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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]