Target id: 1376

Nomenclature: COX-2

Family: Cyclooxygenase

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 604 1q25.2-q25.3 PTGS2 prostaglandin-endoperoxide synthase 2
Mouse - 604 1 63.84 cM Ptgs2 prostaglandin-endoperoxide synthase 2
Rat - 604 13q21 Ptgs2 prostaglandin-endoperoxide synthase 2
Previous and Unofficial Names
cyclooxygenase 2
PGH synthase 2
prostaglandin G/H synthase 2
prostaglandin-endoperoxide synthase 2 (prostaglandin G/H synthase and cyclooxygenase)
Database Links
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Reference Database
KEGG Enzyme
Enzyme Reaction
EC Number: Hydrogen donor + arachidonic acid + 2O2 = hydrogen acceptor + H2O + PGH2
Description Reaction Reference
Arachidonic acid => PGG2 => PGH2
This enzyme is also associated with the following reaction: Docosahexaenoic acid => PGH3

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
lumiracoxib Hs Inhibition 6.5 pKi 4
pKi 6.5 (Ki 3.2x10-7 M) [4]
paracetamol Hs Inhibition 4.6 pKi 10
pKi 4.6 (Ki 2.58x10-5 M) [10]
NS-398 Hs Inhibition 8.7 pIC50 12
pIC50 8.7 (IC50 1.9x10-9 M) [12]
Description: Measuring inhibition of PGE2 production in human IL-1-stimulated synovial cells
celecoxib Hs Inhibition 8.7 pIC50 3
pIC50 8.7 (IC50 2x10-9 M) [3]
benzquinamide Hs Inhibition 8.3 pIC50 1
pIC50 8.3 (IC50 4.8x10-9 M) [1]
valdecoxib Hs Inhibition 8.3 pIC50 22
pIC50 8.3 (IC50 5x10-9 M) [22]
flurbiprofen Hs Inhibition 8.0 pIC50 2
pIC50 8.0 (IC50 1x10-8 M) [2]
(S)-ARN2508 Hs Inhibition 7.9 pIC50 18
pIC50 7.9 (IC50 1.2x10-8 M) [18]
diclofenac Hs Inhibition 7.7 pIC50 5
pIC50 7.7 (IC50 2x10-8 M) [5]
meclofenamic acid Hs Inhibition 7.4 pIC50 13
pIC50 7.4 (IC50 4x10-8 M) [13]
carprofen Hs Inhibition 7.0 pIC50 9
pIC50 7.0 (IC50 1.02x10-7 M) [9]
Description: Inhibition of COX-2-induced conversion of arachadonic acid to 12-HHT.
meloxicam Hs Inhibition 6.3 pIC50 17
pIC50 6.3 (IC50 4.9x10-7 M) [17]
rofecoxib Hs Inhibition 6.1 – 6.5 pIC50 24
pIC50 6.1 – 6.5 [24]
nimesulide Hs Inhibition 6.2 pIC50 19
pIC50 6.2 (IC50 6x10-7 M) [19]
ketoprofen Hs Inhibition 6.2 pIC50 6
pIC50 6.2 (IC50 6.9x10-7 M) [6]
Description: Inhibition of COX2 in human whole blood.
resveratrol Hs Inhibition 6.1 pIC50 11
pIC50 6.1 (IC50 7.5x10-7 M) [11]
etoricoxib Hs Inhibition 6.0 pIC50 20
pIC50 6.0 (IC50 1.1x10-6 M) [20]
ibuprofen Hs Inhibition 5.9 pIC50 23
pIC50 5.9 (IC50 1.35x10-6 M) [23]
aspirin Hs Inhibition 5.6 pIC50 21
pIC50 5.6 (IC50 2.4x10-6 M) [21]
naproxen Hs Inhibition 5.6 pIC50 16
pIC50 5.6 (IC50 2.5x10-6 M) [16]
ketorolac Hs Inhibition 4.2 – 6.9 pIC50 23
pIC50 6.9 (IC50 1.2x10-7 M) [23]
Description: Inhibition of human COX2 measured after pre-incubation of enzyme with compound.
pIC50 4.2 (IC50 6.05x10-5 M) [23]
Description: Instantaneous inhibition of human COX2 by compound (no pre-incubation).
suprofen Hs Inhibition 5.6 pIC50 6
pIC50 5.6 (IC50 2.75x10-6 M) [6]
mefenamic acid Hs Inhibition 5.5 pIC50 7
pIC50 5.5 (IC50 2.9x10-6 M) [7]
(R)-ARN2508 Hs Inhibition 4.6 pIC50 18
pIC50 4.6 (IC50 2.28x10-5 M) [18]
oxaprozin Hs Inhibition 4.4 pIC50 15
pIC50 4.4 (IC50 3.6x10-5 M) [15]
etodolac Hs Inhibition 4.3 pIC50 14
pIC50 4.3 (IC50 5.3x10-5 M) [14]
Description: Measured as LPS-induced PGE2 production in COX-1-inhibited human monocytes.
piroxicam Hs Inhibition 3.7 pIC50 25
pIC50 3.7 (IC50 2.18x10-4 M) [25]
phenylbutazone Hs Inhibition 3.5 pIC50 25
pIC50 3.5 (IC50 2.84x10-4 M) [25]
Inhibitor Comments
Carprofen is a COX-2 selective cyclooxygenase inhibitor, at least when comparing human COX-2 vs. ovine COX-1 in the same assay [8-9].
The data for etodolac in the table above is from Kato et al. (2001) [14]. In the same study etodolac's IC50 for COX-1 was reported to be >100 μM.
Piroxicam inhibits both cyclooxygenase isozymes [17], with maximum inhibition of PGE2 synthesis of approximately 60% for COX-2 and 35% for COX-1. Ketorolac is also a non-selective COX inhibitor.


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13. Kalgutkar AS, Rowlinson SW, Crews BC, Marnett LJ. (2002) Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors. Bioorg. Med. Chem. Lett.12 (4): 521-4. [PMID:11844663]

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Cyclooxygenase: COX-2 . Last modified on 09/02/2016. Accessed on 26/06/2016. IUPHAR/BPS Guide to PHARMACOLOGY,