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Assay Detail

CHEMBL5111975

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

Functional
Induction of cell differentiation in human U-937 cells measured for 2 days by flow cytometric analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Autocuration

Target

U-937 (CHEMBL612794)
Type CELL-LINE
Organism Homo sapiens

Publication

Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-<i>a</i>]pyridine Scaffold: SAR of the Aryloxyaryl Moiety.
Sainas S, Giorgis M, Circosta P, Poli G, Alberti M, Passoni A, Gaidano V, Pippione AC, Vitale N, Bonanni D, Rolando B, Cignetti A, Ramondetti C, Lanno A, Ferraris DM, Canepa B, Buccinnà B, Piccinini M, Rizzi M, Saglio G, Al-Karadaghi S, Boschi D, Miggiano R, Tuccinardi T, Lolli ML.
J Med Chem (2022) 65 : 12701 -12724
PubMed 36162075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.69 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173846 1 7.58
CHEMBL5192490 1 7.21
CHEMBL5196292 1 6.96
CHEMBL38434 BREQUINAR 2.0 1 6.67
CHEMBL5209405 1 6.63
CHEMBL4165815 1 6.12
CHEMBL5183718 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173846 EC50 = 26.0 nM 7.58
CHEMBL5192490 EC50 = 61.0 nM 7.21
CHEMBL5196292 EC50 = 109.0 nM 6.96
CHEMBL38434 BREQUINAR EC50 = 214.0 nM 6.67
CHEMBL5209405 EC50 = 235.0 nM 6.63
CHEMBL4165815 EC50 = 755.0 nM 6.12
CHEMBL5183718 EC50 = 2284.0 nM 5.64