(R)-α-methylhistamine [Ligand Id: 1236] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL268229 ((R)-Alpha-Methylhistamine) |
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| 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 | 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 | 6.37 | pKi | 426.58 | 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 | 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]N-methylhistamine from SP-FLAG tagged human histamine H3 receptor expressed in SK-N-MC cells incubated for 40 mins | B | 8.2 | pKi | 6.31 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Displacement of [3H]NAMH from human C-terminal Nluc-tagged Halo tag fused between T229/F348 residue histamine H3 receptor expressed in HEK293-A cells incubated for 2 hrs by scintillation counter analysis | B | 8.3 | pKi | 5.01 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Binding affinity to histamine H3 receptor (unknown origin) | B | 8.4 | pKi | 3.98 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 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]
