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Assay Detail

CHEMBL863477

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Binding
Inhibitory activity against COX2 in canine whole blood
31
Total Activities
31
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

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

Publication

5-heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure-activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog.
Sakya SM, DeMello KM, Minich ML, Rast B, Shavnya A, Rafka RJ, Koss DA, Cheng H, Li J, Jaynes BH, Ziegler CB, Mann DW, Petras CF, Seibel SB, Silvia AM, George DM, Lund LA, St Denis S, Hickman A, Haven ML, Lynch MP.
Bioorg Med Chem Lett (2006) 16 : 288 -292
PubMed 16275075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.62 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370579 1 7.52
CHEMBL201696 1 7.20
CHEMBL199344 1 7.02
CHEMBL199992 1 6.96
CHEMBL380595 1 6.94
CHEMBL199991 1 6.90
CHEMBL199337 1 6.90
CHEMBL199346 1 6.89
CHEMBL197705 1 6.89
CHEMBL199431 1 6.88
CHEMBL200518 1 6.85
CHEMBL201179 1 6.85
CHEMBL198024 1 6.84
CHEMBL198189 1 6.82
CHEMBL199901 1 6.72
CHEMBL381251 1 6.72
CHEMBL382095 1 6.71
CHEMBL200152 1 6.70
CHEMBL197869 1 6.70
CHEMBL199682 1 6.68
CHEMBL381879 1 6.64
CHEMBL200812 1 6.62
CHEMBL382524 1 6.53
CHEMBL174219 1 6.51
CHEMBL372393 1 6.44
CHEMBL200406 1 6.44
CHEMBL199681 1 6.38
CHEMBL426475 1 5.90
CHEMBL200559 1 5.73
CHEMBL200909 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370579 IC50 = 30.0 nM 7.52
CHEMBL201696 IC50 = 63.0 nM 7.20
CHEMBL199344 IC50 = 95.0 nM 7.02
CHEMBL199992 IC50 = 110.0 nM 6.96
CHEMBL380595 IC50 = 115.0 nM 6.94
CHEMBL199991 IC50 = 126.0 nM 6.90
CHEMBL199337 IC50 = 125.0 nM 6.90
CHEMBL199346 IC50 = 130.0 nM 6.89
CHEMBL197705 IC50 = 130.0 nM 6.89
CHEMBL199431 IC50 = 132.0 nM 6.88
CHEMBL200518 IC50 = 140.0 nM 6.85
CHEMBL201179 IC50 = 140.0 nM 6.85
CHEMBL198024 IC50 = 144.0 nM 6.84
CHEMBL198189 IC50 = 150.0 nM 6.82
CHEMBL199901 IC50 = 190.0 nM 6.72
CHEMBL381251 IC50 = 190.0 nM 6.72
CHEMBL382095 IC50 = 197.0 nM 6.71
CHEMBL200152 IC50 = 200.0 nM 6.70
CHEMBL197869 IC50 = 200.0 nM 6.70
CHEMBL199682 IC50 = 210.0 nM 6.68
CHEMBL381879 IC50 = 230.0 nM 6.64
CHEMBL200812 IC50 = 240.0 nM 6.62
CHEMBL382524 IC50 = 297.0 nM 6.53
CHEMBL174219 IC50 = 310.0 nM 6.51
CHEMBL372393 IC50 = 360.0 nM 6.44
CHEMBL200406 IC50 = 360.0 nM 6.44
CHEMBL199681 IC50 = 420.0 nM 6.38
CHEMBL426475 IC50 = 1250.0 nM 5.90
CHEMBL200559 IC50 = 1870.0 nM 5.73
CHEMBL200909 IC50 = 5000.0 nM 5.30
CHEMBL383151 IC50 = 7900.0 nM 5.10