naphazoline [Ligand Id: 5509] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL761 (Nafazair, Nafazolin, Naphazoline) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts. | F | 7.2 | pEC50 | 63.1 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2871-2874 [PMID:11597419] |
| ChEMBL | In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay | F | 7.2 | pEC50 | 63.1 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 575-579 [PMID:11844675] |
| GtoPdb | - | - | 8.9 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Potency against cloned human alpha 1B adrenoceptor expressed in rat-1 fibroblasts. | F | 5.3 | pEC50 | <5011.87 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2871-2874 [PMID:11597419] |
| ChEMBL | In vitro activation of human Alpha-1B receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay | F | 5.3 | pEC50 | <5011.87 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 575-579 [PMID:11844675] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Potency against cloned human alpha 1D-adrenoceptor expressed in rat-1 fibroblasts. | F | 5.3 | pEC50 | <5011.87 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2871-2874 [PMID:11597419] |
| ChEMBL | In vitro activation of human alpha-1D receptor expressed in rat-1 fibroblasts via calcium using mobilization through the Gq coupled PLC pathway as functional assay | F | 5.3 | pEC50 | <5011.87 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 575-579 [PMID:11844675] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Displacement of [3H]-UK14304 from recombinant human alpha2c adrenergic receptor expressed in CHOK1 cell membranes after 30 mins by scintillation counting analysis | B | 8.64 | pKi | 2.29 | nM | Ki | Bioorg Med Chem (2015) 23: 3991-3999 [PMID:25648685] |
| GtoPdb | inhibition of cAMP production | - | 7.1 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis | F | 7.26 | pEC50 | 54.95 | nM | EC50 | Bioorg Med Chem (2015) 23: 3991-3999 [PMID:25648685] |
| GtoPdb | ERK1/2 phosphorylation | - | 7.69 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 6.91 | pKi | 121.62 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 6.92 | pKi | 121.6 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017] | ||||||||
| ChEMBL | Binding affinity to I1 imidazoline binding site in Rattus norvegicus (rat) PC12 cells | B | 6.61 | pKi | 245.47 | nM | Ki | Med Chem Res (2004) 13: 170-189 |
| α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.8 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
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]
