[3H]N-methylspiperone [Ligand Id: 196] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267932 (3-n-methylspiperone, N-methylspiroperidol) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity to human frontal cortex homogenate 5-HT2A by ketanserin assay | B | 8.06 | pKi | 8.8 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| GtoPdb | - | - | 9.1 | pKd | - | - | - | Mol Pharmacol (2000) 58: 877-86 [PMID:11040033] |
| ChEMBL | Binding affinity to rat frontal cortex homogenate 5-HT2A by ketanserin assay | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Displacement of [3H]prazosin from rat cerebral cortex alpha1 adrenergic receptor | B | 8 | pIC50 | 10.1 | nM | IC50 | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Affinity constant of compound was evaluated in human brain | B | 10.01 | pKd | 0.1 | nM | Kd | J Med Chem (1988) 31: 1039-1043 [PMID:2966245] |
| ChEMBL | Binding affinity to DRD2 in human HEK293T cells membrane assessed as dissociation constant incubated for 2 hrs by radioligand saturation assay | B | 10.14 | pKd | 0.07 | nM | Kd | Science (2017) 358: 381-386 [PMID:29051383] |
| ChEMBL | Binding affinity to DRD2 in human HEK293T cells membrane assessed as dissociation constant incubated for 2 hrs by radioligand saturation assay | B | 10.15 | pKd | 0.07 | nM | Kd | 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 | 9.34 | pKi | 0.46 | 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 | 9.34 | pKi | 0.46 | nM | Ki | Science (2017) 358: 381-386 [PMID:29051383] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 9.88 | pKi | 0.13 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
| D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Evaluated in vivo for the affinity towards Dopamine receptor D2 of rat striatal tissue | B | 10.01 | pKd | 0.1 | nM | Kd | J Med Chem (1990) 33: 171-178 [PMID:2136916] |
| ChEMBL | Binding affinity towards Dopamine receptor D2 by displacing [3H]spiperone | B | 9.93 | pKi | 0.12 | nM | Ki | J Med Chem (1992) 35: 423-430 [PMID:1531364] |
| GtoPdb | - | - | 10.7 | pKi | - | - | - | Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
| ChEMBL | Displacement of [3H]-spiperone from rat striatum D2 receptor | B | 9.64 | pIC50 | 0.23 | nM | IC50 | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| 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 human dopamine D3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 9.58 | pKi | 0.27 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
| D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Binding affinity to human DRD4 fused with E.coli BRIL expressed in Sf9 insect cells assessed as dissociation constant incubated for 2 hrs by radioligand saturation assay | B | 8.52 | pKd | 3.02 | nM | Kd | Science (2017) 358: 381-386 [PMID:29051383] |
| ChEMBL | Binding affinity to human DRD4 fused with E.coli BRIL expressed in Sf9 insect cells assessed as dissociation constant incubated for 2 hrs by radioligand saturation assay | B | 8.53 | pKd | 2.98 | nM | Kd | Science (2017) 358: 381-386 [PMID:29051383] |
| ChEMBL | Binding affinity to DRD4 in human HEK293T cells membrane assessed as dissociation constant incubated for 2 hrs by radioligand saturation assay | B | 9.32 | pKd | 0.48 | nM | Kd | Science (2017) 358: 381-386 [PMID:29051383] |
| ChEMBL | Binding affinity to DRD4 in human HEK293T cells membrane assessed as dissociation constant incubated for 2 hrs by radioligand saturation assay | B | 9.32 | pKd | 0.48 | nM | Kd | 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 | 8.82 | pKi | 1.5 | 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 | 8.85 | pKi | 1.41 | nM | Ki | Science (2017) 358: 381-386 [PMID:29051383] |
| D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
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]
