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] |
| ChEMBL | Agonist activity at FXR (unknown origin) | B | 4.82 | pEC50 | 15000 | nM | EC50 | J Med Chem (2021) 64: 17545-17571 [PMID:34889100] |
| 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] |
| ChEMBL | Antagonist activity at human CysLT1 receptor | F | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (2021) 64: 16512-16529 [PMID:34767347] |
| 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] |
| ChEMBL | Antagonist activity at human CysLT2 receptor | F | 5.52 | pIC50 | >3000 | nM | IC50 | J Med Chem (2021) 64: 16512-16529 [PMID:34767347] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
