nemonapride [Ligand Id: 983] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL20734 (Emilace, Emonapride, Nemonapride) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 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]
