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 Picrotoxinin Ligand Info
Canonical SMILES CC(=C)C1C2C3C4(C(C1C(=O)O2)(CC5C4(O5)C(=O)O3)O)C
InChI 1S/C15H16O6/c1-5(2)7-8-11(16)19-9(7)10-13(3)14(8,18)4-6-15(13,21-6)12(17)20-10/h6-10,18H,1,4H2,2-3H3/t6-,7+,8-,9-,10-,13-,14-,15+/m1/s1
InChIKey PIMZUZSSNYHVCU-YKWPQBAZSA-N
PubChem Compound ID 442292
Drug Binding Sites of Target  Top
PDB ID: 6HUJ      CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with picrotoxin, GABA and megabody Mb38.
Method Electron microscopy Resolution 3.04 Å Mutation No [1]
PDB Sequence
DVTVILNNLL
35
EGYDNKLRPD
45
IGVKPTLIHT
55
DMYVNSIGPV
65
NAINMEYTID
75

IFFAQTWYDR
85
RLKFNSTIKV
95
LRLNSNMVGK
105
IWIPDTFFRN
115
SKKADAHWIT
125

TPNRMLRIWN
135
DGRVLYTLRL
145
TIDAECQLQL
155
HNFPMDEHSC
165
PLEFSSYGYP
175

REEIVYQWKR
185
SSVEVGDTRS
195
WRLYQFSFVG
205
LRNTTEVVKT
215
TSGDYVVMSV
225

YFDLSRRMGY
235
FTIQTYIPCT
245
LIVVLSWVSF
255
WINKDAVPAR
265
TSLGITTVLT
275

MTTLSTIARK
285
SLPKVSYVTA
295
MDLFVSVCFI
305
FVFSALVEYG
315
TLHYFVSNRR
406

IAKMDSYARI
416
FFPTAFCLFN
426
LVYWVSYLYL
436
Residue
Distance (Å)
SER267
2.687
ILE270
4.233
Residue
Distance (Å)
THR271
2.329
LEU274
3.760
PDB ID: 6HUG      CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with picrotoxin and megabody Mb38.
Method Electron microscopy Resolution 3.10 Å Mutation No [1]
PDB Sequence
DVTVILNNLL
35
EGYDNKLRPD
45
IGVKPTLIHT
55
DMYVNSIGPV
65
NAINMEYTID
75

IFFAQTWYDR
85
RLKFNSTIKV
95
LRLNSNMVGK
105
IWIPDTFFRN
115
SKKADAHWIT
125

TPNRMLRIWN
135
DGRVLYTLRL
145
TIDAECQLQL
155
HNFPMDEHSC
165
PLEFSSYGYP
175

REEIVYQWKR
185
SSVEVGDTRS
195
WRLYQFSFVG
205
LRNTTEVVKT
215
TSGDYVVMSV
225

YFDLSRRMGY
235
FTIQTYIPCT
245
LIVVLSWVSF
255
WINKDAVPAR
265
TSLGITTVLT
275

MTTLSTIARK
285
SLPKVSYVTA
295
MDLFVSVCFI
305
FVFSALVEYG
315
TLHYFVSNRR
406

IAKMDSYARI
416
FFPTAFCLFN
426
LVYWVSYLYL
436
Residue
Distance (Å)
SER267
2.834
ILE270
4.193
Residue
Distance (Å)
THR271
2.319
LEU274
3.737
References  Top
REF 1 GABA(A) receptor signalling mechanisms revealed by structural pharmacology. Nature. 2019 Jan;565(7740):454-459.

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