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Assay Detail

CHEMBL4137385

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Functional
Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Jurkat (CHEMBL397)
Type CELL-LINE
Organism Homo sapiens

Publication

Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.
Sainas S, Pippione AC, Lupino E, Giorgis M, Circosta P, Gaidano V, Goyal P, Bonanni D, Rolando B, Cignetti A, Ducime A, Andersson M, Järvå M, Friemann R, Piccinini M, Ramondetti C, Buccinnà B, Al-Karadaghi S, Boschi D, Saglio G, Lolli ML.
J Med Chem (2018) 61 : 6034 -6055
PubMed 29939742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.36 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173846 1 6.12
CHEMBL4165923 1 6.09
CHEMBL38434 BREQUINAR 2.0 1 6.04
CHEMBL4165815 1 5.83
CHEMBL4177202 1 5.81
CHEMBL4062046 1 5.73
CHEMBL973 TERIFLUNOMIDE 4.0 1 4.36
CHEMBL4167855 1 4.17
CHEMBL4175712 1 4.05
CHEMBL4169359 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173846 IC50 = 750.0 nM 6.12
CHEMBL4165923 IC50 = 820.0 nM 6.09
CHEMBL38434 BREQUINAR IC50 = 910.0 nM 6.04
CHEMBL4165815 IC50 = 1470.0 nM 5.83
CHEMBL4177202 IC50 = 1560.0 nM 5.81
CHEMBL4062046 IC50 = 1880.0 nM 5.73
CHEMBL973 TERIFLUNOMIDE IC50 = 43220.0 nM 4.36
CHEMBL4167855 IC50 = 67550.0 nM 4.17
CHEMBL4175712 IC50 = 89660.0 nM 4.05
CHEMBL4169359 IC50 - -