SB357134 [Ligand Id: 3235] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL329383
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/5-hydroxytryptamine receptor 1F in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • α1B-adrenoceptor/Alpha-1B adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 1D 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/5-hydroxytryptamine receptor 1E 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/5-hydroxytryptamine receptor 1F 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2B 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 4 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/5-hydroxytryptamine receptor 6 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/5-hydroxytryptamine receptor 7 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]
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/D(2) dopamine 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/D(3) dopamine 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]

ChEMBL data shown on this page come from version 36:

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]