ChEMBL ligand: CHEMBL462605 (Bf2.649, BF-2649, BF-2.649, BF2.649, HBS-101, Pitolisant, Tiprolisant, Wakix, Wakix, europe)
Cholinesterase in Equus caballus [ChEMBL: CHEMBL5763] [UniProtKB: P81908] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] 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]
ChEMBL	Inhibition of equine serum BChE using BTCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method	B	5.08	pIC50	8400	nM	IC50	Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
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 [3H]N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cells by microbeta scintillation analysis	B	7.52	pKi	30	nM	Ki	Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
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 recombinant human histamine H3 receptor expressed in human HEK293 cells incubated for 90 mins by microbeta scintillation analysis	B	7.92	pKi	12	nM	Ki	Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
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 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 [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor expressed in HEK293 cells incubated for 90 mins by competition binding assay	B	7.95	pKi	11.3	nM	Ki	Bioorg Med Chem (2021) 50: 116462-116462 [PMID:34695709]
ChEMBL	Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor stably transfected in HEK-293T cells membrane incubated for 90 mins by scintillation counting method	B	8.1	pKi	8	nM	Ki	Eur J Med Chem (2020) 191: 112150-112150 [PMID:32105981]
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 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 [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 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 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	Antagonist activity at histamine H3 receptor (unknown origin)	F	8.6	pKi	2.51	nM	Ki	Bioorg Med Chem (2021) 50: 116462-116462 [PMID:34695709]
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	Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay	B	8.6	pKi	2.51	nM	Ki	J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
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 in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay	B	9.04	pKi	0.91	nM	Ki	J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL	Binding affinity to human H3R	B	9.52	pKi	0.3	nM	Ki	Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
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 recombinant human H3 receptor expressed in CHO-K1 cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay	F	9.8	pKi	0.16	nM	Ki	Eur J Med Chem (2020) 205: 112667-112667 [PMID:32911308]
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]
ChEMBL	Binding affinity to rat H3R	B	7.77	pKi	17	nM	Ki	Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
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	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	Binding affinity to human H4R	B	4	pKi	>100000	nM	Ki	Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]