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

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ChEMBL ligand: CHEMBL487387 (L-Stepholidine, (-)-Stepholidine, L-(S)-Stepholidine)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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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 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4081] [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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]