SB 258719 [Ligand Id: 281] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12264 (SB-258719) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards adrenergic alpha-1B receptors | B | 4.8 | pKi | <15848.93 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human Dopamine receptor D2 in CHO cells using [125I]iodosulpiride. | B | 5.4 | pKi | 3981.07 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| ChEMBL | Displacement of [3H]raclopride from human dopamine receptor D2A expressed in mouse Ltk cells | B | 5.4 | pKi | 3981 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human Dopamine receptor D3 in CHO cells using [125I]iodosulpiride. | B | 5.4 | pKi | 3981.07 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1A receptor in HEK 293 cells using [3H]8-OH-DPAT. | B | 5.1 | pKi | <7943.28 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in CHO cells | B | 5.1 | pKi | >7943 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| ChEMBL | Antagonist activity at 5-HT1A receptor (unknown origin) | B | 5.52 | pKi | >3000 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT | B | 5.3 | pKi | <5011.87 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1D receptor in CHO cells using [3H]5-HT. | B | 5.5 | pKi | 3162.28 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1E receptor in CHO cells using [3H]5-HT. | B | 4.8 | pKi | <15848.93 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 1F receptor in CHO cells using [3H]5-HT. | B | 5.2 | pKi | <6309.57 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 2A receptor in HEK293 cells using [3H]-ketanserin. | B | 4.8 | pKi | <15848.93 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 2B receptors in HEK293 cells using [3H]5-HT. | B | 5.3 | pKi | <5011.87 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 2C receptor in HEK293 cells using [3H]mesulergine. | B | 4.8 | pKi | <15848.93 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards 5-hydroxytryptamine 4 receptor in guinea pig hippocampus using [125I]SB-207710. | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]5-LSD. | B | 4.8 | pKi | <15848.93 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD | B | 7.49 | pKi | 32 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2451-2454 [PMID:12161155] |
| GtoPdb | - | - | 7.5 | pKi | 31.6 | nM | Ki | Br J Pharmacol (1998) 124: 1300-6 [PMID:9720804] |
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 7 receptor expressed in HEK 293 cells using [3H]5-CT. | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1097-1100 [PMID:10843226] |
| ChEMBL | The compound was tested for its binding affinity towards cloned human 5-hydroxytryptamine 7 receptor in HEK 293 cells using [3H]5-CT. | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (1998) 41: 655-657 [PMID:9513592] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
| ChEMBL | Binding affinity to 5HT7 receptor (unknown origin) | B | 7.5 | pKi | 31.6 | nM | Ki | Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835] |
| ChEMBL | Binding affinity to 5-HT7 receptor (unknown origin) | B | 7.5 | pKi | 31.6 | nM | Ki | J Med Chem (2018) 61: 8475-8503 [PMID:29767995] |
| ChEMBL | Antagonist activity at 5-HT7 receptor (unknown origin) | B | 7.5 | pKi | 31.6 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand. | B | 7.1 | pKi | 79.43 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
| ChEMBL | Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells | B | 7.5 | pKi | 31.6 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
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]
