(-)-stepholidine [Ligand Id: 8370] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL487387 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A 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] |
| 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] |
| D1 receptor/D(1A) dopamine 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]SCH-23390 from human dopamine D1 receptor assessed as inhibition constant | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| GtoPdb | - | - | 8.29 | pKi | 5.1 | nM | Ki | Psychopharmacology (Berl.) (2015) 232: 917-30 [PMID:25231919] |
| ChEMBL | Binding affinity to D1 receptor (unknown origin) assessed as inhibition constant | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (2024) 67: 12463-12484 [PMID:39038276] |
| 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/D(1A) dopamine 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] |
| D5 receptor/D(1B) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Binding affinity to D5 receptor (unknown origin) assessed as inhibition constant | B | 8.24 | pKi | 5.8 | nM | Ki | J Med Chem (2024) 67: 12463-12484 [PMID:39038276] |
| GtoPdb | - | - | 8.24 | pKi | 5.8 | nM | Ki | Psychopharmacology (Berl.) (2015) 232: 917-30 [PMID:25231919] |
| 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] |
| D2 receptor/D(2) dopamine 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]N-methylspiperone from human dopamine D2 receptor assessed as inhibition constant | B | 6.01 | pKi | 974 | nM | Ki | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| 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] |
| ChEMBL | Binding affinity to D2 receptor (unknown origin) assessed as inhibition constant | B | 7.94 | pKi | 11.6 | nM | Ki | J Med Chem (2024) 67: 12463-12484 [PMID:39038276] |
| 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/D(3) dopamine 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] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor assessed as inhibition constant | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| ChEMBL | Binding affinity to D3 receptor (unknown origin) assessed as inhibition constant | B | 7.63 | pKi | 23.4 | nM | Ki | J Med Chem (2024) 67: 12463-12484 [PMID:39038276] |
| D3 receptor/D(3) dopamine 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/D(4) dopamine 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] |
| ChEMBL | Binding affinity to D4 receptor (unknown origin) assessed as inhibition constant | B | 5.84 | pKi | 1453 | nM | Ki | J Med Chem (2024) 67: 12463-12484 [PMID:39038276] |
| coagulation factor III, tissue factor/Tissue factor 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] |
ChEMBL data shown on this page come from version 36:
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]
