Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T64765 | Target Info | |||
| Target Name | Histamine H3 receptor (H3R) | ||||
| Synonyms | Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97 | ||||
| Target Type | Successful Target | ||||
| Gene Name | HRH3 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Cholesterol | Ligand Info | |||||
| Structure Description | Crystal structure of human histamine receptor H3R in complex with antagonist PF03654746 | PDB:7F61 | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | Yes | [1] |
| PDB Sequence |
RGFSAAWTAV
36 LAALMALLIV46 ATVLGNALVM56 LAFVADSSLR66 TQNNFFLLNL76 AISDFLVGAF 86 CIPLYVPYVL96 TGRWTFGRGL106 CKLWLVVDYL116 LCTSKAFNIV126 LISYDRFLSV 136 TRAVSYRAQQ146 GDTRRAVRKM156 LLVWVLAFLL166 YGPAILSWEY176 LSGGSSIPEG 186 HCYAEFFYNW196 YFLITASTLE206 FFTPFLSVTF216 FNLSIYLNIQ226 RRTRLRLDGA 236 REAAGRFRLS351 RDRKVAKSLA361 VIVSIFGLCW371 APYTLLMIIR381 AACHGHCVPD 391 YWYETSFWLL401 WANSAVNPVL411 YPLCHHSFRR421 AFTKLLCPQK431 L |
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| Ligand Name: N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of human histamine receptor H3R in complex with antagonist PF03654746 | PDB:7F61 | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | Yes | [1] |
| PDB Sequence |
RGFSAAWTAV
36 LAALMALLIV46 ATVLGNALVM56 LAFVADSSLR66 TQNNFFLLNL76 AISDFLVGAF 86 CIPLYVPYVL96 TGRWTFGRGL106 CKLWLVVDYL116 LCTSKAFNIV126 LISYDRFLSV 136 TRAVSYRAQQ146 GDTRRAVRKM156 LLVWVLAFLL166 YGPAILSWEY176 LSGGSSIPEG 186 HCYAEFFYNW196 YFLITASTLE206 FFTPFLSVTF216 FNLSIYLNIQ226 RRTRLRLDGA 236 REAAGRFRLS351 RDRKVAKSLA361 VIVSIFGLCW371 APYTLLMIIR381 AACHGHCVPD 391 YWYETSFWLL401 WANSAVNPVL411 YPLCHHSFRR421 AFTKLLCPQK431 L |
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis for recognition of antihistamine drug by human histamine receptor. Nat Commun. 2022 Oct 15;13(1):6105. | ||||
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