lurasidone [Ligand Id: 7461] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1237021 (Latuda, Lurasidone) |
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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 D2L receptor expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method | B | 8.77 | pKi | 1.7 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| GtoPdb | - | - | 8.77 | pKi | 1.68 | nM | Ki | J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009] |
| ChEMBL | Displacement of [3H]-spiperone from D2 receptor in rat striatum measured after 10 mins | B | 8.77 | pKi | 1.68 | nM | Ki | Bioorg Med Chem (2020) 28: 115459-115459 [PMID:32247749] |
| 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 expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 8.17 | pKi | 6.7 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| GtoPdb | - | - | 8.17 | pKi | 6.75 | nM | Ki | J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampus measured after 30 mins | B | 8.17 | pKi | 6.75 | nM | Ki | Bioorg Med Chem (2020) 28: 115459-115459 [PMID:32247749] |
| 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 human 5-HT2A receptor expressed in rat cortex tissue incubated for 30 mins by liquid scintillation counting method | B | 8.7 | pKi | 2 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| GtoPdb | - | - | 8.69 | pKi | 2.03 | nM | Ki | J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009] |
| ChEMBL | Displacement of [3H]-ketanserin from 5HT2A receptor in rat cortex measured after 30 mins | B | 8.69 | pKi | 2.03 | nM | Ki | Bioorg Med Chem (2020) 28: 115459-115459 [PMID:32247749] |
| 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 expressed in HEK293 cells incubated for 1 hr by liquid scintillation counting method | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817] |
| ChEMBL | Displacement of [3H]-5-CT from human recombinant 5HT7b receptor measured after 2 hrs | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem (2020) 28: 115459-115459 [PMID:32247749] |
| GtoPdb | - | - | 9.31 | pKi | 0.5 | nM | Ki | J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009] |
| ChEMBL | Antagonist activity at human 5-HT7A receptor expressed in HEK cell membranes assessed as reduction in serotonin-induced cAMP accumulation incubated for 20 mins by cAMP functional assay | F | 7.8 | pIC50 | 15.72 | nM | IC50 | Eur J Med Chem (2021) 214: 113243-113243 [PMID:33582388] |
| α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - |
J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - |
J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
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]
