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Assay Detail

CHEMBL5543915

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Binding
Inhibition of human COX-2
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A further pocket or conformational plasticity by mapping COX-1 catalytic site through modified-mofezolac structure-inhibitory activity relationships and their antiplatelet behavior.
Solidoro R, Miciaccia M, Bonaccorso C, Fortuna CG, Armenise D, Centonze A, Ferorelli S, Vitale P, Rodrigues P, Guimarães R, de Oliveira A, da Paz M, Rangel L, Sathler PC, Altomare A, Perrone MG, Scilimati A.
Eur J Med Chem (2024) 266 : 116135 -116135
PubMed 38219659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.64 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365033 1 5.60
CHEMBL275809 FR-122047 1 4.19
CHEMBL26915 SC-560 1 4.13
CHEMBL363228 1 -
CHEMBL361504 1 -
CHEMBL5574567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365033 IC50 = 2490.0 nM 5.60
CHEMBL275809 FR-122047 IC50 = 65000.0 nM 4.19
CHEMBL26915 SC-560 IC50 = 74900.0 nM 4.13
CHEMBL363228 IC50 > 100000.0 nM -
CHEMBL361504 IC50 > 1490.0 nM -
CHEMBL5574567 IC50 > 100000.0 nM -