SB656104 [Ligand Id: 3237] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL95104 (SB-656104)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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  • 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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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 32:

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]