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Assay Detail

CHEMBL865933

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

Binding
Inhibition of COX1 by canine whole blood assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Expert

Target

Prostaglandin G/H synthase 1 (CHEMBL4133)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.
Sakya SM, Cheng H, Lundy Demello KM, Shavnya A, Minich ML, Rast B, Dutra J, Li C, Rafka RJ, Koss DA, Li J, Jaynes BH, Ziegler CB, Mann DW, Petras CF, Seibel SB, Silvia AM, George DM, Hickman A, Haven ML, Lynch MP.
Bioorg Med Chem Lett (2006) 16 : 1202 -1206
PubMed 16380252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.67 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426117 1 7.00
CHEMBL202856 1 7.00
CHEMBL381971 1 6.70
CHEMBL381158 1 6.70
CHEMBL381716 1 6.40
CHEMBL204178 1 6.22
CHEMBL204506 1 6.05
CHEMBL204707 1 5.82
CHEMBL203697 1 5.70
CHEMBL380329 1 5.50
CHEMBL427380 1 5.48
CHEMBL264572 1 5.46
CHEMBL205163 1 5.15
CHEMBL381363 1 5.12
CHEMBL381304 1 5.10
CHEMBL383207 1 5.00
CHEMBL204641 1 4.97
CHEMBL413045 1 4.93
CHEMBL204703 1 4.60
CHEMBL377499 1 4.53
CHEMBL200812 1 -
CHEMBL204029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426117 IC50 = 100.0 nM 7.00
CHEMBL202856 IC50 = 100.0 nM 7.00
CHEMBL381971 IC50 = 200.0 nM 6.70
CHEMBL381158 IC50 = 200.0 nM 6.70
CHEMBL381716 IC50 = 400.0 nM 6.40
CHEMBL204178 IC50 = 600.0 nM 6.22
CHEMBL204506 IC50 = 900.0 nM 6.05
CHEMBL204707 IC50 = 1500.0 nM 5.82
CHEMBL203697 IC50 = 2000.0 nM 5.70
CHEMBL380329 IC50 = 3200.0 nM 5.50
CHEMBL427380 IC50 = 3300.0 nM 5.48
CHEMBL264572 IC50 = 3500.0 nM 5.46
CHEMBL205163 IC50 = 7100.0 nM 5.15
CHEMBL381363 IC50 = 7600.0 nM 5.12
CHEMBL381304 IC50 = 8000.0 nM 5.10
CHEMBL383207 IC50 = 10000.0 nM 5.00
CHEMBL204641 IC50 = 10600.0 nM 4.97
CHEMBL413045 IC50 = 11800.0 nM 4.93
CHEMBL204703 IC50 = 25300.0 nM 4.60
CHEMBL377499 IC50 = 29700.0 nM 4.53
CHEMBL200812 IC50 > 50000.0 nM -
CHEMBL204029 IC50 > 50000.0 nM -