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

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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]
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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 Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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  • Proton-coupled Amino acid Transporter 2 in Human [GtoPdb: 1162] [UniProtKB: Q495M3]
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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 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]