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Assay Detail

CHEMBL4189819

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

Functional
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release preincubated for 15 mins followed by LPS challenge measured after 18 hrs by Griess assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type RAW264.7
Confidence 1 — Organism
Curated By Intermediate

Target

RAW264.7 (CHEMBL612557)
Type CELL-LINE
Organism Mus musculus

Publication

Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases.
Ghidini E, Marchini G, Capelli AM, Carnini C, Cenacchi V, Fioni A, Facchinetti F, Rancati F.
J Med Chem (2018) 61 : 4757 -4773
PubMed 29741897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 9.34 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4204230 1 10.10
CHEMBL1676 FLUTICASONE FUROATE 4.0 1 10.00
CHEMBL4204087 1 9.82
CHEMBL4208957 1 9.80
CHEMBL4202463 1 9.66
CHEMBL4205561 1 9.60
CHEMBL4211724 1 9.52
CHEMBL4206713 1 9.52
CHEMBL4208840 1 9.48
CHEMBL4204358 1 9.47
CHEMBL4216231 1 9.40
CHEMBL4217175 1 9.36
CHEMBL4211166 1 9.18
CHEMBL1370 BUDESONIDE 4.0 1 9.09
CHEMBL4214152 1 8.86
CHEMBL4203448 1 8.85
CHEMBL4203139 1 8.43
CHEMBL4213765 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4204230 IC50 = 0.08 nM 10.10
CHEMBL1676 FLUTICASONE FUROATE IC50 = 0.1 nM 10.00
CHEMBL4204087 IC50 = 0.15 nM 9.82
CHEMBL4208957 IC50 = 0.16 nM 9.80
CHEMBL4202463 IC50 = 0.22 nM 9.66
CHEMBL4205561 IC50 = 0.25 nM 9.60
CHEMBL4211724 IC50 = 0.3 nM 9.52
CHEMBL4206713 IC50 = 0.3 nM 9.52
CHEMBL4208840 IC50 = 0.33 nM 9.48
CHEMBL4204358 IC50 = 0.34 nM 9.47
CHEMBL4216231 IC50 = 0.4 nM 9.40
CHEMBL4217175 IC50 = 0.44 nM 9.36
CHEMBL4211166 IC50 = 0.66 nM 9.18
CHEMBL1370 BUDESONIDE IC50 = 0.82 nM 9.09
CHEMBL4214152 IC50 = 1.38 nM 8.86
CHEMBL4203448 IC50 = 1.4 nM 8.85
CHEMBL4203139 IC50 = 3.68 nM 8.43
CHEMBL4213765 IC50 = 11.9 nM 7.92