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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]