idalopirdine [Ligand Id: 8689] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3286580 (Idalopirdina, 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 | Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem (2022) 71: 116950-116950 [PMID:35926324] |
| ChEMBL | Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem (2022) 70: 116917-116917 [PMID:35839536] |
| ChEMBL | Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086] |
| 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 5-HT6 receptor (unknown origin) | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157] |
| 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 | 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 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] |
| ChEMBL | Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis | F | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem (2022) 70: 116917-116917 [PMID:35839536] |
| 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 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]
