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Assay Detail

CHEMBL1781668

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

Binding
Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E synthase (CHEMBL5658)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1.
Greiner C, Zettl H, Koeberle A, Pergola C, Northoff H, Schubert-Zsilavecz M, Werz O.
Bioorg Med Chem (2011) 19 : 3394 -3401
PubMed 21570310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.42 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL551884 1 5.77
CHEMBL564017 1 5.70
CHEMBL563351 1 5.66
CHEMBL558072 1 5.66
CHEMBL29097 1 5.62
CHEMBL563546 1 5.57
CHEMBL558141 1 5.54
CHEMBL561284 1 5.39
CHEMBL551479 1 5.38
CHEMBL551480 1 5.34
CHEMBL559752 1 5.15
CHEMBL549723 1 5.06
CHEMBL1780184 1 5.03
CHEMBL557342 1 5.03
CHEMBL1780185 1 -
CHEMBL1780186 1 -
CHEMBL314360 1 -
CHEMBL562786 1 -
CHEMBL561006 1 -
CHEMBL563311 1 -
CHEMBL552347 1 -
CHEMBL560484 1 -
CHEMBL560205 1 -
CHEMBL550332 1 -
CHEMBL551420 1 -
CHEMBL1780187 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL551884 IC50 = 1700.0 nM 5.77
CHEMBL564017 IC50 = 2000.0 nM 5.70
CHEMBL563351 IC50 = 2200.0 nM 5.66
CHEMBL558072 IC50 = 2200.0 nM 5.66
CHEMBL29097 IC50 = 2400.0 nM 5.62
CHEMBL563546 IC50 = 2700.0 nM 5.57
CHEMBL558141 IC50 = 2900.0 nM 5.54
CHEMBL561284 IC50 = 4100.0 nM 5.39
CHEMBL551479 IC50 = 4200.0 nM 5.38
CHEMBL551480 IC50 = 4600.0 nM 5.34
CHEMBL559752 IC50 = 7100.0 nM 5.15
CHEMBL549723 IC50 = 8800.0 nM 5.06
CHEMBL1780184 IC50 = 9400.0 nM 5.03
CHEMBL557342 IC50 = 9300.0 nM 5.03
CHEMBL1780185 IC50 - -
CHEMBL1780186 IC50 - -
CHEMBL314360 IC50 - -
CHEMBL562786 IC50 > 10000.0 nM -
CHEMBL561006 IC50 > 10000.0 nM -
CHEMBL563311 IC50 > 10000.0 nM -
CHEMBL552347 IC50 > 10000.0 nM -
CHEMBL560484 IC50 > 10000.0 nM -
CHEMBL560205 IC50 > 10000.0 nM -
CHEMBL550332 IC50 > 10000.0 nM -
CHEMBL551420 IC50 > 10000.0 nM -
CHEMBL1780187 IC50 > 10000.0 nM -