Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T83813 | Target Info | |||
| Target Name | 5-HT 2C receptor (HTR2C) | ||||
| Synonyms | Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C | ||||
| Target Type | Successful Target | ||||
| Gene Name | HTR2C | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Lorcaserin | Ligand Info | |||
| Canonical SMILES | CC1CNCCC2=C1C=C(C=C2)Cl | ||||
| InChI | 1S/C11H14ClN/c1-8-7-13-5-4-9-2-3-10(12)6-11(8)9/h2-3,6,8,13H,4-5,7H2,1H3/t8-/m0/s1 | ||||
| InChIKey | XTTZERNUQAFMOF-QMMMGPOBSA-N | ||||
| PubChem Compound ID | 11658860 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 8DPF Cryo-EM structure of the 5HT2C receptor (INI isoform) bound to lorcaserin | ||||||
| Method | Electron microscopy | Resolution | 2.84 Å | Mutation | Yes | [1] |
| PDB Sequence |
SIVIIIIMTI
68 GGNILVIMAV78 SMEKKLHNAT88 NYFLMSLAIA98 DMLVGLLVMP108 LSLLAILYDY 118 VWLCPVWISL133 DVLFSTASIM143 HLCAISLDRY153 VAIRNPIEHS163 RFNSRTKAIM 173 KIAIVWAISI183 GVSVPIPVIG193 LRDEEKVFVN203 TCVLNDPNFV215 LIGSFVAFFI 225 PLTIMVITYC235 LTIYVLRRQA245 LMMQAINNER307 KASKVLGIVF317 FVFLIMWCPF 327 FITNILSVLC337 ECNQKLMEKL349 LNVFVWIGYV359 CSGINPLVYT369 LFNKIYRRAF 379 SNYL
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| PDB ID: 8DPH Cryo-EM structure of the 5HT2C receptor (VGV isoform) bound to lorcaserin | ||||||
| Method | Electron microscopy | Resolution | 3.20 Å | Mutation | Yes | [1] |
| PDB Sequence |
SIVIIIIMTI
68 GGNILVIMAV78 SMEKKLHNAT88 NYFLMSLAIA98 DMLVGLLVMP108 LSLLAILYDY 118 VWLCPVWISL133 DVLFSTASIM143 HLCAISLDRY153 VAVRSPVEHS163 RFNSRTKAIM 173 KIAIVWAISI183 GVSVPIPVIG193 LRDEEKVFVN203 TCVLNDPNFV215 LIGSFVAFFI 225 PLTIMVITYC235 LTIYVLRRQA245 LMMQAINNER307 KASKVLGIVF317 FVFLIMWCPF 327 FITNILSVLC337 ECNQKLMEKL349 LNVFVWIGYV359 CSGINPLVYT369 LFNKIYRRAF 379 SNYL
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| PDB ID: 8DPI Cryo-EM structure of the 5HT2C receptor (VSV isoform) bound to lorcaserin | ||||||
| Method | Electron microscopy | Resolution | 3.40 Å | Mutation | Yes | [1] |
| PDB Sequence |
SIVIIIIMTI
68 GGNILVIMAV78 SMEKKLHNAT88 NYFLMSLAIA98 DMLVGLLVMP108 LSLLAILYDY 118 VWLCPVWISL133 DVLFSTASIM143 HLCAISLDRY153 VAVRSPVEHS163 RFNSRTKAIM 173 KIAIVWAISI183 GVSVPIPVIG193 LRDEEKVFVN203 TCVLNDPNFV215 LIGSFVAFFI 225 PLTIMVITYC235 LTIYVLRRQA245 LMMQAINNER307 KASKVLGIVF317 FVFLIMWCPF 327 FITNILSVLC337 ECNQKLMEKL349 LNVFVWIGYV359 CSGINPLVYT369 LFNKIYRRAF 379 SNYL
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Molecular insights into the regulation of constitutive activity by RNA editing of 5HT(2C) serotonin receptors. Cell Rep. 2022 Aug 16;40(7):111211. | ||||
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