S33084 [Ligand Id: 129] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL65280
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
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 Ability to displace [125I]iodosulpiride from human dopamine D2 (hD2) receptor transfected into CHO cells. B 7.5 pKi 31.62 nM Ki Bioorg Med Chem Lett (1999) 9: 2059-2064 [PMID:10450981]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 6.69 pKi 205 nM Ki Med Chem Res (2004) 13: 25-33
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity for human Dopamine receptor D3 B 8.6 pKi 8.6 nM Log Ki J Med Chem (2005) 48: 3663-3679 [PMID:15916415]
ChEMBL Ability to displace [125I]iodosulpiride from human dopamine D3 (hD3) receptor transfected into CHO cells. B 9.5 pKi 0.32 nM Ki Bioorg Med Chem Lett (1999) 9: 2059-2064 [PMID:10450981]
GtoPdb - - 9.6 pKi 0.25 nM Ki J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 8.62 pKi 2.42 nM Ki Med Chem Res (2004) 13: 25-33
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.1 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 6.9 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 6 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 6.8 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 7.1 pKi - - - J Pharmacol Exp Ther (2000) 293: 1048-62 [PMID:10869410]

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]