idalopirdine [Ligand Id: 8689] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3286580 (Idalopirdine, Lu-ae58054, Lu AE58054, LU AE-58054, LU-AE-58054, LU-AE58054, LY-483518, LY483518, SGS-518, SGS518) |
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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]-raclopride from human D2R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis | B | 5.92 | pKi | 1215 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
| 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 microbeta plate reader analysis | B | 5.4 | pKi | 3936 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity to human 5-HT2AR expressed in HEK293 cells by competitive binding assay | B | 6.1 | pKi | 791 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (2014) 57: 5823-5828 [PMID:24878269] |
| GtoPdb | - | - | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2014) 57: 5823-8 [PMID:24878269] |
| ChEMBL | Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells | B | 6.6 | pKi | 250 | nM | Ki | J Med Chem (2014) 57: 5823-5828 [PMID:24878269] |
| 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 5HT6 receptor expressed in HEK293 cell membrane measured after 60 mins | B | 8.16 | pKi | 6.9 | nM | Ki | Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288] |
| ChEMBL | Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis | B | 8.45 | pKi | 3.54 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2014) 57: 5823-5828 [PMID:24878269] |
| GtoPdb | - | - | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2014) 57: 5823-8 [PMID:24878269] |
| ChEMBL | Binding affinity to 5HT6R (unknown origin) | B | 9.08 | pKi | 0.83 | nM | Ki | Eur J Med Chem (2018) 144: 716-729 [PMID:29291439] |
| ChEMBL | Antagonist activity at 5-HT6 receptor (unknown origin) | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2017) 60: 1843-1859 [PMID:28212021] |
| ChEMBL | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2014) 57: 7160-7181 [PMID:24850589] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2014) 57: 5823-5828 [PMID:24878269] |
| ChEMBL | Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay | F | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| ChEMBL | Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor | B | 9.08 | pKi | 0.83 | nM | Ki | ACS Med Chem Lett (2016) 7: 618-622 [PMID:27326337] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis | B | 5.06 | pKi | 8635 | nM | Ki | Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022] |
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]
