LP-211 [Ligand Id: 8436] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL522691 |
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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 [PMID:30568756] |
| 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 [PMID:30568756] |
| 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 [PMID:30568756] |
| 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 [PMID:30568756] |
| 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 [PMID:30568756] |
| 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 [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/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 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]
