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) |
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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 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]
