LP-211 [Ligand Id: 8436] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL522691
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • 5-hydroxytryptamine receptor 7 in Guinea pig [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor transfected in HEK293-EBNA cells after 120 mins B 6.42 pKi 379 nM Ki Bioorg Med Chem (2014) 22: 1736-1750 [PMID:24508140]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor after 1.5 hrs B 6.42 pKi 379 nM Ki Bioorg Med Chem Lett (2013) 23: 6083-6086 [PMID:24100077]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor after 1.5 hrs by cell based assay B 6.42 pKi 379 nM Ki Eur J Med Chem (2016) 120: 363-379 [PMID:27318552]
ChEMBL Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 cells B 6.73 pKi 188 nM Ki J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr by beta-counting B 6.73 pKi 188 nM Ki Eur J Med Chem (2014) 78: 10-22 [PMID:24675176]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr B 6.73 pKi 188 nM Ki Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
ChEMBL Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis B 6.73 pKi 188 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
GtoPdb - - 6.73 pKi 188 nM Ki J Med Chem (2008) 51: 5813-22 [PMID:18800769]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from recombinant human 5-HT2A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis B 6.2 pKi 626 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis B 6.75 pKi 178 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]-LSD from human 5-HT6 receptor after 1.5 hrs by cell based assay B 5.8 pKi 1571 nM Ki Eur J Med Chem (2016) 120: 363-379 [PMID:27318552]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT6 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis B 5.8 pKi 1571 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]5-CT from human 5HT7 receptor transfected in HEK293 cells after 60 mins B 7.82 pKi 15 nM Ki Bioorg Med Chem (2014) 22: 1736-1750 [PMID:24508140]
ChEMBL Displacement of [3H]-5-CT from human cloned 5HT7 receptor B 7.82 pKi 15 nM Ki J Med Chem (2012) 55: 6375-6380 [PMID:22738316]
ChEMBL Displacement of [3H]LSD from human 5HT7 receptor after 1.5 hrs B 7.82 pKi 15 nM Ki Bioorg Med Chem Lett (2013) 23: 6083-6086 [PMID:24100077]
ChEMBL Displacement of [3H]-LSD from human 5-HT7 receptor after 1.5 hrs by cell based assay B 7.82 pKi 15 nM Ki Eur J Med Chem (2016) 120: 363-379 [PMID:27318552]
ChEMBL Displacement of [3H]LSD from human recombinant 5-HT7 receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis B 9.22 pKi 0.6 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting B 9.24 pKi 0.58 nM Ki Eur J Med Chem (2014) 78: 10-22 [PMID:24675176]
ChEMBL Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr B 9.24 pKi 0.58 nM Ki Eur J Med Chem (2012) 56: 348-360 [PMID:22926225]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Displacement of [3H]LSD from rat cloned 5HT7 receptor expressed in HEK293 cells B 9.24 pKi 0.58 nM Ki J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Binding affinity to rat cloned 5HT7 receptor B 9.24 pKi 0.58 nM Ki J Med Chem (2012) 55: 6375-6380 [PMID:22738316]
ChEMBL Binding affinity to rat 5HT7 receptor B 9.24 pKi 0.58 nM Ki Bioorg Med Chem (2014) 22: 1736-1750 [PMID:24508140]
GtoPdb - - 9.24 pKi 0.58 nM Ki J Med Chem (2008) 51: 5813-22 [PMID:18800769]
5-hydroxytryptamine receptor 7 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
ChEMBL Agonist activity at 5HT7 receptor assessed as relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction F 6.22 pEC50 600 nM EC50 J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity to dopamine D2 receptor (unknown origin) B 6.62 pKi 242 nM Ki Eur J Med Chem (2016) 120: 363-379 [PMID:27318552]
ChEMBL Displacement of [3H]spiroperidol from human cloned dopamine D2L receptor expressed in rat C6 cells B 6.85 pKi 142 nM Ki J Med Chem (2008) 51: 5813-5822 [PMID:18800769]
ChEMBL Displacement of [3H]-raclopride from recombinant human D2 receptor expressed in cell membrane measured after 1.5 hrs by scintillation counting method B 6.85 pKi 142 nM Ki Medchemcomm (2018) 9: 1882-1890 [PMID:30568756]
GtoPdb - - 6.85 pKi 142 nM Ki J Med Chem (2008) 51: 5813-22 [PMID:18800769]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Binding affinity to sigma 1 receptor (unknown origin) by radioligand binding assay B 5.3 pKi >5000 nM Ki Bioorg Med Chem Lett (2013) 23: 6083-6086 [PMID:24100077]

ChEMBL data shown on this page come from version 36:

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]