5-OH-DPAT [Ligand Id: 128] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL273273 |
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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 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]
