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ChEMBL ligand: CHEMBL129542 (JNJ-5207852) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | Antagonist activity at human histamine H3 receptor | F | 9.2 | pKi | 0.63 | nM | Ki | Bioorg Med Chem (2021) 50: 116462-116462 [PMID:34695709] |
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] |
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 | Binding affinity to histamine H3 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2009) 52: 3855-3868 [PMID:19456097] |
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 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 | 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 | 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 human histamine H3 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 4799-4803 [PMID:17616397] |
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 | 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 | 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 | 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 | 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 | 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] |
ChEMBL data shown on this page come from version 33:
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]