(-)-stepholidine [Ligand Id: 8370] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL487387 (L-(S)-Stepholidine, L-Stepholidine, (-)-Stepholidine) |
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Displacement of [125I]-BE2254 from Wistar rat alpha1A adrenoceptor after 20 mins | B | 5.65 | pKi | 2238.72 | nM | Ki | J Med Chem (2016) 59: 9489-9502 [PMID:27709945] |
| coagulation factor III, tissue factor/Coagulation factor III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4081] [GtoPdb: 3192] [UniProtKB: P13726] | ||||||||
| ChEMBL | Inhibition of tissue factor procoagulant activity in LPS-stimulated human THP1 cells preincubated for 1 hr before LPS addition measured after 5 hrs | B | 6.98 | pIC50 | 104.58 | nM | IC50 | Bioorg Med Chem (2013) 21: 62-69 [PMID:23199480] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis | B | 7.91 | pKi | 12.29 | nM | Ki | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells | B | 8.21 | pKi | 6.23 | nM | Ki | Bioorg Med Chem (2012) 20: 4862-4871 [PMID:22748706] |
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem (2009) 17: 6898-6907 [PMID:19744859] |
| ChEMBL | Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method | B | 8.23 | pKi | 5.9 | nM | Ki | Eur J Med Chem (2017) 125: 255-268 [PMID:27688181] |
| ChEMBL | Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346] |
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells | B | 7.91 | pIC50 | 12.29 | nM | IC50 | Bioorg Med Chem (2012) 20: 4862-4871 [PMID:22748706] |
| ChEMBL | Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity | F | 4.39 | pEC50 | 41100 | nM | EC50 | Bioorg Med Chem (2012) 20: 4862-4871 [PMID:22748706] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells by scintillation counting | B | 6.01 | pKi | 974 | nM | Ki | Bioorg Med Chem (2009) 17: 6898-6907 [PMID:19744859] |
| ChEMBL | Displacement of [3H]Spiperone from D2 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis | B | 6.98 | pKi | 105.41 | nM | Ki | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
| ChEMBL | Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells | B | 7.25 | pKi | 56.17 | nM | Ki | Bioorg Med Chem (2012) 20: 4862-4871 [PMID:22748706] |
| GtoPdb | - | - | 7.94 | pKi | 11.6 | nM | Ki | Psychopharmacology (Berl.) (2015) 232: 917-30 [PMID:25231919] |
| ChEMBL | Displacement of [3H]spiperone from dopamine D2 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter | B | 7.96 | pKi | 11 | nM | Ki | Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346] |
| ChEMBL | Antagonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of quinpirole | F | 5.36 | pIC50 | 4380 | nM | IC50 | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
| ChEMBL | Displacement of [3H]Spiprone from human dopamine D2 receptor expressed in HEK293 cells | B | 6.98 | pIC50 | 105.41 | nM | IC50 | Bioorg Med Chem (2012) 20: 4862-4871 [PMID:22748706] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]Spiperone from D3 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis | B | 7.05 | pKi | 90.02 | nM | Ki | Bioorg Med Chem (2014) 22: 5838-5846 [PMID:25308766] |
| ChEMBL | Binding affinity to dopamine D3 receptor (unknown origin) by PDSP assay | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem (2016) 24: 2060-2071 [PMID:27032890] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method | B | 7.52 | pKi | 30 | nM | Ki | Eur J Med Chem (2017) 125: 255-268 [PMID:27688181] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in CHO cells by scintillation counting | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem (2009) 17: 6898-6907 [PMID:19744859] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting | B | 5.43 | pKi | 3748 | nM | Ki | Bioorg Med Chem (2009) 17: 6898-6907 [PMID:19744859] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting | B | 8.36 | pKi | 4.4 | nM | Ki | Bioorg Med Chem (2009) 17: 6898-6907 [PMID:19744859] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor (unknown origin) expressed in HEK293 cells by liquid scintillation counter | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem (2013) 21: 856-868 [PMID:23332346] |
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]
