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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 |
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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 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]