mepyramine [Ligand Id: 1227] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL511 (Mepyramine, Pyrilamine)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.95 pKi 1116 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.53 pIC50 2976 nM IC50 DrugMatrix in vitro pharmacology data
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.52 pIC50 300 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.16 pKi 699 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.06 pIC50 879 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.99 pKi 10337.8 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) B 4.9 pIC50 12618.2 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibitory concentration against IKr potassium channel B 5.96 pIC50 1100 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation counting B 8.35 pKi 4.47 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6274-6280 [PMID:21944853]
ChEMBL Displacement of radiolabeled pyrilamine from human histamine H1 receptor B 8.66 pKi 2.2 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting B 8.68 pKi 2.09 nM Ki J. Med. Chem. (2011) 54: 8195-8206 [PMID:22007643]
ChEMBL Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in HEK-293 cells B 8.77 pKi 1.7 nM Ki Eur. J. Med. Chem. (2015) 92: 221-235 [PMID:25557493]
ChEMBL Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells B 8.77 pKi 1.7 nM Ki J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs B 8.8 pKi 1.6 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis B 8.9 pKi 1.26 nM Ki J Med Chem (2016) 59: 9047-9061 [PMID:27643714]
GtoPdb - - 9 pKi - - - J Pharmacol Exp Ther (2002) 302: 328-36 [PMID:12065734];
Eur J Biochem (2004) 271: 2636-46 [PMID:15206929]
ChEMBL Binding affinity to human histamine H1 receptor by radioligand displacement assay B 9.02 pKi 0.95 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting B 9.15 pKi 0.71 nM Ki J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 9.36 pKi 0.43 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Inverse agonist activity at human wild-type histamine H1 receptor N7.45L mutant assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay F 6.8 pIC50 158.49 nM IC50 Nat. Chem. Biol. (2005) 1: 98-103 [PMID:16408006]
ChEMBL Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay F 7.33 pIC50 46.77 nM IC50 J. Med. Chem. (2012) 55: 7054-7060 [PMID:22793499]
ChEMBL Inhibitory activity against human Histamine H1 receptor B 7.9 pIC50 12.59 nM IC50 J. Med. Chem. (2003) 46: 5812-5824 [PMID:14667234]
ChEMBL Inverse agonist activity at human wild-type histamine H1 receptor assessed as NF-kappaB activation after 48 hrs by luciferase reporter gene assay F 8 pIC50 10 nM IC50 Nat. Chem. Biol. (2005) 1: 98-103 [PMID:16408006]
ChEMBL Displacement of radiolabeled pyrilamine from human histamine H1 receptor B 8.21 pIC50 6.2 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.43 pIC50 3.72 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Displacement of [3H]Pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells after 3 hrs B 8.48 pIC50 3.3 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Antagonist activity at human recombinant H1 receptor assessed as inhibition of histamine-induced intracellular Ca2+ release B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2014) 57: 4543-4557 [PMID:24805037]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor in HEK293 cells after 60 mins by scintillation counting B 8.72 pIC50 1.9 nM IC50 J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL Inhibition of histamine H1 receptor B 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Binding affinity to human histamine H1 receptor by radioligand displacement assay B 8.82 pIC50 1.5 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]pyrilamine from human recombinant H1 receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method B 8.85 pIC50 1.4 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Percent inhibition against Histamine H1 receptor at 1 uM B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Binding affinity to human histamine H1 receptor by radioligand displacement assay B 9.09 pIC50 0.82 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in HEK293 cells B 10.85 pIC50 0.01 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells B 8.59 pEC50 2.6 nM EC50 J. Nat. Prod. (2006) 69: 432-435 [PMID:16562853]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting B 8.24 pIC50 5.75 nM IC50 J. Med. Chem. (2012) 55: 7054-7060 [PMID:22793499]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Antagonist activity at histamine H1 receptor in guinea pig jejunum assessed as reduction in histamine-induced contractions B 8.84 pKd 1.45 nM Kd Bioorg. Med. Chem. Lett. (2015) 25: 1436-1442 [PMID:25752982]
ChEMBL Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as histamine-induced contractions F 8.96 pKd 1.1 nM Kd Eur. J. Med. Chem. (2009) 44: 1674-1681 [PMID:18990469]
ChEMBL In vitro for histamine H1 receptor antagonist activity against histamine-induced contractions on isolated guinea pig ileum F 9 pKd 1 nM Kd J. Med. Chem. (1992) 35: 2910-2912 [PMID:1353796]
ChEMBL Antagonism against H1 histamine receptor of guinea pig ileum F 9.07 pKd 0.85 nM Kd Bioorg. Med. Chem. Lett. (1995) 5: 667-672
ChEMBL Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 mins F 9.07 pKd 0.85 nM Kd Bioorg. Med. Chem. Lett. (2011) 21: 6274-6280 [PMID:21944853]
ChEMBL H1-antihistamine activity in guinea pig ileum F 9.1 pKd 0.79 nM Kd J. Med. Chem. (1986) 29: 2262-2267 [PMID:2431143]
ChEMBL H1-antihistamine activity on guinea pig ileum F 9.1 pKd 0.79 nM Kd J. Med. Chem. (1984) 27: 1452-1457 [PMID:6208360]
ChEMBL Antagonist activity at histamine H1 receptor in guinea pig ileum preincubated for 10 mins followed by histamine addition during 30 mins equilibration period with washing every 10 mins B 9.18 pKd 0.66 nM Kd MedChemComm (2019) 10: 234-251
ChEMBL Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand F 9.42 pKd 0.38 nM Kd Bioorg. Med. Chem. Lett. (2003) 13: 1245-1248 [PMID:12657255]
ChEMBL Antagonist activity at histamine H1 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction B 9.5 pKd 0.32 nM Kd Med Chem Res (2013) 22: 1287-1304
ChEMBL In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum F 7.47 pIC50 34 nM IC50 Bioorg. Med. Chem. Lett. (2000) 10: 1277-1279 [PMID:10866399]
ChEMBL Inhibition of guinea pig histamine H1 receptor B 8.82 pIC50 1.5 nM IC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.55 pKi 285 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6 pIC50 997 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.75 pKi 1774 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.55 pIC50 2788 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.23 pKi 592 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.95 pIC50 1130 nM IC50 DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.6 pKi 25 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.33 pIC50 47 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 6.18 pKi 655 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.81 pIC50 1558 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]