mepyramine [Ligand Id: 1227] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL511 (Mepyramine, NSC-13136, Pyrilamine) |
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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 | F | 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 [PMID:30881612] |
| 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 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]
