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]
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. U.S.A. (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. U.S.A. (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. U.S.A. (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. U.S.A. (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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]