lurasidone [Ligand Id: 7461] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1237021 (Latuda, Lurasidone)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
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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 40.7 nM Ki J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009]
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 7.97 pKi 10.8 nM Ki J Pharmacol Exp Ther (2010) 334: 171-81 [PMID:20404009]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]