHEMBL4565569 EC50 = 14416.0 nM 4.84
CHEMBL4570428 EC50 = 20323.0 nM 4.69
CHEMBL4435983 EC50 = 24916.0 nM 4.60
CHEMBL3793901 EC50 > 20000.0 nM -