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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, 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 |
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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 | 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] |
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 | 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 | 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 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] |
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 31:
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]