7-OH-DPAT [Ligand Id: 950] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL285755
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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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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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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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 Displacement of [3H]spiperone from cloned dopamine D2L receptor expressed in HEK cells B 6.69 pKi 202 nM Ki J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 6.84 pKi 143 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D2 in Sf 9 cells B 6.85 pKi 142 nM Ki J. Med. Chem. (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL Tested for the inhibitory activity against D2H (high-affinity states) receptor in infected HEK 293 cells. B 6.85 pKi 142 nM Ki J. Med. Chem. (1994) 37: 4245-4250 [PMID:7990123]
GtoPdb - - 7.6 pKi - - - J. Pharmacol. Exp. Ther. (1994) 268: 417-26 [PMID:8301582];
Eur. J. Pharmacol. (1994) 266: 79-85 [PMID:7907989];
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]
ChEMBL Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 8.64 pKi 2.27 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 7.4 pEC50 39.8 nM EC50 J. Med. Chem. (2008) 51: 3005-3019 [PMID:18410082]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
GtoPdb - - 6.2 pKi - - - J. Med. Chem. (1994) 37: 4245-50 [PMID:7990123]
ChEMBL Displacement of [3H]Spiperone from rat dopamine D2L receptor expressed in HEK293 cells B 6.51 pKi 311 nM Ki J. Med. Chem. (2008) 51: 7806-7819 [PMID:19053758]
ChEMBL Displacement of [3H]spiperone from rat D2 receptor expressed in HEK293 cells B 6.51 pKi 311 nM Ki Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Displacement of [3H]spiperone from rat dopamine D2L receptor expressed in HEK293 cells B 6.51 pKi 311 nM Ki Bioorg. Med. Chem. (2009) 17: 3923-3933 [PMID:19427222]
ChEMBL Displacement of [3H]spiperone from rat dopamine D2L receptor expressed in HEK293 cells B 6.69 pKi 202 nM Ki J. Med. Chem. (2008) 51: 3005-3019 [PMID:18410082]
ChEMBL Tested for inhibition of the binding of [125I]NCQ298 to D2 receptor B 6.85 pKi 142 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL Binding affinity against dopamine receptor D2 in rat brain tissue using [3H]spiperone B 7.27 pKi 54 nM Ki J. Med. Chem. (1993) 36: 3409-3416 [PMID:8230131]
ChEMBL Displacement of the radioligand [3H]spiperone from D2 receptor B 7.27 pKi 54 nM Ki J. Med. Chem. (1994) 37: 3263-3273 [PMID:7932553]
ChEMBL Tested in vitro for the inhibition of [3H]raclopride binding to Dopamine receptor D2 in rat striatum B 8.6 pKi 2.5 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2759-2764
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 6.72 pIC50 192 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 6.74 pIC50 180 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Potency to displace the specific in vitro binding of [3H]DP-5,6-ADTN to rat striatal membrane B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1988) 31: 2178-2182 [PMID:2903247]
ChEMBL Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min F 8.73 pEC50 1.88 nM EC50 Med Chem Res (2004) 13: 25-33
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]spiperone from human D3 D3.32E mutant receptor expressed in human HEK293 cells B 5.85 pKi 1400 nM Ki J. Med. Chem. (2008) 51: 6829-6838 [PMID:18834111]
ChEMBL Displacement of [3H]spiperone from human D3 F6.51W mutant receptor expressed in human HEK293 cells B 6.57 pKi 270 nM Ki J. Med. Chem. (2008) 51: 6829-6838 [PMID:18834111]
GtoPdb - - 8.4 pKi 3.98 nM Ki J. Pharmacol. Exp. Ther. (1994) 268: 417-26 [PMID:8301582];
Neuroreport (1995) 6: 329-332 [PMID:7756621];
Eur. J. Pharmacol. (1994) 266: 79-85 [PMID:7907989];
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010];
J. Med. Chem. (1994) 37: 4245-50 [PMID:7990123]
ChEMBL Displacement of [3H]spiperone from human wild type D3 receptor expressed in human HEK293 cells B 8.44 pKi 3.6 nM Ki J. Med. Chem. (2008) 51: 6829-6838 [PMID:18834111]
ChEMBL Tested for the inhibitory activity against Dopamine D3 receptor in infected Sf9 cells B 8.54 pKi 2.9 nM Ki J. Med. Chem. (1994) 37: 4245-4250 [PMID:7990123]
ChEMBL Displacement of [3H]spiperone from cloned dopamine D3 receptor expressed in HEK cells B 8.63 pKi 2.35 nM Ki J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 8.76 pKi 1.75 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 8.83 pKi 1.49 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Tested in vitro for the inhibition of [3H]U-86170 binding to Dopamine receptor D3, expressed in cloned CHO cells B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2759-2764
ChEMBL Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding F 9.27 pEC50 0.53 nM EC50 J. Med. Chem. (2008) 51: 3005-3019 [PMID:18410082]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Tested for binding affinity against dopamine receptor D3 B 9.17 pKd 0.67 nM Kd J. Med. Chem. (1993) 36: 4308-4312 [PMID:8277513]
ChEMBL Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells B 8.21 pKi 6.19 nM Ki Bioorg. Med. Chem. (2009) 17: 3923-3933 [PMID:19427222]
ChEMBL Displacement of [3H]spiperone from rat D3 receptor expressed in HEK293 cells B 8.21 pKi 6.19 nM Ki Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Displacement of [3H]Spiperone from rat dopamine D3 receptor expressed in HEK293 cells B 8.21 pKi 6.19 nM Ki J. Med. Chem. (2008) 51: 7806-7819 [PMID:19053758]
ChEMBL Tested for inhibition of the binding of [125I]NCQ298 to dopamine receptor D3 B 8.54 pKi 2.9 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D3 in Sf 9 cells B 8.54 pKi 2.9 nM Ki J. Med. Chem. (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells B 8.63 pKi 2.35 nM Ki J. Med. Chem. (2008) 51: 3005-3019 [PMID:18410082]
ChEMBL Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. B 8.93 pKi 1.18 nM Ki J. Med. Chem. (1993) 36: 1499-1500 [PMID:8098771]
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 8.9 pIC50 1.25 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting B 8.95 pIC50 1.11 nM IC50 Med Chem Res (2004) 13: 25-33
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells B 6.83 pKi 148 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2759-2764
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Tested in vitro for the inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor, expressed in cloned CHO cells. B 7.33 pKi 47 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2759-2764
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Displacement of the radioligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor B 5.55 pKi 2810 nM Ki J. Med. Chem. (1994) 37: 3263-3273 [PMID:7932553]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand B 5.55 pKi 2800 nM Ki J. Med. Chem. (1993) 36: 3409-3416 [PMID:8230131]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain B 7.14 pKi 72.7 nM Ki J. Med. Chem. (1993) 36: 3161-3165 [PMID:8230102]
ChEMBL Tested for the inhibitory activity against 5-hydroxytryptamine 1A receptor in rat hippocampal B 7.14 pKi 72.7 nM Ki J. Med. Chem. (1994) 37: 4245-4250 [PMID:7990123]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Tested for the inhibitory activity against sigma receptor rat cerebellar B 7.63 pKi 23.2 nM Ki J. Med. Chem. (1994) 37: 4245-4250 [PMID:7990123]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]