1-naphthylpiperazine [Ligand Id: 3] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL277120 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | J Med Chem (1997) 40: 3974-8 [PMID:9397179] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.03 | pKi | 9.23 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| ChEMBL | Receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor in HeLa cells | B | 8.04 | pKi | 9.2 | nM | Ki | J Med Chem (1997) 40: 3974-3978 [PMID:9397179] |
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Displacement of [3H]2-(di-N-propylamino)-8-hydroxytetralin from central 5-hydroxytryptamine 1A receptor recognition sites in rat frontal cortex homogenates. | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (1995) 38: 1942-1954 [PMID:7783126] |
| ChEMBL | Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (1988) 31: 1968-1971 [PMID:3172131] |
| ChEMBL | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | B | 7.96 | pKi | 10.96 | nM | Ki | J Med Chem (1996) 39: 126-134 [PMID:8568799] |
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
J Med Chem (1997) 40: 3974-8 [PMID:9397179]; Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658]; J Neurochem (1996) 67: 2096-103 [PMID:8863519] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand | B | 7.97 | pKi | 10.6 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| ChEMBL | Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells | B | 8 | pKi | 10.1 | nM | Ki | J Med Chem (1997) 40: 3974-3978 [PMID:9397179] |
| ChEMBL | The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Antagonist | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| ChEMBL | Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation | F | 6 | pEC50 | >1000 | nM | EC50 | J Med Chem (1997) 40: 3974-3978 [PMID:9397179] |
| 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
J Med Chem (1997) 40: 3974-8 [PMID:9397179]; Proc Natl Acad Sci USA (1992) 89: 3630-4 [PMID:1565658] |
| ChEMBL | Receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor in Cos-7 cells | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (1997) 40: 3974-3978 [PMID:9397179] |
| ChEMBL | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1D receptor using [3H]-5-CT as radioligand | B | 8.21 | pKi | 6.18 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1407-1412 [PMID:9871775] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Inhibitory concentration against 5-hydroxytryptamine 2 receptor | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity for rodent 5-hydroxytryptamine 5A receptor | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966] | ||||||||
| ChEMBL | Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxy tryptamine 6 receptor | B | 6.92 | pKi | 120 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [125I]-2-iodo LSD as radioligand | B | 6.98 | pKi | 104 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 6 receptor | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Mol Pharmacol (1993) 43: 320-7 [PMID:7680751] |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - | J Biol Chem (1993) 268: 23422-6 [PMID:8226867] |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Displacement of [3H]LSD from rat kidney proximal convoluted tubule 5HT7R expressed in COS7 cells | B | 7.08 | pKi | 83 | nM | Ki | J Med Chem (2012) 55: 6375-6380 [PMID:22738316] |
| GtoPdb | - | - | 7.7 | pKi | - | - | - | J Biol Chem (1993) 268: 18200-4 [PMID:8394362] |
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 7 receptor. | B | 7.74 | pKi | 18.2 | nM | Ki | J Med Chem (2003) 46: 5365-5374 [PMID:14640545] |
| D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Inhibitory concentration against dopamine receptor D2 | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| Neutrophil cytosol factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1613743] [UniProtKB: P14598] | ||||||||
| ChEMBL | Binding affinity to immobilized recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by SPR assay | B | 3.44 | pKd | 366000 | nM | Kd | J Med Chem (2020) 63: 1156-1177 [PMID:31922756] |
| ChEMBL | Covalent inhibition of recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells interaction with Cy5-p22phox149-162 incubated for 10 mins by fluorescence polarization competition assay | B | 2.82 | pKi | 1520000 | nM | Ki | J Med Chem (2020) 63: 1156-1177 [PMID:31922756] |
| 5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| ChEMBL | Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells | B | 6.76 | pKi | 175 | nM | Ki | J Med Chem (1996) 39: 4017-4026 [PMID:8831767] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Binding affinity towards sigma receptor in guinea pig brain membranes using [3H]DTG as radioligand | B | 5.57 | pKi | 2720 | nM | Ki | J Med Chem (1991) 34: 3360-3365 [PMID:1662725] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - |
J Neurochem (1996) 67: 2096-103 [PMID:8863519]; Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596] |
| 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| GtoPdb | - | - | 7.3 | pKi | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Neuropharmacology (1997) 36: 569-76 [PMID:9225282] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 9 | pKi | - | - | - |
Mol Pharmacol (1994) 46: 227-34 [PMID:8078486]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 17-24 [PMID:9459568] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Mol Pharmacol (1994) 46: 227-34 [PMID:8078486]; Mol Pharmacol (1993) 43: 419-26 [PMID:8450835] |
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]
