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ChEMBL ligand: CHEMBL527 (Brexidol, CP-16,171, CP-16171, Feldene, Feldene 20, Feldene p, Flamatrol, Kentene, Larapam, NSC-666076, Piroflam 10, Piroflam 20, Piroxicam, Pirozip 10, Pirozip 20) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527] | ||||||||
ChEMBL | Inhibition of 5-lipoxygenase from rat peritoneal neutrophils after oral administration | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1988) 31: 1453-1462 [PMID:3133478] |
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
ChEMBL | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate preincubated for 2 mins followed by substrate addition in presence of TMPD by spectrophotometric analysis | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798] |
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 5.88 | pIC50 | 1313 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Concentration of drug that causes a 50% decrease in the maximal inhibition of Prostaglandin G/H synthase 1 activity as measured by PGE-2 production (''++'' indicates 80-90% inhibition) | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1997) 40: 980-989 [PMID:9083488] |
GtoPdb | - | - | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (1997) 40: 980-9 [PMID:9083488] |
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Tested for inhibitory activity against Prostaglandin G/H synthase 1 from ovine | B | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (1995) 38: 3895-3901 [PMID:7562922] |
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
GtoPdb | - | - | 3.66 | pIC50 | 218000 | nM | IC50 | J Med Chem (1995) 38: 3895-901 [PMID:7562922] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 2 mins followed by substrate addition in presence of TMPD by spectrophotometric analysis relative to control | B | 4.05 | pIC50 | 89125.09 | nM | IC50 | Bioorg Med Chem (2017) 25: 316-326 [PMID:27842798] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
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 Ochratoxin A uptake in OAT1-expressing S2 cells | F | 4.7 | pKi | 19800 | nM | Ki | Life Sci (2001) 69: 2123-2135 [PMID:11669456] |
ChEMBL | TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells | F | 4.69 | pIC50 | 20500 | 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 | 4.28 | pKi | 52000 | nM | Ki | Mol Pharmacol (1999) 55: 847-854 [PMID:10220563] |
Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Ochratoxin A uptake in OAT3-expressing S2 cells | F | 5.31 | pKi | 4880 | nM | Ki | Life Sci (2001) 69: 2123-2135 [PMID:11669456] |
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]