naphazoline [Ligand Id: 5509] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL761 (Nafazair, Nafazolin, Nafazolina, 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 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]
