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Assay Detail

CHEMBL865437

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Binding
Inhibition of COX1 in canine whole blood
19
Total Activities
19
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

Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
Cheng H, Lundy DeMello KM, Li J, Sakya SM, Ando K, Kawamura K, Kato T, Rafka RJ, Jaynes BH, Ziegler CB, Stevens R, Lund LA, Mann DW, Kilroy C, Haven ML, Nimz EL, Dutra JK, Li C, Minich ML, Kolosko NL, Petras C, Silvia AM, Seibel SB.
Bioorg Med Chem Lett (2006) 16 : 2076 -2080
PubMed 16464588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.04 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205308 1 5.70
CHEMBL205351 1 5.70
CHEMBL205938 1 5.57
CHEMBL378649 1 5.47
CHEMBL380457 1 5.42
CHEMBL383409 1 5.30
CHEMBL380148 1 5.26
CHEMBL205331 1 4.96
CHEMBL208450 1 4.92
CHEMBL381834 1 4.90
CHEMBL383272 1 4.81
CHEMBL377797 1 4.80
CHEMBL206359 1 4.74
CHEMBL207702 1 4.64
CHEMBL206207 1 4.63
CHEMBL378875 1 4.55
CHEMBL383210 1 4.30
CHEMBL383064 1 -
CHEMBL377284 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205308 IC50 = 2000.0 nM 5.70
CHEMBL205351 IC50 = 2000.0 nM 5.70
CHEMBL205938 IC50 = 2700.0 nM 5.57
CHEMBL378649 IC50 = 3400.0 nM 5.47
CHEMBL380457 IC50 = 3800.0 nM 5.42
CHEMBL383409 IC50 = 5000.0 nM 5.30
CHEMBL380148 IC50 = 5500.0 nM 5.26
CHEMBL205331 IC50 = 11100.0 nM 4.96
CHEMBL208450 IC50 = 12000.0 nM 4.92
CHEMBL381834 IC50 = 12700.0 nM 4.90
CHEMBL383272 IC50 = 15500.0 nM 4.81
CHEMBL377797 IC50 = 16000.0 nM 4.80
CHEMBL206359 IC50 = 18200.0 nM 4.74
CHEMBL207702 IC50 = 22700.0 nM 4.64
CHEMBL206207 IC50 = 23400.0 nM 4.63
CHEMBL378875 IC50 = 27900.0 nM 4.55
CHEMBL383210 IC50 = 50000.0 nM 4.30
CHEMBL383064 IC50 > 50000.0 nM -
CHEMBL377284 IC50 > 50000.0 nM -