amthamine [Ligand Id: 4025] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL293762 (Amthamine)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
  • H2 receptor/Histamine H2 receptor in Rat [ChEMBL: CHEMBL4654] [GtoPdb: 263] [UniProtKB: P25102]
  • Histamine H2 receptor in Guinea pig [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
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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
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay F 4.8 pEC50 15848.93 nM EC50 Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
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 5.2 pKi 6309.57 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]
GtoPdb - - 6.4 pEC50 450 nM EC50 ChemMedChem (2009) 4: 232-40 [PMID:19072936]
ChEMBL Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay F 6.72 pEC50 190.55 nM EC50 J Med Chem (2012) 55: 1147-1160 [PMID:22216892]
H2 receptor/Histamine H2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4654] [GtoPdb: 263] [UniProtKB: P25102]
ChEMBL Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand B 4.94 pKd 11481.54 nM Kd Bioorg Med Chem Lett (1994) 4: 1913-1916
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Agonist activity at H2R in spontaneously beating guinea pig right atrium assessed as increase in heart rate F 6.21 pEC50 616.6 nM EC50 J Med Chem (2012) 55: 1147-1160 [PMID:22216892]
ChEMBL Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay F 6.72 pEC50 190.55 nM EC50 J Med Chem (2012) 55: 1147-1160 [PMID:22216892]
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 5.3 pKi 5011.87 nM Ki Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842]

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]