imetit [Ligand Id: 1250] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL19439 (Imetit)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Mouse [ChEMBL: CHEMBL3263] [GtoPdb: 264] [UniProtKB: P58406]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
  • Histamine H3 receptor in Guinea pig [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
  • H4 receptor in Mouse [GtoPdb: 265] [UniProtKB: Q91ZY2]
  • H4 receptor in Rat [GtoPdb: 265] [UniProtKB: Q91ZY1]
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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 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]