impromidine [Ligand Id: 1226] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12608 (Impromidina, Impromidine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 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]
