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: CHEMBL268229 ((R)-Alpha-Methylhistamine) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Binding affinity against H1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1995) 38: 1593-1599 [PMID:7752184] |
ChEMBL | Binding affinity to H-1 receptor was determined in guinea pig brain tissue using [3H]- N alpha-methylhistamine ligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 243-248 [PMID:9871662] |
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
ChEMBL | Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells | B | 8.2 | pKi | 6.31 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
ChEMBL | Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptor | B | 8.36 | pKi | 4.37 | nM | Ki | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
ChEMBL | Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay | F | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2004) 47: 2833-2838 [PMID:15139761] |
ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2008) 51: 2944-2953 [PMID:18433114] |
ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHOK1 cells after 2 hrs | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Inhibition of Histamine H3 receptor | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (2003) 46: 1980-1988 [PMID:12723960] |
ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | B | 9.1 | pKi | 0.8 | nM | Ki | Eur J Med Chem (2009) 44: 4413-4425 [PMID:19577344] |
ChEMBL | Binding affinity to the human histamine H3 receptor | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
GtoPdb | - | - | 9.2 | pKi | - | - | - |
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; Biochem J (2001) 355: 279-88 [PMID:11284713]; J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]; Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]; Mol Pharmacol (2001) 59: 420-6 [PMID:11179434] |
ChEMBL | Displacement of [3H[N-alpha-methylhistamine form human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation counting | B | 9.26 | pKi | 0.55 | nM | Ki | J Med Chem (2010) 53: 3840-3844 [PMID:20384344] |
ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHOK1 cells after 2 hrs | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method | F | 7.4 | pEC50 | 40 | nM | EC50 | Eur J Med Chem (2020) 191: 112150-112150 [PMID:32105981] |
ChEMBL | Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting | F | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2010) 53: 3840-3844 [PMID:20384344] |
ChEMBL | Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor | B | 9.17 | pEC50 | 0.68 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 9.5 | pEC50 | 0.32 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406] | ||||||||
GtoPdb | - | - | 8.4 | pKi | - | - | - | Eur J Pharmacol (2003) 467: 57-65 [PMID:12706455] |
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
GtoPdb | - | - | 8.7 | pKi | - | - | - |
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; Br J Pharmacol (2000) 131: 1247-50 [PMID:11090094]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
ChEMBL | Inhibition of rat histamine H3 receptor | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
ChEMBL | pD2 values against H3 receptor of guinea pig jejunum were determined. | B | 7.8 | pKd | 15.85 | nM | Kd | J Med Chem (1995) 38: 266-271 [PMID:7830269] |
ChEMBL | Binding affinity against Histamine H3 receptor | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (1995) 38: 1593-1599 [PMID:7752184] |
ChEMBL | Binding affinity of compound towards Histamine H3 receptor was determined in guinea pig brain tissue using [3H]- N alpha-methylhistamine radioligand | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 243-248 [PMID:9871662] |
ChEMBL | Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig ileum LMMP homogenates | B | 9.82 | pKi | 0.15 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1825-1830 [PMID:10406649] |
ChEMBL | Binding affinity towards histamine H3 receptor using [3H](R)-alpha-methylhistamine as radioligand in guinea pig cortical homogenates | B | 10.07 | pKi | 0.09 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1825-1830 [PMID:10406649] |
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
ChEMBL | Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 | B | 6.6 | pKi | 251.19 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells | B | 6.74 | pKi | 184 | nM | Ki | J Med Chem (2008) 51: 3145-3153 [PMID:18459760] |
ChEMBL | Binding affinity to the human histamine H4 receptor | B | 6.84 | pKi | 146 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
GtoPdb | - | - | 6.9 | pKi | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436] |
ChEMBL | Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor | B | 5.95 | pEC50 | 1122.02 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 6.2 | pEC50 | 630.96 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
GtoPdb | - | - | 6.4 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
GtoPdb | - | - | 6.2 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
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]