L-tryptophan [Ligand Id: 717] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL54976 (Tryptophan, L-Tryptophan, Optimax Wv, Pacitron, Tryptophan, l-, Optimax, NSC-13119, Gppe Pdr Sach)
  • Alkaline phosphatase, tissue-nonspecific isozyme in Human [ChEMBL: CHEMBL5979] [UniProtKB: P05186]
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  • Intestinal alkaline phosphatase in Human [ChEMBL: CHEMBL5573] [UniProtKB: P09923]
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  • Phospholipase A-2-activating protein in Human [ChEMBL: CHEMBL6114] [UniProtKB: Q9Y263]
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  • GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
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  • CaS receptor in Human [GtoPdb: 54] [UniProtKB: P41180]
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  • GPR139 in Human [GtoPdb: 130] [UniProtKB: Q6DWJ6]
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  • Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alkaline phosphatase, tissue-nonspecific isozyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5979] [UniProtKB: P05186]
ChEMBL Inhibition of TNAP by analogous luminescence assay B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. (2010) 18: 573-579 [PMID:20031422]
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL null: A commercially available P450-GLO Assay kit (Promega Corporation, Madison Wis.) is used to screen various compounds for CYP3A4A inhibition activity. CYP3A4A is thought to be one of the primary CYP isoforms responsible for retinoic acid metabolism in the skin. Three benchmark agents, liarozole, climbazole, and ketoconazole, were assessed for CYP3A4 inhibition to confirm that the inhibition activity (the IC50 for CYP3A4 inhibition) measured by the assay corresponds to the activity reported by the published literature. The results show that the substituted azole compounds having the specific structure set forth herein are CYP inhibitors, and thus function as RAMBAs. B 5 pIC50 >10000 nM IC50 US-9138393-B2. Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin (2015)
ChEMBL In vitro CYP3A4 Inhibition Assay: Cytochrome P450 is a large and diverse group of enzymes that catalyze the oxidation of organic substances. Some members of the CYP family contribute to the elimination of ATRA by catalyzing its 4-hydroxylation in the mammalian liver and skin, including that of humans as well as swine. Applicant evaluated the potential RAMBA activity of several azoles using pig liver microsomes, a rich source of CYP activity, comprising many different CYP 450 isoforms. Therefore, this approach, while a reasonable way to assess CYP inhibitors with broad activities may or may not be the best way to discover RAMBAs with selectivity for the skin, which has a much more narrow complement of CYP expression. As understanding in this area has progressed, a more specific CYP inhibition assay can be used to provide better predictivity of activity in human skin. Nevertheless, this assay may still be used as a general predictor of overall CYP activity. B 5 pIC50 >10000 nM IC50 US-9144538-B2. Cosmetic compositions containing substituted azole and methods for alleviating the signs of photoaged skin (2015)
Intestinal alkaline phosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5573] [UniProtKB: P09923]
ChEMBL Inhibition of IAP by analogous luminescence assay B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. (2010) 18: 573-579 [PMID:20031422]
Phospholipase A-2-activating protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6114] [UniProtKB: Q9Y263]
ChEMBL Inhibition of PLAP by analogous luminescence assay B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. (2010) 18: 573-579 [PMID:20031422]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
ChEMBL Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J Med Chem (2018) 61: 8136-8154 [PMID:30048589]
CaS receptor in Human [GtoPdb: 54] [UniProtKB: P41180]
GtoPdb - - 4.4 pKd - - - Proc. Natl. Acad. Sci. U.S.A. (2000) 97: 4814-9 [PMID:10781086];
J. Biol. Chem. (2004) 279: 38151-9 [PMID:15234970]
GPR139 in Human [GtoPdb: 130] [UniProtKB: Q6DWJ6]
GtoPdb Inhibition equilibrium constant from a radioligand membrane binding assay. - 3.13 pKi 738000 nM Ki Mol. Pharmacol. (2015) 88: 911-25 [PMID:26349500]
GtoPdb Measured using a GTPγS assay in transfected COS7 cells. - 4.59 pIC50 26000 nM IC50 Mol. Pharmacol. (2015) 88: 911-25 [PMID:26349500]
GtoPdb - - 3.66 pEC50 220000 nM EC50 J Chem Inf Model (2014) 54: 1553-7 [PMID:24826842]
Proton-coupled Amino acid Transporter 1 in Human [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
GtoPdb - - 2.3 pKi 4600000 nM Ki FASEB J. (2005) 19: 1468-73 [PMID:16126914]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]