AC264613 [Ligand Id: 9460] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL494502 (AC-264613)
  • PAR2/Proteinase-activated receptor 2 in Human [ChEMBL: CHEMBL5963] [GtoPdb: 348] [UniProtKB: P55085]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
PAR2/Proteinase-activated receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5963] [GtoPdb: 348] [UniProtKB: P55085]
ChEMBL Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay F 5 pEC50 >10000 nM EC50 J. Med. Chem. (2008) 51: 5490-5493 [PMID:18720984]
GtoPdb - - 7.5 pEC50 31.6 nM EC50 J Med Chem (2008) 51: 5490-3 [PMID:18720984]
ChEMBL Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay F 7.5 pEC50 31.62 nM EC50 J. Med. Chem. (2008) 51: 5490-5493 [PMID:18720984]
ChEMBL Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay F 7.5 pEC50 31.62 nM EC50 J. Med. Chem. (2008) 51: 5490-5493 [PMID:18720984]
ChEMBL Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay F 7.52 pEC50 30 nM EC50 J. Med. Chem. (2013) 56: 7477-7497 [PMID:23895492]
ChEMBL Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis F 7.52 pEC50 30 nM EC50 J. Med. Chem. (2013) 56: 7477-7497 [PMID:23895492]
ChEMBL Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay B 7.52 pEC50 30 nM EC50 J. Med. Chem. (2013) 56: 7477-7497 [PMID:23895492]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]