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 to SP-FLAG tagged human histamine H3 receptor expressed in HEK293T cells using sodium containing Leibovitz's L-15 medium incubated for 60 min by scintillation counter analysis | B | 7.55 | pKi | 28.18 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 | Displacement of [3H]UR-MN259 from SP-FLAG tagged human histamine H3 receptor expressed in HEK293T cells assessed as inhibition constant incubated for 60 min by scintillation counter analysis | B | 8.24 | pKi | 5.75 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| ChEMBL | Displacement of Clobenpropit-BODIPY-630/650 from Nluc-tagged human histamine H3 receptor expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay | B | 8.3 | pKi | 5.01 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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]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 [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]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]N-methylhistamine from SP-FLAG tagged human histamine H3 receptor expressed in SK-N-MC cells incubated for 40 mins | B | 8.8 | pKi | 1.58 | nM | Ki | ACS Med Chem Lett (2023) 14: 1589-1595 [PMID:37974943] |
| 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 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]
