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 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]