lurasidone [Ligand Id: 7461] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1237021 (Latuda, Lurasidona, 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 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]
