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 32:
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]
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