nemonapride [Ligand Id: 983] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL20734 (Emilace, Nemonaprida, Nemonapride)
  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/D(3) dopamine receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT2A receptor/5-hydroxytryptamine receptor 2A 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]
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/D(2) dopamine 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]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD2 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 8.79 pKi 1.62 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD2 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 8.79 pKi 1.62 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
D2 receptor/D(2) dopamine 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/D(3) dopamine 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/D(3) dopamine 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/D(4) dopamine 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 DRD4 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 8.98 pKi 1.04 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
ChEMBL Displacement of 3H-N-Methylspiperone from DRD4 in human HEK293T cells membrane assessed as inhibition constant incubated for 2 hrs by radioligand competition assay B 8.99 pKi 1.02 nM Ki Science (2017) 358: 381-386 [PMID:29051383]
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]
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 36:

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]