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Assay Detail

CHEMBL4052361

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

ADMET
Inhibition of human COX-1 preincubated for 15 mins followed by fluorometric substrate/heme addition for 15 mins subsequently incubated with arachidonic acid for 2 mins by fluorescence analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pentafluorosulfanyl-Substituted Benzopyran Analogues As New Cyclooxygenase-2 Inhibitors with Excellent Pharmacokinetics and Efficacy in Blocking Inflammation.
Zhang Y, Wang Y, He C, Liu X, Lu Y, Chen T, Pan Q, Xiong J, She M, Tu Z, Qin X, Li M, Tortorella MD, Talley JJ.
J Med Chem (2017) 60 : 4135 -4146
PubMed 28475316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.28 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26915 SC-560 1 7.28
CHEMBL4075294 1 -
CHEMBL42485 DUP-697 1 -
CHEMBL118 CELECOXIB 4.0 1 -
CHEMBL4098347 1 -
CHEMBL4080317 1 -
CHEMBL4090622 1 -
CHEMBL4069602 1 -
CHEMBL4088012 1 -
CHEMBL4095906 1 -
CHEMBL4084676 1 -
CHEMBL4072067 1 -
CHEMBL4081499 1 -
CHEMBL4062140 1 -
CHEMBL4074716 1 -
CHEMBL4091547 1 -
CHEMBL4068589 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26915 SC-560 IC50 = 53.0 nM 7.28
CHEMBL4075294 IC50 > 10000.0 nM -
CHEMBL42485 DUP-697 IC50 > 10000.0 nM -
CHEMBL118 CELECOXIB IC50 > 10000.0 nM -
CHEMBL4098347 IC50 > 10000.0 nM -
CHEMBL4080317 IC50 > 10000.0 nM -
CHEMBL4090622 IC50 > 10000.0 nM -
CHEMBL4069602 IC50 > 10000.0 nM -
CHEMBL4088012 IC50 > 10000.0 nM -
CHEMBL4095906 IC50 > 10000.0 nM -
CHEMBL4084676 IC50 > 10000.0 nM -
CHEMBL4072067 IC50 > 10000.0 nM -
CHEMBL4081499 IC50 > 10000.0 nM -
CHEMBL4062140 IC50 > 10000.0 nM -
CHEMBL4074716 IC50 > 30000.0 nM -
CHEMBL4091547 IC50 > 10000.0 nM -
CHEMBL4068589 IC50 > 10000.0 nM -