5-hydroxy-L-tryptophan [Ligand Id: 4671] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL350221 (5-hydroxy-l-tryptophan, 5-hydroxytryptophan, 5-hydroxytryptophan, dl-, 5-hydroxytryptophan l-form, Cincofarm, Dl-5-htp, Dl-5-hydroxytryptophan, Dl-hydroxytryptophan, Dl-oxitriptan, Hydroxytryptophan, L-5-htp, L-5-hydroxytryptophan, Levothym, Levotinine, Levotonine, NSC-92523, Oxitriptan, Oxyfan, Pretonine, Quietim, Serotonyl, Telesol, Triptene, Tryptophan, 5-hydroxy-, dl)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
There should be some charts here, you may need to enable JavaScript!
  • Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
There should be some charts here, you may need to enable JavaScript!
  • Proton-coupled Amino acid Transporter 2 in Human [GtoPdb: 1162] [UniProtKB: Q495M3]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry B 8.74 pKi 1.8 nM Ki Bioorg Med Chem Lett (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis B 9.04 pKi 0.91 nM Ki Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Agonist activity at 5-HT2A receptor (unknown origin) expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding incubated for 30 mins by liquid scintillation counting method F 6.89 pEC50 130 nM EC50 Bioorg Med Chem Lett (2015) 25: 3970-3974 [PMID:26227779]
ChEMBL Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay F 8.72 pEC50 1.9 nM EC50 J Med Chem (2016) 59: 578-591 [PMID:26704965]
ChEMBL Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay F 8.87 pEC50 1.35 nM EC50 J Med Chem (2016) 59: 578-591 [PMID:26704965]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay F 8.89 pEC50 1.29 nM EC50 J Med Chem (2016) 59: 578-591 [PMID:26704965]
ChEMBL Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay F 9 pEC50 1 nM EC50 J Med Chem (2016) 59: 578-591 [PMID:26704965]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay F 9.66 pEC50 0.22 nM EC50 J Med Chem (2016) 59: 578-591 [PMID:26704965]
ChEMBL Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay F 9.74 pEC50 0.18 nM EC50 J Med Chem (2016) 59: 578-591 [PMID:26704965]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Tested for its binding affinity by measuring its ability to displace [3H]granisetron from 5-hydroxytryptamine 3 receptor in rat cortex B 6.8 pKi 158.49 nM Ki Bioorg Med Chem Lett (1993) 3: 633-634
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor located in the rat esophageal tunica muscularis mucosae F 8.01 pEC50 9.77 nM EC50 Bioorg Med Chem Lett (1993) 3: 633-634
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis B 8.67 pKi 2.12 nM Ki Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032]
Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
GtoPdb - - 3 pKi 900000 nM Ki FASEB J (2005) 19: 1468-73 [PMID:16126914]
Proton-coupled Amino acid Transporter 2 in Human [GtoPdb: 1162] [UniProtKB: Q495M3]
GtoPdb - - 2.8 pIC50 1600000 nM IC50 Biochim Biophys Acta (2011) 1808: 260-70 [PMID:20691150]

ChEMBL data shown on this page come from version 33:

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]