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Assay Detail

CHEMBL4254484

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

Functional
Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages preincubated for 6 hrs followed by PMA stimulation by phase contrast microscopic method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
Moussa G, Alaaeddine R, Alaeddine LM, Nassra R, Belal ASF, Ismail A, El-Yazbi AF, Abdel-Ghany YS, Hazzaa A.
Eur J Med Chem (2018) 144 : 635 -650
PubMed 29289887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.45 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4279764 1 6.89
CHEMBL4285920 1 5.91
CHEMBL4289748 1 5.32
CHEMBL139 DICLOFENAC 4.0 1 5.31
CHEMBL4290032 1 5.25
CHEMBL4279346 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4279764 IC50 = 130.0 nM 6.89
CHEMBL4285920 IC50 = 1230.0 nM 5.91
CHEMBL4289748 IC50 = 4770.0 nM 5.32
CHEMBL139 DICLOFENAC IC50 = 4860.0 nM 5.31
CHEMBL4290032 IC50 = 5630.0 nM 5.25
CHEMBL4279346 IC50 = 99390.0 nM 4.00