ChEMBL ligand: CHEMBL301523 (FEMA NO. 3585, Fenilalanina, Laevo-phenyl alanine, L-phenylalanine, NSC-79477, Phenylalanine)
Alkaline phosphatase, tissue-nonspecific isozyme in Human [ChEMBL: CHEMBL5979] [UniProtKB: P05186] There should be some charts here, you may need to enable JavaScript!
X-linked inhibitor of apoptosis/E3 ubiquitin-protein ligase XIAP in Human [ChEMBL: CHEMBL4198] [GtoPdb: 2790] [UniProtKB: P98170] There should be some charts here, you may need to enable JavaScript!
Intestinal-type alkaline phosphatase in Human [ChEMBL: CHEMBL5573] [UniProtKB: P09923] Intestinal-type alkaline phosphatase in Bovine [ChEMBL: CHEMBL5695] [UniProtKB: P19111] There should be some charts here, you may need to enable JavaScript!
L-type amino acid transporter 1/Large neutral amino acids transporter small subunit 1 in Human [ChEMBL: CHEMBL4459] [GtoPdb: 896] [UniProtKB: Q01650] L-type amino acid transporter 1/Large neutral amino acids transporter small subunit 1 in Rat [ChEMBL: CHEMBL4149] [GtoPdb: 896] [UniProtKB: Q63016] There should be some charts here, you may need to enable JavaScript!
Phospholipase A-2-activating protein in Human [ChEMBL: CHEMBL6114] [UniProtKB: Q9Y263] There should be some charts here, you may need to enable JavaScript!
pyruvate kinase M1/2/Pyruvate kinase PKM in Human [ChEMBL: CHEMBL1075189] [GtoPdb: 3006] [UniProtKB: P14618] There should be some charts here, you may need to enable JavaScript!
Voltage-dependent calcium channel subunit alpha-2/delta-1 in Mouse [ChEMBL: CHEMBL4676] [UniProtKB: O08532] There should be some charts here, you may need to enable JavaScript!
xanthine dehydrogenase/Xanthine dehydrogenase/oxidase in Human [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989] There should be some charts here, you may need to enable JavaScript!
GPR139 in Human [GtoPdb: 130] [UniProtKB: Q6DWJ6] 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
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]
X-linked inhibitor of apoptosis/E3 ubiquitin-protein ligase XIAP in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4198] [GtoPdb: 2790] [UniProtKB: P98170]
ChEMBL	Inhibition of human IAP expressed in COS7 cells using CDP-star as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 20 mins by luminescence-based assay	B	4.1	pIC50	80200	nM	IC50	Eur J Med Chem (2018) 156: 461-478 [PMID:30015078]
Intestinal-type alkaline phosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5573] [UniProtKB: P09923]
ChEMBL	Inhibition of human IAP expressed in African green monkey COS7 cell membranes using CDP-star as substrate pretreated for 5 to 10 mins followed by substrate addition and measured after 15 to 20 mins by spectrophotometric method	B	4	pIC50	100000	nM	IC50	Eur J Med Chem (2018) 159: 282-291 [PMID:30296687]
ChEMBL	Inhibition of IAP by analogous luminescence assay	B	5.3	pIC50	>5000	nM	IC50	Bioorg Med Chem (2010) 18: 573-579 [PMID:20031422]
Intestinal-type alkaline phosphatase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5695] [UniProtKB: P19111]
ChEMBL	Inhibition of calf intestinal alkaline phosphatase using CDP-star chemiluminescent substrate assessed as change in luminescence by spectrophotometric method	B	4.1	pIC50	80210	nM	IC50	Bioorg Med Chem (2015) 23: 2435-2444 [PMID:25865133]
ChEMBL	Inhibition of calf intestinal alkaline phosphatase using CDP-star as substrate preincubated for 5 to 7 mins followed by substrate addition measured after 15 mins by spectrophotometric method	B	4.1	pIC50	80210	nM	IC50	Eur J Med Chem (2017) 126: 408-420 [PMID:27907877]
L-type amino acid transporter 1/Large neutral amino acids transporter small subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4459] [GtoPdb: 896] [UniProtKB: Q01650]
ChEMBL	Cis-inhibition of human LAT1 expressed in TREx HEK293 cells at 200 uM assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis relative to BCH	B	4.16	pIC50	69000	nM	IC50	J Med Chem (2018) 61: 7358-7373 [PMID:30048132]
ChEMBL	Cis-inhibition of human LAT1 expressed in TREx HEK293 cells assessed as inhibition of [3H]-gabapentin uptake preincubated for 3 mins at 37 degC followed by washing with choline buffer and measured after 3 hrs by scintillation counting analysis	B	4.16	pIC50	69000	nM	IC50	Bioorg Med Chem Lett (2019) 29: 2254-2258 [PMID:31248771]
L-type amino acid transporter 1/Large neutral amino acids transporter small subunit 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4149] [GtoPdb: 896] [UniProtKB: Q63016]
ChEMBL	Inhibition of LAT1-mediated L-[14C]leucine uptake in Sprague-Dawley rat brain by duel-labeled liquid scintillation counting	B	4.26	pKi	55000	nM	Ki	Bioorg Med Chem Lett (2010) 20: 3688-3691 [PMID:20466543]
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]
pyruvate kinase M1/2/Pyruvate kinase PKM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075189] [GtoPdb: 3006] [UniProtKB: P14618]
ChEMBL	Inhibition of recombinant human PKM2 expressed in Escherichia coli preincubated for 30 mins followed by beta-NADH addition and measured over 20 mins by LDH-coupled enzyme assay	B	10.26	pIC50	0.06	nM	IC50	J Med Chem (2024) 67: 3339-3357 [PMID:38408027]
Voltage-dependent calcium channel subunit alpha-2/delta-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4676] [UniProtKB: O08532]
ChEMBL	Displacement of [3H]L-leucine from alpha-2delta containing calcium channel in murine brain	B	6.01	pKi	980	nM	Ki	Bioorg Med Chem Lett (2006) 16: 1138-1141 [PMID:16380257]
ChEMBL	Displacement of [3H]L-leucine from alpha-2delta containing calcium channel in murine brain	B	6.01	pKi	977.24	nM	Ki	Bioorg Med Chem Lett (2006) 16: 1138-1141 [PMID:16380257]
xanthine dehydrogenase/Xanthine dehydrogenase/oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1929] [GtoPdb: 2646] [UniProtKB: P47989]
ChEMBL	Determination of Xanthine Oxidase Inhibitory Activity of Aryl Benzofuran Amidated Derivatives and Reagents (Amino Derivatives): 11.1 Preparation of Reagents and Standard Solutions(1) 75 mM phosphate buffer (PB, pH 7.4): containing KH2PO4 0.0956 g, K2HPO4 0.6946 g, EDTA 1.862 mg, dilute to 50 mL with pure water, to be used to dilute samples and other reagents;(2) XOD solution: Take 25 U/2.6 mL of XOD, dilute to 0.08 U/mL of XOD working solution with 75 mM PB solution, mix well with a pipette, store on ice for future use;(3) Substrate preparation: accurately weigh the appropriate amount of xanthine (XA) into 5 mL of 0.1 N NaOH solution, dissolve it ultrasonically, and add 95 mL of 75 mM PB solution to prepare a substrate mother liquor with a final concentration of 0.48 mM, perform vortex mixing for 1 min; it is to be freshly prepared before each experiment;(4) Preparation of the test drug: accurately weigh the appropriate amount of the test drug, dissolve it in DMSO to prepare a 10 mM stock solution, and store at −20° C. in the dark. Use DB to dilute to different concentrations (0-100 mM) before the experiment, and the DMSO content is less than 0.1%.11.2 Steps(1) Add 100 μL of different concentrations of the sample solution to be tested onto a 96-well plate, add 0.08 U/mL XOD 50 μL, and use the same volume of PB as a blank control and allopurinol as a positive control; incubate for 3 min at 37° C. on a microplate reader, and set up 4 replicate wells in parallel for each group.(2) Add the substrate 0.48 mM XA 50 μL to start the reaction, read every 15 s at a wavelength of 295 nm and record the absorbance for a total of 7 min. Data processing: Data is processed by using Excel analysis and half-inhibitory concentration (IC50) is calculated by using GraphPad Prism 6.0.2.(3) Measurement results are shown in Table 1, which indicate that most of the synthesized benzofuran amidated derivatives have significantly xanthine oxidase inhibitory activity.	B	4.22	pIC50	>60000	nM	IC50	US-11021454-B2. Type of aryl benzofuran amidated derivative and medical use thereof (2021)
GPR139 in Human [GtoPdb: 130] [UniProtKB: Q6DWJ6]
GtoPdb	Inhibition equilibrium constant from a radioligand membrane binding assay.	-	3.06	pKi	872000	nM	Ki	Mol Pharmacol (2015) 88: 911-25 [PMID:26349500]
GtoPdb	Measured using a GTPγS assay in transfected COS7 cells.	-	4.51	pIC50	31000	nM	IC50	Mol Pharmacol (2015) 88: 911-25 [PMID:26349500]
GtoPdb	-	-	3.49	pEC50	320000	nM	EC50	J Chem Inf Model (2014) 54: 1553-7 [PMID:24826842]

ChEMBL data shown on this page come from version 36:

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]