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ChEMBL ligand: CHEMBL293762 (Amthamine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]