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Assay Detail

CHEMBL3606528

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Binding
Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol.
Noha SM, Fischer K, Koeberle A, Garscha U, Werz O, Schuster D.
Bioorg Med Chem (2015) 23 : 4839 -4845
PubMed 26088337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.63 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL567696 — — 1 9.40
CHEMBL565406 — — 1 9.00
CHEMBL1289402 — — 1 9.00
CHEMBL1683210 — — 1 9.00
CHEMBL3604189 — — 1 9.00
CHEMBL1289055 — — 1 8.40
CHEMBL3604190 — — 1 7.22
CHEMBL1934808 — — 1 7.22
CHEMBL2152710 — — 1 6.75
CHEMBL2049148 — — 1 6.75
CHEMBL2046483 — — 1 6.75
CHEMBL521164 — — 1 6.70
CHEMBL225421 ARZANOL — 1 6.40
CHEMBL1934794 — — 1 6.40
CHEMBL1934797 — — 1 6.30
CHEMBL3604284 — — 1 6.30
CHEMBL411326 — — 1 6.25
CHEMBL520317 — — 1 6.22
CHEMBL490461 — — 1 6.22
CHEMBL1934792 — — 1 6.05
CHEMBL1289286 — — 1 6.03
CHEMBL1288905 — — 1 5.89
CHEMBL521286 — — 1 5.89
CHEMBL1290049 — — 1 5.85
CHEMBL1934795 — — 1 5.82
CHEMBL527421 — — 1 5.77
CHEMBL1683191 — — 1 5.77
CHEMBL29097 — — 1 5.62
CHEMBL261604 — — 1 5.60
CHEMBL1288945 — — 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL567696 — IC50 = 0.4 nM 9.40
CHEMBL565406 — IC50 = 1.0 nM 9.00
CHEMBL3604189 — IC50 = 1.0 nM 9.00
CHEMBL1289402 — IC50 = 1.0 nM 9.00
CHEMBL1683210 — IC50 = 1.0 nM 9.00
CHEMBL1289055 — IC50 = 4.0 nM 8.40
CHEMBL3604190 — IC50 = 60.0 nM 7.22
CHEMBL1934808 — IC50 = 60.0 nM 7.22
CHEMBL2152710 — IC50 = 180.0 nM 6.75
CHEMBL2049148 — IC50 = 180.0 nM 6.75
CHEMBL2046483 — IC50 = 180.0 nM 6.75
CHEMBL521164 — IC50 = 200.0 nM 6.70
CHEMBL1934794 — IC50 = 395.0 nM 6.40
CHEMBL225421 ARZANOL IC50 = 400.0 nM 6.40
CHEMBL3604284 — IC50 = 500.0 nM 6.30
CHEMBL1934797 — IC50 = 506.0 nM 6.30
CHEMBL411326 — IC50 = 560.0 nM 6.25
CHEMBL520317 — IC50 = 600.0 nM 6.22
CHEMBL490461 — IC50 = 600.0 nM 6.22
CHEMBL1934792 — IC50 = 900.0 nM 6.05
CHEMBL1289286 — IC50 = 940.0 nM 6.03
CHEMBL1288905 — IC50 = 1300.0 nM 5.89
CHEMBL521286 — IC50 = 1300.0 nM 5.89
CHEMBL1290049 — IC50 = 1400.0 nM 5.85
CHEMBL1934795 — IC50 = 1500.0 nM 5.82
CHEMBL527421 — IC50 = 1700.0 nM 5.77
CHEMBL1683191 — IC50 = 1700.0 nM 5.77
CHEMBL29097 — IC50 = 2400.0 nM 5.62
CHEMBL261604 — IC50 = 2500.0 nM 5.60
CHEMBL1288945 — IC50 = 3700.0 nM 5.43
CHEMBL3604187 — IC50 = 3800.0 nM 5.42
CHEMBL3604186 — IC50 = 4500.0 nM 5.35
CHEMBL519337 — IC50 = 9200.0 nM 5.04
CHEMBL21156 — IC50 > 10000.0 nM -
CHEMBL436640 — IC50 > 10000.0 nM -
CHEMBL261385 — IC50 > 10000.0 nM -
CHEMBL1683218 — IC50 > 10000.0 nM -
CHEMBL3604285 — IC50 > 10000.0 nM -
CHEMBL1288946 — IC50 > 30000.0 nM -
CHEMBL1934681 — IC50 - — -
CHEMBL595490 — IC50 - — -
CHEMBL2046488 — IC50 - — -
CHEMBL2046491 — IC50 - — -
CHEMBL2046492 — IC50 - — -
CHEMBL1934793 — IC50 - — -
CHEMBL1934796 — IC50 - — -