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Assay Detail

CHEMBL5053607

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

Functional
Induction of cell differentiation in human U-937 cells assessed as CD11b expression after 3 days by flow cytometric analysis
8
Total Activities
8
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 Biphenyl Moiety.
Sainas S, Giorgis M, Circosta P, Gaidano V, Bonanni D, Pippione AC, Bagnati R, Passoni A, Qiu Y, Cojocaru CF, Canepa B, Bona A, Rolando B, Mishina M, Ramondetti C, Buccinnà B, Piccinini M, Houshmand M, Cignetti A, Giraudo E, Al-Karadaghi S, Boschi D, Saglio G, Lolli ML.
J Med Chem (2021) 64 : 5404 -5428
PubMed 33844533 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.58 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5090281 1 8.34
CHEMBL5090431 1 8.07
CHEMBL4173846 1 7.58
CHEMBL5084878 1 7.51
CHEMBL5078949 1 7.47
CHEMBL5092556 1 7.39
CHEMBL38434 BREQUINAR 2.0 1 6.72
CHEMBL5077508 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5090281 EC50 = 4.6 nM 8.34
CHEMBL5090431 EC50 = 8.6 nM 8.07
CHEMBL4173846 EC50 = 26.0 nM 7.58
CHEMBL5084878 EC50 = 31.1 nM 7.51
CHEMBL5078949 EC50 = 34.2 nM 7.47
CHEMBL5092556 EC50 = 40.7 nM 7.39
CHEMBL38434 BREQUINAR EC50 = 188.6 nM 6.72
CHEMBL5077508 EC50 - -