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 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]