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 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]