1-naphthylpiperazine [Ligand Id: 3] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL277120
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Mouse [ChEMBL: CHEMBL3597] [GtoPdb: 10] [UniProtKB: P30966]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
  • 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
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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: 377374373376375] [UniProtKB: A5X5Y0O95264P46098Q70Z44Q8WXA8]
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 34:

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]