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 T27376 Target Info
Target Name GABA(A) receptor delta (GABRD)
Synonyms Gammaaminobutyric acid receptor subunit delta; GABRD; GABA(A) receptor subunit delta
Target Type Successful Target
Gene Name GABRD
Biochemical Class Ligand-gated ion channel
UniProt ID
GBRD_HUMAN
Ligand General Information  Top
Ligand Name Gaboxadol Ligand Info
Canonical SMILES C1CNCC2=C1C(=O)NO2
InChI 1S/C6H8N2O2/c9-6-4-1-2-7-3-5(4)10-8-6/h7H,1-3H2,(H,8,9)
InChIKey ZXRVKCBLGJOCEE-UHFFFAOYSA-N
PubChem Compound ID 3448
Drug Binding Sites of Target  Top
PDB ID: 7QNC      Cryo-EM structure of human full-length extrasynaptic alpha4beta3delta GABA(A)R in complex with THIP (gaboxadol), histamine and nanobody Nb25
Method Electron microscopy Resolution 2.90 Å Mutation No [1]
PDB Sequence
PNLDGLIAGY
51
ARNFRPGIGG
61
PPVNVALALE
71
VASIDHISEA
81
NMEYTMTVFL
91

HQSWRDSRLS
101
YNHTNETLGL
111
DSRFVDKLWL
121
PDTFIVNAKS
131
AWFHDVTVEN
141

KLIRLQPDGV
151
ILYSIRITST
161
VACDMDLAKY
171
PMDEQECMLD
181
LESYGYSSED
191

IVYYWSESQE
201
HIHGLDKLQL
211
AQFTITSYRF
221
TTELMNFKSA
231
GQFPRLSLHF
241

HLRRNRGVYI
251
IQSYMPSVLL
261
VAMSWVSFWI
271
SQAAVPARVS
281
LGITTVLTMT
291

TLMVSARSSL
301
PRASAIKALD
311
VYFWICYVFV
321
FAALVEYAFA
331
HFNADADTID
428

IYARAVFPAA
438
FAAVNVIYWA
448
AYA
Residue
Distance (Å)
PHE125
3.988
GLU183
3.340
SER184
4.136
TYR185
3.039
Residue
Distance (Å)
LYS229
3.289
SER230
4.759
ALA231
4.486
PHE234
3.662
PDB ID: 7QND      Cryo-EM structure of human full-length extrasynaptic beta3delta GABA(A)R in complex with THIP (gaboxadol), histamine and nanobody Nb25
Method Electron microscopy Resolution 3.40 Å Mutation No [1]
PDB Sequence
LPNLDGLIAG
50
YARNFRPGIG
60
GPPVNVALAL
70
EVASIDHISE
80
ANMEYTMTVF
90

LHQSWRDSRL
100
SYNHTNETLG
110
LDSRFVDKLW
120
LPDTFIVNAK
130
SAWFHDVTVE
140

NKLIRLQPDG
150
VILYSIRITS
160
TVACDMDLAK
170
YPMDEQECML
180
DLESYGYSSE
190

DIVYYWSESQ
200
EHIHGLDKLQ
210
LAQFTITSYR
220
FTTELMNFKS
230
AGQFPRLSLH
240

FHLRRNRGVY
250
IIQSYMPSVL
260
LVAMSWVSFW
270
ISQAAVPARV
280
SLGITTVLTM
290

TTLMVSARSS
300
LPRASAIKAL
310
DVYFWICYVF
320
VFAALVEYAF
330
AHFNADADTI
427

DIYARAVFPA
437
AFAAVNVIYW
447
AAYA
Residue
Distance (Å)
PHE125
4.057
GLU183
3.450
SER184
4.349
TYR185
2.765
Residue
Distance (Å)
GLY186
4.912
LYS229
3.231
SER230
4.007
PHE234
3.592
References  Top
REF 1 Differential assembly diversifies GABA(A) receptor structures and signalling. Nature. 2022 Apr;604(7904):190-194.

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