imetit [Ligand Id: 1250] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19439 (Imetit) |
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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 | Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
| ChEMBL | Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2021) 64: 11695-11708 [PMID:34309390] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation counting | B | 8.8 | pKi | 1.58 | nM | Ki | Bioorg Med Chem (2009) 17: 3987-3994 [PMID:19414267] |
| ChEMBL | Displacement of [3H]histamine from human H3 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting | B | 8.8 | pKi | 1.58 | 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 | 8.8 | pKi | 1.58 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| ChEMBL | Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem (2011) 19: 2850-2858 [PMID:21498080] |
| ChEMBL | Displacement of [3H[N-alpha-methylhistamine form human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation counting | B | 9.24 | pKi | 0.57 | nM | Ki | J Med Chem (2010) 53: 3840-3844 [PMID:20384344] |
| ChEMBL | Displacement of [3]-RAMH from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation counting | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2019) 62: 1203-1217 [PMID:30629436] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; Biochem J (2001) 355: 279-88 [PMID:11284713]; J Pharmacol Exp Ther (2001) 299: 908-14 [PMID:11714875]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057]; Mol Pharmacol (2001) 59: 420-6 [PMID:11179434] |
| ChEMBL | Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay | F | 8.54 | pEC50 | 2.9 | nM | EC50 | Eur J Med Chem (2020) 191: 112150-112150 [PMID:32105981] |
| ChEMBL | Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2010) 53: 3840-3844 [PMID:20384344] |
| ChEMBL | Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine | B | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2003) 46: 1980-1988 [PMID:12723960] |
| ChEMBL | Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay | F | 9.9 | pEC50 | 0.13 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7191-7199 [PMID:21044842] |
| H3 receptor/Histamine H3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406] | ||||||||
| ChEMBL | Displacement of 3-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone from mouse histamine H3 receptor expressed in HEK293 cells | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4075-4078 [PMID:19553110] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
Eur J Pharmacol (2003) 467: 57-65 [PMID:12706455]; J Neurochem (2004) 90: 1331-8 [PMID:15341517] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
J Pharmacol Exp Ther (2000) 293: 771-8 [PMID:10869375]; Biochem Biophys Res Commun (2001) 280: 75-80 [PMID:11162480]; Eur J Pharmacol (2002) 453: 33-41 [PMID:12393057] |
| ChEMBL | In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex | B | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (1999) 42: 4269-4274 [PMID:10514298] |
| ChEMBL | In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex | B | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (1999) 42: 4269-4274 [PMID:10514298] |
| Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35] | ||||||||
| ChEMBL | Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum. | F | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 77-78 |
| 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 human SK-N-MC cells by liquid scintillation counting | B | 8.2 | pKi | 6.31 | nM | Ki | Bioorg Med Chem (2009) 17: 3987-3994 [PMID:19414267] |
| ChEMBL | Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2 | B | 8.2 | pKi | 6.31 | 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 | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2011) 54: 8136-8147 [PMID:22003888] |
| ChEMBL | Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2008) 51: 3145-3153 [PMID:18459760] |
| ChEMBL | Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem (2011) 19: 2850-2858 [PMID:21498080] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - |
Mol Pharmacol (2001) 59: 420-6 [PMID:11179434]; J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071]; J Pharmacol Exp Ther (2001) 296: 1058-66 [PMID:11181941]; Mol Pharmacol (2001) 59: 434-41 [PMID:11179436] |
| ChEMBL | Inhibition of human Histamine H4 receptor | B | 7.29 | pEC50 | 51 | nM | EC50 | J Med Chem (2003) 46: 1980-1988 [PMID:12723960] |
| 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 | Agonist activity at human histamine H4 receptor | F | 7.9 | pEC50 | 12.59 | nM | EC50 | J Med Chem (2011) 54: 26-53 [PMID:21062081] |
| H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
| H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | J Pharmacol Exp Ther (2001) 299: 121-30 [PMID:11561071] |
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]
