iodoproxyfan [Ligand Id: 1253] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19010 (Iodoproxyfan) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells | B | 7.39 | pKi | 41 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 951-954 [PMID:11294398] |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells | B | 9.2 | pKi | 0.63 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| GtoPdb | - | - | 10 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 10.3 | pEC50 | 0.05 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells | B | 7.15 | pKi | 71 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 951-954 [PMID:11294398] |
| ChEMBL | In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex | F | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (1996) 39: 1220-1226 [PMID:8632428] |
| ChEMBL | In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex | F | 8.3 | pKi | 5 | 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 | 9 | pKi | 1 | nM | Ki | J Med Chem (1996) 39: 1220-1226 [PMID:8632428] |
| ChEMBL | Histamine H3 receptor affinity of compound was determined in rat cortical membranes using the H3 selective agonist ligand, [3H]N-alpha-methylhistamine | F | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 3017-3022 |
| GtoPdb | - | - | 9.6 | pKi | - | - | - | Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from histamine H3 receptors in homogenates of rat cerebral cortex | B | 8.3 | pKd | 5.01 | nM | Kd | J Med Chem (2001) 44: 1666-1674 [PMID:11356102] |
| 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 | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [3H]histamine from human H4 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.9 | pEC50 | 12.59 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
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]
