pranlukast [Ligand Id: 3634] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL21333 (Azlaire, CCN 00401, CCN-00401, ONO 1078, ONO-1078, Pranlukast, RS 411, RS-411, SB 205312, SB-205312)
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
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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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  • GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay B 4.82 pEC50 15000 nM EC50 J Med Chem (2019) 62: 6175-6189 [PMID:31188588]
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL TP_TRANSPORTER: inhibition of DNP-SG uptake in bile canalicular membrane vesicles from SD rat F 4.39 pKi 41100 nM Ki Drug Metabol Pharmacokin (2002) 17: 23-33 [PMID:15618649]
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 B 4.17 pIC50 68000 nM IC50 J Med Chem (2010) 53: 4259-4265 [PMID:20426472]
ChEMBL Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 B 5.15 pIC50 7000 nM IC50 J Med Chem (2010) 53: 4259-4265 [PMID:20426472]
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 - 8.8 pKi - - - Biochem Pharmacol (2002) 63: 1537-46 [PMID:11996896];
Br J Pharmacol (1998) 123: 590-8 [PMID:9504401]
ChEMBL Inhibition of cysteinyl leukotriene receptor 1 (unknown origin) expressed in HEK293 cell membranes after 45 mins by scintillation spectrometry B 8.36 pIC50 4.4 nM IC50 J Med Chem (2017) 60: 5235-5266 [PMID:28252961]
ChEMBL Antagonist activity at human CysLT1 B 8.37 pIC50 4.3 nM IC50 J Med Chem (2015) 58: 6093-6113 [PMID:26200813]
GtoPdb - - 8.37 pIC50 4.3 nM IC50 Nature (1999) 399: 789-93 [PMID:10391245];
Mol Pharmacol (1999) 56: 657-63 [PMID:10462554]
ChEMBL Antagonist activity at CysLT1 receptor in human dU937 cells assessed as inhibition of LTD4-induced increase of calcium level treated 30 mins before LTD4 challenge F 9.1 pIC50 0.8 nM IC50 Bioorg Med Chem (2010) 18: 5519-5527 [PMID:20621485]
GtoPdb - - 10 pIC50 0.1 nM IC50 Mol Pharmacol (1999) 56: 657-63 [PMID:10462554]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL In vitro binding of Cysteinyl leukotriene receptor 1 to guinea pig lung membranes B 9.1 pKi 0.8 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 9.1 pKi 0.8 nM Ki Bioorg Med Chem Lett (1998) 8: 3577-3582 [PMID:9934474]
ChEMBL Binding affinity towards Cysteinyl leukotriene D4 receptor (cysLT1) was measured by the displacement of [3H]LTD4 radioligand B 9 pIC50 1 nM IC50 J Med Chem (1998) 41: 1439-1445 [PMID:9554877]
ChEMBL Displacement of [3H]ICI from cysteinyl leukotriene receptor 1 in Hartley guinea pig lung membrane after 30 mins by liquid scintillation counting method B 10.36 pIC50 0.04 nM IC50 J Med Chem (2017) 60: 5235-5266 [PMID:28252961]
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
GtoPdb against [3H]LTD4 in COS-7 cells - 5.44 pIC50 3620 nM IC50 J Biol Chem (2000) 275: 30531-6 [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 5.44 pIC50 3620 nM IC50 J Med Chem (2015) 58: 6093-6113 [PMID:26200813]
GtoPdb against LTC4 Ca2+ mobilization assay in HUVEC - 7.1 pA2 - - - Prostaglandins Other Lipid Mediat (2015) 120: 115-25 [PMID:25839425]
GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
ChEMBL Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay B 5.39 pKi 4060 nM Ki ACS Med Chem Lett (2014) 5: 326-330 [PMID:24900835]

ChEMBL data shown on this page come from version 32:

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]