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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 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]