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ChEMBL ligand: CHEMBL316446 (Endomorphin 1) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | Displacement of [3H]DPDPE from Myc-tagged delta opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | B | 5.22 | pKi | 6080 | nM | Ki | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
ChEMBL | Displacement of [3H]-DPDPE from delta opioid receptor (unknown origin) transfected in HEK293 cells | B | 5.22 | pKi | 6080 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5393-5397 [PMID:26403932] |
ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranes | B | 5.29 | pKi | 5100 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418] |
ChEMBL | Displacement of [3H]DPDPE from delta-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | B | 5.56 | pKi | 2765 | nM | Ki | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
ChEMBL | Displacement of [3H]DPDPE from DOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method | B | 5.56 | pKi | 2765 | nM | Ki | Bioorg Med Chem (2012) 20: 6335-6343 [PMID:23022277] |
GtoPdb | - | - | 6.1 | pKi | - | - | - | FEBS Lett (1998) 439: 152-6 [PMID:9849897] |
ChEMBL | Activity at delta opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay | F | 6.03 | pEC50 | 932 | nM | EC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically evoked muscle contractions | F | 6.55 | pIC50 | 283 | nM | IC50 | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
ChEMBL | Agonist activity at delta opioid receptor in Kunming mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 7.52 | pIC50 | 30.4 | nM | IC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
ChEMBL | Agonist activity at delta opioid receptor by inhibition of electrically evoked muscle contraction in isolated mouse vas deferens | F | 7.58 | pIC50 | 26.3 | nM | IC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
ChEMBL | Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418] |
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
ChEMBL | Displacement of [3H]-DPDPE from Wistar rat delta opioid receptor incubated for 3 hrs by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
ChEMBL | Displacement of [3H]Ile5,6-deltorphin II from opioid receptor delta 1 of rat brain membranes | B | 5.19 | pKi | 6390 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
ChEMBL | Displacement of [3H]DPDPE from DOR in Wistar rat brain membranes measured after 3 hrs by scintillation counting method | B | 5.21 | pKi | 6105 | nM | Ki | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
ChEMBL | Displacement of [3H]DPDPE from delta-opioid receptor in Wistar rat brain membrane after 3 hrs by microbeta scintillation counting method | B | 5.24 | pKi | 5775 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 2119-2123 [PMID:28377055] |
ChEMBL | Displacement of [3H]-DPDPE from delta opioid receptor in Wistar rat brain membranes preincubated for 3 hrs measured after 1 hr by scintillation counting method | B | 5.29 | pKi | 5093 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 1557-1560 [PMID:28256374] |
ChEMBL | Displacement of [3H][Ile5,6]deltorphin2 from delta opioid receptor in rat brain membrane homogenate by liquid scintillation counting | B | 5.38 | pKi | 4169 | nM | Ki | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
ChEMBL | Displacement of [3H]Ile5,6deltorphin-2 from delta opioid receptor in Wistar rat brain | B | 5.72 | pKi | 1909 | nM | Ki | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
ChEMBL | Displacement of [3H]deltorphin 2 from delta opioid receptor in rat brain P2 synaptosome | B | 5.76 | pKi | 1750 | nM | Ki | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
ChEMBL | Displacement of [3H]DAMGO from delta opioid receptor in rat brain membrane | B | 5.89 | pKi | 1280 | nM | Ki | Bioorg Med Chem (2008) 16: 6286-6296 [PMID:18468445] |
ChEMBL | Displacement of [3H]DPDPE from rat cortex delta opioid receptor after 2.5 hrs by liquid scintillation counting analysis | B | 6.14 | pKi | 729 | nM | Ki | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
ChEMBL | Displacement of [3H]DPDPE from rat cortical DOR after 2.5 hrs by liquid scintillation counting method | B | 6.24 | pKi | 575 | nM | Ki | J Med Chem (2016) 59: 1239-1245 [PMID:26789491] |
ChEMBL | Displacement of [3H]deltorphin2 from delta opioid receptor in rat brain membrane | B | 5.45 | pIC50 | 3580 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
ChEMBL | Displacement of [3H][Ile5,6]deltorphin-2 from delta opioid receptor in Wistar rat brain membrane | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2009) 17: 3789-3794 [PMID:19435668] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Displacement of [3H]U69593 from KOP (unknown origin) stably expressed in HEK293 cells by liquid scintillation counter analysis | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
ChEMBL | Displacement of [3H]diprenorphine from kappa-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | B | 5.69 | pKi | 2048 | nM | Ki | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
ChEMBL | Displacement of[3H]-U69,593 from Wistar rat kappa opioid receptor incubated for 1.5 hrs by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
ChEMBL | Displacement of [3H]-U69593 from KOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
ChEMBL | Displacement of [3H]dynorphin A from Opioid receptor kappa 1 of rat brain membranes (DAMGO/DADLE quenching of mu/delta receptor binding) | B | 7.28 | pKi | 52.7 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
ChEMBL | Displacement of [3H]U69,593 from guinea pig KOR after 2 hrs by liquid scintillation counting method | B | 5.3 | pKi | 5069 | nM | Ki | J Med Chem (2016) 59: 1239-1245 [PMID:26789491] |
ChEMBL | Displacement of [3H]U69,593 from guinea pig cortex/cerebella kappa opioid receptor after 2 hrs by liquid scintillation counting analysis | B | 5.63 | pKi | 2354 | nM | Ki | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
GtoPdb | - | - | 8.3 | pKi | 5.01 | nM | Ki |
FEBS Lett (1998) 439: 152-6 [PMID:9849897]; Nature (1997) 386: 499-502 [PMID:9087409] |
ChEMBL | Binding affinity to human mu opioid receptor | B | 8.34 | pKi | 4.55 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 5387-5391 [PMID:19679474] |
ChEMBL | Displacement of [3H]DAMGO from FLAG-tagged mu opioid receptor expressed in HEK293 cells after 60 mins by liquid scintillation counter | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
ChEMBL | Displacement of [3H]DAMGO from human cloned mu-opioid receptor by radioligand binding assay | B | 8.59 | pKi | 2.6 | nM | Ki | J Med Chem (2022) 65: 13483-13504 [PMID:36206553] |
ChEMBL | Displacement of [3H]-DAMGO from mu opioid receptor (unknown origin) transfected in HEK293 cells | B | 8.59 | pKi | 2.6 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5393-5397 [PMID:26403932] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in human SH-SY5Y cells | B | 8.84 | pKi | 1.45 | nM | Ki | Bioorg Med Chem (2008) 16: 4341-4346 [PMID:18329886] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in human SHSY5Y cells | B | 8.95 | pKi | 1.11 | nM | Ki | Bioorg Med Chem (2008) 16: 6286-6296 [PMID:18468445] |
ChEMBL | Displacement of [3H]DAMGO from MOP receptor expressed in CHO-K1 cells after overnight incubation by beta counting method | B | 9.12 | pKi | 0.76 | nM | Ki | Bioorg Med Chem (2012) 20: 6335-6343 [PMID:23022277] |
ChEMBL | Displacement of [3H]DAMGO from mu-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay | B | 9.54 | pKi | 0.29 | nM | Ki | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
ChEMBL | Agonist activity at mu-opioid receptor in human SH-SY5Y cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by immunoassay | F | 7.18 | pIC50 | 65.4 | nM | IC50 | J Med Chem (2012) 55: 5859-5867 [PMID:22680612] |
ChEMBL | Agonist activity at mu opioid receptor in human SHSY5Y cells assessed as inhibition of forskolin-stimulated cAMP production | F | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem (2008) 16: 6286-6296 [PMID:18468445] |
ChEMBL | Agonist activity at MOP receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins | F | 8.49 | pIC50 | 3.2 | nM | IC50 | Bioorg Med Chem (2012) 20: 6335-6343 [PMID:23022277] |
ChEMBL | Agonist activity at mu opioid receptor (unknown origin) expressed in human HEK293 cells assessed as increase in cAMP accumulation using [3H]-cAMP as substrate measured after 30mins by liquid scintillation counting method | F | 7.21 | pEC50 | 61 | nM | EC50 | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
ChEMBL | Agonist activity at mu-opioid receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 15 mins by ELISA | F | 7.68 | pEC50 | 21.1 | nM | EC50 | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
ChEMBL | Agonist activity at mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by liquid scintillation counter | F | 7.84 | pEC50 | 14.4 | nM | EC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
ChEMBL | Agonist activity at mu opioid receptor (unknown origin) transfected in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 7.84 | pEC50 | 14.4 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 5393-5397 [PMID:26403932] |
ChEMBL | Agonist activity at human MOP assessed as forskolin stimulated cAMP accumulation | F | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
ChEMBL | Inhibition of Mu opioid receptor of mouse vas deferens | B | 7.44 | pIC50 | 36.3 | nM | IC50 | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
ChEMBL | Displacement of [3H]-DAMGO from Wistar rat mu opioid receptor incubated for 1 hr by liquid scintillation counting method | B | 7.75 | pKi | 17.8 | nM | Ki | Bioorg Med Chem (2020) 28: 115438-115438 [PMID:32199689] |
ChEMBL | Binding affinity towards Opioid receptor mu 1 | B | 7.95 | pKi | 11.1 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2755-2758 [PMID:11133084] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane by liquid scintillation counting | B | 7.97 | pKi | 10.7 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4115-4118 [PMID:19560919] |
ChEMBL | Displacement of [3H]DAMGO from mu-opioid receptor in Wistar rat brain membrane after 1 hr by microbeta scintillation counting method | B | 8.21 | pKi | 6.19 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 2119-2123 [PMID:28377055] |
ChEMBL | Displacement of [3H]DAMGO from MOR in Wistar rat brain membranes measured after 1 hr by scintillation counting method | B | 8.33 | pKi | 4.63 | nM | Ki | J Med Chem (2021) 64: 16801-16819 [PMID:34781680] |
ChEMBL | Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membranes | B | 8.34 | pKi | 4.6 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418] |
ChEMBL | Displacement of [3H]-DAMGO from mu opioid receptor in Wistar rat brain membranes preincubated for 1 hr measured after 1hr by scintillation counting method | B | 8.34 | pKi | 4.53 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 1557-1560 [PMID:28256374] |
ChEMBL | Displacement of [3H]DAMGO from Opioid receptor mu 1 of rat brain membranes | B | 8.38 | pKi | 4.21 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
ChEMBL | Displacement of [3H]DAMGO from rat cortex mu opioid receptor after 30 mins by liquid scintillation counting analysis | B | 8.4 | pKi | 4 | nM | Ki | Eur J Med Chem (2015) 92: 270-281 [PMID:25559207] |
ChEMBL | Displacement of [3H]endomorphin-2 from mu opioid receptor in Wistar rat brain | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
ChEMBL | Displacement of [3H]endomorphin-2 from Opioid receptor mu 1 of rat brain membranes | B | 8.79 | pKi | 1.62 | nM | Ki | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane homogenate by liquid scintillation counting | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | B | 8.94 | pKi | 1.15 | nM | Ki | Bioorg Med Chem (2008) 16: 6286-6296 [PMID:18468445] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain | B | 9.13 | pKi | 0.74 | nM | Ki | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
ChEMBL | Displacement of [3H]DAMGO from rat cortical MOR by liquid scintillation counting method | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2016) 59: 1239-1245 [PMID:26789491] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain P2 synaptosome | B | 9.25 | pKi | 0.56 | nM | Ki | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
ChEMBL | Binding affinity towards Opioid receptor mu 1 by displacing [3H]DAMGO in rat brain membranes. | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2002) 45: 2571-2578 [PMID:12036366] |
ChEMBL | Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2004) 47: 5198-5203 [PMID:15456262] |
ChEMBL | Concentration required for inhibition of [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 2755-2758 [PMID:11133084] |
ChEMBL | Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane | B | 8.72 | pIC50 | 1.89 | nM | IC50 | Bioorg Med Chem (2007) 15: 3883-3888 [PMID:17395470] |
ChEMBL | Inhibitory activity against [3H]DAMGO binding to Opioid receptor mu 1 in rat brain membranes | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2002) 45: 2571-2578 [PMID:12036366] |
ChEMBL | Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2004) 47: 5198-5203 [PMID:15456262] |
ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain membrane | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem (2009) 17: 3789-3794 [PMID:19435668] |
ChEMBL | Agonist activity at mu opioid receptor in rat brain membrane by [35S]GTPgammaS binding assay | F | 6.78 | pEC50 | 166 | nM | EC50 | J Med Chem (2011) 54: 1462-1472 [PMID:21287991] |
ChEMBL | Activity at mu opioid receptor in Wistar rat brain assessed as stimulation of [35S]GTPgammaS binding | F | 6.98 | pEC50 | 104 | nM | EC50 | J Med Chem (2008) 51: 4270-4279 [PMID:18572932] |
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated contraction | F | 4.55 | pIC50 | 28000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4115-4118 [PMID:19560919] |
ChEMBL | Agonist activity at mu opioid receptor by inhibition of electrically evoked muscle contraction in guinea pig ileum | F | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2007) 50: 512-520 [PMID:17266203] |
ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 7.85 | pIC50 | 14.1 | nM | IC50 | J Med Chem (2012) 55: 6224-6236 [PMID:22724433] |
ChEMBL | Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated muscle contraction | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418] |
ChEMBL | Inhibition of Opioid receptor mu 1 of guinea pig ileum | B | 8 | pIC50 | 10.1 | nM | IC50 | J Med Chem (2004) 47: 735-743 [PMID:14736254] |
ChEMBL | Agonist activity at mu opioid receptor in Hartley guinea pig intestine assessed as inhibition of electrically evoked myenteric plexus longitudinal muscle contractions | F | 8.39 | pIC50 | 4.03 | nM | IC50 | Bioorg Med Chem (2007) 15: 1237-1251 [PMID:17142049] |
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]