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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 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]