VUF 8430 [Ligand Id: 1274] 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: CHEMBL1196470 (2-Guanidinoethyl Carbamimidothioate) |
|---|
|
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 |
|---|---|---|---|---|---|---|---|---|
| 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 | 6 | pKi | 1000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 6.5 | pEC50 | 316.23 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | 31.6 | nM | Ki | J Med Chem (2006) 49: 6650-1 [PMID:17154494] |
| ChEMBL | Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| ChEMBL | Displacement of [3H]histamine from wild type human histamine H4 receptor transfected in HEK293T cells after 1 hr by liquid scintillation counting analysis | B | 7.6 | pKi | 25.12 | nM | Ki | Medchemcomm (2013) 4: 193-204 |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.3 | pEC50 | 50.12 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human H4R by [35S]-GTPgammaS-binding assay | F | 7.42 | pEC50 | 38.02 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| H4 receptor/Histamine H4 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5657] [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
| ChEMBL | Agonist activity at mouse H4R by [35S]-GTPgammaS-binding assay | F | 5.06 | pEC50 | 8709.64 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
| H4 receptor/Histamine H4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4468] [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
| ChEMBL | Agonist activity at rat H4R by [35S]-GTPgammaS-binding assay | F | 4.47 | pEC50 | 33884.42 | nM | EC50 | J Med Chem (2019) 62: 8338-8356 [PMID:31469288] |
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]
