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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
