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ChEMBL ligand: CHEMBL12608 (Impromidine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
ChEMBL | Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity | F | 5.47 | pKd | 3388.44 | nM | Kd | J Med Chem (2008) 51: 7193-7204 [PMID:18950149] |
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 | 6.3 | pKi | 501.19 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
GtoPdb | - | - | 7.2 | pKi | - | - | - | J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198] |
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747] | ||||||||
ChEMBL | Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity | F | 7.7 | pEC50 | 19.95 | nM | EC50 | J Med Chem (2008) 51: 7193-7204 [PMID:18950149] |
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Binding affinity to the human histamine H3 receptor | B | 7.17 | pKi | 67 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
GtoPdb | - | - | 7.2 | pKi | - | - | - | Mol Pharmacol (2001) 59: 420-6 [PMID:11179434] |
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
ChEMBL | In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex | F | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (1996) 39: 1220-1226 [PMID:8632428] |
ChEMBL | Binding affinity towards Histamine H3 receptor on synaptosomes from rat cerebral cortex | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (1996) 39: 1220-1226 [PMID:8632428] |
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 | 7.6 | pKi | 25.12 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
GtoPdb | - | - | 7.9 | pKi | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036] |
ChEMBL | Binding affinity to the human histamine H4 receptor | B | 7.91 | pKi | 12.3 | nM | Ki | J Med Chem (2003) 46: 3957-3960 [PMID:12954048] |
ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.6 | pEC50 | 25.12 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
GtoPdb | - | - | 5.2 | pKi | - | - | - | J Pharmacol Exp Ther (2006) 317: 139-46 [PMID:16394198] |
ChEMBL data shown on this page come from version 32:
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]