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8ZMG

Crystal structure of an inverse agonist antipsychotic drug pimavanserin-bound 5-HT2A

This is a non-PDB format compatible entry.
Summary for 8ZMG
Entry DOI10.2210/pdb8zmg/pdb
Descriptor5-hydroxytryptamine receptor 2A,Soluble cytochrome b562, Pimavanserin (2 entities in total)
Functional Keywordsclass a g protein-coupled receptor, inverse agonist, membrane protein
Biological sourceHomo sapiens (human)
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Total number of polymer chains2
Total formula weight94067.70
Authors
Oguma, T.,Asada, H.,Sekiguchi, Y.,Imono, M.,Iwata, S.,Kusakabe, K. (deposition date: 2024-05-23, release date: 2024-08-28)
Primary citationOguma, T.,Jino, K.,Nakahara, K.,Asada, H.,Fuchino, K.,Nagatani, K.,Kouki, K.,Okamoto, R.,Takai, N.,Koda, K.,Fujita, S.,Sekiguchi, Y.,Yasuo, K.,Mayumi, K.,Abe, A.,Imono, M.,Horiguchi, N.,Iwata, S.,Kusakabe, K.I.
Dual 5-HT 2A and 5-HT 2C Receptor Inverse Agonist That Affords In Vivo Antipsychotic Efficacy with Minimal hERG Inhibition for the Treatment of Dementia-Related Psychosis.
J.Med.Chem., 2024
Cited by
PubMed: 39137033
DOI: 10.1021/acs.jmedchem.4c01244
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (3.4 Å)
Structure validation

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