naproxen [Ligand Id: 5230] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL154 (Aleve, Anaprox, Arthrosin 250, Arthrosin 250 ec, Arthrosin 500, Arthrosin 500 ec, Condrotec, Ec-naprosyn, Equiproxen, Feminax ultra, Grenoxal, Kenosyn, Laraflex, Napratec op, Naprelan, Naprosyn, Naprosyn 375, Naprosyn ec, Naproxen, Naproxene, Naproxeno, NSC-750183, NSC-757239, Nycopren, PN400 COMPONENT NAPROXEN, Pranoxen continus, Prosaid, Rheuflex 250, Rheuflex 500, Rimoxyn, RS-3540, Stirlescent, Timpron, Timpron 250 ec, Timpron 500 ec, Valrox, Vimovo) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C1 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
| Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C2 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 4.5 | pIC50 | 31300 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
| ChEMBL | Inhibition of human recombinant AKR1C2 using S-tetralol as substrate assessed as reduction in NADP+-dependent S-tetralol oxidation preincubated for 10 mins followed by protein addition by fluorometric assay | B | 5.9 | pIC50 | 1260 | nM | IC50 | J Med Chem (2016) 59: 7431-7444 [PMID:27486833] |
| AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C3 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
| ChEMBL | Inhibition of recombinant human AKR1C3 | B | 6.32 | pIC50 | 480 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5170-5175 [PMID:16183274] |
| ChEMBL | Inhibition of human recombinant AKR1C3 using S-tetralol as substrate assessed as reduction in NADP+-dependent S-tetralol oxidation preincubated for 10 mins followed by protein addition by fluorometric assay | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2016) 59: 7431-7444 [PMID:27486833] |
| Aldo-keto reductase family 1 member C4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4999] [UniProtKB: P17516] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal His6-tagged AKR1C4 expressed in Escherichia coli BL21(DE3) cells using 8-Acetyl-2,3,5,6-tetrahydro-1H,4H-11-oxa-3a-aza-benzo[de]anthracen-10-one as substrate after 1 hr by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 7746-7758 [PMID:22877157] |
| 5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527] | ||||||||
| ChEMBL | Inhibitory activity against 5-lipoxygenase catalysis (5-LO) in sonicated rat basophilic leukemia cell lysate | F | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
| COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
| ChEMBL | Inhibition of COX1-catalyzed prostaglandin biosynthesis 10 mins of preincubation | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Nat Prod (1998) 61: 1212-1215 [PMID:9784154] |
| ChEMBL | Inhibitory activity against prostaglandin G/H synthase 1 | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2000) 43: 214-223 [PMID:10649977] |
| ChEMBL | Inhibition of PGHS1 assessed as conversion of arachidonic acid to prostaglandin | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Nat Prod (1999) 62: 294-296 [PMID:10075763] |
| ChEMBL | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by immunoassay | B | 5.06 | pIC50 | 8650 | nM | IC50 | J Med Chem (2022) 65: 12219-12239 [PMID:36074863] |
| GtoPdb | - | - | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (1997) 40: 819-24 [PMID:9057869] |
| ChEMBL | Inhibition activity against recombinant human Prostaglandin G/H synthase 1 | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
| ChEMBL | Compound was tested in vitro for inhibition of human platelet Prostaglandin G/H synthase 1 at 10 uM | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2281-2282 |
| ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 6.68 | pIC50 | 211 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664] | ||||||||
| ChEMBL | Inhibition of bovine seminal microsomal COX1 assessed as PGE2 production preincubated for 10 mins | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Nat Prod (1998) 61: 2-7 [PMID:9461646] |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately | B | 4.28 | pIC50 | 52200 | nM | IC50 | J Nat Prod (2017) 80: 2472-2477 [PMID:28885836] |
| ChEMBL | Inhibition of ovine COX1 assessed as inhibition of PGF2a production by enzyme immunoassay | B | 4.31 | pIC50 | 49000 | nM | IC50 | Bioorg Med Chem (2013) 21: 532-539 [PMID:23219856] |
| ChEMBL | Inhibitory concentration against Prostaglandin H2 synthase 1 (PGHS-1) from ram seminal vesicle | B | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (1996) 39: 3929-3937 [PMID:8831759] |
| ChEMBL | Inhibition of ovine COX1 assessed as PGF2alpha production by enzyme immunoassay | B | 4.71 | pIC50 | 19500 | nM | IC50 | Eur J Med Chem (2012) 47: 111-124 [PMID:22119153] |
| ChEMBL | Tested for inhibitory activity against Prostaglandin G/H synthase 1 from ovine | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (1995) 38: 3895-3901 [PMID:7562922] |
| ChEMBL | Inhibition of ovine COX1 | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247] |
| ChEMBL | Inhibition of ovine COX-1 | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2011) 54: 1356-1364 [PMID:21280601] |
| ChEMBL | Inhibition of COX1 in ram seminal vesicles using arachidonic acid as substrate assessed as reduction in PGH2 conversion to PGG2 by measuring TMPD oxidation preincubated for 5 mins followed by substrate/TMPD addition measured for 5 mins by colorimetric assay | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2016) 59: 7431-7444 [PMID:27486833] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Inhibition of human COX2 expressed in insect cells using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately | B | 4.28 | pIC50 | 52200 | nM | IC50 | J Nat Prod (2017) 80: 2472-2477 [PMID:28885836] |
| ChEMBL | Inhibition of human recombinant COX-2 by enzyme immunoassay | B | 4.3 | pIC50 | 50000 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
| ChEMBL | Compound was tested in vitro for inhibition of human umbilical cord endothelial cells(ECV-304 cell line) Prostaglandin G/H synthase 2 at 10 uM | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2281-2282 |
| ChEMBL | Inhibitory activity against prostaglandin G/H synthase 2 | B | 4.72 | pIC50 | 18900 | nM | IC50 | J Med Chem (2000) 43: 214-223 [PMID:10649977] |
| ChEMBL | DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) | B | 4.77 | pIC50 | 17001 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of human recombinant COX2 | B | 4.91 | pIC50 | 12400 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247] |
| ChEMBL | Inhibition of human recombinant COX-2 | B | 4.91 | pIC50 | 12400 | nM | IC50 | J Med Chem (2011) 54: 1356-1364 [PMID:21280601] |
| ChEMBL | Inhibition of COX-2 (unknown origin) | B | 5 | pIC50 | 10070 | nM | IC50 | J Med Chem (2022) 65: 13436-13451 [PMID:36170566] |
| ChEMBL | Tested for inhibitory activity against Prostaglandin G/H synthase 2 from human | B | 5.01 | pIC50 | 9700 | nM | IC50 | J Med Chem (1995) 38: 3895-3901 [PMID:7562922] |
| GtoPdb | - | - | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (1997) 40: 819-24 [PMID:9057869] |
| ChEMBL | Inhibition activity against recombinant human Prostaglandin G/H synthase 2 | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (1997) 40: 819-824 [PMID:9057869] |
| ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by immunoassay | B | 5.62 | pIC50 | 2390 | nM | IC50 | J Med Chem (2022) 65: 12219-12239 [PMID:36074863] |
| ChEMBL | Inhibition of COX2 (unknown origin) using arachidonic acid as substrate assessed as reduction in PGH2 conversion to PGG2 by measuring TMPD oxidation preincubated for 5 mins followed by substrate/TMPD addition measured for 5 mins by colorimetric assay | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2016) 59: 7431-7444 [PMID:27486833] |
| Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
| ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay | B | 5.47 | pIC50 | 3360 | nM | IC50 | Bioorg Med Chem (2018) 26: 4113-4126 [PMID:29980364] |
| lipase E, hormone sensitive type/Hormone-sensitive lipase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5582] [GtoPdb: 2593] [UniProtKB: P15304] | ||||||||
| ChEMBL | Inhibition of HSL in Wistar rat isolated fat cells by spectrophotometric assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2008) 51: 6478-6494 [PMID:18808096] |
| L-PGDS/Prostaglandin-H2 D-isomerase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4334] [GtoPdb: 1380] [UniProtKB: O09114] | ||||||||
| ChEMBL | Concentration required to inhibit 50% activity of prostaglandin synthetase was determined in vitro in mouse brain microsomes | B | 4.89 | pIC50 | 13000 | nM | IC50 | J Med Chem (1991) 34: 1099-1110 [PMID:1900533] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Inhibition of N-terminal His-tagged SARS-CoV-2 3CLpro by microplate reader assay | B | 5.46 | pIC50 | 3450 | nM | IC50 | Eur J Med Chem (2023) 257: 115491-115491 [PMID:37244162] |
| Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells | F | 5.24 | pIC50 | 5800 | nM | IC50 | J Pharmacol Exp Ther (2000) 295: 10-15 [PMID:10991954] |
| Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes | F | 5.7 | pKi | 2000 | nM | Ki | Mol Pharmacol (1999) 55: 847-854 [PMID:10220563] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
