4-methylhistamine [Ligand Id: 1269] activity data from GtoPdb and ChEMBL
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: CHEMBL275443 (4-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!
|
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 |
|---|---|---|---|---|---|---|---|---|
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay | F | 4.8 | pEC50 | 15848.93 | nM | EC50 | J Med Chem (2009) 52: 6297-6313 [PMID:19791743] |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells | B | 5.1 | pKi | 7943.28 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay | F | 5.5 | pEC50 | 3162.28 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay | F | 5.54 | pEC50 | 2884.03 | nM | EC50 | J Med Chem (2009) 52: 6297-6313 [PMID:19791743] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells | B | 5.2 | pKi | 6309.57 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay | F | 4.91 | pEC50 | 12400 | nM | EC50 | J Med Chem (2016) 59: 3452-3470 [PMID:27007611] |
| 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 | 7.3 | pKi | 50.12 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| GtoPdb | - | - | 8.2 | pKi | 6.31 | nM | Ki |
J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]; Br J Pharmacol (2006) 147: 744-54 [PMID:16432504] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19 protein by steady-state GTPase assay | F | 7.15 | pEC50 | 70.79 | nM | EC50 | J Med Chem (2009) 52: 6297-6313 [PMID:19791743] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human recombinant histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 by steady-state GTPase activity assay | F | 7.5 | pEC50 | 31.62 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
| ChEMBL | Agonist activity at mouse histamine H4 receptor | F | 5.8 | pEC50 | 1584.89 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H4 receptor/Histamine H4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4468] [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
| ChEMBL | Agonist activity at rat histamine H4 receptor | F | 5.6 | pEC50 | 2511.89 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
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]
