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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
