(S)-α-methylhistamine [Ligand Id: 1238] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL11919 ((S)-Alpha-Methylhistamine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 5.79 | pKi | 1621.81 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
| ChEMBL | Displacement of Clobenpropit-BODIPY-630/650 from Nluc-tagged human histamine H3 receptor expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay | B | 6.4 | pKi | 398.11 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| ChEMBL | Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay | B | 6.4 | pKi | 398.11 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
| 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 | 7.12 | pKi | 75.86 | 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 | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| 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 | 7.2 | pKi | 63.1 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | 7.3 | pKi | 50.12 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| ChEMBL | Binding affinity to histamine H3 receptor (unknown origin) | B | 7.6 | pKi | 25.12 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| 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 | 5.4 | pKi | 3981.07 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| GtoPdb | - | - | 5.5 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 4.9 | pEC50 | 12589.25 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
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]
