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 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]
