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

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ChEMBL ligand: CHEMBL49302 (LY-223982, LY-333982)
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • BLT1 receptor/Leukotriene B4 receptor 1 in Human [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL PDSP Secondary Binding target: DRD3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. B 5.71 pKi 1958.39 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
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 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]