LTB4 [Ligand Id: 2487] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL65061 (Leukotriene B4)
  • BLT1 receptor/Leukotriene B4 receptor 1 in Human [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
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  • BLT2 receptor in Human [GtoPdb: 268] [UniProtKB: Q9NPC1]
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  • TRPV1 in Rat [GtoPdb: 507] [UniProtKB: O35433]
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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]
ChEMBL Displacement of [3H]LTB4 from LTB4R B 8.54 pKi 2.9 nM Ki J. Nat. Prod. (1993) 56: 441-455 [PMID:8496700]
ChEMBL Tested for inhibition of specific binding of [3H]LTB4 to human neutrophil expressing LTB4 receptor B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1993) 36: 3982-3984 [PMID:8254628]
ChEMBL LTB4 receptor antagonist activity was determined by inhibition of specific binding of [3H]LTB4 in human neutrophil B 8.72 pKi 1.9 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 2077-2082
GtoPdb - - 9.4 pKi 0.38 nM Ki
ChEMBL Tested for inhibition of specific binding of [3H]LTB4 to guinea pig lung membranes expressing LTB4 receptor B 9.92 pKi 0.12 nM Ki J. Med. Chem. (1993) 36: 3982-3984 [PMID:8254628]
ChEMBL Compound was evaluated for inhibition of binding of [3H]LTB4 to LTB4 receptor in guinea-pig lung membranes B 9.92 pKi 0.12 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 1981-1984
ChEMBL LTB4 receptor antagonist activity was determined by inhibition of specific binding of [3H]LTB4 in guinea pig lung membranes B 9.92 pKi 0.12 nM Ki Bioorg. Med. Chem. Lett. (1994) 4: 2077-2082
ChEMBL Inhibitory activity against leukotriene B4 receptor B 7.49 pIC50 32 nM IC50 Bioorg. Med. Chem. Lett. (1994) 4: 811-816
ChEMBL In vitro antagonistic activity towards LTB4 receptor was evaluated by inhibition of binding of [3H]LTB4 to human neutrophils B 8.72 pIC50 1.9 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 1981-1984
ChEMBL Inhibition of specific binding of [3H]LTB4 to Leukotriene B4 receptor in human neutrophils B 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (1990) 33: 2807-2813 [PMID:2170648]
BLT2 receptor in Human [GtoPdb: 268] [UniProtKB: Q9NPC1]
GtoPdb - - 7.64 pKd 22.7 nM Kd J Exp Med (2000) 192: 421-32 [PMID:10934230]
GtoPdb - - 7.6 pIC50 25 nM IC50 J Exp Med (2008) 205: 759-66 [PMID:18378794]
GtoPdb - - 6.85 pEC50 142 nM EC50 J Exp Med (2008) 205: 759-66 [PMID:18378794]
TRPV1 in Rat [GtoPdb: 507] [UniProtKB: O35433]
GtoPdb - - 4.9 pEC50 12500 nM EC50 Proc Natl Acad Sci USA (2000) 97: 6155-60 [PMID:10823958]

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]