LP-44 [Ligand Id: 8435] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL225284 |
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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 | Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor | B | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| GtoPdb | - | - | 8.14 | pKi | 7.3 | nM | Ki | J Med Chem (2007) 50: 4214-21 [PMID:17649988] |
| 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 5-HT1A receptor expressed in HEK293 cells after 1 hr by beta-counting | B | 7.28 | pKi | 52.7 | nM | Ki | Eur J Med Chem (2014) 78: 10-22 [PMID:24675176] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 7.28 | pKi | 52.7 | nM | Ki | Eur J Med Chem (2014) 85: 716-726 [PMID:25128671] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 1 hr | B | 7.28 | pKi | 52.7 | nM | Ki | Eur J Med Chem (2015) 92: 202-211 [PMID:25555143] |
| GtoPdb | - | - | 7.28 | pKi | 52.7 | nM | Ki | J Med Chem (2007) 50: 4214-21 [PMID:17649988] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Wistar Han rat hippocampal membranes | B | 7.28 | pKi | 52.7 | nM | Ki | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6.49 | pKi | 326 | nM | Ki | J Med Chem (2007) 50: 4214-21 [PMID:17649988] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from 5HT2A receptor in Wistar Han rat cortex membranes | B | 6.49 | pKi | 326 | nM | Ki | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Activity at SB-269970 desensitized 5HT7 receptor assessed as reduction of substance P-induced contraction of Dunkin-Hartley guinea pig ileum | B | 7.7 | pKd | 19.95 | nM | Kd | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by beta-counting | B | 9.66 | pKi | 0.22 | nM | Ki | Eur J Med Chem (2014) 78: 10-22 [PMID:24675176] |
| ChEMBL | Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 9.66 | pKi | 0.22 | nM | Ki | Eur J Med Chem (2014) 85: 716-726 [PMID:25128671] |
| ChEMBL | Displacement of [3H]-5-CT from human 5HT7 receptor expressed in HEK293 cells after 1 hr | B | 9.66 | pKi | 0.22 | nM | Ki | Eur J Med Chem (2015) 92: 202-211 [PMID:25555143] |
| GtoPdb | - | - | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2007) 50: 4214-21 [PMID:17649988] |
| ChEMBL | Activity at 5HT7 receptor assessed as relaxation of substance P-induced contraction of Dunkin-Hartley guinea pig ileum | F | 5.59 | pEC50 | 2560 | nM | EC50 | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| 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 recombinant 5HT7 receptor expressed in HEK293 cells | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2004) 47: 6616-6624 [PMID:15588097] |
| ChEMBL | Displacement of [3H]LSD from rat cloned 5-Hydroxytryptamine receptor 7 after 60 mins | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
| ChEMBL | Displacement of [3H]LSD from rat recombinant 5-HT7 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2018) 61: 8475-8503 [PMID:29767995] |
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]
