zafirlukast [Ligand Id: 3322] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL603 (Zafirlukast, Accolate, ICI-204219)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
  • Cysteinyl leukotriene receptor 1 in Guinea pig [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
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  • CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
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  • cPLA2-4A/Cytosolic phospholipase A2 in Human [ChEMBL: CHEMBL3816] [GtoPdb: 1424] [UniProtKB: P47712]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231]
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  • epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Inhibitory concentration against Adenosine A1 receptor B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 6.11 pKi 770 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) B 5.87 pIC50 1363 nM IC50 DrugMatrix in vitro pharmacology data
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb against [3H]LTD4 in human lung parenchyma - 8.9 pKi - - - Biochem. Pharmacol. (2002) 63: 1537-1546 [PMID:11996896];
Br. J. Pharmacol. (1998) 123: 590-8 [PMID:9504401]
ChEMBL DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) B 9.06 pKi 0.86 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.7 pIC50 20 nM IC50 Br. J. Pharmacol. (2010) 160: 399-409 [PMID:20423349]
ChEMBL Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay B 7.85 pIC50 14 nM IC50 ACS Med. Chem. Lett. (2016) 7: 335-339 [PMID:26985325]
ChEMBL Antagonist activity at human CysLT1 B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (2015) 58: 6093-6113 [PMID:26200813]
GtoPdb against [3H]LTD4 in COS-7 or HEK-293 cells - 8.74 pIC50 1.8 nM IC50 Nature (1999) 399: 789-793 [PMID:10391245];
Mol. Pharmacol. (1999) 56: 657-663 [PMID:10462554]
ChEMBL Inhibition of cysteinyl leukotriene receptor 1 (unknown origin) expressed in HEK293 cell membranes after 45 mins by scintillation spectrometry B 8.74 pIC50 1.8 nM IC50 J Med Chem (2017) 60: 5235-5266 [PMID:28252961]
ChEMBL DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) B 8.76 pIC50 1.73 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb - - 9.59 pIC50 0.26 nM IC50 Mol. Pharmacol. (1999) 56: 657-663 [PMID:10462554]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL Displacement of [3H]leukotriene D4 (LTD4) from receptor in guinea pig lung membranes B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
ChEMBL In vitro binding of cysLT1 receptor to guinea pig lung membranes. B 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2773-2778 [PMID:10509933]
ChEMBL Antagonism of Cysteinyl leukotriene receptor 1 from guinea pig lung membranes F 8.7 pKi 2 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 3577-3582 [PMID:9934474]
ChEMBL Inhibition constant for displacement of [3H]LTD4 on guinea pig lung parenchymal membranes B 9.47 pKi 0.34 nM Ki J. Med. Chem. (1994) 37: 1282-1297 [PMID:8176706]
ChEMBL Displacement of [3H]LTD4 from cysteinyl leukotriene receptor 1 in Hartley guinea pig parenchymal membrane after 30 mins by liquid scintillation counting method B 9.52 pKi 0.3 nM Ki J Med Chem (2017) 60: 5235-5266 [PMID:28252961]
ChEMBL Binding affinity towards Cysteinyl leukotriene D4 receptor (cysLT1) was measured by the displacement of [3H]LTD4 radioligand B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1998) 41: 1439-1445 [PMID:9554877]
ChEMBL Compound was evaluated for its ability to displace [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranes B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1991) 34: 1235-1242 [PMID:1849993]
ChEMBL Displacement of [3H]LTD4 on guinea pig lung parenchymal membranes B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1990) 33: 1781-1790 [PMID:2342072]
ChEMBL In vitro inhibition of [3H]LTD4 binding to guinea pig lung membrane B 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 965-970 [PMID:9871521]
ChEMBL Binding affinity against leukotriene D4 receptor in [3H]LTD4 binding assay B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2451-2456 [PMID:9873560]
ChEMBL Concentration required for inhibition of binding of [3H]LTD4 to guinea pig lung membranes B 9.36 pIC50 0.44 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 283-288
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
ChEMBL Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay B 4.24 pIC50 58000 nM IC50 ACS Med. Chem. Lett. (2016) 7: 335-339 [PMID:26985325]
GtoPdb - - 5.13 pIC50 7397 nM IC50 J. Biol. Chem. (2000) 275: 30531-30536 [PMID:10851239]
ChEMBL Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay B 5.13 pIC50 7397 nM IC50 J. Med. Chem. (2015) 58: 6093-6113 [PMID:26200813]
GtoPdb - - 5.15 pIC50 7000 nM IC50 Br. J. Pharmacol. (2010) 160: 399-409 [PMID:20423349]
GtoPdb - - 6.9 pA2 - - - Prostaglandins Other Lipid Mediat. (2015) 120: 115-25 [PMID:25839425]
CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712]
ChEMBL DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.65 pIC50 2257.5 nM IC50 DrugMatrix in vitro pharmacology data
cPLA2-4A/Cytosolic phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3816] [GtoPdb: 1424] [UniProtKB: P47712]
ChEMBL In vitro inhibition of cystolic phospholipase A2 alpha. B 4.07 pIC50 85000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 4501-4504 [PMID:14643356]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Inhibitory concentration against Dopamine receptor D2 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.24 pIC50 5751 nM IC50 DrugMatrix in vitro pharmacology data
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
ChEMBL Inhibition of Gamma-aminobutyric acid receptor B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Inhibitory concentration against H1 receptor B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein) B 5.36 pIC50 4376 nM IC50 DrugMatrix in vitro pharmacology data
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) B 6.27 pIC50 538 nM IC50 DrugMatrix in vitro pharmacology data
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) B 6.45 pIC50 353 nM IC50 DrugMatrix in vitro pharmacology data
Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
ChEMBL Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 5.89 pIC50 1300 nM IC50 J. Med. Chem. (2013) 56: 781-795 [PMID:23241029]
MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
ChEMBL Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay B 5.12 pIC50 7600 nM IC50 J. Med. Chem. (2013) 56: 781-795 [PMID:23241029]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Inhibitory concentration against Opioid receptor mu 1 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
Platelet activating factor receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
ChEMBL Displacement of [3H]ligand from platelet activating factor (PAF) receptor in rabbit platelets B 4.3 pKi >50000 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 1377-1382
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684]
ChEMBL Inhibition of microsomal PGES1 in ILbeta/TNFalpha-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by LC-MS/MS analysis B 4.74 pIC50 18100 nM IC50 MedChemComm (2015) 6: 2081-2123
Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
ChEMBL Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay B 5.01 pIC50 9700 nM IC50 J. Med. Chem. (2013) 56: 781-795 [PMID:23241029]
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 5.42 pIC50 3810 nM IC50 DrugMatrix in vitro pharmacology data
Peroxisome proliferator-activated receptor-γ in Human [GtoPdb: 595] [UniProtKB: P37231]
GtoPdb - - 5.61 pEC50 2440 nM EC50 J. Med. Chem. (2018) 61: 5758-5764 [PMID:29878767]
epoxide hydrolase 2 in Human [GtoPdb: 2970] [UniProtKB: P34913]
GtoPdb - - 5.7 pIC50 2000 nM IC50 J. Med. Chem. (2018) 61: 5758-5764 [PMID:29878767]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]