ChEMBL ligand: CHEMBL29097 (MK-886)
5-lipoxygenase activating protein in Human [ChEMBL: CHEMBL4550] [UniProtKB: P20292] There should be some charts here, you may need to enable JavaScript!
5-LOX/5-lipoxygenase/FLAP in Human [ChEMBL: CHEMBL2111402] [GtoPdb: 1385] [UniProtKB: P09917, P20292] There should be some charts here, you may need to enable JavaScript!
5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527] There should be some charts here, you may need to enable JavaScript!
Cyclooxygenase-1 in Sheep [ChEMBL: CHEMBL2949] [UniProtKB: P05979] There should be some charts here, you may need to enable JavaScript!
COX-2 /Cyclooxygenase-2 in Human [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] There should be some charts here, you may need to enable JavaScript!
Macrophage-expressed gene 1 protein in Human [ChEMBL: CHEMBL3414409] [UniProtKB: Q2M385] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
mPGES1/Prostaglandin E synthase in Human [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] There should be some charts here, you may need to enable JavaScript!
mPGES2/Prostaglandin E synthase 2 in Human [ChEMBL: CHEMBL4411] [GtoPdb: 1378] [UniProtKB: Q9H7Z7] There should be some charts here, you may need to enable JavaScript!
Peroxisome proliferator-activated receptor-α in Mouse [GtoPdb: 593] [UniProtKB: P23204] There should be some charts here, you may need to enable JavaScript!

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 15 mins by ELISA	B	5.85	pIC50	1400	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 5 hrs by ELISA	B	5.96	pIC50	1100	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 11 hrs by ELISA	B	6	pIC50	1000	nM	IC50	J Med Chem (2011) 54: 8013-8029 [PMID:22059882]
ChEMBL	Inhibition of FLAP in human leukocytes assessed as decrease in ionophore A23187-induced LT biosynthesis after 10 mins	B	6.99	pIC50	102	nM	IC50	Medchemcomm (2018) 9: 212-225 [PMID:30108915]
ChEMBL	Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 3 hr by ELISA in presence of 0.5% human serum albumin	B	7.57	pIC50	27	nM	IC50	J Med Chem (2011) 54: 8013-8029 [PMID:22059882]
ChEMBL	Binding affinity to FLAP	B	7.59	pIC50	26	nM	IC50	J Med Chem (2009) 52: 4968-4972 [PMID:19719242]
ChEMBL	Inhibition of FLAP	B	7.59	pIC50	26	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1604-1609 [PMID:20144869]
ChEMBL	Inhibition of FLAP	B	7.59	pIC50	26	nM	IC50	J Med Chem (2008) 51: 4059-4067 [PMID:18459759]
ChEMBL	Inhibition of FLAP (unknown origin)	B	7.59	pIC50	26	nM	IC50	Bioorg Med Chem Lett (2013) 23: 907-911 [PMID:23266122]
ChEMBL	Binding affinity of compound for 5-lipoxygenase activating protein protein by FLAP binding assay	B	7.64	pIC50	23	nM	IC50	J Med Chem (1996) 39: 2629-2654 [PMID:8709092]
ChEMBL	The compound was tested for the inhibition of binding of [125I]- L- 691,831 binding to 5-lipoxygenase activating protein (FLAP)	B	7.64	pIC50	23	nM	IC50	Bioorg Med Chem Lett (1992) 2: 1395-1398
ChEMBL	Inhibition of 5-lipoxygenase activating protein using human leukocyte membrane preparations	B	7.64	pIC50	23	nM	IC50	J Med Chem (1995) 38: 4538-4547 [PMID:7473582]
ChEMBL	Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 10 mins by ELISA in presence of 0.5% human serum albumin	B	7.72	pIC50	19	nM	IC50	J Med Chem (2011) 54: 8013-8029 [PMID:22059882]
ChEMBL	Inhibition of FLAP in A23187-stimulated human neutrophils assessed as 5-LO product formation preincubated for 15 mins measured after 10 mins	B	7.77	pIC50	17	nM	IC50	Bioorg Med Chem (2012) 20: 3728-3741 [PMID:22607880]
ChEMBL	Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 1 hr by ELISA in absence of human serum albumin	B	8.24	pIC50	5.7	nM	IC50	J Med Chem (2011) 54: 8013-8029 [PMID:22059882]
ChEMBL	Antagonist activity at FLAP in human PMNC assessed as inhibition of A23187-induced LTB4 biosynthesis pre-incubated for 2 mins followed by addition of A23187 measured after 5 mins by radioimmunoassay	B	8.6	pIC50	2.5	nM	IC50	J Med Chem (2016) 59: 5970-5986 [PMID:26791385]
ChEMBL	Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calcium ionophore A23187-induced LTB4 production after 5 mins by ELISA in absence of human serum albumin	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (2011) 54: 8013-8029 [PMID:22059882]
5-LOX/5-lipoxygenase/FLAP in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111402] [GtoPdb: 1385] [UniProtKB: P09917, P20292]
ChEMBL	Human whole blood was stimulated with calcium ionophore (A23187) and LTB 4 measured by enzyme immunoassay	F	6.47	pIC50	340	nM	IC50	Bioorg Med Chem Lett (1996) 6: 1547-1552
ChEMBL	Inhibition of calcium ionophore (A23187) stimulated LTB4 formation in human neutrophils	F	7.52	pIC50	30	nM	IC50	Bioorg Med Chem Lett (1996) 6: 1547-1552
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL	Inhibition of recombinant human 5-LO expressed in Escherichia coli BL21 incubated for 15 mins prior to prewarming for 30 secs followed by CaCl2+ and arachidonic acid addition and measured after 10 mins by RP-HPLC analysis	B	5.52	pIC50	3000	nM	IC50	Eur J Med Chem (2018) 150: 876-899 [PMID:29597170]
ChEMBL	Inhibition of 5-LO in PMNL cells	B	7.05	pIC50	90	nM	IC50	J Med Chem (2008) 51: 8068-8076 [PMID:19053751]
ChEMBL	Inhibition of 5-lipoxygenase in A23187-stimulated human PMNL assessed as enzyme product formation preincubated 15 mins by RP-HPLC analysis in presence of exogenous arachidonic acid	B	7.05	pIC50	90	nM	IC50	Bioorg Med Chem (2011) 19: 3394-3401 [PMID:21570310]
ChEMBL	Inhibition of 5-lipoxygenase-mediated 5(S)-H(p)ETE formation in fMLP-stimulated human PMNL incubated 10 mins prior to fMLP challenge	B	7.05	pIC50	90	nM	IC50	J Med Chem (2011) 54: 4490-4507 [PMID:21591611]
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	7.05	pIC50	90	nM	IC50	J Med Chem (2013) 56: 9031-9044 [PMID:24171493]
ChEMBL	The compound was tested for inhibitory activity against LT synthesis in human polymorphonuclear leukocytes[PMNS]	B	7.22	pIC50	60	nM	IC50	J Med Chem (1992) 35: 2501-2524 [PMID:1635053]
ChEMBL	Inhibition of Human 5-lipoxygenase	B	8	pIC50	>10	nM	IC50	J Med Chem (1995) 38: 4538-4547 [PMID:7473582]
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
ChEMBL	The compound was tested for inhibitory activity against 5-lipoxygenase translocation inhibitor in rat RBL-2H3 cells	F	8.3	pIC50	5	nM	IC50	J Med Chem (1992) 35: 2501-2524 [PMID:1635053]
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979]
ChEMBL	Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 5 mins by HPLC analysis	B	5.1	pIC50	8000	nM	IC50	Eur J Med Chem (2018) 153: 2-28 [PMID:29329790]
ChEMBL	Inhibition of ovine COX-1 assessed as 12-HHT formation preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 5 mins by HPLC analysis	B	5.1	pIC50	8000	nM	IC50	J Med Chem (2016) 59: 5970-5986 [PMID:26791385]
ChEMBL	Inhibition of ovine COX1	B	8	pIC50	>10	nM	IC50	J Med Chem (2008) 51: 8068-8076 [PMID:19053751]
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL	Inhibition of human recombinant COX2 in cell-free system by enzyme immunoassay	B	4.24	pIC50	58000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5418-5422 [PMID:25453800]
ChEMBL	Inhibition of human recombinant COX2	B	8	pIC50	>10	nM	IC50	J Med Chem (2008) 51: 8068-8076 [PMID:19053751]
Macrophage-expressed gene 1 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3414409] [UniProtKB: Q2M385]
ChEMBL	Inhibition of mPGES1 in IL-1beta stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 synthase activity after 15 mins using PGH2 substrate by RP-HPLC method	B	5.66	pIC50	2200	nM	IC50	Eur J Med Chem (2015) 94: 132-139 [PMID:25765759]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum D10 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 Dd2 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 HB3 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 3D7 after 72 hrs by SYBR green assay	F	5.2	pIC50	6309.57	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	5.2	pIC50	6309.57	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	5.2	pIC50	6309.57	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	5.5	pIC50	3162.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL	Inhibition of mPGES-1 activity in IL-1beta stimulated human A549 cells by cell-free assay	B	5.41	pIC50	3900	nM	IC50	Bioorg Med Chem Lett (2021) 41: 127992-127992 [PMID:33775835]
ChEMBL	Inhibition of mPGES1 (unknown origin) using PGH2 as substrate incubated for 30 mins prior to substrate addition by PGH2-coupled spectrophotometric analysis	B	5.41	pIC50	3900	nM	IC50	Bioorg Med Chem Lett (2013) 23: 75-80 [PMID:23218602]
ChEMBL	Inhibition of microsomal PGES1 using PGH2 as substrate by RP-HPLC method	B	5.49	pIC50	3200	nM	IC50	Bioorg Med Chem Lett (2012) 22: 7335-7339 [PMID:23147075]
ChEMBL	Inhibition of mPGES-1 expressed in LPS-stimulated human A549 cells mitochondrial fraction assessed as conversion of PGH2 to PGE2	B	5.52	pIC50	3000	nM	IC50	Bioorg Med Chem Lett (2011) 21: 1329-1333 [PMID:21310608]
ChEMBL	Inhibition of mPGES-1 in interleukin-1 beta-stimulated human A549 cells microsomal membranes assessed as reduction in conversion of PGH2 to PGE2 pre-incubated for 15 mins followed by PGH2 substrate addition measured after 1 min by RP-HPLC method	B	5.57	pIC50	2700	nM	IC50	J Nat Prod (2017) 80: 731-734 [PMID:28165233]
ChEMBL	Inhibition of human recombinant microsomal PGES-1 expressed in freestyle 293-f cells assessed as conversion of PGH2 to PGE2 after 15 mins by enzyme immunoassay	B	5.59	pIC50	2600	nM	IC50	Bioorg Med Chem (2011) 19: 6077-6086 [PMID:21920764]
ChEMBL	Inhibition of human A549 cell microsomal membrane-derived mPGES-1 assessed as reduction in conversion of PGH2 to PGE2 preincubated for 15 mins followed by PGH2 addition measured after 1 min by RP-HPLC analysis	B	5.6	pIC50	2500	nM	IC50	J Nat Prod (2017) 80: 699-706 [PMID:28240894]
ChEMBL	Inhibition of mPGES1	B	5.62	pIC50	2400	nM	IC50	J Med Chem (2008) 51: 8068-8076 [PMID:19053751]
ChEMBL	Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method	B	5.62	pIC50	2400	nM	IC50	Bioorg Med Chem (2015) 23: 4839-4845 [PMID:26088337]
ChEMBL	Inhibition of microsomal PGES1 isolated from IL-1beta-stimulated human A549 cells preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis	B	5.62	pIC50	2400	nM	IC50	J Nat Prod (2014) 77: 1445-1451 [PMID:24844534]
ChEMBL	Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis	B	5.62	pIC50	2400	nM	IC50	J Med Chem (2013) 56: 9031-9044 [PMID:24171493]
ChEMBL	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	B	5.62	pIC50	2400	nM	IC50	J Med Chem (2011) 54: 4490-4507 [PMID:21591611]
ChEMBL	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as reduction of PGE2 formation from PGH2 after 15 mins	B	5.62	pIC50	2400	nM	IC50	Bioorg Med Chem (2011) 19: 3394-3401 [PMID:21570310]
ChEMBL	Inhibition of mPGES-1 in human IL-1beta-stimulated A549 cell microsomes assessed as inhibition of PGE2 formation from PGH2 after 15 mins by RP-HPLC analysis	B	5.64	pIC50	2300	nM	IC50	J Med Chem (2012) 55: 8958-8962 [PMID:22992107]
ChEMBL	Inhibition of mPGES1 in IL1-beta treated human A549 cell microsomal membrane assessed as residual enzyme activity after 1 min by measuring PGE2 level using RP-HPLC method	B	5.68	pIC50	2110	nM	IC50	J Med Chem (2009) 52: 4968-4972 [PMID:19719242]
ChEMBL	Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay	B	5.68	pIC50	2100	nM	IC50	J Med Chem (2008) 51: 8068-8076 [PMID:19053751]
ChEMBL	Inhibition of PGES-1 in IL-1beta stimulated human A549 cell microsomes using PGH2 as substrate assessed as suppression of PGE2 formation preincubated for 15 mins followed by substrate addition by reversed phase-HPLC analysis	B	5.68	pIC50	2100	nM	IC50	Bioorg Med Chem (2016) 24: 820-826 [PMID:26777299]
ChEMBL	Inhibition of mPGES-1 activity in IL-1beta stimulated human A549 cells microsomes assessed as reduction in PGE2 production preincubated for 15 mins followed by PGH2 addition and measured after 1 mins by EIA	B	5.68	pIC50	2100	nM	IC50	Bioorg Med Chem Lett (2021) 41: 127992-127992 [PMID:33775835]
ChEMBL	Inhibition of mPGES1 in IL-1beta treated human A549 cell microsomal membrane assessed as inhibition of PGE2 formation incubated for 15 mins before addition of PGH2 by RP-HPLC method	B	5.68	pIC50	2100	nM	IC50	J Nat Prod (2011) 74: 1779-1786 [PMID:21800856]
ChEMBL	Inhibition of mPGES1 in human A549 cell microsomes	B	5.68	pIC50	2100	nM	IC50	Eur J Med Chem (2018) 153: 2-28 [PMID:29329790]
ChEMBL	Inhibition of mPGES1 in human A549 cell microsomal membrane using pGH2 as substrate pretreated for 15 mins followed by substrate addition and measured after 1 min by RP-HPLC method	B	5.68	pIC50	2100	nM	IC50	Eur J Med Chem (2018) 153: 2-28 [PMID:29329790]
ChEMBL	Inhibition of mPGES1 in IL1-beta induced human A549 cell microsomal membrane assessed as blockade of conversion of PGH2 to PGE2	B	5.7	pIC50	2000	nM	IC50	Bioorg Med Chem (2009) 17: 7924-7932 [PMID:19884011]
ChEMBL	Inhibition of PGES-1 in human A549 cell microsomes using PGH2 as substrate assessed as suppression of interleukin-1beta-stimulated PGE2 production incubated for 15 mins post interleukin-1beta challenge for 72 hrs by RP-HPLC analysis	B	5.7	pIC50	2000	nM	IC50	Bioorg Med Chem Lett (2016) 26: 94-99 [PMID:26602278]
ChEMBL	Inhibition of microsomal PGES1 (unknown origin)	B	5.8	pIC50	1600	nM	IC50	Medchemcomm (2015) 6: 2081-2123
ChEMBL	Inhibition of human mPGES1	B	5.8	pIC50	1600	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1604-1609 [PMID:20144869]
ChEMBL	Inhibition of mPGES-1	B	5.8	pIC50	1600	nM	IC50	Eur J Med Chem (2012) 48: 153-163 [PMID:22209272]
ChEMBL	Inhibition of human recombinant mPGES-1 using PGH2 as substrate incubated 20 mins prior to substrate addition measured after 30 secs by EIA	B	5.8	pIC50	1600	nM	IC50	Bioorg Med Chem Lett (2013) 23: 907-911 [PMID:23266122]
ChEMBL	Inhibition of microsomal PGES	B	5.8	pIC50	1600	nM	IC50	Bioorg Med Chem (2011) 19: 6077-6086 [PMID:21920764]
ChEMBL	Inhibition of human recombinant mPGES-1 in assessed as conversion of PGH2 into PGE2 at 20 degC after 5 mins by HPLC-UV analysis	B	5.89	pIC50	1300	nM	IC50	Eur J Med Chem (2012) 48: 153-163 [PMID:22209272]
ChEMBL	Inhibition of microsomal PGES1 in human whole blood	B	5.96	pIC50	1100	nM	IC50	Medchemcomm (2015) 6: 2081-2123
ChEMBL	Inhibition of microsomal PGES-1 (unknown origin)	B	8.52	pIC50	3	nM	IC50	J Med Chem (2013) 56: 3296-3309 [PMID:23527738]
mPGES2/Prostaglandin E synthase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4411] [GtoPdb: 1378] [UniProtKB: Q9H7Z7]
ChEMBL	Inhibitory concentration against human prostaglandin E2 synthase (mPGES-1)	B	5.8	pIC50	1600	nM	IC50	Bioorg Med Chem Lett (2005) 15: 3352-3355 [PMID:15953724]
Peroxisome proliferator-activated receptor-α in Mouse [GtoPdb: 593] [UniProtKB: P23204]
GtoPdb	-	-	6	pIC50	-	-	-	Biochem J (2001) 353: 253-8 [PMID:11139388]

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]