RO5101576 [Ligand Id: 6158] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1098560
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  • BLT1 receptor/Leukotriene B4 receptor 1 in Human [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
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  • BLT2 receptor/Leukotriene B4 receptor 2 in Human [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells assessed as reduction of current amplitude B 5.52 pIC50 >3000 nM IC50 J. Med. Chem. (2010) 53: 3502-3516 [PMID:20380377]
BLT1 receptor/Leukotriene B4 receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
ChEMBL Antagonist activity at FLAG-tagged human BLT1 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge F 6.94 pIC50 114 nM IC50 J. Med. Chem. (2010) 53: 3502-3516 [PMID:20380377]
GtoPdb - - 8.1 pIC50 8 nM IC50 Prostaglandins Other Lipid Mediat (2010) 92: 33-43 [PMID:20214997]
ChEMBL Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins F 9.36 pIC50 0.44 nM IC50 J. Med. Chem. (2010) 53: 3502-3516 [PMID:20380377]
BLT2 receptor/Leukotriene B4 receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1]
ChEMBL Antagonist activity at FLAG-tagged human BLT2 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge F 6.79 pIC50 164 nM IC50 J. Med. Chem. (2010) 53: 3502-3516 [PMID:20380377]

ChEMBL data shown on this page come from version 28:

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]