EMDT [Ligand Id: 12] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267615 |
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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 its binding affinity towards human 5-hydroxytryptamine 1A receptor | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - | J Med Chem (2000) 43: 1011-8 [PMID:10715164] |
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1A receptor in rat | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] | ||||||||
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1B receptor in rat | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | J Med Chem (2000) 43: 1011-8 [PMID:10715164] |
| ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1D receptor | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 1D receptor in calf | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1E receptor | B | 6.28 | pKi | 520 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| GtoPdb | - | - | 6.3 | pKi | - | - | - | J Med Chem (2000) 43: 1011-8 [PMID:10715164] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 2A receptor in human | B | 6.21 | pIC50 | 620 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 2C receptor in human | B | 5.26 | pIC50 | 5500 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity towards rat 5-hydroxytryptamine 2C receptor | B | 5.74 | pKi | 1810 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| 5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 3 receptor expressed in NG 108 cells | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-hydroxytryptamine receptor 4 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 4 receptor in guinea pig | B | 7.36 | pIC50 | 44 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | - | - | - | J Med Chem (2000) 43: 1011-8 [PMID:10715164] |
| ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor | B | 5.34 | pKi | 4620 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor expressed in HEK 293 human embryonic kidney cells, [3H]-lysergic acid diethylamide as radioligand | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 7.3 | pKi | <50 | nM | Ki | J Med Chem (2005) 48: 1781-1795 [PMID:15771424] |
| ChEMBL | Binding affinity against 5 Hydroxy tryptamine 6 receptor | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 6 receptor | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4569-4573 [PMID:15357994] |
| ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2008) 51: 603-611 [PMID:18201064] |
| ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2009) 52: 675-687 [PMID:19159187] |
| ChEMBL | Binding affinity to 5HT6 receptor | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2009) 17: 7387-7397 [PMID:19758807] |
| ChEMBL | Binding affinity to 5-HT6 receptor (unknown origin) | B | 7.8 | pKi | 16 | nM | Ki | Med Chem Res (2005) 14: 1-18 |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]lysergic acid diethylamide from human 5-HT6 receptor transfected in HEK293 cells after 60 mins by liquid scintillation spectrometry | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2015) 58: 7901-7912 [PMID:26099069] |
| ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 6 receptor | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - | J Med Chem (2000) 43: 1011-8 [PMID:10715164] |
| ChEMBL | Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor stably expressed in HEK cells | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 6 receptor in human | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | J Med Chem (2000) 43: 1011-8 [PMID:10715164] |
| ChEMBL | Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| ChEMBL | Inhibitory activity against 5-hydroxytryptamine 7 receptor in human | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3230-4234 [PMID:16055331] |
| NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity towards human NET(norepinephrine) transporter | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
| SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity towards human serotonin transporter | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 1011-1018 [PMID:10715164] |
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]
