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 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]
