pitolisant [Ligand Id: 8924] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL462605 (BF-2649, BF-2.649, HBS-101, Wakix, Tiprolisant, Wakix, europe, Pitolisant, BF2.649)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Mouse [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
  • Histamine H3 receptor in Guinea pig [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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  • H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5.78 pKi - - - Pharmacol. Rev. (2015) 67: 601-55 [PMID:26084539]
ChEMBL Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis B 5.94 pKi 1148.15 nM Ki Eur. J. Med. Chem. (2014) 77: 269-279 [PMID:24650714]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in HEK293 cells B 7.83 pKi 14.8 nM Ki Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in HEK-293 cell membrane after 90 mins by liquid scintillation counting analysis B 7.94 pKi 11.48 nM Ki Eur. J. Med. Chem. (2014) 77: 269-279 [PMID:24650714]
ChEMBL Displacement of [3H]N-alpha-Methylhistamine from human recombinant H3 receptor expressed in HEK293 cells by competitive binding assay B 7.94 pKi 11.48 nM Ki Eur. J. Med. Chem. (2014) 86: 578-588 [PMID:25218907]
ChEMBL Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cells B 8.57 pKi 2.7 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2172-2175 [PMID:19286376]
ChEMBL Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in rat C6 cells B 8.57 pKi 2.7 nM Ki Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
ChEMBL Displacement of [125I]iodoproxyfan human histamine H3 receptor B 8.57 pKi 2.7 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 5879-5882 [PMID:20728354]
ChEMBL Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cells B 8.57 pKi 2.7 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 5883-5886 [PMID:20727744]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells B 8.57 pKi 2.7 nM Ki Eur. J. Med. Chem. (2009) 44: 4413-4425 [PMID:19577344]
ChEMBL Displacement of [125I]-iodoproxyfan from human striatal full length H3 receptor after 60 mins by gamma counting method B 8.57 pKi 2.7 nM Ki Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486]
GtoPdb Measured in a [125I]iodoproxyfan binding assay in cells exogenously expressing the human H3 receptor. - 8.57 pKi 2.7 nM Ki Pharmacol. Rev. (2015) 67: 601-55 [PMID:26084539];
Bioorg. Med. Chem. (2009) 17: 3037-42 [PMID:19329325]
ChEMBL Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in CHO-K1 cells B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. (2008) 16: 8729-8736 [PMID:18774720]
ChEMBL Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in CHO-K1 cells B 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
ChEMBL Binding affinity to human histamine H3 receptor B 9.52 pKi 0.3 nM Ki Bioorg Med Chem (2017) 25: 2701-2712 [PMID:28372935]
ChEMBL Inhibition of human H3 receptor B 9.52 pKi 0.3 nM Ki Eur J Med Chem (2018) 152: 223-234 [PMID:29723785]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]gammaS binding assay B 9.8 pKi 0.16 nM Ki J. Med. Chem. (2009) 52: 3855-3868 [PMID:19456097]
ChEMBL Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding F 7.92 pIC50 12 nM IC50 J. Med. Chem. (2008) 51: 6889-6901 [PMID:18841880]
H3 receptor/Histamine H3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406]
ChEMBL Displacement of [125I]-iodoproxyfan from mouse brain cortex H3 receptor after 60 mins by gamma counting method B 7.85 pKi 14 nM Ki Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Binding affinity to histamine H3 receptor in rat cerebral cortex B 7.77 pKi 17 nM Ki Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
ChEMBL Displacement of [125I]-iodoproxyfan from rat brain cortex H3 receptor after 60 mins by gamma counting method B 7.77 pKi 17 nM Ki Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486]
ChEMBL Binding affinity to rat histamine H3 receptor B 7.77 pKi 17 nM Ki Bioorg Med Chem (2017) 25: 2701-2712 [PMID:28372935]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL Antagonist activity at histamine H3 receptor in isolated guinea pig ileum F 8.25 pKd 5.62 nM Kd Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay F 9.8 pKi 0.16 nM Ki Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
ChEMBL Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay F 8.82 pEC50 1.5 nM EC50 Bioorg. Med. Chem. (2009) 17: 3037-3042 [PMID:19329325]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
GtoPdb - - 4 pKi >100000 nM Ki Pharmacol. Rev. (2015) 67: 601-55 [PMID:26084539]
ChEMBL Inhibition of human H4 receptor B 4 pKi >100000 nM Ki Eur J Med Chem (2018) 152: 223-234 [PMID:29723785]
ChEMBL Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis B 5 pKi >10000 nM Ki Eur. J. Med. Chem. (2014) 77: 269-279 [PMID:24650714]
H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
GtoPdb - - 4.96 pKi - - - Pharmacol. Rev. (2015) 67: 601-55 [PMID:26084539]

ChEMBL data shown on this page come from version 27:

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]