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
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

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
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PDB entries from 2020-08-12