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ChEMBL ligand: CHEMBL82298 (Immethridine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]