impromidine [Ligand Id: 1226] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12608 (Impromidine)
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
  • Histamine H2 receptor in Guinea pig [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity F 5.47 pKd 3388.44 nM Kd J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
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 6.3 pKi 501.19 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
GtoPdb - - 7.2 pKi - - - J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198]
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity F 7.7 pEC50 19.95 nM EC50 J Med Chem (2008) 51: 7193-7204 [PMID:18950149]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Binding affinity to the human histamine H3 receptor B 7.17 pKi 67 nM Ki J Med Chem (2003) 46: 3957-3960 [PMID:12954048]
GtoPdb - - 7.2 pKi - - - Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex F 7.2 pKi 63.1 nM Ki J Med Chem (1996) 39: 1220-1226 [PMID:8632428]
ChEMBL Binding affinity towards Histamine H3 receptor on synaptosomes from rat cerebral cortex B 7.4 pKi 39.81 nM Ki J Med Chem (1996) 39: 1220-1226 [PMID:8632428]
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 7.6 pKi 25.12 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
GtoPdb - - 7.9 pKi - - - Mol Pharmacol (2001) 59: 420-6 [PMID:11179434];
J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]
ChEMBL Binding affinity to the human histamine H4 receptor B 7.91 pKi 12.3 nM Ki J Med Chem (2003) 46: 3957-3960 [PMID:12954048]
ChEMBL Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 7.6 pEC50 25.12 nM EC50 Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5.2 pKi - - - J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198]

ChEMBL data shown on this page come from version 32:

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]