histaprodifen [Ligand Id: 4026] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL275507
  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944]
There should be some charts here, you may need to enable JavaScript!
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
There should be some charts here, you may need to enable JavaScript!
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 5.45 pKd 3548.13 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 4.34 pKd 45708.82 nM Kd J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5.7 pKi - - - J Pharmacol Exp Ther (2005) 314: 1310-21 [PMID:15947036]
ChEMBL Inhibitory activity against human Histamine H1 receptor B 6.1 pIC50 794.33 nM IC50 J. Med. Chem. (2003) 46: 5812-5824 [PMID:14667234]
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 rat aorta (relaxation) at a mepyramine concentration of 100 nM F 8.04 pKd 9.12 nM Kd J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Maximum response (E max) against Histamine H1 receptor in rat aorta F 8.04 pKd 9.12 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 6.07 pEC50 851.14 nM EC50 J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration against histamine H1 receptor in rat aorta B 6.07 pEC50 851.14 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 8.8 pKd 1.58 nM Kd J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Compound was evaluated for mepyramine antagonism effects in guinea pig aorta (contraction) at a mepyramine concentration of 100 nM F 9.01 pKd 0.98 nM Kd J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Antagonism of guinea pig ileum contraction at 100 nM mepyramine F 9.11 pKd 0.78 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 5.71 pEC50 1949.84 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 6.51 pEC50 309.03 nM EC50 J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration for agonist activity in guinea pig ileum whole segment F 6.74 pEC50 181.97 nM EC50 J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]
ChEMBL Effective concentration against histamine H1 receptor in guinea pig ileum B 6.74 pEC50 181.97 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 6.8 pEC50 158.49 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 4.46 pKd 34673.69 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 5.55 pKd 2818.38 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 4.85 pKd 14125.38 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 5.19 pKd 6456.54 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: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
ChEMBL Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 3 receptor of guinea pig F 5.7 pKd >1995.26 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 5.5 pKd >3162.28 nM Kd J. Med. Chem. (2000) 43: 1071-1084 [PMID:10737740]

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]