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Assay Detail

CHEMBL945869

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

Binding
Inhibition of human recombinant mPGES1
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors.
Côté B, Boulet L, Brideau C, Claveau D, Ethier D, Frenette R, Gagnon M, Giroux A, Guay J, Guiral S, Mancini J, Martins E, Massé F, Méthot N, Riendeau D, Rubin J, Xu D, Yu H, Ducharme Y, Friesen RW.
Bioorg Med Chem Lett (2007) 17 : 6816 -6820
PubMed 18029174 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.90 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412099 1 9.00
CHEMBL180650 1 8.52
CHEMBL408218 1 8.05
CHEMBL411327 1 7.92
CHEMBL406392 1 7.77
CHEMBL408965 1 7.72
CHEMBL270094 1 7.68
CHEMBL270347 1 7.44
CHEMBL270095 1 7.35
CHEMBL406679 1 7.33
CHEMBL405474 1 7.29
CHEMBL270508 1 7.14
CHEMBL271956 1 7.12
CHEMBL270718 1 7.06
CHEMBL270348 1 7.00
CHEMBL272424 1 6.85
CHEMBL273089 1 6.48
CHEMBL407548 1 6.39
CHEMBL261386 1 6.28
CHEMBL411326 1 6.25
CHEMBL272858 1 6.16
CHEMBL272184 1 6.15
CHEMBL260525 1 5.89
CHEMBL270507 1 5.70
CHEMBL261604 1 5.60
CHEMBL270719 1 5.18
CHEMBL405697 1 5.10
CHEMBL261385 1 -
CHEMBL399902 1 -
CHEMBL270702 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412099 IC50 = 1.0 nM 9.00
CHEMBL180650 IC50 = 3.0 nM 8.52
CHEMBL408218 IC50 = 9.0 nM 8.05
CHEMBL411327 IC50 = 12.0 nM 7.92
CHEMBL406392 IC50 = 17.0 nM 7.77
CHEMBL408965 IC50 = 19.0 nM 7.72
CHEMBL270094 IC50 = 21.0 nM 7.68
CHEMBL270347 IC50 = 36.0 nM 7.44
CHEMBL270095 IC50 = 45.0 nM 7.35
CHEMBL406679 IC50 = 47.0 nM 7.33
CHEMBL405474 IC50 = 51.0 nM 7.29
CHEMBL270508 IC50 = 73.0 nM 7.14
CHEMBL271956 IC50 = 75.0 nM 7.12
CHEMBL270718 IC50 = 87.0 nM 7.06
CHEMBL270348 IC50 = 100.0 nM 7.00
CHEMBL272424 IC50 = 140.0 nM 6.85
CHEMBL273089 IC50 = 330.0 nM 6.48
CHEMBL407548 IC50 = 410.0 nM 6.39
CHEMBL261386 IC50 = 530.0 nM 6.28
CHEMBL411326 IC50 = 560.0 nM 6.25
CHEMBL272858 IC50 = 700.0 nM 6.16
CHEMBL272184 IC50 = 710.0 nM 6.15
CHEMBL260525 IC50 = 1300.0 nM 5.89
CHEMBL270507 IC50 = 2000.0 nM 5.70
CHEMBL261604 IC50 = 2500.0 nM 5.60
CHEMBL270719 IC50 = 6600.0 nM 5.18
CHEMBL405697 IC50 = 8000.0 nM 5.10
CHEMBL436640 IC50 > 10000.0 nM -
CHEMBL403987 IC50 > 10000.0 nM -
CHEMBL260527 IC50 > 10000.0 nM -
CHEMBL269896 IC50 > 10000.0 nM -
CHEMBL269895 IC50 > 10000.0 nM -
CHEMBL21156 IC50 > 10000.0 nM -
CHEMBL270702 IC50 > 10000.0 nM -
CHEMBL399902 IC50 > 10000.0 nM -
CHEMBL261385 IC50 > 10000.0 nM -