histaprodifen [Ligand Id: 4026] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275507 |
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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 | 5.45 | 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: 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 | 5.7 | 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 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]
