COX-2-IN-34 is a selective, orally potent COX-2 inhibitor that shows anti-inflammatory activity without gastric ulcer toxicity during experiments in mice.

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

COX-2-IN-1 is a potent and selective COX-2 inhibitor (IC50: 3.9 μM).

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

COX-2-IN-31 (compound 7b) is an orally active dual inhibitor targeting COX-2 (IC50=60 nM) and 5-LOX (IC50=1.9 μM). Additionally, it inhibits the activity of transmembrane hCA IX (Ki=48.9 nM) and hCA XII (Ki=5.8 nM). This compound demonstrates anti-inflammatory and analgesic activity [1].

COX-1/2-IN-4 (compound 2b) is a dual COX-1 and COX-2 inhibitor with respective IC50 values of 0.239 μM for COX-1 and 0.191 μM for COX-2. Additionally, it demonstrates moderate anticancer activity, exhibiting IC50 values of 30.79 μM against COLO205 cancer cell lines and 74.15 μM against B16F1 cancer cell lines [1].

COX-2-IN-32 (Compound 2f) is a dual inhibitor of iNOS and COX-2, known to downregulate NF-κB expression. Demonstrating anti-inflammatory properties, it impedes NO production in LPS-induced RAW264.7 macrophages with an IC50 value of 11.2 μM [1].

COX-2/NO-IN-1 is an orally active nitric oxide synthase (iNOS) and NO ( IC 50 of 3.52 μM) inhibitor as well as suppresses the expression of COX-2. COX-2/NO-IN-1 has anti-inflammatory effects and reduces pathological damage to kidney tissues[1].

COX-2-IN-11 (compound 7b2) is a potent and selective COX-2 inhibitor. COX-2-IN-11 has the potential in inflammation disease research[1].

COX-2-IN-7 (compound 4a) is a potent, selective, and orally active COX-2 inhibitor which is higher selectivity than Celecoxib with an IC 50 value of 6.585 uM. COX-2-IN-7 has good anti-inflammatory and low ulcerogenic activity in vivo[1].

COX-2-IN-18 (Compound 3) is a highly effective COX-2 inhibitor with strong inhibitory activity against COX-2 (IC 50 = 0.775 μM). Its potency is comparable to the reference drug Celecoxib (IC 50 = 0.153 μM). This compound, COX-2-IN-18, shows promise in the field of cancer research [1].

COX-2-IN-35 (compound 7) is a selective inhibitor of COX-2, demonstrating anti-inflammatory activity, with an inhibitory concentration (IC 50) of 4.37 nM [1].

COX-2-IN-16 (compound 2b) is a potent, selective, and orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 102 μM. It effectively reduces nitric oxide (NO) production and demonstrates anti-inflammatory activity [1].

COX-2/15-LOX-IN-1 (Compound 14) is a COX-2 and 15-lipoxygenase (15-LOX) inhibitor that acts on COX-1 (IC50: 10.65 μM), COX-2 (IC50: 0.075 μM) and 15-LOX (IC50: 2.98 μM). 25 has an anti-inflammatory effect.

COX-2-IN-8 (Compound 6a) is a potent, selective, orally active COX-2 inhibitor (IC50: 6.585 μM) with a higher COX-2 selectivity than Celecoxib.

COX-2-IN-19 (Compound 24) is a highly potent inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 1.76 μM. Notably, COX-2-IN-19 exhibits robust in vivo anti-inflammatory activity [1].

COX-2-IN-13 (compound 13e) is a highly potent and selective inhibitor of COX-2, demonstrating a remarkable IC50 value of 0.98 μM. It exhibits strong anti-inflammatory activity and has shown favorable results in vivo acute toxicity studies [1].

COX-2-IN-23 is a selective inhibitor of COX-2, with IC50 values of 0.28 and 20.14 μM for COX-2 and COX-1, respectively.COX-2-IN-23 exhibits anti-inflammatory effects as well as low ulcerogenic effects.

COX-2-IN-22 is a COX-2 inhibitor (IC50: 8.6 μM) that can cross the blood-brain barrier and also exhibits inhibitory effects on AChE (IC50: 2.8 μM), BChE (IC50: 6.3 μM), β-Secretase (IC50: 15.3 μM), LOX-5 (IC50: 13.9 μM) and DPPH ( IC50: 6.8 μM) showed inhibitory effects.

COX-2-IN-10 is a potent inhibitor of COX-2. COX-2-IN-10 exhibits inhibitory effects on the production of IL-6, TNF-α and IL-1β. COX-2-IN-10 inhibits PGE2 production in a concentration-dependent manner with an IC50 value of 2.54 μM. COX-2-IN-10 inhibits the expression of iNOS and COX-2 at the mRNA and protein levels. COX-2-IN-10 inhibited the expression of iNOS and COX-2 at the mRNA and protein levels.

COX-2-IN-14 (compound 2a) is a highly potent and selective inhibitor of COX-2 (cyclooxygenase-2), with strong binding affinity at the active site of COX-2 co-crystal. Demonstrating remarkable in vivo anti-inflammatory activity, COX-2-IN-14 effectively reduces ear edema and myeloperoxidase (MPO) activity in mice [1].

COX-2/PI3K-IN-2 (compound 5f) has properties of anti-inflammatory and anti-cancer. COX-2/PI3K-IN-2 is a selective inhibitor of COX-2 (Ki = 3.02 nM) as well as a potent inhibitor of PI3K (IC 50 = 2.78 nM) [1].

COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX. It inhibits LPS-induced production of pro-inflammatory cytokines (IL-6, ROS) and exhibits targeted anti-inflammatory effects [1].

COX-2-IN-28 is a potent and selective COX-2 inhibitor capable of acting on COX-2 (IC50: 0.054 μM), 15-LOX (IC50: 2.14 μM) and COX-1 (IC50: 13.21 μM).

Topo I/COX-2-IN-2 (Compound W10) is a potent dual Topo I (IC50: 0.90 μM) and COX-2 (IC50: 2.31 μM) inhibitor.Topo I/COX-2-IN-2 induces apoptosis in cancer cells using the mitochondrial pathway.

COX-2/sEH-IN-1 is an orally active dual inhibitor of COX-2 (IC50: 1.24 μM) and sEH (IC50: 0.40 μM), a soluble epoxide hydrolase. COX-2/sEH-IN-1 increases anti-inflammatory effects and significantly reduces cardiovascular risk.

COX-2-IN-20 (Compound 5d) is a selective and orally active inhibitor of COX-2 (IC 50 = 17.9 nM) with anti-inflammatory activity [1].

COX-2-IN-12 (compound 3b) is a potent and selective COX-2 inhibitor with an IC 50 of 19.98 μM. COX-2-IN-12 is an anti-inflammatory agent that shows safety in-vivo acute toxicity studies [1].

COX-2/5-LOX-IN-3 (compound 5b) is a powerful and dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. This compound, COX-2/5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].

COX-2-IN-24 is an orally active COX-2 inhibitor (IC50: 0.17 μM) with anti-inflammatory and hypo-ulcerogenic effects.

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

COX-2/15-LOX-IN-2 is a potent inhibitor of both COX-2 and 15-LOX, demonstrating IC50 values of 0.065 μM for COX-2 and 1.86 μM for 15-LOX. Additionally, it exhibits significant antioxidant activity [1].

COX-2/5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent and dual inhibitor of COX-2 / 5-LOX. It exhibits superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 displays strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

COX-2-IN-26 is a potent, orally active, selective COX-2 inhibitor that acts on COX-1 (IC50: 10.61 μM), COX-2 (IC50: 0.067 μM), and 15-LOX (IC50: 1.96 μM).COX-2-IN-26 is anti-inflammatory and has a gastrointestinal safety profile.

COX-2/PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K (IC50: 1.14 nM). COX-2/PI3K-IN-1 is a selective inhibitor of COX-2 (Ki: 3.24 nM).

COX-2-IN-9 is a selective, potent, orally active COX-2 inhibitor (IC50: 10.17 μM).COX-2-IN-9 has a higher COX-2 selectivity than Celecoxib.COX-2-IN-9 exhibits good in vivo anti-inflammatory activity and low ulcerogenic effect.

FK 3311 (COX-2 Inhibitor V) is a cell permeable and orally available sulfonanilide that acts as a COX-2 inhibitor and non-steroidal anti-inflammatory drug (NSAID)

COX-1/2-IN-5 (compound 2a) functions as a dual inhibitor of COX1/2, demonstrating inhibitory concentrations (IC50) of 2.650 μM and 0.958 μM, respectively, and exhibits anticancer activity by inhibiting liver cancer HepG2 cells with an IC50 of 60.75 μM [1].

COX-2/15-LOX-IN-3 (compound 5k) serves as a dual inhibitor for COX-2 and 15-LOX, demonstrating inhibitory concentrations (IC50) of 0.075 μM and 1.97 μM, respectively. This compound effectively suppresses LPS-induced cellular production of pro-inflammatory cytokines (IL-6, ROS, and NO), exhibiting targeted anti-inflammatory effects [1].

COX-2-IN-33 (compound 5f) is a selective COX-2 inhibitor with an IC50 value of 45.5 nM and exhibits potential as an anti-inflammatory agent. It effectively suppresses pro-inflammatory cytokine production in vivo while maintaining gastric safety [1].

COX-2-IN-29 is a selective inhibitor of orally active COX-2 (IC50: 0.005 μM).

COX-2-IN-17 is a potent, blood-brain barrier permeable COX-2 (cyclooxygenase-2) inhibitor (IC50: 0.02 μM) with anti-inflammatory and analgesic activity.

COX-1/2-IN-3 (Compound 7a) is a dual inhibitor of COX-1 and COX-2. COX-1/2-IN-3 has anti-inflammatory activity with low toxicity [1].

COX-1/2-IN-2 is a potent inhibitor of both COX-1 and COX-2, displaying significant inhibitory effects with IC50 values of 9.7 ± 0.09 μM for COX-1 and 4.6 ± 1.45 μM for COX-2, respectively [1].

COX-2/5-LOX-IN-2 is a benzothiophen-2-ylpyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 (5b) inhibited both COX-2 and 5-LOX. The IC50s of COX-2/5-LOX-IN-2 inhibiting COX-1, COX-2 and 5-LOX were 5.40, 0.01 and 1.78 μM, respectively. COX-2/5-LOX-IN-2 showed more analgesic and anti-inflammatory activities than Celecoxib and Indomethacin.

COX-1/2-IN-2, a potent inhibitor of both COX-1 and COX-2, demonstrates significant inhibitory activity, with IC50 values of 13.9 ± 3.21 μM for COX-1 and 6.4 ± 0.74 μM for COX-2, respectively [1].

COX-2-IN-21 (Compound 5c) is an orally active, selective COX-2 inhibitor (IC50: 0.039 μM). COX-2-IN-21 has good anti-inflammatory potential.

Topo I/COX-2-IN-1 (1H-30) is a potent Topo I/COX-2 inhibitor with the IC50 of 0.24 μM and 4.42 μM for COX-2 and Topo I, respectively. Topo I/COX-2-IN-1 induces apoptosis and inhibits migration of cancer cells, shows anti-cancer activity.

Iptacopan (LNP023) is an inhibitor with high affinity for factor B.

Diclofenac Potassium (CGP-45840B) is a nonsteroidal anti-inflammatory drug taken to reduce inflammation and as an analgesic reducing pain in certain conditions.