methylhistaprodifen [Ligand Id: 1205] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL275035
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-1d adrenergic receptorpKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
Created with Highcharts 10.3.3ValuesChart context menuBeta-1 adrenergic receptorpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig0123456Highcharts.com
  • H1 receptor in Human [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]
Created with Highcharts 10.3.3ValuesChart context menuH1 receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 RatpKd Guinea pigpKi Guinea pigpIC50 Guinea​pigpEC50 Guinea​pig0246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuHistamine H2 receptorpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuHistamine H3 receptorpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig01234567Highcharts.com
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
Created with Highcharts 10.3.3ValuesChart context menuMuscarinic acetylcholine receptor M3pKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig0123456Highcharts.com
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 1b (5-HT1b) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 2a (5-HT2a) receptorpKd RatpKi RatpIC50 RatpEC50 Rat0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 3 (5-HT3) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 4 (5-HT4) receptorpKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
ChEMBL Compound was evaluated for its antagonist affinity towards Alpha-1D adrenergic receptor of rat F 5.24 pKd 5754.4 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
ChEMBL Compound was evaluated for its antagonist affinity towards Beta-1 adrenergic receptor of guinea pig F 4.84 pKd 14454.4 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 6.4 pKi 398 nM Ki J Pharmacol Exp Ther (2003) 305: 1104-15 [PMID:12626648]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (relaxation) at a mepyramine concentration of 100 nM F 8.02 pKd 9.55 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Maximum response (E max) against Histamine H1 receptor in guinea pig ileum F 8.02 pKd 9.55 nM Kd J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
ChEMBL Effective concentration for agonism activity in relaxed rat aortic rings with intact endothelium, submaximally precontracted with 15.8 nM U-46,619 F 6.8 pEC50 158.49 nM EC50 J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration against histamine H1 receptor in rat aorta B 6.8 pEC50 158.49 nM EC50 J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM F 8.75 pKd 1.78 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Antagonism of guinea pig ileum contraction at 100 nM mepyramine F 8.87 pKd 1.35 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Antagonism of guinea pig ileum contraction at 100 nM mepyramine F 9.13 pKd 0.74 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration for agonism activity in endothelium-denuded guinea pig aortic segment F 6.31 pEC50 489.78 nM EC50 J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration for agonism activity in Endothelium-Denuded guinea pig aortic segment F 7.11 pEC50 77.62 nM EC50 J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration for agonist activity in guinea pig ileum whole segment F 7.24 pEC50 57.54 nM EC50 J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration against histamine H1 receptor in guinea pig ileum B 7.24 pEC50 57.54 nM EC50 J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
ChEMBL Effective concentration against histamine H1 receptor in endothelium-Denuded rings of guinea pig Aorta B 7.4 pEC50 39.81 nM EC50 J Med Chem (2003) 46: 5458-5470 [PMID:14640554]
Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
ChEMBL Compound was evaluated for its antagonist affinity towards Histamine H2 receptor of guinea pig F 4.9 pKd 12589.25 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
Histamine H3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5076] [UniProtKB: Q9JI35]
ChEMBL Compound was evaluated for its antagonist affinity towards Histamine H3 receptor of guinea pig F 5.8 pKd >1584.89 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Compound was evaluated for its antagonist affinity towards Muscarinic acetylcholine receptor M3 of guinea pig F 5.45 pKd 3548.13 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig F 5.09 pKd 8128.31 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 2A receptor of rat F 5.39 pKd 4073.8 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8]
ChEMBL Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 3 receptor of guinea pig F 5.8 pKd >1584.89 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 4 receptor of rat F 5.8 pKd >1584.89 nM Kd J Med Chem (2000) 43: 1071-1084 [PMID:10737740]

ChEMBL data shown on this page come from version 35:

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]