immepip [Ligand Id: 1251] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL18661 (Immepip) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | Displacement of [125I]aminopotentidine binding to CHO cell membranes expressing human histamine H2 receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (2005) 48: 2100-2107 [PMID:15771452] |
| ChEMBL | Displacement of [125I]aminopotentidine from human histamine H2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting | B | 6 | pKi | >1000 | nM | Ki | Bioorg Med Chem (2010) 18: 5441-5448 [PMID:20541426] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| ChEMBL | Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [3H]N-R-methylhistamine binding to SK-N-MC cell membranes expressing human H3 receptor | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2005) 48: 2100-2107 [PMID:15771452] |
| ChEMBL | Inhibitory activity measured by [3H]- N alpha- methyl-histamine binding to membranes of SK-N-MC cells expressing the human Histamine H3 receptor | B | 9.32 | pKi | 0.48 | nM | Ki | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells | B | 9.32 | pKi | 0.48 | nM | Ki | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| ChEMBL | Displacement of [3H]-NR-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells by liquid scintillation counter | B | 9.32 | pKi | 0.48 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2008) 51: 2944-2953 [PMID:18433114] |
| ChEMBL | Displacement of [3H] (R)-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation counting | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem (2010) 18: 5441-5448 [PMID:20541426] |
| ChEMBL | Displacement of [3H](R)-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells by liquid scintillation counting | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2010) 53: 6445-6456 [PMID:20690643] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; Biochem J (2001) 355: 279-88 [PMID:11284713]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]; Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Med Chem (2003) 46: 5445-57 [PMID:14640553] |
| ChEMBL | Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting | F | 9.17 | pEC50 | 0.67 | nM | EC50 | Bioorg Med Chem (2010) 18: 5441-5448 [PMID:20541426] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding | F | 9.17 | pEC50 | 0.67 | nM | EC50 | J Med Chem (2010) 53: 6445-6456 [PMID:20690643] |
| ChEMBL | Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor | B | 9.88 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor | B | 9.88 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| ChEMBL | Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor | F | 9.9 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2005) 48: 2100-2107 [PMID:15771452] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406] | ||||||||
| GtoPdb | - | - | 9.8 | pKi | - | - | - | Eur J Pharmacol (2003) 467: 57-65 [PMID:12706455] |
| H3 receptor in Rat [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| GtoPdb | - | - | 8.9 | pKi | - | - | - |
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; 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]N-alpha-methylhistamine from histamine H3 receptor in guinea pig brain | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 395-399 [PMID:16246552] |
| 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 CHO-K1 cells after 1 hr by liquid scintillation counting | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem (2010) 18: 5441-5448 [PMID:20541426] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-N-MC cells | B | 7.66 | pKi | 21.88 | nM | Ki | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| ChEMBL | Displacement of [3H]histamine binding to SK-N-MC cell membranes expressing human histamine H4 receptor | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (2005) 48: 2100-2107 [PMID:15771452] |
| ChEMBL | Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 | B | 7.7 | pKi | 19.95 | 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 | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| GtoPdb | - | - | 8 | pKi | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Med Chem (2003) 46: 5445-57 [PMID:14640553]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436] |
| ChEMBL | Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor | B | 7.25 | pEC50 | 56.23 | nM | EC50 | J Med Chem (2003) 46: 5445-5457 [PMID:14640553] |
| ChEMBL | Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H4 receptor | B | 7.25 | pEC50 | 56.23 | nM | EC50 | J Med Chem (2004) 47: 2414-2417 [PMID:15115383] |
| ChEMBL | Agonist activity at human histamine H4 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Agonist activity at human histamine H4 receptor | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
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]
