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

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ChEMBL ligand: CHEMBL522691
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • 6.85
1 CHEMBL522691_lig_chart_1 Dopamine D2 receptor Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 6.73
2 CHEMBL522691_lig_chart_2 Serotonin 1a (5-HT1a) receptor Human
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 6.2
3 CHEMBL522691_lig_chart_3 Serotonin 2a (5-HT2a) receptor Human
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • This target only has 1 pki data point
  • 6.75
4 CHEMBL522691_lig_chart_4 Serotonin 5a (5-HT5a) receptor Human
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5.8
5 CHEMBL522691_lig_chart_5 Serotonin 6 (5-HT6) receptor Human
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
  • Serotonin 7 (5-HT7) receptor in Guinea pig [ChEMBL: CHEMBL5494] [UniProtKB: P50407]
  • 0
6 CHEMBL522691_lig_chart_6 Serotonin 7 (5-HT7) receptor HumanRatGuinea pig
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • This target only has 1 pki data point
  • 5.3
7 CHEMBL522691_lig_chart_7 Sigma opioid receptor Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 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
GtoPdb - - 6.85 pKi 142 nM Ki J Med Chem (2008) 51: 5813-22 [PMID:18800769]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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
GtoPdb - - 6.73 pKi 188 nM Ki J Med Chem (2008) 51: 5813-22 [PMID:18800769]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor 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
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor 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
5-HT6 receptor/Serotonin 6 (5-HT6) receptor 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
5-HT7 receptor/Serotonin 7 (5-HT7) receptor 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
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/Serotonin 7 (5-HT7) receptor 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]
Serotonin 7 (5-HT7) receptor 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]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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 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]