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ChEMBL ligand: CHEMBL20734 (Emilace, Emonapride, Nemonapride) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | Binding affinity to the alpha-1 adrenergic receptor using a radioligand [3H]prazosin binding assay in rat brain membranes | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (1996) 39: 3723-3738 [PMID:8809161] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]N-methylspiperone from dopamine D2 receptor (unknown origin) | B | 8.58 | pKi | 2.61 | nM | Ki | Bioorg Med Chem Lett (2021) 42: 128047-128047 [PMID:33882273] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Binding affinity to Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 10.8 | pKd | 0.02 | nM | Kd | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Binding affinity to Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 10.85 | pKd | 0.01 | nM | Kd | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
ChEMBL | Binding affinity to dopamine receptor D2 using a [3H]-spiperone binding assay in rat cortical membranes | B | 9.32 | pIC50 | 0.48 | nM | IC50 | J Med Chem (1996) 39: 3723-3738 [PMID:8809161] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Displacement of [3H]-N-Methylspiperone from dopamine D3 receptor (unknown origin) incubated for 90 mins by microbeta counting method | B | 8.93 | pKi | 1.18 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
ChEMBL | Displacement of [3H]-methylspiperone from dopamine D3 receptor (unknown origin) | B | 9.07 | pKi | 0.86 | nM | Ki | Bioorg Med Chem Lett (2021) 42: 128047-128047 [PMID:33882273] |
GtoPdb | - | - | 9.3 | pKi | - | - | - |
Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592] |
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
ChEMBL | Binding affinity to Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 10.19 | pKd | 0.06 | nM | Kd | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Binding affinity to Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 10.22 | pKd | 0.06 | nM | Kd | Med Chem Res (2004) 13: 25-33 |
ChEMBL | Binding affinity to rat Dopamine receptor D3 expressed in CHO cells was determined using [125 I] iodosulpride as radioligand | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand | B | 9.68 | pKd | 0.21 | nM | Kd | J Med Chem (1996) 39: 2764-2772 [PMID:8709107] |
GtoPdb | - | - | 10 | pKd | - | - | - | Synapse (1993) 14: 247-253 [PMID:8248849] |
ChEMBL | Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method | B | 9.07 | pKi | 0.86 | nM | Ki | Bioorg Med Chem (2020) 28: 115578-115578 [PMID:32631561] |
ChEMBL | Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin) | B | 9.12 | pKi | 0.75 | nM | Ki | Bioorg Med Chem Lett (2021) 42: 128047-128047 [PMID:33882273] |
ChEMBL | Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay | B | 7.01 | pIC50 | 98.2 | nM | IC50 | J Med Chem (2019) 62: 5132-5147 [PMID:31021617] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | Binding affinity to serotonin 5-hydroxytryptamine 2A receptors using a radioligand [3H]ketanserin binding assay in rat cortical membranes | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (1996) 39: 3723-3738 [PMID:8809161] |
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
ChEMBL | Displacement of [3H]DTG from sigma2 receptor(unknown origin) | B | 8.14 | pKi | 7.21 | nM | Ki | Bioorg Med Chem Lett (2021) 42: 128047-128047 [PMID:33882273] |
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]