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]
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  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
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  • 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]
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  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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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 33:

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]