pitolisant [Ligand Id: 8924] 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: CHEMBL462605 (BF-2649, BF-2.649, Wakix, Tiprolisant, Wakix, europe, Pitolisant, Bf2.649, BF2.649, HBS-101)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
There should be some charts here, you may need to enable JavaScript!
  • H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
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
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method B 5.07 pIC50 8420 nM IC50 Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method B 5.77 pIC50 1700 nM IC50 Bioorg Med Chem (2017) 25: 5341-5354 [PMID:28797771]
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 recombinant full length H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method B 7.93 pKi 11.7 nM Ki Bioorg Med Chem (2017) 25: 5341-5354 [PMID:28797771]
ChEMBL Displacement of [3H]-N-alpha-methylhistamine from human histamine H3 receptor stably expressed in HEK293 cell membrane after 90 mins B 7.93 pKi 11.7 nM Ki Eur J Med Chem (2020) 185: 111785-111785 [PMID:31669851]
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 [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 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]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 [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]-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 Inhibition of human H3 receptor B 9.52 pKi 0.3 nM Ki Eur J Med Chem (2018) 152: 223-234 [PMID:29723785]
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 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 Inhibition of Guinea Pig Ileum H3R B 9.8 pKi 0.16 nM Ki Eur J Med Chem (2019) 181: 111569-111569 [PMID:31404862]
ChEMBL Inhibition of Guinea Pig Ileum H3R B 9.8 pKi 0.16 nM Ki Eur J Med Chem (2019) 181: 111569-111569 [PMID:31404862]
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 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]