Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T77913 | Target Info | |||
| Target Name | Histamine H1 receptor (H1R) | ||||
| Synonyms | HH1R; H1R | ||||
| Target Type | Successful Target | ||||
| Gene Name | HRH1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Ergotidine | Ligand Info | |||||
| Structure Description | Cryo-EM structure of histamine H1 receptor Gq complex | PDB:7DFL | ||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | No | [1] |
| PDB Sequence |
MPLVVVLSTI
37 CLVTVGLNLL47 VLYAVRSERK57 LHTVGNLYIV67 SLSVADLIVG77 AVVMPMNILY 87 LLMSKWSLGR97 PLCLFWLSMD107 YVASTASIFS117 VFILCIDRYR127 SVQQPLRYLK 137 YRTKTRASAT147 ILGAWFLSFL157 WVIPILGWNH167 FMQQTSVRRE177 DKCETDFYDV 187 TWFKVMTAII197 NFYLPTLLML207 WFYAKIYKAV217 RQHCLHMNRE410 RKAAKQLGFI 420 MAAFILCWIP430 YFIFFMVIAF440 CKNCCNEHLH450 MFTIWLGYIN460 STLNPLIYPL 470 CNENFKKTFK480 RILHI
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| Ligand Name: Doxepin | Ligand Info | |||||
| Structure Description | Structure of the human histamine H1 receptor in complex with doxepin | PDB:3RZE | ||||
| Method | X-ray diffraction | Resolution | 3.10 Å | Mutation | Yes | [2] |
| PDB Sequence |
MPLVVVLSTI
37 CLVTVGLNLL47 VLYAVRSERK57 LHTVGNLYIV67 SLSVADLIVG77 AVVMPMNILY 87 LLMSKWSLGR97 PLCLFWLSMD107 YVASTASIFS117 VFILCIDRYR127 SVQQPLRYLK 137 YRTKTRASAT147 ILGAWFLSFL157 WVIPILGWNH167 RREDKCETDF184 YDVTWFKVMT 194 AIINFYLPTL204 LMLWFYAKIY214 KAVRQHCNIF1004 EMLRIDEGLR1014 LKIYKDTEGY 1024 YTIGIGHLLT1034 KSPSLNAAKS1044 ELDKAIGRNT1054 NGVITKDEAE1064 KLFNQDVDAA 1074 VRGILRNAKL1084 KPVYDSLDAV1094 RRAALINMVF1104 QMGETGVAGF1114 TNSLRMLQQK 1124 RWDEAAVNLA1134 KSRWYNQTPN1144 RAKRVITTFR1154 TGTWDAYLHM407 NRERKAAKQL 417 GFIMAAFILC427 WIPYFIFFMV437 IAFCKNCCNE447 HLHMFTIWLG457 YINSTLNPLI 467 YPLCNENFKK477 TFKRILHI
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| Ligand Name: Doxepin | Ligand Info | |||||
| Structure Description | Structure of the human histamine H1 receptor in complex with doxepin | PDB:3RZE | ||||
| Method | X-ray diffraction | Resolution | 3.10 Å | Mutation | Yes | [2] |
| PDB Sequence |
MPLVVVLSTI
37 CLVTVGLNLL47 VLYAVRSERK57 LHTVGNLYIV67 SLSVADLIVG77 AVVMPMNILY 87 LLMSKWSLGR97 PLCLFWLSMD107 YVASTASIFS117 VFILCIDRYR127 SVQQPLRYLK 137 YRTKTRASAT147 ILGAWFLSFL157 WVIPILGWNH167 RREDKCETDF184 YDVTWFKVMT 194 AIINFYLPTL204 LMLWFYAKIY214 KAVRQHCNIF1004 EMLRIDEGLR1014 LKIYKDTEGY 1024 YTIGIGHLLT1034 KSPSLNAAKS1044 ELDKAIGRNT1054 NGVITKDEAE1064 KLFNQDVDAA 1074 VRGILRNAKL1084 KPVYDSLDAV1094 RRAALINMVF1104 QMGETGVAGF1114 TNSLRMLQQK 1124 RWDEAAVNLA1134 KSRWYNQTPN1144 RAKRVITTFR1154 TGTWDAYLHM407 NRERKAAKQL 417 GFIMAAFILC427 WIPYFIFFMV437 IAFCKNCCNE447 HLHMFTIWLG457 YINSTLNPLI 467 YPLCNENFKK477 TFKRILHI
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Click to Show 3D Structure of This Binding Site
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Cryo-EM structure of the human histamine H(1) receptor/G(q) complex. Nat Commun. 2021 Apr 7;12(1):2086. | ||||
| REF 2 | Structure of the human histamine H1 receptor complex with doxepin. Nature. 2011 Jun 22;475(7354):65-70. | ||||
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