BAYu9773 [Ligand Id: 3381] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL285954
  • 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]
  • CysLT2 receptor in Rat [GtoPdb: 270] [UniProtKB: Q924T9]
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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 - - 5.3 pIC50 5000 nM IC50 Br. J. Pharmacol. (2010) 160: 399-409 [PMID:20423349]
ChEMBL Antagonist activity at human CysLT1 receptor expressed in CHO cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay F 6.36 pIC50 440 nM IC50 ACS Med. Chem. Lett. (2014) 5: 1230-1234 [PMID:25408836]
GtoPdb - - 6.36 pIC50 440 nM IC50 Mol. Pharmacol. (2000) 58: 1601-8 [PMID:11093801]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL Compound was evaluated for its binding affinity on guinea-pig ileum B 7 pKi 100 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 1517-1522
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
GtoPdb - - 5.34 pIC50 4600 nM IC50 J. Pharmacol. Exp. Ther. (2011) 339: 768-78 [PMID:21903747]
GtoPdb - - 6.4 pIC50 400 nM IC50 J. Biol. Chem. (2000) 275: 30531-6 [PMID:10851239];
Mol. Pharmacol. (2000) 58: 1601-8 [PMID:11093801];
Br. J. Pharmacol. (2010) 160: 399-409 [PMID:20423349]
GtoPdb - - 6.52 pIC50 300 nM IC50 Mol. Pharmacol. (2000) 58: 1601-8 [PMID:11093801]
ChEMBL Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay F 6.52 pIC50 300 nM IC50 ACS Med. Chem. Lett. (2014) 5: 1230-1234 [PMID:25408836]
GtoPdb - - 7.74 pIC50 18 nM IC50 Br. J. Pharmacol. (2010) 160: 399-409 [PMID:20423349]
GtoPdb - - 7.04 pEC50 92 nM EC50 Mol. Pharmacol. (2000) 58: 1601-8 [PMID:11093801]
GtoPdb - - 7.16 pEC50 69 nM EC50 Br. J. Pharmacol. (2010) 160: 399-409 [PMID:20423349]
CysLT2 receptor in Rat [GtoPdb: 270] [UniProtKB: Q924T9]
GtoPdb against LTC4 and LTD4 induced contraction in smooth muscle preparation - 7.7 pA2 - - - Eur. J. Pharmacol. (1994) 264: 317-323 [PMID:7698171]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]