LTC4 [Ligand Id: 3354] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL451509
  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
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  • CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
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  • GPR17 in Human [GtoPdb: 88] [UniProtKB: Q13304]
  • GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb - - 8.1 pKi - - - Mol Pharmacol (1998) 53: 750-8 [PMID:9547367]
GtoPdb - - 6.46 pIC50 346 nM IC50 Nature (1999) 399: 789-93 [PMID:10391245]
ChEMBL Agonist activity at human CysLT1 receptor F 7.37 pEC50 43 nM EC50 J Med Chem (2021) 64: 16512-16529 [PMID:34767347]
GtoPdb - - 7.68 pEC50 21 nM EC50 Nature (1999) 399: 789-93 [PMID:10391245]
GtoPdb - - 7.7 pEC50 20 nM EC50 Mol Pharmacol (1999) 56: 657-63 [PMID:10462554];
Biochem Biophys Res Commun (2000) 274: 316-22 [PMID:10913337];
Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
GtoPdb - - 8.48 pIC50 3.3 nM IC50 J Biol Chem (2000) 275: 30531-6 [PMID:10851239];
Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]
GtoPdb - - 7.24 pEC50 58 nM EC50 J Biol Chem (2000) 275: 30531-6 [PMID:10851239];
Mol Pharmacol (2011) 79: 270-8 [PMID:21078884]
GtoPdb - - 7.24 pEC50 57 nM EC50 FASEB J (2011) 25: 3519-28 [PMID:21753081]
GtoPdb - - 7.27 pEC50 54 nM EC50 Mol Pharmacol (2011) 79: 270-8 [PMID:21078884]
ChEMBL Agonist activity at human CysLT2 receptor F 8.05 pEC50 8.9 nM EC50 J Med Chem (2021) 64: 16512-16529 [PMID:34767347]
GtoPdb - - 8.64 pEC50 2.3 nM EC50 Biochem Biophys Res Commun (2000) 274: 316-22 [PMID:10913337];
Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]
GPR17 in Human [GtoPdb: 88] [UniProtKB: Q13304]
GtoPdb [35S]GTPγS binding to 1321N1 cell membranes expressing hGPR17. - 9.48 pEC50 0.33 nM EC50 EMBO J (2006) 25: 4615-27 [PMID:16990797]
GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
GtoPdb - - 9.13 pEC50 0.74 nM EC50 PLoS ONE (2008) 3: e3579 [PMID:18974869]

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]