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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]