Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T18664 | Target Info | |||
| Target Name | Monoglyceride lipase (MAGL) | ||||
| Synonyms | Monoacylglycerol lipase; MGL; Lysophospholipaselike; Lysophospholipase-like; Lysophospholipase homolog; HUK5; HU-K5 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | MGLL | ||||
| Biochemical Class | Carboxylic ester hydrolase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: (2-Cyclohexyl-1,3-Benzoxazol-6-Yl){3-[4-(Pyrimidin-2-Yl)piperazin-1-Yl]azetidin-1-Yl}methanone | Ligand Info | |||||
| Structure Description | Crystal Structure of a soluble form of human MGLL in complex with an inhibitor | PDB:3PE6 | ||||
| Method | X-ray diffraction | Resolution | 1.35 Å | Mutation | Yes | [1] |
| PDB Sequence |
PRRTPQSIPY
16 QDLPHLVNAD26 GQYLFCRYWA36 PTGTPKALIF46 VSHGAGEHSG56 RYEELARMLM 66 GLDLLVFAHD76 HVGHGQSEGE86 RMVVSDFHVF96 VRDVLQHVDS106 MQKDYPGLPV 116 FLLGHSMGGA126 IAILTAAERP136 GHFAGMVLIS146 PLVLANPESA156 TTFKVLAAKV 166 LNSVLPNLSS176 GPIDSSVLSR186 NKTEVDIYNS196 DPLICRAGLK206 VCFGIQLLNA 216 VSRVERALPK226 LTVPFLLLQG236 SADRLCDSKG246 AYLLMELAKS256 QDKTLKIYEG 266 AYHVLHKELP276 EVTNSVFHEI286 NMWVSQRTA
|
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|
|
GLY50
2.463
ALA51
1.986
GLY52
4.848
GLU53
2.595
ARG57
3.782
TYR58
4.411
HIS121
2.743
SER122
2.178
MET123
2.072
GLY124
4.147
LEU148
2.856
ALA151
2.474
ASN152
4.302
SER155
3.002
ALA156
2.467
PHE159
2.997
LYS160
4.667
ILE179
2.588
ASP180
4.985
|
|||||
| Ligand Name: (4R)-1-(2'-chloro[1,1'-biphenyl]-3-yl)-4-[4-(1,3-thiazole-2-carbonyl)piperazin-1-yl]pyrrolidin-2-one | Ligand Info | |||||
| Structure Description | Crystal structure of human monoacylglycerol lipase in complex with compound 3l | PDB:5ZUN | ||||
| Method | X-ray diffraction | Resolution | 1.35 Å | Mutation | Yes | [2] |
| PDB Sequence |
PRRTPQSIPY
16 QDLPHLVNAD26 GQYLFCRYWA36 PTGTPKALIF46 VSHGAGEHSG56 RYEELARMLM 66 GLDLLVFAHD76 HVGHGQSEGE86 RMVVSDFHVF96 VRDVLQHVDS106 MQKDYPGLPV 116 FLLGHSMGGA126 IAILTAAERP136 GHFAGMVLIS146 PLVLANPESA156 TTFKVLAAKV 166 LNSVLPNLSS176 GPIDSSVLSR186 NKTEVDIYNS196 DPLICRAGLK206 VCFGIQLLNA 216 VSRVERALPK226 LTVPFLLLQG236 SADRLCDSKG246 AYLLMELAKS256 QDKTLKIYEG 266 AYHVLHKELP276 EVTNSVFHEI286 NMWVSQRTA
|
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|
|
GLY50
3.362
ALA51
2.795
GLU53
3.217
ARG57
2.823
MET88
3.603
HIS121
3.459
SER122
2.879
MET123
2.887
GLY124
4.602
LEU148
4.498
GLY177
3.432
PRO178
3.666
ILE179
3.609
|
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| Ligand Name: (2s,4R)-2-{4-[(2-chloro-4-fluorophenoxy)methyl]piperidine-1-carbonyl}-7-oxa-5-azaspiro[3.4]octan-6-one | Ligand Info | |||||
| Structure Description | Crystal structure of human monoacylglycerol lipase in complex with compound 2d | PDB:7L4W | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [3] |
| PDB Sequence |
PRRTPQSIPY
16 QDLPHLVNAD26 GQYLFCRYWA36 PTGTPKALIF46 VSHGAGEHSG56 RYEELARMLM 66 GLDLLVFAHD76 HVGHGQSEGE86 RMVVSDFHVF96 VRDVLQHVDS106 MQKDYPGLPV 116 FLLGHSMGGA126 IAILTAAERP136 GHFAGMVLIS146 PLVLANPESA156 TTFKVLAAKV 166 LNSVLPNLSS176 GPIDSSVLSR186 NKTEVDIYNS196 DPLICRAGLK206 VCFGIQLLNA 216 VSRVERALPK226 LTVPFLLLQG236 SADRLCDSKG246 AYLLMELAKS256 QDKTLKIYEG 266 AYHVLHKELP276 EVTNSVFHEI286 NMWVSQRT
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .XOV or .XOV2 or .XOV3 or :3XOV;style chemicals stick;color identity;select .A:50 or .A:51 or .A:53 or .A:57 or .A:121 or .A:122 or .A:123 or .A:124 or .A:148 or .A:151 or .A:179 or .A:184 or .A:194 or .A:205 or .A:210 or .A:211 or .A:213 or .A:214 or .A:217 or .A:241 or .A:242 or .A:269 or .A:270 or .A:272; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
GLY50
3.514
ALA51
2.959
GLU53
3.400
ARG57
3.021
HIS121
2.980
SER122
2.810
MET123
2.800
GLY124
4.714
LEU148
3.816
ALA151
4.858
ILE179
4.448
LEU184
3.992
|
|||||
| Ligand Name: 6-{4-[(2-chloro-4-fluorophenoxy)methyl]piperidine-1-carbonyl}-2H-1,4-benzoxazin-3(4H)-one | Ligand Info | |||||
| Structure Description | Crystal structure of human monoacylglycerol lipase in complex with compound 1 | PDB:7L4T | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [3] |
| PDB Sequence |
PRRTPQSIPY
16 QDLPHLVNAD26 GQYLFCRYWA36 PTGTPKALIF46 VSHGAGEHSG56 RYEELARMLM 66 GLDLLVFAHD76 HVGHGQSEGE86 RMVVSDFHVF96 VRDVLQHVDS106 MQKDYPGLPV 116 FLLGHSMGGA126 IAILTAAERP136 GHFAGMVLIS146 PLVLANPESA156 TTFKVLAAKV 166 LNSVLPNLSS176 GPIDSSVLSR186 NKTEVDIYNS196 DPLICRAGLK206 VCFGIQLLNA 216 VSRVERALPK226 LTVPFLLLQG236 SADRLCDSKG246 AYLLMELAKS256 QDKTLKIYEG 266 AYHVLHKELP276 EVTNSVFHEI286 NMWVSQRT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .XPD or .XPD2 or .XPD3 or :3XPD;style chemicals stick;color identity;select .A:50 or .A:51 or .A:53 or .A:57 or .A:121 or .A:122 or .A:123 or .A:148 or .A:150 or .A:151 or .A:152 or .A:155 or .A:179 or .A:184 or .A:194 or .A:205 or .A:210 or .A:213 or .A:214 or .A:217 or .A:241 or .A:242 or .A:269 or .A:270; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
GLY50
3.918
ALA51
3.074
GLU53
3.240
ARG57
3.422
HIS121
2.999
SER122
2.761
MET123
3.024
LEU148
3.884
LEU150
4.356
ALA151
3.905
ASN152
4.493
SER155
3.962
|
|||||
| Ligand Name: (5S)-5-(3-{4-[(2-chloro-4-fluorophenoxy)methyl]piperidin-1-yl}-3-oxopropyl)pyrrolidin-2-one | Ligand Info | |||||
| Structure Description | Crystal structure of human monoacylglycerol lipase in complex with compound 1h | PDB:7L4U | ||||
| Method | X-ray diffraction | Resolution | 2.25 Å | Mutation | No | [3] |
| PDB Sequence |
SPRRTPQSIP
15 YQDLPHLVNA25 DGQYLFCRYW35 APTGTPKALI45 FVSHGAGEHS55 GRYEELARML 65 MGLDLLVFAH75 DHVGHGQSEG85 ERMVVSDFHV95 FVRDVLQHVD105 SMQKDYPGLP 115 VFLLGHSMGG125 AIAILTAAER135 PGHFAGMVLI145 SPLVLATTFK160 VLAAKVLNSV 170 LPNLSSGPID180 SSVLSRNKTE190 VDIYNSDPLI200 CRAGLKVCFG210 IQLLNAVSRV 220 ERALPKLTVP230 FLLLQGSADR240 LCDSKGAYLL250 MELAKSQDKT260 LKIYEGAYHV 270 LHKELPEVTN280 SVFHEINMWV290 SQRTA
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .XP7 or .XP72 or .XP73 or :3XP7;style chemicals stick;color identity;select .A:50 or .A:51 or .A:53 or .A:57 or .A:58 or .A:121 or .A:122 or .A:123 or .A:148 or .A:150 or .A:179 or .A:184 or .A:194 or .A:205 or .A:210 or .A:213 or .A:214 or .A:217 or .A:241 or .A:242 or .A:269 or .A:270 or .A:272 or .A:273; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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GLY50
3.647
ALA51
2.755
GLU53
3.102
ARG57
3.197
TYR58
4.930
HIS121
3.011
SER122
2.975
MET123
3.277
LEU148
3.850
LEU150
4.501
ILE179
3.920
LEU184
4.014
|
|||||
| Ligand Name: Magl-IN-4 | Ligand Info | |||||
| Structure Description | Crystal structure of human monoacylglycerol lipase in complex with compound 4f | PDB:7L50 | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | No | [3] |
| PDB Sequence |
MPEESSPRRT
10 PQSIPYQDLP20 HLVNADGQYL30 FCRYWAPTGT40 PKALIFVSHG50 AGEHSGRYEE 60 LARMLMGLDL70 LVFAHDHVGH80 GQSEGERMVV90 SDFHVFVRDV100 LQHVDSMQKD 110 YPGLPVFLLG120 HSMGGAIAIL130 TAAERPGHFA140 GMVLISPLVL150 ANPESATTFK 160 VLAAKVGPID180 SSVLSRNKTE190 VDIYNSDPLI200 CRAGLKVCFG210 IQLLNAVSRV 220 ERALPKLTVP230 FLLLQGSADR240 LCDSKGAYLL250 MELAKSQDKT260 LKIYEGAYHV 270 LHKELPEVTN280 SVFHEINMWV290 SQRTA
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .XOM or .XOM2 or .XOM3 or :3XOM;style chemicals stick;color identity;select .A:50 or .A:51 or .A:53 or .A:57 or .A:58 or .A:121 or .A:122 or .A:123 or .A:124 or .A:148 or .A:151 or .A:155 or .A:156 or .A:159 or .A:184 or .A:194 or .A:205 or .A:210 or .A:213 or .A:214 or .A:241 or .A:242 or .A:269 or .A:270 or .A:272; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
GLY50
3.504
ALA51
2.797
GLU53
3.319
ARG57
3.133
TYR58
4.747
HIS121
3.168
SER122
2.790
MET123
3.151
GLY124
4.863
LEU148
3.769
ALA151
4.262
SER155
3.252
ALA156
4.202
|
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| Ligand Name: 4-({[(4-Chlorophenyl)sulfonyl]amino}methyl)piperidine-1-Carboxylic Acid | Ligand Info | |||||
| Structure Description | Crystal structure of human mono-glyceride lipase in complex with SAR127303 | PDB:4UUQ | ||||
| Method | X-ray diffraction | Resolution | 2.36 Å | Mutation | No | [4] |
| PDB Sequence |
SPRRTPQSIP
25 YQDLPHLVNA35 DGQYLFCRYW45 KPTGTPKALI55 FVSHGAGEHS65 GRYEELARML 75 MGLDLLVFAH85 DHVGHGQSEG95 ERMVVSDFHV105 FVRDVLQHVD115 SMQKDYPGLP 125 VFLLGHSMGG135 AIAILTAAER145 PGHFAGMVLI155 SPLVLANPES165 ATTFKVLAAK 175 VLNLVLPNLS185 LGPIDSSVLS195 RNKTEVDIYN205 SDPLICRAGL215 KVCFGIQLLN 225 AVSRVERALP235 KLTVPFLLLQ245 GSADRLCDSK255 GAYLLMELAK265 SQDKTLKIYE 275 GAYHVLHKEL285 PEVTNSVFHE295 INMWVSQRTA305
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .64D or .64D2 or .64D3 or :364D;style chemicals stick;color identity;select .A:60 or .A:61 or .A:131 or .A:132 or .A:133 or .A:134 or .A:158 or .A:160 or .A:161 or .A:162 or .A:165 or .A:166 or .A:174 or .A:186 or .A:215 or .A:220 or .A:221 or .A:223 or .A:224 or .A:227 or .A:251 or .A:252 or .A:279; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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GLY60
3.606
ALA61
3.039
HIS131
4.566
SER132
1.412
MET133
2.956
GLY134
4.933
LEU158
3.574
LEU160
4.222
ALA161
4.014
ASN162
3.132
SER165
3.372
ALA166
4.030
|
|||||
| Ligand Name: 1-[bis(4-fluorophenyl)methyl]-4-(1H-1,2,4-triazol-1-ylcarbonyl)piperazine | Ligand Info | |||||
| Structure Description | Crystal structure of human mono-glyceride lipase in complex with SAR629 | PDB:3JWE | ||||
| Method | X-ray diffraction | Resolution | 2.70 Å | Mutation | No | [5] |
| PDB Sequence |
SPRRTPQSIP
25 YQDLPHLVNA35 DGQYLFCRYW45 KPTGTPKALI55 FVSHGAGEHS65 GRYEELARML 75 MGLDLLVFAH85 DHVGHGQSEG95 ERMVVSDFHV105 FVRDVLQHVD115 SMQKDYPGLP 125 VFLLGHSMGG135 AIAILTAAER145 PGHFAGMVLI155 SPLVLALPNL184 SLGPIDSSVL 194 SRNKTEVDIY204 NSDPLICRAG214 LKVCFGIQLL224 NAVSRVERAL234 PKLTVPFLLL 244 QGSADRLCDS254 KGAYLLMELA264 KSQDKTLKIY274 EGAYHVLHKE284 LPEVTNSVFH 294 EINMWVSQRT304 A
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .F4P or .F4P2 or .F4P3 or :3F4P;style chemicals stick;color identity;select .A:60 or .A:61 or .A:131 or .A:132 or .A:133 or .A:134 or .A:158 or .A:160 or .A:161 or .A:186 or .A:187 or .A:189 or .A:215 or .A:223 or .A:224 or .A:227 or .A:251 or .A:252 or .A:279; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: MAGLi 432 | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN MONOGLYCERIDE LIPASE WITH LIGAND | PDB:7ZPG | ||||
| Method | X-ray diffraction | Resolution | 1.16 Å | Mutation | Yes | [6] |
| PDB Sequence |
PRRTPQSIPY
16 QDLPHLVNAD26 GQYLFCRYWA36 PTGTPKALIF46 VSHGAGEHSG56 RYEELARMLM 66 GLDLLVFAHD76 HVGHGQSEGE86 RMVVSDFHVF96 VRDVLQHVDS106 MQKDYPGLPV 116 FLLGHSMGGA126 IAILTAAERP136 GHFAGMVLIS146 PLVLANPESA156 TTFKVLAAKV 166 LNSVLPNLSS176 GPIDSSVLSR186 NKTEVDIYNS196 DPLICRAGLK206 VCFGIQLLNA 216 VSRVERALPK226 LTVPFLLLQG236 SADRLCDSKG246 AYLLMELAKS256 QDKTLKIYEG 266 AYHVLHKELP276 EVTNSVFHEI286 NMWVSQRTA
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .JQX or .JQX2 or .JQX3 or :3JQX;style chemicals stick;color identity;select .A:51 or .A:52 or .A:88 or .A:122 or .A:123 or .A:148 or .A:151 or .A:155 or .A:156 or .A:160 or .A:161 or .A:164 or .A:179 or .A:184 or .A:194 or .A:201 or .A:205 or .A:210 or .A:211 or .A:213 or .A:214 or .A:217 or .A:241 or .A:242 or .A:269; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ALA51
3.525
GLY52
4.024
MET88
3.951
SER122
3.456
MET123
4.258
LEU148
3.779
ALA151
3.884
SER155
3.250
ALA156
3.931
LYS160
3.558
VAL161
3.950
ALA164
3.271
ILE179
4.051
|
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| Ligand Name: (4~{R})-1-[4-(4-fluorophenyl)phenyl]-4-[4-(furan-2-ylcarbonyl)piperazin-1-yl]pyrrolidin-2-one | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN MONOGLYCERIDE LIPASE WITH COMPOUND 13 | PDB:7PRM | ||||
| Method | X-ray diffraction | Resolution | 1.65 Å | Mutation | Yes | [7] |
| PDB Sequence |
MPEESSPRRT
10 PQSIPYQDLP20 HLVNADGQYL30 FCRYWAPTGT40 PKALIFVSHG50 AGEHSGRYEE 60 LARMLMGLDL70 LVFAHDHVGH80 GQSEGERMVV90 SDFHVFVRDV100 LQHVDSMQKD 110 YPGLPVFLLG120 HSMGGAIAIL130 TAAERPGHFA140 GMVLISPLVL150 ANPESATTFK 160 VLAAKVLNSV170 LPNLSSGPID180 SSVLSRNKTE190 VDIYNSDPLI200 CRAGLKVCFG 210 IQLLNAVSRV220 ERALPKLTVP230 FLLLQGSADR240 LCDSKGAYLL250 MELAKSQDKT 260 LKIYEGAYHV270 LHKELPEVTN280 SVFHEINMWV290 SQRTA
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .81I or .81I2 or .81I3 or :381I;style chemicals stick;color identity;select .A:50 or .A:51 or .A:53 or .A:57 or .A:121 or .A:122 or .A:123 or .A:124 or .A:148 or .A:151 or .A:155 or .A:156 or .A:159 or .A:179 or .A:181 or .A:184 or .A:185 or .A:190 or .A:191 or .A:194 or .A:205 or .A:213 or .A:214 or .A:241 or .A:242 or .A:269 or .A:270 or .A:273; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
GLY50
3.615
ALA51
2.925
GLU53
3.390
ARG57
2.804
HIS121
3.521
SER122
2.837
MET123
2.913
GLY124
4.787
LEU148
4.010
ALA151
3.789
SER155
3.232
ALA156
3.756
PHE159
3.618
ILE179
4.039
|
|||||
| Ligand Name: 1,1,1,3,3,3-Hexafluoropropan-2-yl 3-(3-phenyl-1,2,4-oxadiazol-5-yl)azetidine-1-carboxylate | Ligand Info | |||||
| Structure Description | Structure of human monoacylglycerol lipase bound to a covalent inhibitor | PDB:6AX1 | ||||
| Method | X-ray diffraction | Resolution | 2.26 Å | Mutation | No | [8] |
| PDB Sequence |
DLPHLVNADG
27 QYLFCRYWKP37 TGTPKALIFV47 SHGAGEHSGR57 YEELARMLMG67 LDLLVFAHDH 77 VGHGQSEGER87 MVVSDFHVFV97 RDVLQHVDSM107 QKDYPGLPVF117 LLGHSMGGAI 127 AILTAAERPG137 HFAGMVLISP147 LVLANPESAT157 TFKVLAAKVL167 NLVLPNLSLG 177 PIDSSVLSRN187 KTEVDIYNSD197 PLICRAGLKV207 CFGIQLLNAV217 SRVERALPKL 227 TVPFLLLQGS237 ADRLCDSKGA247 YLLMELAKSQ257 DKTLKIYEGA267 YHVLHKELPE 277 VTNSVFHEIN287 MWVSQRTATA297
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .C0S or .C0S2 or .C0S3 or :3C0S;style chemicals stick;color identity;select .A:50 or .A:51 or .A:121 or .A:122 or .A:123 or .A:124 or .A:148 or .A:150 or .A:151 or .A:152 or .A:155 or .A:176 or .A:205 or .A:210 or .A:213 or .A:214 or .A:217 or .A:241 or .A:242 or .A:269; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 1-({(1R,5S,6r)-6-[1-(4-fluorophenyl)-1H-pyrazol-3-yl]-3-azabicyclo[3.1.0]hexane-3-carbonyl}oxy)pyrrolidine-2,5-dione | Ligand Info | |||||
| Structure Description | Structure of human monoacylglycerol lipase bound to a covalent inhibitor | PDB:6BQ0 | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [9] |
| PDB Sequence |
DLPHLVNADG
27 QYLFCRYWKP37 TGTPKALIFV47 SHGAGEHSGR57 YEELARMLMG67 LDLLVFAHDH 77 VGHGQSEGER87 MVVSDFHVFV97 RDVLQHVDSM107 QKDYPGLPVF117 LLGHSMGGAI 127 AILTAAERPG137 HFAGMVLISP147 LVLANPESAT157 TFKVLAAKVL167 NLVLPNLSLG 177 PIDSSVLSRN187 KTEVDIYNSD197 PLICRAGLKV207 CFGIQLLNAV217 SRVERALPKL 227 TVPFLLLQGS237 ADRLCDSKGA247 YLLMELAKSQ257 DKTLKIYEGA267 YHVLHKELPE 277 VTNSVFHEIN287 MWVSQRTATA297
|
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .E3A or .E3A2 or .E3A3 or :3E3A;style chemicals stick;color identity;select .A:50 or .A:51 or .A:121 or .A:122 or .A:123 or .A:148 or .A:176 or .A:177 or .A:179 or .A:205 or .A:213 or .A:241 or .A:242 or .A:269; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 ? resolution. Protein Sci. 2011 Apr;20(4):670-83. | ||||
| REF 2 | Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors. J Med Chem. 2018 Oct 25;61(20):9205-9217. | ||||
| REF 3 | Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl Moiety. J Med Chem. 2021 Aug 12;64(15):11014-11044. | ||||
| REF 4 | Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents. Sci Rep. 2015 Jan 6;5:7642. | ||||
| REF 5 | Structural basis for human monoglyceride lipase inhibition. J Mol Biol. 2010 Feb 26;396(3):663-73. | ||||
| REF 6 | A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature. PLoS One. 2022 Sep 9;17(9):e0268590. | ||||
| REF 7 | Development of High Brain-Penetrant and Reversible Monoacylglycerol Lipase PET Tracers for Neuroimaging. J Med Chem. 2022 Feb 10;65(3):2191-2207. | ||||
| REF 8 | Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase. J Med Chem. 2017 Dec 14;60(23):9860-9873. | ||||
| REF 9 | Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation. J Med Chem. 2018 Apr 12;61(7):3008-3026. | ||||
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