(R)-asimilobine [Ligand Id: 13235] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL469423
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of electric eel AChE by Ellman's assay B 4 pIC50 >100000 nM IC50 J Nat Prod (2006) 69: 1341-1346 [PMID:16989531]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of human AChE by Ellman's assay B 4 pIC50 >100000 nM IC50 J Nat Prod (2006) 69: 1341-1346 [PMID:16989531]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of horse serum BuChE by Ellman's method B 4 pIC50 >100000 nM IC50 J Nat Prod (2006) 69: 1341-1346 [PMID:16989531]
ChEMBL Inhibition of equine serum BuChE using BTCI as substrate pre-incubated for 10 mins followed by substrate addition measured after 5 mins by microplate reader analysis B 5 pIC50 10080 nM IC50 Eur J Med Chem (2023) 256: 115414-115414 [PMID:37172474]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Antagonist activity at D1R (unknown origin) transfected in HEK293 cells by FLIPR assay F 5.14 pIC50 7200 nM IC50 Eur J Med Chem (2023) 256: 115414-115414 [PMID:37172474]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Antagonist activity at D2R (unknown origin) transfected in HEK293 cells by FLIPR assay F 5.24 pIC50 5730 nM IC50 Eur J Med Chem (2023) 256: 115414-115414 [PMID:37172474]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Partial agonist activity at human 5-HT2C stably transfected in HEK293T cells measured after 18 to 24 hrs by FLIPR assay F 6.19 pEC50 653 nM EC50 Eur J Med Chem (2023) 256: 115414-115414 [PMID:37172474]
ChEMBL Partial agonist activity at 5-HT2CR (unknown origin) expressed in HEK293T cells assessed as increase in calcium flux measured for 3 mins by FLIPR assay F 6.51 pEC50 308 nM EC50 ACS Med Chem Lett (2024) 15: 99-106 [PMID:38229745]

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]