ChEMBL ligand: CHEMBL129542 (JNJ-5207852)
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] 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 Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] There should be some charts here, you may need to enable JavaScript!
Sigma-1 receptor in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] 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
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL	Inhibition of AChE	B	5.49	pIC50	3200	nM	IC50	Bioorg Med Chem (2008) 16: 2968-2973 [PMID:18249544]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL	Activity against human histamine H3 receptor by histamine induced inhibition of forskolin stimulated cAMP accumulation in SK-N-MC cells	F	9.08	pKd	0.83	nM	Kd	Bioorg Med Chem Lett (2006) 16: 897-900 [PMID:16300945]
ChEMBL	Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor	F	9.84	pKd	0.14	nM	Kd	J Med Chem (2003) 46: 3938-3944 [PMID:12930154]
ChEMBL	Mean functional activity against human H3 receptor	B	9.84	pKd	0.14	nM	Kd	J Med Chem (2005) 48: 2229-2238 [PMID:15771465]
ChEMBL	Antagonist activity at human histamine H3 receptor	F	9.84	pKd	0.14	nM	Kd	Bioorg Med Chem Lett (2007) 17: 3670-3675 [PMID:17498953]
ChEMBL	Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs	F	9.84	pKd	0.14	nM	Kd	Eur J Med Chem (2009) 44: 4413-4425 [PMID:19577344]
ChEMBL	Binding affinity to human histamine H3 receptor	B	8.03	pKi	9.24	nM	Ki	J Med Chem (2011) 54: 26-53 [PMID:21062081]
ChEMBL	Binding affinity to human histamine H3 receptor	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem Lett (2007) 17: 3670-3675 [PMID:17498953]
ChEMBL	Binding affinity to human histamine H3 receptor	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2014) 24: 2236-2239 [PMID:24745967]
ChEMBL	Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells	B	9.01	pKi	0.97	nM	Ki	Bioorg Med Chem Lett (2008) 18: 5796-5796 [PMID:18922693]
ChEMBL	Binding affinity to human histamine H3 receptor	B	9.01	pKi	0.97	nM	Ki	Bioorg Med Chem Lett (2010) 20: 2755-2760 [PMID:20382018]
ChEMBL	Binding affinity to histamine H3 receptor (unknown origin)	B	9.2	pKi	0.63	nM	Ki	ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943]
ChEMBL	Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cells after 60 mins by scintillation counting	B	9.2	pKi	0.63	nM	Ki	Bioorg Med Chem Lett (2010) 20: 1581-1584 [PMID:20138762]
ChEMBL	Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay	B	9.2	pKi	0.63	nM	Ki	J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL	Antagonist activity at human histamine H3 receptor	F	9.2	pKi	0.63	nM	Ki	Bioorg Med Chem (2021) 50: 116462-116462 [PMID:34695709]
GtoPdb	-	-	9.2	pKi	-	-	-	J Med Chem (2003) 46: 3938-44 [PMID:12930154]
ChEMBL	Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor expressed in C6 cells	B	9.2	pKi	0.63	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1443-1446 [PMID:17169555]
ChEMBL	Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells	B	9.22	pKi	0.6	nM	Ki	Eur J Med Chem (2009) 44: 4413-4425 [PMID:19577344]
ChEMBL	Binding affinity to human histamine H3 receptor	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2007) 17: 4799-4803 [PMID:17616397]
ChEMBL	Binding affinity to histamine H3 receptor	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2009) 52: 3855-3868 [PMID:19456097]
ChEMBL	Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells after 1 hr by fluid scintillation counting	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2010) 20: 6226-6230 [PMID:20843691]
ChEMBL	Inverse agonist activity at human histamine H3 receptor expressed in SK-N-MC cells	F	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2011) 21: 5384-5388 [PMID:21783360]
ChEMBL	Binding affinity to Homo sapiens (human) H3 receptor	B	9.22	pKi	0.6	nM	Ki	Med Chem Res (2013) 22: 3640-3652 [PMID:23807824]
ChEMBL	Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cells	B	9.24	pKi	0.58	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2172-2175 [PMID:19286376]
ChEMBL	Binding affinity to human recombinant histamine H3 receptor	B	9.24	pKi	0.58	nM	Ki	Bioorg Med Chem (2012) 20: 2889-2896 [PMID:22483590]
ChEMBL	In vitro binding affinity for human Histamine H3 receptor by displacing N-[3H]-methylhistamine in SK-N-MC cells was determined	B	9.24	pKi	0.58	nM	Ki	J Med Chem (2003) 46: 3938-3944 [PMID:12930154]
ChEMBL	Binding affinity to human histamine H3 receptor	B	9.24	pKi	0.58	nM	Ki	Bioorg Med Chem Lett (2007) 17: 3670-3675 [PMID:17498953]
ChEMBL	Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor expressed in monkey COS7 cells	B	9.24	pKi	0.57	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2288-2291 [PMID:18353639]
ChEMBL	Displacement of N-[3H]methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells	B	9.4	pKi	0.4	nM	Ki	Bioorg Med Chem Lett (2006) 16: 897-900 [PMID:16300945]
ChEMBL	Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor stably expressed in HEK293 cells assessed as inhibition constant by competitive binding based radioligand depletion assay	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2023) 66: 9658-9683 [PMID:37418295]
ChEMBL	Binding affinity to human H3R	B	9.56	pKi	0.28	nM	Ki	Eur J Med Chem (2021) 213: 113041-113041 [PMID:33261900]
ChEMBL	Displacement of [3H]UR-P1294 from human H3R receptor expressed in HEK293 cells by radioligand competition binding assay	B	9.68	pKi	0.21	nM	Ki	J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL	Antagonist potency against human H3 receptor in GTPgamma-S-Assay	F	9.7	pKi	0.2	nM	Ki	J Med Chem (2005) 48: 306-311 [PMID:15634025]
ChEMBL	Displacement of [3H]UR-MN259 from SP-FLAG tagged human histamine H3 receptor expressed in HEK293T cells assessed as inhibition constant incubated for 60 min by scintillation counter analysis	B	9.98	pKi	0.1	nM	Ki	ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943]
ChEMBL	Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay	B	10.22	pKi	0.06	nM	Ki	J Med Chem (2021) 64: 11695-11708 [PMID:34309390]
ChEMBL	Inhibition of histamine H3 receptor	B	9.28	pIC50	0.53	nM	IC50	Bioorg Med Chem (2008) 16: 2968-2973 [PMID:18249544]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL	Displacement of [3H]N-alpha-methylhistamine from histamine H3 receptor in rat striatal membrane	B	8.9	pKi	1.26	nM	Ki	Bioorg Med Chem Lett (2008) 18: 2288-2291 [PMID:18353639]
ChEMBL	Binding affinity to rat histamine H3 receptor	B	8.9	pKi	1.26	nM	Ki	Bioorg Med Chem (2012) 20: 2889-2896 [PMID:22483590]
ChEMBL	Displacement of N-[3H]methylhistamine from rat histamine H3 receptor in rat cortical hemispheres	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2006) 16: 897-900 [PMID:16300945]
ChEMBL	Binding affinity to rat histamine H3 receptor	B	9.2	pKi	0.63	nM	Ki	Bioorg Med Chem Lett (2014) 24: 2236-2239 [PMID:24745967]
ChEMBL	Binding affinity to rat histamine H3 receptor	B	9.24	pKi	0.58	nM	Ki	Bioorg Med Chem Lett (2014) 24: 2236-2239 [PMID:24745967]
ChEMBL	In vitro binding affinity for rat Histamine H3 receptor by displacing N-[3H]-methylhistamine in SK-N-MC cells was determined	B	9.34	pKi	0.46	nM	Ki	J Med Chem (2003) 46: 3938-3944 [PMID:12930154]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane assessed as inhibition constant by liquid scintillation counter analysis	B	5.93	pKi	1174.9	nM	Ki	J Med Chem (2023) 66: 9658-9683 [PMID:37418295]

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]