SB357134 [Ligand Id: 3235] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL329383 (SB-357134) |
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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 | Compound was evaluated for binding affinity against Alpha-1B adrenergic receptor | B | 5.1 | pKi | >7943.28 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against Dopamine receptor D2 in CHO cells using [125I]iodosulpiride as the radioligand | B | 5.3 | pKi | >5011.87 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against Dopamine receptor D3 in CHO cells using [125I]iodosulpiride as the radioligand | B | 5.3 | pKi | >5011.87 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1A receptor in HEK 293 cells using [3H]8-OH-DPAT as the radioligand | B | 5.2 | pKi | >6309.57 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as the radioligand | B | 5.4 | pKi | >3981.07 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1D receptor in CHO cells using [3H]5-HT as the radioligand | B | 5.4 | pKi | >3981.07 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1E receptor in CHO cells using [3H]5-HT as the radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1F receptor in CHO cells using [3H]-5-HT as the radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 2A receptor in HEK 293 cells using [3H]ketanserin as the radioligand | B | 5.1 | pKi | >7943.28 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-HT2B receptor in HEK 293 cells using [3H]5-HT as the radioligand | B | 5.4 | pKi | >3981.07 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 2C receptor in HEK 293 cells using [3H]mesulergine as the radioligand | B | 5.3 | pKi | >5011.87 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Compound was evaluated for the binding affinity against human cloned 5-hydroxytryptamine 4 receptor in HeLa cells using [3H]-LSD as the radioligand | B | 5.3 | pKi | >5011.87 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| GtoPdb | - | - | 8.5 | pKi | - | - | - | Bioorg Med Chem Lett (2001) 11: 55-8 [PMID:11140733] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2005) 48: 4216-4219 [PMID:15974573] |
| ChEMBL | Binding affinity against human 5-hydroxytryptamine 6 receptor | B | 8.5 | pKi | 3.16 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713] |
| ChEMBL | Binding affinity against 5 Hydroxy tryptamine 6 receptor | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826] |
| ChEMBL | Binding affinity towards [3H]LSD-labeled human 5-hydroxytryptamine 6 receptor | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2014) 57: 7160-7181 [PMID:24850589] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]-5-CT from human 5-hydroxytryptamine 7 receptor expressed in HEK-293 cells | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 55-58 [PMID:11140733] |
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]
