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Assay Detail

CHEMBL760077

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Binding
In vitro inhibitory activity against canine prostaglandin G/H synthase 2.
ChEMBL ↗
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cyclooxygenase-2 (CHEMBL4033) ↗
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Li J, DeMello KM, Cheng H, Sakya SM, Bronk BS, Rafka RJ, Jaynes BH, Ziegler CB, Kilroy C, Mann DW, Nimz EL, Lynch MP, Haven ML, Kolosko NL, Minich ML, Li C, Dutra JK, Rast B, Crosson RM, Morton BJ, Kirk GW, Callaghan KM, Koss DA, Shavnya A, Lund LA, Seibel SB, Petras CF, Silvia A.
Bioorg Med Chem Lett (2004) 14 : 95 -98
PubMed 14684306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.66 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175485 — — 1 7.36
CHEMBL176983 — — 1 7.36
CHEMBL174724 — — 1 7.30
CHEMBL360705 — — 1 7.22
CHEMBL369315 — — 1 7.22
CHEMBL368724 — — 1 7.21
CHEMBL177244 — — 1 7.19
CHEMBL367123 — — 1 7.16
CHEMBL174982 — — 1 7.10
CHEMBL176934 — — 1 6.92
CHEMBL366726 — — 1 6.92
CHEMBL174860 — — 1 6.92
CHEMBL176265 — — 1 6.89
CHEMBL367179 — — 1 6.77
CHEMBL366677 — — 1 6.77
CHEMBL367785 — — 1 6.75
CHEMBL367550 — — 1 6.72
CHEMBL366992 — — 1 6.62
CHEMBL176642 — — 1 6.60
CHEMBL176387 — — 1 6.57
CHEMBL177397 — — 1 6.54
CHEMBL173770 — — 1 6.52
CHEMBL443302 — — 1 6.52
CHEMBL368173 — — 1 6.51
CHEMBL174219 — — 1 6.51
CHEMBL366517 — — 1 6.48
CHEMBL367617 — — 1 6.41
CHEMBL355812 — — 1 6.40
CHEMBL175826 — — 1 6.39
CHEMBL174586 — — 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175485 — IC50 = 44.0 nM 7.36
CHEMBL176983 — IC50 = 44.0 nM 7.36
CHEMBL174724 — IC50 = 50.0 nM 7.30
CHEMBL360705 — IC50 = 60.0 nM 7.22
CHEMBL369315 — IC50 = 60.0 nM 7.22
CHEMBL368724 — IC50 = 62.0 nM 7.21
CHEMBL177244 — IC50 = 64.0 nM 7.19
CHEMBL367123 — IC50 = 69.0 nM 7.16
CHEMBL174982 — IC50 = 80.0 nM 7.10
CHEMBL176934 — IC50 = 120.0 nM 6.92
CHEMBL366726 — IC50 = 120.0 nM 6.92
CHEMBL174860 — IC50 = 120.0 nM 6.92
CHEMBL176265 — IC50 = 130.0 nM 6.89
CHEMBL367179 — IC50 = 170.0 nM 6.77
CHEMBL366677 — IC50 = 170.0 nM 6.77
CHEMBL367785 — IC50 = 180.0 nM 6.75
CHEMBL367550 — IC50 = 190.0 nM 6.72
CHEMBL366992 — IC50 = 240.0 nM 6.62
CHEMBL176642 — IC50 = 250.0 nM 6.60
CHEMBL176387 — IC50 = 270.0 nM 6.57
CHEMBL177397 — IC50 = 290.0 nM 6.54
CHEMBL173770 — IC50 = 300.0 nM 6.52
CHEMBL443302 — IC50 = 300.0 nM 6.52
CHEMBL368173 — IC50 = 310.0 nM 6.51
CHEMBL174219 — IC50 = 310.0 nM 6.51
CHEMBL366517 — IC50 = 330.0 nM 6.48
CHEMBL367617 — IC50 = 390.0 nM 6.41
CHEMBL355812 — IC50 = 400.0 nM 6.40
CHEMBL175826 — IC50 = 410.0 nM 6.39
CHEMBL174586 — IC50 = 450.0 nM 6.35
CHEMBL28636 DERACOXIB IC50 = 630.0 nM 6.20
CHEMBL118 CELECOXIB IC50 = 900.0 nM 6.05
CHEMBL177649 — IC50 = 1500.0 nM 5.82
CHEMBL176677 — IC50 = 2000.0 nM 5.70
CHEMBL175340 — IC50 = 8100.0 nM 5.09