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)
  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
  • Histamine H2 receptor in Guinea pig [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
There should be some charts here, you may need to enable JavaScript!
  • H3 receptor in Human [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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 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]