L-tryptophan [Ligand Id: 717] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL54976 (Gppe pdr sach, L-tryptophan, NSC-13119, Optimax, Optimax wv, Pacitron, (-)-tryptophan, Tryptophan, Tryptophan, l-, Tryptophan ((-),l,s), Trytophan-) |
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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] |
| myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164] | ||||||||
| ChEMBL | Inhibition of MPO (unknown origin) using H2O2 as substrate | B | 5.65 | pIC50 | 2250 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1-7 [PMID:30466896] |
| 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 USA (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 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]
