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Assay Detail

CHEMBL4135375

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Binding
Inhibition of dog kidney microsomal COX assessed as PGE2 level using arachidonic acid as substrate preincubated for 5 to 15 mins followed by substrate addition measured after 40 mins by radio immunoassay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Tissue Kidney
Subcellular Microsomal
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.
Kassab SE, Khedr MA, Ali HI, Abdalla MM.
Eur J Med Chem (2017) 141 : 306 -321
PubMed 29031075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.25 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4169347 1 7.47
CHEMBL4173526 1 7.41
CHEMBL4177185 1 7.40
CHEMBL4162061 1 7.35
CHEMBL4172740 1 7.28
CHEMBL4165597 1 7.25
CHEMBL4176892 1 7.21
CHEMBL4169030 1 7.11
CHEMBL4161755 1 7.10
CHEMBL118 CELECOXIB 4.0 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4169347 IC50 = 34.0 nM 7.47
CHEMBL4173526 IC50 = 39.0 nM 7.41
CHEMBL4177185 IC50 = 40.0 nM 7.40
CHEMBL4162061 IC50 = 45.0 nM 7.35
CHEMBL4172740 IC50 = 53.0 nM 7.28
CHEMBL4165597 IC50 = 56.0 nM 7.25
CHEMBL4176892 IC50 = 61.0 nM 7.21
CHEMBL4169030 IC50 = 77.0 nM 7.11
CHEMBL4161755 IC50 = 80.0 nM 7.10
CHEMBL118 CELECOXIB IC50 = 112.0 nM 6.95