naproxen [Ligand Id: 5230] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL154 (Ec-Naprosyn, Equiproxen, Timpron 250 EC, Feminax Ultra, Nycopren, Kenosyn, Arthrosin 250 EC, Laraflex, Valrox, Condrotec, Arthrosin 250, Rheuflex 500, Vimovo, Prosaid, RS-3540, Rimoxyn, Grenoxal, Naprosyn 375, Rheuflex 250, Timpron, Napratec OP, Naprosyn, Arthrosin 500 EC, Naproxen, Naprelan, Stirlescent, Anaprox, Arthrosin 500, Naprosyn EC, Timpron 500 EC, Aleve, Pranoxen Continus)
  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • Aldo-keto reductase family 1 member C4 in Human [ChEMBL: CHEMBL4999] [UniProtKB: P17516]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • lipase E, hormone sensitive type/Hormone-sensitive lipase in Rat [ChEMBL: CHEMBL5582] [GtoPdb: 2593] [UniProtKB: P15304]
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  • L-PGDS/Prostaglandin-H2 D-isomerase in Mouse [ChEMBL: CHEMBL4334] [GtoPdb: 1380] [UniProtKB: O09114]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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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]
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]
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 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 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 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]
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]
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 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 COX-2 B 4.91 pIC50 12400 nM IC50 J. Med. Chem. (2011) 54: 1356-1364 [PMID:21280601]
ChEMBL Inhibition of human recombinant COX2 B 4.91 pIC50 12400 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 163-168 [PMID:23200247]
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]
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]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]