(-)-stepholidine [Ligand Id: 8370] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL487387 (L-(S)-Stepholidine, L-Stepholidine, (-)-Stepholidine)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • coagulation factor III, tissue factor/Coagulation factor III in Human [ChEMBL: CHEMBL4081] [GtoPdb: 3192] [UniProtKB: P13726]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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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]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]
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]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]
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]
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]
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 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]