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 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]
