4OO9
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STRUCTURE OF THE HUMAN CLASS C GPCR METABOTROPIC GLUTAMATE RECEPTOR 5 TRANSMEMBRANE DOMAIN IN COMPLEX WITH THE NEGATIVE ALLOSTERIC MODULATOR MAVOGLURANT
Descriptor:Metabotropic glutamate receptor 5, Lysozyme, Metabotropic glutamate receptor 5 chimera, ...
Authors:Dore, A.S., Okrasa, K., Patel, J.C., Serrano-Vega, M., Bennett, K., Cooke, R.M., Errey, J.C., Jazayeri, A., Khan, S., Tehan, B., Weir, M., Wiggin, G.R., Marshall, F.H.
Deposit date:2014-01-31
Release date:2014-07-02
Last modified:2017-07-26
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.
Nature, 511, 2014
4OR2
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HUMAN CLASS C G PROTEIN-COUPLED METABOTROPIC GLUTAMATE RECEPTOR 1 IN COMPLEX WITH A NEGATIVE ALLOSTERIC MODULATOR
Descriptor:Soluble cytochrome b562, Metabotropic glutamate receptor 1, 4-fluoro-N-methyl-N-{4-[6-(propan-2-ylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl}benzamide, ...
Authors:Wu, H., Wang, C., Gregory, K.J., Han, G.W., Cho, H.P., Xia, Y., Niswender, C.M., Katritch, V., Cherezov, V., Conn, P.J., Stevens, R.C., GPCR Network (GPCR)
Deposit date:2014-02-10
Release date:2014-03-19
Last modified:2017-11-22
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator
Science, 344, 2014
5CGC
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STRUCTURE OF THE HUMAN CLASS C GPCR METABOTROPIC GLUTAMATE RECEPTOR 5 TRANSMEMBRANE DOMAIN IN COMPLEX WITH THE NEGATIVE ALLOSTERIC MODULATOR 3-CHLORO-4-FLUORO-5-[6-(1H-PYRAZOL-1-YL)PYRIMIDIN-4-YL]BENZONITRILE
Descriptor:Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, OLEIC ACID, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ...
Authors:Christopher, J.A., Aves, S.J., Bennett, K.A., Dore, A.S., Errey, J.C., Jazayeri, A., Marshall, F.H., Okrasa, K., Serrano-Vega, M.J., Tehan, B.G., Wiggin, G.R., Congreve, M.
Deposit date:2015-07-09
Release date:2015-08-12
Last modified:2015-12-16
Method:X-RAY DIFFRACTION (3.101 Å)
Cite:Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
J.Med.Chem., 58, 2015
5CGD
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STRUCTURE OF THE HUMAN CLASS C GPCR METABOTROPIC GLUTAMATE RECEPTOR 5 TRANSMEMBRANE DOMAIN IN COMPLEX WITH THE NEGATIVE ALLOSTERIC MODULATOR 3-CHLORO-5-[6-(5-FLUOROPYRIDIN-2-YL)PYRIMIDIN-4-YL]BENZONITRILE - (HTL14242)
Descriptor:Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, OLEIC ACID, 3-chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile
Authors:Christopher, J.A., Aves, S.J., Bennett, K.A., Dore, A.S., Errey, J.C., Jazayeri, A., Marshall, F.H., Okrasa, K., Serrano-Vega, M.J., Tehan, B.G., Wiggin, G.R., Congreve, M.
Deposit date:2015-07-09
Release date:2015-08-12
Last modified:2015-12-16
Method:X-RAY DIFFRACTION (2.603 Å)
Cite:Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
J.Med.Chem., 58, 2015
6FFH
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CRYSTAL STRUCTURE OF MGLUR5 IN COMPLEX WITH FENOBAM AT 2.65 A
Descriptor:Metabotropic glutamate receptor 5,Endolysin, OLEIC ACID, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ...
Authors:Christopher, J.A., Orgovan, Z., Congreve, M., Dore, A.S., Errey, J.C., Marshall, F.H., Mason, J.S., Okrasa, K., Rucktooa, P., Serrano-Vega, M.J., Ferenczy, G.G., Keseru, G.M.
Deposit date:2018-01-08
Release date:2018-03-07
Last modified:2018-03-28
Method:X-RAY DIFFRACTION (2.65 Å)
Cite:Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.
J. Med. Chem., 2018
6FFI
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CRYSTAL STRUCTURE OF MGLUR5 IN COMPLEX WITH MMPEP AT 2.2 A
Descriptor:Metabotropic glutamate receptor 5,Endolysin,Metabotropic glutamate receptor 5, OLEIC ACID, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ...
Authors:Christopher, J.A., Orgovan, Z., Congreve, M., Dore, A.S., Errey, J.C., Marshall, F.H., Mason, J.S., Okrasa, K., Rucktooa, P., Serrano-Vega, M.J., Ferenczy, G.G., Keseru, G.M.
Deposit date:2018-01-08
Release date:2018-03-07
Last modified:2018-03-28
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Structure-Based Optimization Strategies for G Protein-Coupled Receptor (GPCR) Allosteric Modulators: A Case Study from Analyses of New Metabotropic Glutamate Receptor 5 (mGlu5) X-ray Structures.
J. Med. Chem., 2018
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