SB656104 [Ligand Id: 3237] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL95104 (SB-656104) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for Alpha 1B adrenergic receptor | B | 6.66 | pKi | 218.78 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1A receptor in HEK 293 using [3H]5-CT as a radioligand | B | 6.25 | pKi | 562.34 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr | B | 6.6 | pKi | 250 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand | B | 6.2 | pKi | 630.96 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1D receptor in CHO using [3H]5-HT as a radioligand | B | 7.6 | pKi | 25.12 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1E receptor in CHO using [3H]5-HT as a radioligand | B | 5.3 | pKi | <5011.87 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1F receptor in CHO using [3H]5-HT as a radioligand | B | 5.7 | pKi | <1995.26 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2A receptor in HEK 293 using [3H]ketanserin as a radioligand | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2B receptor in HEK 293 using [3H]ketanserin as a radioligand | B | 7.04 | pKi | 91.2 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 2C receptor in HEK 293 using [3H]mesulergine as a radioligand | B | 6.57 | pKi | 269.15 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Compound was tested for its binding affinity for 5-hydroxytryptamine 4 receptor | B | 5.72 | pKi | 1905.46 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand ) | B | 6.74 | pKi | 181.97 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Compound was tested for its binding affinity in 5-hydroxytryptamine 6 receptor (using human cloned receptors in HeLa and [3H]LSD as a radioligand ) | B | 6.07 | pKi | 851.14 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 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-HT7b receptor expressed in HEK293 cells after 1 hr | B | 8.49 | pKi | 3.2 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]5-CT from recombinant human 5-HT7 receptor expressed in COS-7 cell membranes after 30 mins by liquid scintillation counting method | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2418-2421 [PMID:29910079] |
| GtoPdb | - | - | 8.7 | pKi | 1.9 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-4 [PMID:12392747] |
| ChEMBL | Compound was tested for its binding affinity in 5-hydroxytryptamine 7 receptor (using human cloned receptors in HEK 293 and [3H]5-CT as a radioligand ) | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 3341-3344 [PMID:12392747] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity for rat serotonin 5-HT7 receptor expressed in Sf9 cells using [3H]5-HT radioligand | B | 8.7 | pKi | 1.99 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 747-750 [PMID:15664850] |
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]
