L-798,106 [Ligand Id: 1941] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL218071 (L-798106)
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • DP1 receptor/Prostanoid DP receptor in Human [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
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  • EP1 receptor/Prostanoid EP1 receptor in Human [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
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  • EP2 receptor/Prostanoid EP2 receptor in Human [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
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  • EP3 receptor/Prostanoid EP3 receptor in Human [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
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  • EP4 receptor/Prostanoid EP4 receptor in Human [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
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  • FP receptor/Prostanoid FP receptor in Human [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
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  • IP receptor/Prostanoid IP receptor in Human [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
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  • TP receptor/Thromboxane A2 receptor in Human [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
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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 6.23 pKi 582.44 nM Ki EUbOPEN Chemogenomics Library - PDSP Secondary Binding
DP1 receptor/Prostanoid DP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4427] [GtoPdb: 338] [UniProtKB: Q13258]
ChEMBL Binding affinity to DP receptor B 6.3 pKi >500 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
EP1 receptor/Prostanoid EP1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1811] [GtoPdb: 340] [UniProtKB: P34995]
ChEMBL Binding affinity to EP1 receptor B 4.41 pKi 39000 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
EP2 receptor/Prostanoid EP2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1881] [GtoPdb: 341] [UniProtKB: P43116]
ChEMBL Binding affinity to EP2 receptor B 4.3 pKi >50000 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
EP3 receptor/Prostanoid EP3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3710] [GtoPdb: 342] [UniProtKB: P43115]
ChEMBL Binding affinity to EP3 receptor in presence of HSA B 8.16 pKi 6.9 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
ChEMBL Binding affinity to EP3 receptor B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
GtoPdb - - 9.68 pKi 0.21 nM Ki Bioorg Med Chem (2001) 9: 1977-84 [PMID:11504634];
Am J Physiol Renal Physiol (2008) 295: F984-94 [PMID:18632791];
Br J Pharmacol (2009) 158: 372-81 [PMID:19486006]
ChEMBL Antagonist activity at EP3 receptor (unknown origin) B 7.48 pIC50 33.02 nM IC50 ACS Med Chem Lett (2023) 14: 727-736 [PMID:37312837]
EP4 receptor/Prostanoid EP4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1836] [GtoPdb: 343] [UniProtKB: P35408]
ChEMBL Binding affinity to EP4 receptor B 6.05 pKi 890 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
FP receptor/Prostanoid FP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1987] [GtoPdb: 344] [UniProtKB: P43088]
ChEMBL Binding affinity to FP receptor B 6.3 pKi >500 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
IP receptor/Prostanoid IP receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1995] [GtoPdb: 345] [UniProtKB: P43119]
ChEMBL Binding affinity to IP receptor B 6.3 pKi >500 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]
TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731]
ChEMBL Binding affinity to TP receptor B 6.3 pKi >500 nM Ki Bioorg Med Chem Lett (2006) 16: 5639-5642 [PMID:16931013]

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]