Target Binding Site Detail

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Target General Information
Ligand General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T08910 Target Info
Target Name GABA(A) receptor gamma-2 (GABRG2)
Synonyms Gamma-aminobutyric acid receptor subunit gamma-2; GABA(A) receptor subunit gamma-2
Target Type Successful Target
Gene Name GABRG2
Biochemical Class Neurotransmitter receptor
UniProt ID
GBRG2_HUMAN
Ligand General Information  Top
Ligand Name Cholesterol hemisuccinate Ligand Info
Canonical SMILES CC(C)CCCC(C)C1CCC2C1(CCC3C2CC=C4C3(CCC(C4)OC(=O)CCC(=O)O)C)C
InChI 1S/C31H50O4/c1-20(2)7-6-8-21(3)25-11-12-26-24-10-9-22-19-23(35-29(34)14-13-28(32)33)15-17-30(22,4)27(24)16-18-31(25,26)5/h9,20-21,23-27H,6-8,10-19H2,1-5H3,(H,32,33)/t21-,23+,24+,25-,26+,27+,30+,31-/m1/s1
InChIKey WLNARFZDISHUGS-MIXBDBMTSA-N
PubChem Compound ID 65082
Drug Binding Sites of Target  Top
PDB ID: 6D6U      Human GABA-A receptor alpha1-beta2-gamma2 subtype in complex with GABA and flumazenil, conformation A
Method Electron microscopy Resolution 3.92 Å Mutation No [1]
PDB Sequence
GDVTVILNNL
34
LEGYDNKLRP
44
DIGVKPTLIH
54
TDMYVNSIGP
64
VNAINMEYTI
74

DIFFAQTWYD
84
RRLKFNSTIK
94
VLRLNSNMVG
104
KIWIPDTFFR
114
NSKKADAHWI
124

TTPNRMLRIW
134
NDGRVLYTLR
144
LTIDAECQLQ
154
LHNFPMDEHS
164
CPLEFSSYGY
174

PREEIVYQWK
184
RSSVEVGDTR
194
SWRLYQFSFV
204
GLRNTTEVVK
214
TTSGDYVVMS
224

VYFDLSRRTI
238
QTYIPCTLIV
248
VLSWVSFWIN
258
KDAVPARTSL
268
GITTVLTMTT
278

LSTIARKSYV
293
TAMDLFVSVC
303
FIFVFSALVE
313
YGTLHYFVSS
323
QPARAAKMDS
333

YARIFFPTAF
343
CLFNLVYWVS
353
YL
Residue
Distance (Å)
TYR334
4.687
PHE338
3.671
ALA342
3.982
LEU345
4.356
ILE305
4.892
PHE306
3.874
SER309
3.850
Residue
Distance (Å)
GLU313
3.352
MET331
2.540
TYR334
4.460
ALA335
4.248
PHE338
4.177
PHE339
4.249
ALA342
4.242
PDB ID: 6D6T      Human GABA-A receptor alpha1-beta2-gamma2 subtype in complex with GABA and flumazenil, conformation B
Method Electron microscopy Resolution 3.86 Å Mutation No [1]
PDB Sequence
.
Residue
Distance (Å)
PRO263
4.429
ALA264
4.780
Residue
Distance (Å)
THR266
4.432
References  Top
REF 1 Structure of a human synaptic GABA(A) receptor. Nature. 2018 Jul;559(7712):67-72.

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