dimaprit [Ligand Id: 1248] 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: CHEMBL12344 (Dimaprit) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| 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 | 4.6 | pKi | 25118.86 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747] | ||||||||
| ChEMBL | Compound is evaluated for histamine H2 receptor agonistic activity in guinea pig cerebral cortex using [3H]tiotidine as radioligand | F | 4.58 | pKd | 26302.68 | nM | Kd | J Med Chem (1992) 35: 3239-3246 [PMID:1507209] |
| Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
| ChEMBL | In vitro binding affinity for histamine H3 receptor was determined in guinea-pig cerebral cortex using [3H](R)-alpha-methylhistamine | B | 7.32 | pKi | 47.86 | nM | Ki | J Med Chem (2000) 43: 2362-2370 [PMID:10882362] |
| 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 | 6.5 | pKi | 316.23 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in human SK-N-MC cells after 1 hr | B | 6.5 | pKi | 316.23 | nM | Ki | Medchemcomm (2013) 4: 193-204 |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436]; J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (2008) 51: 3145-3153 [PMID:18459760] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 5.8 | pEC50 | 1584.89 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H3 receptor in Human [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| GtoPdb | - | - | 6.1 | pKi | - | - | - | Mol Pharmacol (2001) 59: 420-6 [PMID:11179434] |
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]
