immethridine [Ligand Id: 4024] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL82298 (Immethridine)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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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]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells B 9.07 pKi 0.85 nM Ki J Med Chem (2004) 47: 2414-2417 [PMID:15115383]
GtoPdb - - 9.1 pKi - - - J Med Chem (2004) 47: 2414-7 [PMID:15115383]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells B 9.1 pKi 0.79 nM Ki J Med Chem (2008) 51: 2944-2953 [PMID:18433114]
ChEMBL Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells B 9.1 pKi 0.79 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Displacement of [3H](R)-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells by liquid scintillation counting B 9.11 pKi 0.77 nM Ki J Med Chem (2010) 53: 6445-6456 [PMID:20690643]
ChEMBL Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding F 8.96 pEC50 1.1 nM EC50 J Med Chem (2010) 53: 6445-6456 [PMID:20690643]
ChEMBL Agonist activity at human histamine H3 receptor assessed as beta galactosidase activity F 9.7 pEC50 0.2 nM EC50 J Med Chem (2008) 51: 2944-2953 [PMID:18433114]
ChEMBL Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor B 9.74 pEC50 0.18 nM EC50 J Med Chem (2004) 47: 2414-2417 [PMID:15115383]
ChEMBL Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 9.8 pEC50 0.16 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]
ChEMBL Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 B 6.6 pKi 251.19 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells B 6.61 pKi 245.47 nM Ki J Med Chem (2004) 47: 2414-2417 [PMID:15115383]
ChEMBL Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay F 6 pEC50 1000 nM EC50 Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
ChEMBL Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor B 6.04 pEC50 912.01 nM EC50 J Med Chem (2004) 47: 2414-2417 [PMID:15115383]

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]