zileuton [Ligand Id: 5297] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL93 (ABBOTT-64077, A-64077, Zileuton, Zyflo, Zyflo cr)
  • 5-lipoxygenase activating protein in Human [ChEMBL: CHEMBL4550] [UniProtKB: P20292]
  • This target only has 0 pki data point
  • 0
1 CHEMBL93_lig_chart_1 5-lipoxygenase activating protein Human
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  • 12S-LOX/Arachidonate 12-lipoxygenase in Human [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054]
  • This target only has 0 pki data point
  • 0
2 CHEMBL93_lig_chart_2 Arachidonate 12-lipoxygenase Human
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  • 15-LOX-1/Arachidonate 15-lipoxygenase in Human [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
  • This target only has 0 pki data point
  • 0
3 CHEMBL93_lig_chart_3 Arachidonate 15-lipoxygenase Human
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  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
  • 5-LOX/Arachidonate 5-lipoxygenase in Mouse [ChEMBL: CHEMBL5211] [GtoPdb: 1385] [UniProtKB: P48999]
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
  • This target only has 0 pki data point
  • 0
4 CHEMBL93_lig_chart_4 Arachidonate 5-lipoxygenase HumanMouseRat
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  • COX-1 /Cyclooxygenase-1 in Human [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
  • This target only has 0 pki data point
  • 0
5 CHEMBL93_lig_chart_5 Cyclooxygenase-1 Human
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  • COX-2 /Cyclooxygenase-2 in Human [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
  • This target only has 0 pki data point
  • 0
6 CHEMBL93_lig_chart_6 Cyclooxygenase-2 Human
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
  • This target only has 0 pki data point
  • 0
7 CHEMBL93_lig_chart_7 Epoxide hydratase Human
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  • Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
  • This target only has 0 pki data point
  • 0
8 CHEMBL93_lig_chart_8 Leukotriene A4 hydrolase Human
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  • BLT1 receptor/Leukotriene B4 receptor 1 in Human [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
  • This target only has 0 pki data point
  • 0
9 CHEMBL93_lig_chart_9 Leukotriene B4 receptor 1 Human
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  • mPGES1/Prostaglandin E synthase in Human [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
  • This target only has 0 pki data point
  • 0
10 CHEMBL93_lig_chart_10 Prostaglandin E synthase Human
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  • CYP5A1/Thromboxane-A synthase in Rat [ChEMBL: CHEMBL4028] [GtoPdb: 1353] [UniProtKB: P49430]
  • This target only has 0 pki data point
  • 0
11 CHEMBL93_lig_chart_11 Thromboxane-A synthase Rat
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  • Tumor necrosis factor ligand superfamily member 11 in Mouse [ChEMBL: CHEMBL3596084] [UniProtKB: O35235]
  • This target only has 0 pki data point
  • 0
12 CHEMBL93_lig_chart_12 Tumor necrosis factor ligand superfamily member 11 Mouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-lipoxygenase activating protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4550] [UniProtKB: P20292]
ChEMBL Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionophore A23187-induced LTB4 production preincubated for 5 hrs by ELISA B 5.38 pIC50 4200 nM IC50 J. Med. Chem. (2011) 54: 8013-8029 [PMID:22059882]
ChEMBL Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionophore A23187-induced LTB4 production preincubated for 15 mins by ELISA B 5.66 pIC50 2200 nM IC50 J. Med. Chem. (2011) 54: 8013-8029 [PMID:22059882]
ChEMBL Inhibition of FLAP in Ca+2 ionophore A23187 stimulated human neutrophils assessed as 5-LO product formation preincubated for 15 mins measured after 10 mins by RP-HPLC analysis B 6.24 pIC50 580 nM IC50 Eur. J. Med. Chem. (2016) 113: 1-10 [PMID:26922224]
12S-LOX/Arachidonate 12-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3687] [GtoPdb: 1387] [UniProtKB: P18054]
ChEMBL Inhibitory concentration against human platelet 12-lipoxygenase F 4.26 pIC50 55000 nM IC50 J. Med. Chem. (1993) 36: 3580-3594 [PMID:8246226]
15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050]
ChEMBL Inhibition of 15-LOX in human primary polymorphonuclear leukocytes B 6.4 pIC50 400 nM IC50 Bioorg Med Chem Lett (2017) 27: 1649-1653 [PMID:28318946]
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of 5-LO in fMLP-stimulated human neutrophils by HPLC analysis B 4 pIC50 100000 nM IC50 Bioorg Med Chem (2017) 25: 4533-4552 [PMID:28720329]
ChEMBL Inhibition of 5-LO in LPS-stimulated human neutrophils by HPLC analysis B 4 pIC50 100000 nM IC50 Bioorg Med Chem (2017) 25: 4533-4552 [PMID:28720329]
ChEMBL Inhibition of human recombinant 5-LOX expressed in insect cells assessed as decrease in production of 5-HPETE and 5-HETE using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins in dark by ferric ion oxidation-xylenol orange method B 4.62 pIC50 23900 nM IC50 J Nat Prod (2019) 82: 3311-3320 [PMID:31774676]
ChEMBL Inhibition of human recombinant 5-LOX expressed in insect cells assessed as decrease in production of 5-HPETE and 5-HETE using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins in dark by ferric ion oxidation-xylenol orange method B 4.62 pIC50 23900 nM IC50 J Nat Prod (2019) 82: 3311-3320 [PMID:31774676]
ChEMBL Inhibition of 5-lipoxygenase in human neutrophils assessed as inhibition of LTB4 production B 5.2 pIC50 6300 nM IC50 J. Nat. Prod. (2011) 74: 1779-1786 [PMID:21800856]
ChEMBL Inhibition of 5-LOX (unknown origin) B 5.28 pIC50 5300 nM IC50 Eur J Med Chem (2019) 180: 486-508 [PMID:31330449]
ChEMBL Inhibitory concentration against human platelet 5-lipoxygenase in human whole blood F 5.29 pIC50 5120 nM IC50 J. Med. Chem. (1993) 36: 3580-3594 [PMID:8246226]
ChEMBL Inhibition of 5LOX-mediated LTB4 formation in stimulated human polymorphonuclear leukocytes B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. (2009) 17: 4459-4465 [PMID:19481465]
ChEMBL Inhibition of 5-LOX-mediated LTB4 production in stimulated human neutrophile granulocytes after 10 mins by EIA B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2809-2815 [PMID:20236826]
ChEMBL Inhibition of oxidation of arachidonic acid by human 5-Lipoxygenase using spectrophotometric assay F 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1997) 40: 2866-2875 [PMID:9288168]
ChEMBL Inhibition of 5-LOX in human whole blood assessed as inhibition of A23187-induced LTB4 production preincubated for 15 mins followed by A23187 induction measured after 30 mins by ELISA B 5.43 pIC50 3700 nM IC50 Bioorg. Med. Chem. (2014) 22: 2396-2402 [PMID:24685113]
ChEMBL Inhibition of 5LOX (unknown origin) using arachidonic acid as substrate after 5 mins by spectrophotometric analysis B 5.43 pIC50 3700 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1433-1437 [PMID:23337599]
ChEMBL Potency to inhibit oxidation of arachidonic acid by recombinant human 5-lipoxygenase B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1996) 39: 3951-3970 [PMID:8831761]
ChEMBL In vitro potency against human 5-Lipoxygenase B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1994) 37: 512-518 [PMID:8120869]
ChEMBL Tested for activity against 5-lipoxygenase B 5.46 pIC50 3500 nM IC50 J. Med. Chem. (1994) 37: 1153-1164 [PMID:8164257]
ChEMBL The compound was tested in vitro for inhibition against 5-lipoxygenase in intact human neutrophils B 5.48 pIC50 3300 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 2565-2570
ChEMBL Inhibition of human 5-LOX in A23187-induced human whole blood assessed as reduction in LTB4 production pre-incubated for 20 mins before A23187 addition by enzyme immunoassay B 5.48 pIC50 3300 nM IC50 J. Med. Chem. (2012) 55: 2597-2605 [PMID:22380511]
ChEMBL Inhibition of 5-LO in human neutrophils assessed as product formation by cell-intact assay relative to control in presence of 20 uM A23187/AA ionophore B 5.52 pIC50 3000 nM IC50 J. Med. Chem. (2014) 57: 3715-3723 [PMID:24697244]
ChEMBL The compound was evaluated for its inhibitory activity against 5-lipoxygenase using granulocytes-type cells B 5.54 pIC50 2900 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 779-782 [PMID:11859001]
ChEMBL In vitro inhibition of leukotriene B4 synthesis in human whole blood by inhibiting 5-lipoxygenase B 5.59 pIC50 2600 nM IC50 J. Med. Chem. (1992) 35: 2600-2609 [PMID:1321908]
ChEMBL Inhibition of 5-LOX in A23187-stimulated human blood PMNL assessed as reduction in lipoxygenase products formation in presence of arachidonic acid pre-incubated for 15 mins followed by stimulation with A23187 for 10 mins by RP-HPLC based cell based assay B 5.6 pIC50 2500 nM IC50 Eur. J. Med. Chem. (2015) 94: 132-139 [PMID:25765759]
ChEMBL Inhibition of 5-LO in human PMNL cells assessed as reduction in leukotriene formation preincubated for 5 mins followed by thapsigargin stimulation measured after 15 mins by RP-HPLC analysis B 5.64 pIC50 2310 nM IC50 Eur J Med Chem (2019) 179: 347-357 [PMID:31260889]
ChEMBL Inhibition of 5-LO in human PMNL cells assessed as reduction in leukotriene formation preincubated for 5 mins followed by thapsigargin stimulation measured after 15 mins by RP-HPLC analysis B 5.64 pIC50 2310 nM IC50 Eur J Med Chem (2019) 179: 347-357 [PMID:31260889]
ChEMBL In vitro inhibitory activity against 5-lipoxygenase by reduction of LTB4 formed in guinea pig polymorphonuclear leukocytes (PMNs). B 5.66 pIC50 2200 nM IC50 J. Med. Chem. (1993) 36: 3580-3594 [PMID:8246226]
ChEMBL In vitro 5-lipoxygenase inhibitory activity against A-23187-stimulated conversion of [14C]AA to LTB4 in guinea pig peritoneal polymorphonuclear leukocytes B 5.66 pIC50 2200 nM IC50 J. Med. Chem. (1995) 38: 68-75 [PMID:7837242]
ChEMBL In vitro 5-lipoxygenase inhibition in guinea pig PMNs was determined based on LTB4 production B 5.66 pIC50 2200 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 549-552
ChEMBL Inhibitory activity against partially-purified Guinea pig PMN 5-lipoxygenase B 5.7 pIC50 2000 nM IC50 J. Med. Chem. (1995) 38: 669-685 [PMID:7861415]
ChEMBL In vitro inhibitory activity against 5-lipoxygenase by reduction of 5-hydroxyeicosatetraenoic acid (5-HETE) formed in guinea pig polymorphonuclear leukocytes (PMNs). B 5.74 pIC50 1800 nM IC50 J. Med. Chem. (1993) 36: 3580-3594 [PMID:8246226]
ChEMBL In vitro 5-lipoxygenase inhibition in guinea pig PMNs was determined based on 5-hydroxyeicosapentaenoic acid (5-HETE) production B 5.74 pIC50 1800 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 549-552
ChEMBL In vitro 5-lipoxygenase inhibitory activity against A-23187-stimulated conversion of [14C]-AA to 5-HETE in guinea pig peritoneal polymorphonuclear leukocytes B 5.74 pIC50 1800 nM IC50 J. Med. Chem. (1995) 38: 68-75 [PMID:7837242]
ChEMBL Inhibition of 5-LO in human neutrophils assessed as product formation by cell-intact assay relative to control in presence of 2.5 uM A23187 ionophore B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (2014) 57: 3715-3723 [PMID:24697244]
ChEMBL Inhibition of 5-LO in human peripheral blood neutrophils using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition measured after 10 mins in presence of Ca2+ ionophore A23187 by RP-HPLC analysis B 5.77 pIC50 1700 nM IC50 J Nat Prod (2017) 80: 699-706 [PMID:28240894]
GtoPdb Inhibition of purified recombinant human 5-LOX in a cell-free assay. - 5.82 pIC50 1500 nM IC50 Eur J Med Chem (2018) 158: 34-50 [PMID:30199704]
ChEMBL Inhibition of recombinant human 5-LOX expressed in Escherichia coli BL21 using arachidonic acid as substrate by UV-vis spectrophotometric method B 5.82 pIC50 1500 nM IC50 Eur J Med Chem (2018) 158: 34-50 [PMID:30199704]
ChEMBL Inhibition of recombinant human 5-LOX expressed in Escherichia coli using arachidonic acid as substrate by UV-vis spectrophotometric method B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem (2019) 27: 604-619 [PMID:30638966]
ChEMBL Inhibition of recombinant human 5-LOX expressed in Escherichia coli using arachidonic acid as substrate by UV-vis spectrophotometric method B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem (2019) 27: 604-619 [PMID:30638966]
ChEMBL Inhibition of human 5-LOX expressed in Escherichia coli Bl21 (DE3) assessed as reduction in LTB4 and 5-H(P)ETE) formation pre-incubated for 10 mins before arachidonic acid substrate addition by RP-HPLC method B 5.89 pIC50 1300 nM IC50 Eur. J. Med. Chem. (2015) 101: 573-583 [PMID:26197161]
ChEMBL Inhibition of human recombinant 5-LOX expressed in Escherichia coli BL2-DE3 incubated 10 mins before substrate addition by fluorescence spectrophotometry based cell free system assay B 5.95 pIC50 1110 nM IC50 J. Med. Chem. (2012) 55: 2597-2605 [PMID:22380511]
ChEMBL Inhibition of human 5-LOX using arachidonic acid as substrate measured as H2DCFDA conversion to 2',7'-dichlorofluorescein preincubated for 10 mins by fluorescence spectrophotometric analysis B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2764-2767 [PMID:24794107]
ChEMBL Inhibition of 5-LO in human PMNL using arachidonic acid as substrate preincubated for 15 mins B 5.96 pIC50 1100 nM IC50 Eur. J. Med. Chem. (2013) 67: 269-279 [PMID:23871907]
ChEMBL Inhibition of human 5-LOX using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition by H2DCFDA staining-based fluorometric analysis B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. (2014) 22: 2396-2402 [PMID:24685113]
ChEMBL Inhibition of 5-LO (unknown origin) by cell based assay B 5.96 pIC50 1100 nM IC50 Eur. J. Med. Chem. (2013) 67: 269-279 [PMID:23871907]
ChEMBL Inhibition of human recombinant 5-LOX expressed in Escherichia coli BL21 assessed as conversion of arachidonic acid to 5-HPETE using arachidonic acid as substrate in presence of ATP by UV-vis spectrophotometry analysis B 5.98 pIC50 1050 nM IC50 ACS Med Chem Lett (2019) 10: 1415-1422 [PMID:31620227]
ChEMBL Inhibition of human recombinant 5-lipoxygenase using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 10 mins by HPLC analysis B 6 pIC50 1000 nM IC50 J. Nat. Prod. (2014) 77: 441-445 [PMID:24568174]
ChEMBL Inhibition of human recombinant 5-LOX expressed in Escherichia coli BL21 assessed as decrease in 5-HPETE production preincubated with enzyme followed by arachidonic acid substrate addition by UV-vis spectrophotometry B 6 pIC50 1000 nM IC50 Eur J Med Chem (2016) 124: 428-434 [PMID:27597418]
ChEMBL Inhibition of recombinant human 5-LO expressed in Escherichia coli BL21 assessed as 5-LO product formation preincubated for 15 mins followed by addition of arachidonic acid as substrate measured after 10 mins by RP-HPLC analysis B 6.04 pIC50 910 nM IC50 Eur. J. Med. Chem. (2016) 113: 1-10 [PMID:26922224]
ChEMBL Inhibition of 5-lipoxygenase in A23187-stimulated human polymorphonuclear leukocytes using arachidonic acid as substrate incubated 15 mins prior to substrate addition measured after 10 mins by HPLC analysis B 6.05 pIC50 900 nM IC50 J. Med. Chem. (2013) 56: 9031-9044 [PMID:24171493]
ChEMBL Inhibition of 5-lipoxygenase in A-23817-challenged human neutrophils assessed as 5LO product formation by intact cell based assay in presence of exogenous arachidonic acid B 6.05 pIC50 900 nM IC50 J. Med. Chem. (2009) 52: 3474-3483 [PMID:19492852]
ChEMBL Inhibition of 5-LOX in A23187-stimulated human blood PMNL assessed as reduction in lipoxygenase products formation pre-incubated for 15 mins followed by stimulation with A23187 for 10 mins by RP-HPLC based cell based assay B 6.05 pIC50 900 nM IC50 Eur. J. Med. Chem. (2015) 94: 132-139 [PMID:25765759]
ChEMBL Inhibitory concentration against 5-lipoxygenase in human whole blood F 6.06 pIC50 873 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1083-1085 [PMID:15686917]
ChEMBL Inhibition of 5-lipoxygenase activity in human whole blood assay B 6.06 pIC50 873 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 5591-5594 [PMID:15482930]
ChEMBL In vitro inhibitory activity against 5-lipoxygenase in a human whole blood assay B 6.06 pIC50 873 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 2265-2268 [PMID:15081022]
ChEMBL Inhibitory concentration against human platelet 5-lipoxygenase in dog whole blood F 6.08 pIC50 840 nM IC50 J. Med. Chem. (1993) 36: 3580-3594 [PMID:8246226]
ChEMBL Inhibition of human recombinant 5-LO expressed in Escherichia coli MV1190 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by RP-HPLC analysis B 6.1 pIC50 800 nM IC50 J Nat Prod (2017) 80: 699-706 [PMID:28240894]
ChEMBL Inhibition of human recombinant 5-lipoxygenase expressed in Escherichia coli MV1190 pre-incubated for 10 mins before arachidonic acid substrate addition and measured after 10 mins by RP-HPLC method B 6.1 pIC50 800 nM IC50 J Nat Prod (2017) 80: 731-734 [PMID:28165233]
ChEMBL Inhibition of 5-lipoxygenase in human whole blood assessed as inhibition of 5-hydroxyeicosatetraenoic acid production by HPLC method B 6.1 pIC50 800 nM IC50 Bioorg. Med. Chem. (2010) 18: 3910-3924 [PMID:20451397]
ChEMBL Inhibition of 5-Lipoxygenase in arachidonic acid-stimulated human neutrophils after 15 mins by HPLC analysis in presence of A23187 B 6.1 pIC50 800 nM IC50 Eur. J. Med. Chem. (2011) 46: 5021-5033 [PMID:21868137]
ChEMBL Inhibition of human recombinant 5-lipoxygenase expressed in Escherichia coli assessed as 5LO product formation by cell free assay B 6.1 pIC50 800 nM IC50 J. Med. Chem. (2009) 52: 3474-3483 [PMID:19492852]
ChEMBL Inhibitory activity against 5-lipoxygenase in Human whole blood (HWBL) stimulated with calcium ionophore (A23187) and LTB4 measured by enzyme immunoassay F 6.12 pIC50 760 nM IC50 J. Med. Chem. (1997) 40: 819-824 [PMID:9057869]
ChEMBL 5-lipoxygenase Inhibitory activity was measured by enzyme immunoassay using human whole blood stimulated with calcium ionophore (A23187) and LTB4 (leukotriene B4) B 6.13 pIC50 740 nM IC50 J. Med. Chem. (1995) 38: 4768-4775 [PMID:7490726]
ChEMBL Inhibition of 5-lipoxygenase (5-LO) measured as LTB4 production in human whole blood stimulated with calcium ionophore (A23187). F 6.13 pIC50 740 nM IC50 J. Med. Chem. (1997) 40: 1955-1968 [PMID:9207936]
ChEMBL Inhibition of 5-lipoxygenase in human whole blood B 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. (2010) 18: 3910-3924 [PMID:20451397]
ChEMBL Inhibition of 5-lipoxygenase in human whole blood assessed as inhibition of LTB4 production by HPLC method B 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. (2010) 18: 3910-3924 [PMID:20451397]
ChEMBL Inhibition of 5-LO in human polymorphonuclear leukocytes assessed as inhibition of LTB4 production from arachidonic acid preincubated for 15 mins by HPLC analysis B 6.15 pIC50 700 nM IC50 Eur. J. Med. Chem. (2014) 81: 492-498 [PMID:24871899]
ChEMBL Inhibition of human recombinant 5-LO expressed in Escherichia coli BL21 using arachidonic acid as substrate preincubated for 5 to 10 mins by HPLC analysis B 6.22 pIC50 600 nM IC50 Eur. J. Med. Chem. (2014) 81: 492-498 [PMID:24871899]
ChEMBL Inhibition of human recombinant 5-lipoxygenase expressed in Escherichia coli BL21 using arachidonic acid as substrate incubated 5 to 10 mins prior to substrate addition measured after 10 mins by HPLC analysis B 6.22 pIC50 600 nM IC50 J. Med. Chem. (2013) 56: 9031-9044 [PMID:24171493]
ChEMBL Inhibition of human recombinant 5-LO assessed as product formation by cell-free assay relative to control B 6.22 pIC50 600 nM IC50 J. Med. Chem. (2014) 57: 3715-3723 [PMID:24697244]
ChEMBL Inhibition of human 5-LOX using arachidonic acid as substrate measured after 10 mins by ELISA B 6.23 pIC50 590 nM IC50 Bioorg Med Chem (2019) 27: 604-619 [PMID:30638966]
ChEMBL Inhibition of human recombinant 5-LOX expressed in Escherichia coli BL21 incubated for 10 mins in presence of arachidonic acid by RP-HPLC based cell-free assay B 6.23 pIC50 590 nM IC50 Eur. J. Med. Chem. (2015) 94: 132-139 [PMID:25765759]
ChEMBL Inhibition of human 5-LOX using arachidonic acid as substrate measured after 10 mins by ELISA B 6.23 pIC50 590 nM IC50 Bioorg Med Chem (2019) 27: 604-619 [PMID:30638966]
ChEMBL Inhibition of 5-LO (unknown origin) B 6.25 pIC50 560 nM IC50 Eur. J. Med. Chem. (2013) 67: 269-279 [PMID:23871907]
ChEMBL Inhibition of human recombinant 5-LO expressed in Escherichia coli BL21 using arachidonic acid as substrate after 10 mins B 6.25 pIC50 560 nM IC50 Eur. J. Med. Chem. (2013) 67: 269-279 [PMID:23871907]
ChEMBL Inhibition of 5-LOX in human neutrophils assessed as reduction in LTB4 and 5-H(P)ETE) formation pre-incubated for 15 mins before A23187 and arachidonic acid substrate addition by RP-HPLC method B 6.27 pIC50 540 nM IC50 Eur. J. Med. Chem. (2015) 101: 573-583 [PMID:26197161]
ChEMBL Inhibitory concentration against human 5-lipoxygenase B 6.29 pIC50 518 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1083-1085 [PMID:15686917]
ChEMBL Inhibition of recombinant human 5-lipoxygenase expressed in Escherichia coli BL21 (DE3) cells using arachidonic acid as substrate preincubated for 10 mins followed by susbtrate addition and measured after 10 mins by reverse phase HPLC method B 6.3 pIC50 500 nM IC50 J Nat Prod (2019) 82: 2544-2549 [PMID:31465225]
ChEMBL Inhibition of 5-LOX in stimulated leukocytes B 6.3 pIC50 500 nM IC50 J. Med. Chem. (2012) 55: 2597-2605 [PMID:22380511]
ChEMBL Inhibition of recombinant human 5-lipoxygenase expressed in Escherichia coli BL21 (DE3) cells using arachidonic acid as substrate preincubated for 10 mins followed by susbtrate addition and measured after 10 mins by reverse phase HPLC method B 6.3 pIC50 500 nM IC50 J Nat Prod (2019) 82: 2544-2549 [PMID:31465225]
ChEMBL Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. (2012) 20: 3575-3583 [PMID:22551629]
ChEMBL Inhibition of 5-lipoxygenase in human polynuclear leukocytes assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. (2012) 20: 3575-3583 [PMID:22551629]
ChEMBL Inhibition of 5-LOX B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. (2012) 20: 5027-5032 [PMID:22789707]
ChEMBL Inhibition of 5-lipoxygenase B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1969-1975 [PMID:22326163]
ChEMBL Inhibition of 5-LOX (unknown origin)-mediated leukotriene (LT)B4 biosynthesis B 6.39 pIC50 410 nM IC50 J. Med. Chem. (2013) 56: 7997-8007 [PMID:24074025]
ChEMBL Inhibition of human recombinant 5-LO expressed in Escherichia coli by cell-free assay B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2008) 51: 8068-8076 [PMID:19053751]
GtoPdb Inhibition of leukotriene B4 biosynthesis by human polymorphonuclear leukocytes. - 6.4 pIC50 400 nM IC50 J Pharmacol Exp Ther (1991) 256: 929-37 [PMID:1848634]
ChEMBL Inhibition of human recombinant 5-LOX assessed as reduction in leukotriene B4 production pre-incubated for 10 mins before arachidonic acid addition and measured after 10 mins by ELISA B 6.46 pIC50 350 nM IC50 J Nat Prod (2017) 80: 999-1006 [PMID:28322565]
ChEMBL Inhibition of calcium ionophore (A-23187)-stimulated LTB4 formation in human neutrophil assay F 6.49 pIC50 320 nM IC50 J. Med. Chem. (2000) 43: 690-705 [PMID:10691695]
GtoPdb Inhibition of recombinant 5-LOX in vitro. - 6.52 pIC50 300 nM IC50 Bioorg Med Chem (2014) 22: 1642-8 [PMID:24508141]
ChEMBL Inhibition of 5-LOX (unknown origin) using arachidonic acid as substrate after 5 mins by EIA B 6.52 pIC50 300 nM IC50 Bioorg. Med. Chem. (2014) 22: 1642-1648 [PMID:24508141]
ChEMBL Inhibition of human 5-lipoxygenase using arachidonic acid as substrate pretreated for 10 mins followed by substrate and ATP addition and measured after 20 mins by H2DCFDA probe based fluorescence assay B 6.82 pIC50 150 nM IC50 Eur J Med Chem (2018) 156: 534-553 [PMID:30025348]
ChEMBL Inhibition of human recombinant 5-LOX assessed as reduction in leukotriene B4 synthesis using arachidonic acid substrate by ELISA B 7 pIC50 100 nM IC50 J Nat Prod (2019) 82: 1839-1848 [PMID:31268709]
ChEMBL In vitro inhibition of ionophore stimulated LTB4 release from human peripheral blood leukocytes. F 6.33 pEC50 470 nM EC50 J. Med. Chem. (1992) 35: 3180-3183 [PMID:1324317]
5-LOX/Arachidonate 5-lipoxygenase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5211] [GtoPdb: 1385] [UniProtKB: P48999]
ChEMBL Inhibition of 5-LO in mouse BMM cells assessed as formation of LTC4 after 30 mins by enzyme immunoassay B 6.72 pIC50 190 nM IC50 Bioorg. Med. Chem. (2015) 23: 7069-7078 [PMID:26432605]
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL Inhibitory activity against rat 5-lipoxygenase by using continuous oxygen consumption assay. B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (1996) 39: 5035-5046 [PMID:8978834]
ChEMBL Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (1996) 39: 3929-3937 [PMID:8831759]
ChEMBL Inhibition of 5-LOX in Sprague Dawley rat Leukocytes assessed as reduction in calcium ionophore A23187-induced LTB4 production preincubated for 30 mins followed by calcium ionophore A23187 addition measured after 30 mins by ELISA B 5.87 pIC50 1350 nM IC50 Bioorg Med Chem Lett (2017) 27: 3653-3660 [PMID:28720504]
ChEMBL In vitro inhibition of 5-lipoxygenase in RBL-2H3 (Rat basophilic leukemia) cells. F 5.9 pIC50 1250 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 643-648
ChEMBL Inhibition of Sprague-Dawley rat 5-LOX assessed as calcium ionophore A23187-stimulated LTB4 production preincubated for 30 mins followed by calcium ionophore A23187 addition and measured after 30 mins by ELISA B 6.08 pIC50 830 nM IC50 Eur J Med Chem (2019) 169: 168-184 [PMID:30877972]
ChEMBL Inhibition of 5-LOX in rat peritoneal leukocytes B 6.08 pIC50 830 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 2414-2420 [PMID:17336065]
ChEMBL Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells B 6.09 pIC50 804 nM IC50 J. Med. Chem. (1998) 41: 1970-1979 [PMID:9599246]
ChEMBL Inhibition of 5-LOX in Sprague-Dawley rat leukocytes assessed as A23187 stimulated LTB4 production pretreated for 30 mins followed by addition of A23187 for 30 mins by EIA B 6.1 pIC50 800 nM IC50 Eur. J. Med. Chem. (2016) 108: 89-103 [PMID:26638042]
ChEMBL In vitro inhibition of 5-lipoxygenase (5-lo) from the 20000 g supernatant of RBI-1 cells B 6.22 pIC50 600 nM IC50 J. Med. Chem. (1991) 34: 2158-2165 [PMID:2066989]
ChEMBL Inhibitory activity against 5-lipoxygenase catalysis (5-LO) in sonicated rat basophilic leukemia cell lysate F 6.3 pIC50 500 nM IC50 J. Med. Chem. (1997) 40: 819-824 [PMID:9057869]
ChEMBL Inhibition of 5-lipoxygenase on rat basophil leukemia cell line lysate (RBL-1 2H3 subline) by measuring 5-HETE production F 6.3 pIC50 500 nM IC50 J. Med. Chem. (1997) 40: 1955-1968 [PMID:9207936]
ChEMBL The compound was tested for inhibitory activity against 5-Lipoxygenase in rat RBL-1 B 6.3 pIC50 500 nM IC50 J. Med. Chem. (1992) 35: 2501-2524 [PMID:1635053]
ChEMBL Inhibitory activity against 5-lipoxygenase obtained from rat basophilic leukemia cells B 6.3 pIC50 500 nM IC50 J. Med. Chem. (1998) 41: 420-427 [PMID:9484493]
ChEMBL In vitro inhibition of 5-lipoxygenase (5-HETE) derived from the 9000xg supernatant of RBL broken cell assay B 6.43 pIC50 370 nM IC50 J. Med. Chem. (1994) 37: 3663-3667 [PMID:7932593]
ChEMBL The compound was tested for its inhibitory activity against arachidonic acid in rat 5-lipoxygenase B 6.49 pIC50 320 nM IC50 J. Med. Chem. (1992) 35: 1299-1318 [PMID:1313879]
ChEMBL Compound was tested for its inhibitory activity against 5-lipoxygenase in rat. B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1699-1702
ChEMBL Inhibition of rat 5-LOX expressed in Sf21 insect cells preincubated for 4 mins followed by AA substrate addition and measured after 4 mins by FOX assay B 6.74 pIC50 180 nM IC50 MedChemComm (2018) 9: 212-225
ChEMBL Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells B 6.85 pIC50 140 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1079-1084
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL The compound was evaluated for its inhibitory activity against Prostaglandin G/H synthase 1 using monocytes-like cells B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 779-782 [PMID:11859001]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL The compound was evaluated for its inhibitory activity against Prostaglandin G/H synthase 2 using osteosarcomes cells B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2002) 12: 779-782 [PMID:11859001]
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
ChEMBL Inhibition of human recombinant soluble epoxide hydrolase expressed in Escherichia coli using 3-phenyl-cyano(6-methoxy-2-naphthalenyl)methylester-2-oxiraneacetic acid as substrate after 30 mins by fluorescence-based assay B 6.23 pIC50 591 nM IC50 J. Med. Chem. (2013) 56: 1777-1781 [PMID:23356879]
Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960]
ChEMBL Inhibitory activity was determined against Leukotriene A4 hydrolase B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2000) 43: 721-735 [PMID:10691697]
ChEMBL Inhibitory activity was determined for LTB4 production in human whole blood. F 6.07 pIC50 850 nM IC50 J. Med. Chem. (2000) 43: 721-735 [PMID:10691697]
BLT1 receptor/Leukotriene B4 receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
ChEMBL In vitro activities of Leukotriene B4 receptor (LTB4) in human neutrophils B 6.38 pIC50 420 nM IC50 J. Med. Chem. (1996) 39: 3148-3157 [PMID:8759636]
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Inhibition of mPGES-1 isolated from microsomes of interleukin-1 beta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis B 6.22 pIC50 600 nM IC50 Eur J Med Chem (2018) 156: 815-830 [PMID:30053720]
CYP5A1/Thromboxane-A synthase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4028] [GtoPdb: 1353] [UniProtKB: P49430]
ChEMBL