(-)-sulpiride [Ligand Id: 958] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267044 (Lesuride, Levobren, Levopraid, Levopride, Levosulpiride, L-sulpiride, S-(-)-sulpiride, (-)-sulpiride, Sulpiride, (-)-, Sulpiride l-form, Sulpiride, (s)-)
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement. B 4.3 pKi 50000 nM Ki Bioorg Med Chem Lett (1999) 9: 841-846 [PMID:10206547]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2L stably expressed in CHO cells B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL Binding affinity towards human Dopamine receptor D2 (long) by [3H]-spiperone displacement. B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (1999) 9: 841-846 [PMID:10206547]
ChEMBL In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D2 short form expressed in CHO cells B 7.29 pKi 51 nM Ki Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL Binding affinity towards human Dopamine receptor D2 (short) by [3H]-spiperone displacement. B 7.29 pKi 51 nM Ki Bioorg Med Chem Lett (1999) 9: 841-846 [PMID:10206547]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 7.37 pKi 43 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 8 pKi 10 nM Ki J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 6.89 pIC50 128 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat B 7.41 pKi 39 nM Ki J Med Chem (1987) 30: 2099-2104 [PMID:2889830]
ChEMBL Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI B 7.41 pKi 39 nM Ki J Med Chem (1992) 35: 2355-2363 [PMID:1535660]
ChEMBL Binding affinity towards dopamine receptor D2 using as [3H]-spiperone radioligand. B 7.54 pKi 29 nM Ki J Med Chem (1991) 34: 261-267 [PMID:1825115]
ChEMBL Binding affinity towards dopamine receptor D2 by displacing [3H]spiperone radioligand in rat striatum B 7.69 pKi 20.6 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]
ChEMBL Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 B 8.16 pKi 6.9 nM Ki J Med Chem (1990) 33: 1155-1163 [PMID:1969484]
ChEMBL Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor F 6.63 pIC50 233 nM IC50 J Med Chem (1992) 35: 2355-2363 [PMID:1535660]
ChEMBL In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes. B 6.68 pIC50 210 nM IC50 J Med Chem (1990) 33: 1155-1163 [PMID:1969484]
ChEMBL Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor B 6.77 pIC50 170 nM IC50 J Med Chem (1992) 35: 2355-2363 [PMID:1535660]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells B 7.06 pKi 88 nM Ki Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL Binding affinity towards human dopamine D3 receptor by [3H]spiperone displacement. B 7.06 pKi 88 nM Ki Bioorg Med Chem Lett (1999) 9: 841-846 [PMID:10206547]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 7.38 pKi 42 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 7.7 pKi 20 nM Ki J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.91 pIC50 123 nM IC50 DrugMatrix in vitro pharmacology data
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells B 5.68 pKi 2100 nM Ki Bioorg Med Chem Lett (2000) 10: 2041-2044 [PMID:10987445]
ChEMBL Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement. B 5.68 pKi 2100 nM Ki Bioorg Med Chem Lett (1999) 9: 841-846 [PMID:10206547]
GtoPdb - - 7.7 pKi 20 nM Ki J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592];
Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990]
myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164]
ChEMBL Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins B 5.11 pIC50 7680 nM IC50 J Med Chem (2017) 60: 6563-6586 [PMID:28671460]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus B 6 pKi >1000 nM Ki J Med Chem (1992) 35: 552-558 [PMID:1346653]

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]