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Assay Detail

CHEMBL4006963

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

Functional
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Jurkat (CHEMBL397)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis, biological evaluation and X-ray structural studies of potent human dihydroorotate dehydrogenase inhibitors based on hydroxylated azole scaffolds.
Sainas S, Pippione AC, Giorgis M, Lupino E, Goyal P, Ramondetti C, Buccinnà B, Piccinini M, Braga RC, Andrade CH, Andersson M, Moritzer AC, Friemann R, Mensa S, Al-Kadaraghi S, Boschi D, Lolli ML.
Eur J Med Chem (2017) 129 : 287 -302
PubMed 28235702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.15 6.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38434 BREQUINAR 2.0 1 6.03
CHEMBL4105330 1 5.98
CHEMBL4062046 1 5.73
CHEMBL4088968 1 5.65
CHEMBL4081077 1 5.60
CHEMBL4090575 1 5.49
CHEMBL4098306 1 5.24
CHEMBL4071260 1 5.15
CHEMBL4061824 1 4.88
CHEMBL4089886 1 4.45
CHEMBL973 TERIFLUNOMIDE 4.0 1 4.36
CHEMBL1946659 1 4.22
CHEMBL1946851 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38434 BREQUINAR IC50 = 930.0 nM 6.03
CHEMBL4105330 IC50 = 1040.0 nM 5.98
CHEMBL4062046 IC50 = 1880.0 nM 5.73
CHEMBL4088968 IC50 = 2220.0 nM 5.65
CHEMBL4081077 IC50 = 2500.0 nM 5.60
CHEMBL4090575 IC50 = 3220.0 nM 5.49
CHEMBL4098306 IC50 = 5820.0 nM 5.24
CHEMBL4071260 IC50 = 7130.0 nM 5.15
CHEMBL4061824 IC50 = 13280.0 nM 4.88
CHEMBL4089886 IC50 = 35690.0 nM 4.45
CHEMBL973 TERIFLUNOMIDE IC50 = 43220.0 nM 4.36
CHEMBL1946659 IC50 = 59700.0 nM 4.22
CHEMBL1946851 IC50 = 68300.0 nM 4.17