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 |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 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-HT1A receptor/Serotonin 1a (5-HT1a) receptor 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/Serotonin 1a (5-HT1a) receptor 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/Serotonin 1b (5-HT1b) receptor 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/Serotonin 1d (5-HT1d) receptor 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/Serotonin 2a (5-HT2a) receptor 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-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] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor 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/Serotonin 5a (5-HT5a) receptor 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/Serotonin 6 (5-HT6) receptor 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/Serotonin 7 (5-HT7) receptor 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/Serotonin 7 (5-HT7) receptor 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] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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 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]
