fluperlapine [Ligand Id: 279] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL63756 (Fluperlapine)
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
  • 6.85
1 CHEMBL63756_lig_chart_1 Dopamine D1 receptor Rat
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  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
  • 6.88
2 CHEMBL63756_lig_chart_2 Dopamine D2 receptor Rat
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • 7.8
3 CHEMBL63756_lig_chart_3 5-HT6 receptor HumanRat
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  • 5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
  • 8.3
4 CHEMBL63756_lig_chart_4 5-HT7 receptor HumanRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Binding affinity against dopamine receptor D1 B 6.85 pKi 141.25 nM Ki J. Med. Chem. (1994) 37: 519-525 [PMID:7907148]
ChEMBL In vitro binding affinity against Dopamine receptor D1 in rat striatal tissue B 6.85 pKi 141 nM Ki J. Med. Chem. (1993) 36: 2107-2114 [PMID:8101877]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro binding affinity against Dopamine D2 receptor in rat striatal tissue. B 6.88 pKi 133 nM Ki J. Med. Chem. (1993) 36: 2107-2114 [PMID:8101877]
ChEMBL Binding affinity against dopamine D2 receptor B 6.88 pKi 131.83 nM Ki J. Med. Chem. (1994) 37: 519-525 [PMID:7907148]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 7.5 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988];
Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.8 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor in Human [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 7.5 pKi - - - Psychopharmacology (Berl.) (2005) 179: 461-9 [PMID:15821958]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]