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ChEMBL ligand: CHEMBL301523 (FEMA NO. 3585, Laevo-phenyl alanine, L-phenylalanine, NSC-79477, Phenylalanine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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/Inhibitor of apoptosis protein 3 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 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 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 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 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] |
Voltage-gated calcium channel alpha2/delta subunit 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] |
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 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]