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 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]
