zileuton [Ligand Id: 5297] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL93 (A-64077, ABBOTT-64077, NSC-730712, NSC-759277, Zileuton, Zyflo, Zyflo cr) |
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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 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 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 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 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 | 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 | 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 | 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 | 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 | 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 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 thapsigargin stimulated human PMNL cells assessed as reduction in 5-LO product level preincubated for 5 mins followed by thapsigargin addition and measured after 15 mins by RP-HPLC analysis | B | 5.64 | pIC50 | 2310 | nM | IC50 | J Nat Prod (2022) 85: 225-236 [PMID:34995066] |
| 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 | 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 | 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 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 (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 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 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 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 recombinant human 5-LO expressed in Escherichia coli BL21(DE3) assessed as reduction in LTB4 and 5-H(P)ETE formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 10 mins by RP-HPLC method | B | 6.09 | pIC50 | 810 | nM | IC50 | Eur J Med Chem (2020) 202: 112518-112518 [PMID:32668380] |
| 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-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 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 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 | 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 | 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-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 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 human recombinant 5-LOX assessed as reduction in LTB4 level using 800 uM arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 10 mins by ELISA | B | 6.18 | pIC50 | 660 | nM | IC50 | Eur J Med Chem (2020) 204: 112620-112620 [PMID:32738413] |
| ChEMBL | Inhibition of recombinant human 5LOX expressed in baculovirus infected Sf insect cells using linoleic acid as substrate preincubated for 5 mins followed by substrate addition | B | 6.2 | pIC50 | 630 | nM | IC50 | Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050] |
| 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 5-Lipoxygenase (unknown origin) | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2020) 63: 12116-12127 [PMID:32940035] |
| 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 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 | Inhibition of 5-LO in human PMNL cells assessed as reduction in LTB4, 5-H(P)ETE, 12-HETE and 15-HETE products formation using arachidonic acid as substrate preincubated for 10 mins followed by addition of substrate and measured after 10 mins by RP-HPLC method | B | 6.28 | pIC50 | 521 | nM | IC50 | Eur J Med Chem (2020) 202: 112518-112518 [PMID:32668380] |
| 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 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 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1969-1975 [PMID:22326163] |
| 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 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 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem (2012) 20: 5027-5032 [PMID:22789707] |
| 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 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 5-Lipoxygenase using H2DCFDA as substrate preincubated for 5 mins and measured by Spectrophotometric assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2020) 190: 112090-112090 [PMID:32018096] |
| 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 [PMID:30108915] |
| 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 | Inhibitory concentration against human platelet thromboxane synthetase | F | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (1993) 36: 3580-3594 [PMID:8246226] |
| Tumor necrosis factor ligand superfamily member 11 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3596084] [UniProtKB: O35235] | ||||||||
| ChEMBL | Antiosteoclast activity in mouse BMM cells assessed as reduction of RANKL-induced osteoclasts differentiation by measuring TRAP positive multinucleated cells after 4 days by light microscopy | F | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2015) 23: 7069-7078 [PMID:26432605] |
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]
