5-OH-DPAT [Ligand Id: 128] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL273273
  • 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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  • 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-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
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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 human dopamine D2L receptor expressed in HEK293 cells B 7.23 pKi 58.8 nM Ki J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Displacement of [3H]spiperone from cloned dopamine D2L receptor expressed in HEK cells B 7.23 pKi 58.8 nM Ki J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL In vitro binding affinity is the ability to displace [3H]spiperone from human Dopamine receptor D2 expressed in CHO-K1 cells B 7.59 pKi 26 nM Ki J. Med. Chem. (1995) 38: 3132-3137 [PMID:7636875]
ChEMBL In vitro binding affinity is the ability to displace [3H]N-0437 from human Dopamine receptor D2 expressed in CHO-K1 cells B 8.22 pKi 6 nM Ki J. Med. Chem. (1995) 38: 3132-3137 [PMID:7636875]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding F 7.39 pEC50 41.2 nM EC50 J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 7.98 pEC50 10.4 nM EC50 Bioorg. Med. Chem. (2009) 17: 3923-3933 [PMID:19427222]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]spiperone from rat D2L dopamine receptor expressed in HEK293 cell membranes after 1 hr B 6.82 pKi 153 nM Ki Bioorg Med Chem (2016) 24: 5088-5102 [PMID:27591013]
ChEMBL Displacement of [3H]spiperone from rat dopamine D2L receptor expressed in HEK293 cells B 7.23 pKi 58.8 nM Ki Bioorg. Med. Chem. (2009) 17: 3923-3933 [PMID:19427222]
ChEMBL Displacement of [3H]spiperone from rat D2 receptor expressed in HEK293 cells B 7.23 pKi 58.8 nM Ki Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Binding affinity against dopamine receptor D2 in rat brain tissue using [3H]spiperone B 7.97 pKi 10.8 nM Ki J. Med. Chem. (1993) 36: 3409-3416 [PMID:8230131]
ChEMBL Tested in vitro for the inhibition of [3H]raclopride binding to Dopamine receptor D2 in rat striatum B 9.15 pKi 0.7 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2759-2764
ChEMBL Potency to displace the specific in vitro binding of [3H]DP-5,6-ADTN to rat striatal membrane B 8.4 pIC50 4 nM IC50 J. Med. Chem. (1988) 31: 2178-2182 [PMID:2903247]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Tested in vitro for the inhibition of [3H]U-86170 binding to Dopamine receptor D3, expressed in cloned CHO cells B 8.36 pKi 4.4 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2759-2764
ChEMBL Displacement of [3H]spiperone from human dopamine D3 receptor expressed in HEK293 cells B 8.87 pKi 1.36 nM Ki J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Displacement of [3H]spiperone from cloned dopamine D3 receptor expressed in HEK cells B 8.87 pKi 1.36 nM Ki J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL In vitro binding affinity is the ability to displace [3H]spiperone from human Dopamine receptor D3 expressed in CHO-K1 cells. B 9.18 pKi 0.66 nM Ki J. Med. Chem. (1995) 38: 3132-3137 [PMID:7636875]
ChEMBL Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding F 8.91 pEC50 1.23 nM EC50 J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding F 9.85 pEC50 0.14 nM EC50 Bioorg. Med. Chem. (2009) 17: 3923-3933 [PMID:19427222]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Displacement of [3H]spiperone from rat D3 dopamine receptor expressed in HEK293 cell membranes after 1 hr B 8.68 pKi 2.07 nM Ki Bioorg Med Chem (2016) 24: 5088-5102 [PMID:27591013]
ChEMBL Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells B 8.87 pKi 1.36 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 8.87 pKi 1.36 nM Ki Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
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 6.46 pKi 344 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 Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand B 5.98 pKi 1040 nM Ki J. Med. Chem. (1993) 36: 3409-3416 [PMID:8230131]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Binding affinity to 5-HT7 receptor (unknown origin) B 6.33 pKi 466 nM Ki J Med Chem (2018) 61: 8475-8503 [PMID:29767995]
5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
GtoPdb - - 8.4 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407]

ChEMBL data shown on this page come from version 28:

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]