5ZG2

Crystal structure of the GluA2o LBD in complex with ZK200775 and Compound-2

Summary for 5ZG2

DescriptorGlutamate receptor 2, {[7-morpholin-4-yl-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl]methyl}phosphonic acid, 9-(4-~{tert}-butylphenyl)-3,4-dihydropyrido[2,1-c][1,2,4]thiadiazine 2,2-dioxide, ... (7 entities in total)
Functional Keywordsampa receptor ligand-binding domain, allosteric modulation complex, membrane protein, transport protein
Biological sourceHomo sapiens (Human)
Total number of polymer chains2
Total molecular weight60498.95
Authors
Sogabe, S.,Igaki, S.,Hirokawa, A.,Zama, Y.,Lane, W.,Snell, G. (deposition date: 2018-03-07, release date: 2019-01-16, Last modification date: 2019-03-27)
Primary citation
Kunugi, A.,Tanaka, M.,Suzuki, A.,Tajima, Y.,Suzuki, N.,Suzuki, M.,Nakamura, S.,Kuno, H.,Yokota, A.,Sogabe, S.,Kosugi, Y.,Awasaki, Y.,Kaku, T.,Kimura, H.
TAK-137, an AMPA-R potentiator with little agonistic effect, has a wide therapeutic window.
Neuropsychopharmacology, 44:961-970, 2019
PubMed: 30209408 (PDB entries with the same primary citation)
DOI: 10.1038/s41386-018-0213-7
MImport into Mendeley
Experimental method
X-RAY DIFFRACTION (1.25 Å)
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Structure validation

RfreeClashscoreRamachandran outliersSidechain outliersRSRZ outliers 0.19220 0.5% 0.8%MetricValuePercentile RanksWorseBetterPercentile relative to all X-ray structuresPercentile relative to X-ray structures of similar resolution
Download full validation reportDownload
167518
PDB entries from 2020-08-12