Lysergide [Ligand Id: 17] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL263881 (Dextrolysergic acid diethylamide, D-lsd, Lisergida, LSD, Lsd-25, Lysergic acid diethylamide, Lysergic acid diethylamide tartrate ci, Lysergide, N,n-diethyllysergamide) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Binding affinity towards Beta-1 adrenergic receptor | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Binding affinity towards Beta-2 adrenergic receptor | B | 6.13 | pKi | 740 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Binding affinities towards Dopamine receptor D1 | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity against human Dopamine receptor D2 in CHO cells using [125I]iodosulpiride | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| ChEMBL | Binding affinity towards Dopamine receptor D2 | B | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Binding affinity towards Dopamine receptor D3 | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Binding affinity towards Dopamine receptor D4 | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Binding affinity towards Dopamine receptor D5 | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Binding affinity towards Histamine H1 receptor | B | 5.81 | pKi | 1540 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A human cloned receptors in HEK293 cells using [3H]8-OH-DPAT as radioligand | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| ChEMBL | Tested in vitro for its ability to bind to 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2003) 46: 3526-3535 [PMID:12877591] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| GtoPdb | - | - | 9 | pKi | - | - | - | J Med Chem (2002) 45: 4344-9 [PMID:12213075] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity was measured against 5-hydroxytryptamine 1A receptor by displacement of [3H]8-OH-DPAT by lysergic acid amides | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (1995) 38: 958-966 [PMID:7699712] |
| ChEMBL | Binding affinity of [3H]- -8-OH-DPAT labelled towards Rat Hippocampal 5-hydroxytryptamine 1A receptor using radioligand binding assay | B | 8.29 | pKi | 5.1 | nM | Ki | J Med Chem (1996) 39: 2953-2961 [PMID:8709129] |
| ChEMBL | Affinity in displacing [3H]8-OH-DPAT from rat hippocampal 5-HT1A receptor. | B | 8.3 | pKi | 5.05 | nM | Ki | J Med Chem (1992) 35: 203-211 [PMID:1732537] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1D receptor alpha using [3H]8-OH-DPAT as radioligand | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1E receptor | B | 7.03 | pKi | 93 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human A549 cells | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904] |
| ChEMBL | Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human HEK293 cells | B | 8.46 | pKi | 3.5 | nM | Ki | Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor human cloned receptors in HEK 293 cells using [3H]ketanserin as radioligand | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human HEK293 cells | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904] |
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human A549 cells | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - | J Biol Chem (1996) 271: 14672-5 [PMID:8663249] |
| ChEMBL | Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay | F | 7.8 | pEC50 | 16 | nM | EC50 | ACS Med Chem Lett (2024) 15: 337-339 [PMID:38505858] |
| ChEMBL | Agonist activity at human smBiT-fused 5HT2A receptor expressed in CHO-K1 cells co-expressing IgBiT-fused beta-arrestin2 assessed as beta-arrestin2 recruitment by measuring increase in chemiluminescence intensity incubated for 2 hrs by NanoBiT luciferase assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | ACS Med Chem Lett (2024) 15: 337-339 [PMID:38505858] |
| ChEMBL | Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay | F | 7.88 | pEC50 | 13.2 | nM | EC50 | J Med Chem (2022) 65: 12031-12043 [PMID:36099411] |
| ChEMBL | Agonist activity at human 5HT2A receptor transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay | F | 7.89 | pEC50 | 12.9 | nM | EC50 | J Med Chem (2022) 65: 12031-12043 [PMID:36099411] |
| ChEMBL | Agonist activity at human 5HT2A S159A mutant transfected in HEK293T cells assessed as mini Galphaq recruitment measured for 2 hrs by luminescent assay | B | 8.27 | pEC50 | 5.38 | nM | EC50 | J Med Chem (2022) 65: 12031-12043 [PMID:36099411] |
| ChEMBL | Agonist activity at human 5HT2A S159A mutant transfected in HEK293T cells assessed as beta arrestin-2 recruitment measured for 2 hrs by luminescent assay | B | 8.28 | pEC50 | 5.19 | nM | EC50 | J Med Chem (2022) 65: 12031-12043 [PMID:36099411] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding affinity was measured against 5-hydroxytryptamine 2A receptor by displacement of [3H]- ketanserin by lysergic acid amides | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (1995) 38: 958-966 [PMID:7699712] |
| ChEMBL | Binding affinity of [3H]- ketanserin labelled towards Rat cortical 5-hydroxytryptamine 2A receptor using radioligand binding assay | B | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (1996) 39: 2953-2961 [PMID:8709129] |
| ChEMBL | In vitro binding to 5-hydroxytryptamine 2A receptor using [125 I]-DOI | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2003) 46: 3526-3535 [PMID:12877591] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor using [125I]DOI as radioligand | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| ChEMBL | Displacement of [125I]DOI from rat 5HT2A receptor | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2006) 49: 4269-4274 [PMID:16821786] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - | J Med Chem (2002) 45: 4344-9 [PMID:12213075] |
| ChEMBL | Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor | B | 8.01 | pEC50 | 9.8 | nM | EC50 | J Med Chem (2003) 46: 3526-3535 [PMID:12877591] |
| ChEMBL | Activity at rat 5HT2A receptor assessed as 5-HT-stimulated IP3 accumulation | F | 8.01 | pEC50 | 9.8 | nM | EC50 | J Med Chem (2006) 49: 4269-4274 [PMID:16821786] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2B receptor using [125I]DOI as radioligand | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| GtoPdb | Biased for β-arrestin sihnalling. | - | 8.43 | pKi | - | - | - | Science (2013) 340: 615-9 [PMID:23519215] |
| 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Med Chem (2002) 45: 4344-9 [PMID:12213075] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2C receptor human cloned receptors in HEK 293 cells using [3H]mesulergine as radioligand | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - | Synapse (2000) 35: 144-50 [PMID:10611640] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | In vitro binding to 5-hydroxytryptamine 2C receptor using [125 I]-DOI | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (2003) 46: 3526-3535 [PMID:12877591] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2C receptor using [125I]DOI as radioligand | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| ChEMBL | Displacement of [125I]DOI from rat 5HT2C receptor | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (2006) 49: 4269-4274 [PMID:16821786] |
| ChEMBL | Compound was tested for binding affinity towards 5-hydroxytryptamine 1C receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]mesulergine as radioligand | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (1992) 35: 734-740 [PMID:1542100] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity for rodent 5-hydroxytryptamine 5A receptor | B | 8 | pKi | <10 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinities towards 5-hydroxytryptamine 5A receptor | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinities towards 5-hydroxytryptamine 6 receptor | B | 8.16 | pKi | 6.9 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 6 human cloned receptors in HeLa cells | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - | Mol Pharmacol (1998) 54: 577-83 [PMID:9730917] |
| 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Neuropharmacology (1997) 36: 713-20 [PMID:9225298]; Mol Pharmacol (1998) 54: 577-83 [PMID:9730917] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinities towards 5-hydroxytryptamine 7 receptor | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2002) 45: 4344-4349 [PMID:12213075] |
| ChEMBL | Binding affinity against 5-hydroxytryptamine 7 human receptors | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2003) 46: 5117-5120 [PMID:14613313] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity at rat 5-hydroxytryptamine 7 receptor. | B | 8.02 | pKi | 9.55 | nM | Ki | J Med Chem (2003) 46: 5365-5374 [PMID:14640545] |
| ChEMBL | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
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]
