[3H]CGS23131 [Ligand Id: 3415] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL49302 (LY-223982, LY-333982)
  • BLT1 receptor/Leukotriene B4 receptor 1 in Human [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
  • 7.28
1 CHEMBL49302_lig_chart_1 Leukotriene B4 receptor 1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BLT1 receptor/Leukotriene B4 receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
GtoPdb - - 7.9 pKd 13 nM Kd J Pharmacol Exp Ther (1992) 262: 80-9 [PMID:1320692]
ChEMBL Binding affinity against Leukotriene B4 receptor on intact differentiated U-937 cells in competitive binding assay with [3H]LTB4 B 6.44 pKi 360 nM Ki J. Med. Chem. (1993) 36: 3333-3340 [PMID:8230123]
ChEMBL Compound was evaluated for inhibition of binding of [3H]LTB4 to LTB4 receptor in guinea-pig lung membranes B 8.11 pKi 7.8 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 1981-1984
ChEMBL Inhibition of LTB4-induced elastase release in human polymorphonuclear leukocytes F 6 pIC50 1000 nM IC50 J. Med. Chem. (1992) 35: 4315-4324 [PMID:1333012]
ChEMBL Inhibition of specific binding of [3H]LTB4 ( 0.1 nM) to LTB4 receptor on intact human neutrophils B 7.88 pIC50 13.2 nM IC50 J. Med. Chem. (1993) 36: 1726-1734 [PMID:8389876]
ChEMBL Inhibition of specific binding of [3H]LTB4 to Leukotriene B4 receptor in human neutrophils B 7.88 pIC50 13.2 nM IC50 J. Med. Chem. (1990) 33: 2807-2813 [PMID:2170648]
ChEMBL Compound was tested for inhibitory activity against human neutrophil LTB4 receptor binding F 7.89 pIC50 13 nM IC50 J. Med. Chem. (1996) 39: 2629-2654 [PMID:8709092]
ChEMBL In vitro antagonistic activity towards LTB4 receptor was evaluated by inhibition of binding of [3H]LTB4 to human neutrophils B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 1981-1984
ChEMBL Antagonistic activity against human polymorphonuclear (PMN) LTB4 receptor F 7.92 pIC50 12 nM IC50 J. Med. Chem. (1992) 35: 4253-4255 [PMID:1331462]
ChEMBL Binding affinity to leukotriene B4 receptor on intact human PMNs by displacing radioligand [3H]LTB4 B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1994) 37: 3327-3336 [PMID:7932560]
ChEMBL Inhibitory concentration against leukotriene receptor B4 (LTB4) in human polymorphonuclear cells (PMNs) B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1993) 36: 2703-2705 [PMID:8410983]
ChEMBL Inhibition of [3H]-LTB4 binding to Leukotriene B4 receptor in the human polymorphonuclear leukocytes. B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (1992) 35: 4315-4324 [PMID:1333012]
ChEMBL Inhibition of [3H]LTB4 binding to Leukotriene B4 receptor in the human polymorphonuclear leukocytes B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (1992) 35: 4306-4314 [PMID:1333011]
ChEMBL Inhibition of [3H]LTB4 binding to Leukotriene B4 receptor in the guinea pig spleen membranes B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1992) 35: 4306-4314 [PMID:1333011]
ChEMBL Inhibition of [3H]LTB4 binding to Leukotriene B4 receptor in the guinea pig spleen membranes. B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1992) 35: 4315-4324 [PMID:1333012]
ChEMBL Inhibition of binding of [3H]LTB4 to receptor on nonradioactive LTB4 B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (1993) 36: 1726-1734 [PMID:8389876]

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]