Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T00156 | Target Info | |||
| Target Name | Short transient receptor potential channel 5 (TRPC5) | ||||
| Synonyms | hTRP5; hTRP-5; TrpC5; Transient receptor protein 5; TRP-5 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | TRPC5 | ||||
| Biochemical Class | Transient receptor potential catioin channel | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Cholesterol hemisuccinate | Ligand Info | |||
| Canonical SMILES | CC(C)CCCC(C)C1CCC2C1(CCC3C2CC=C4C3(CCC(C4)OC(=O)CCC(=O)O)C)C | ||||
| InChI | 1S/C31H50O4/c1-20(2)7-6-8-21(3)25-11-12-26-24-10-9-22-19-23(35-29(34)14-13-28(32)33)15-17-30(22,4)27(24)16-18-31(25,26)5/h9,20-21,23-27H,6-8,10-19H2,1-5H3,(H,32,33)/t21-,23+,24+,25-,26+,27+,30+,31-/m1/s1 | ||||
| InChIKey | WLNARFZDISHUGS-MIXBDBMTSA-N | ||||
| PubChem Compound ID | 65082 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 7WDB Human TRPC5 channel in complex with riluzole | ||||||
| Method | Electron microscopy | Resolution | 2.40 Å | Mutation | No | [1] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYQFSEFTPD 142 ITPIMLAAHT152 NNYEIIKLLV162 QKRVTIPRPH172 QIRCNCVECV182 SSSEVDSLRH 192 SRSRLNIYKA202 LASPSLIALS212 SEDPILTAFR222 LGWELKELSK232 VENEFKAEYE 242 ELSQQCKLFA252 KDLLDQARSS262 RELEIILNHR272 DDLAKLKVAI294 KYHQKEFVAQ 304 PNCQQLLATL314 WYDGFPGWRR324 KHWVVKLLTC334 MTIGFLFPML344 SIAYLISPRS 354 NLGLFIKKPF364 IKFICHTASY374 LTFLFMLLLA384 SQHVQGPPPT401 VVEWMILPWV 411 LGFIWGEIKE421 MWDGGFTEYI431 HDWWNLMDFA441 MNSLYLATIS451 LKIVAYVKYN 461 GSRPREEWEM471 WHPTLIAEAL481 FAISNILSSL491 RLISLFTANS501 HLGPLQISLG 511 RMLLDILKFL521 FIYCLVLLAF531 ANGLNQLYFY541 YETRAIDEPN551 NCKGIRCEKQ 561 NNAFSTLFET571 LQSLFWSVFG581 LLNLYVTNVK591 ARHEFTEFVG601 ATMFGTYNVI 611 SLVVLLNMLI621 AMMNNSYQLI631 ADHADIEWKF641 ARTKLWMSYF651 DEGGTLPPPF 661 NIISLIQNQH712 YQEVIRNLVK722 RYVAAMIRNS732 KTTEENFKEL746 KQDISSFRYE 756 VLDLL
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| PDB ID: 7D4P Structure of human TRPC5 in complex with clemizole | ||||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [2] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYTQFSEFTP 141 DITPIMLAAH151 TNNYEIIKLL161 VQKRVTIPRP171 HQIRCNCVEC181 VSSSEVDSLR 191 HSRSRLNIYK201 ALASPSLIAL211 SSEDPILTAF221 RLGWELKELS231 KVENEFKAEY 241 EELSQQCKLF251 AKDLLDQARS261 SRELEIILNH271 RDDLAKLKVA293 IKYHQKEFVA 303 QPNCQQLLAT313 LWYDGFPGWR323 RKHWVVKLLT333 CMTIGFLFPM343 LSIAYLISPR 353 SNLGLFIKKP363 FIKFICHTAS373 YLTFLFMLLL383 ASQDLHVQGP398 PPTVVEWMIL 408 PWVLGFIWGE418 IKEMWDGGFT428 EYIHDWWNLM438 DFAMNSLYLA448 TISLKIVAYV 458 KYNGSRPREE468 WEMWHPTLIA478 EALFAISNIL488 SSLRLISLFT498 ANSHLGPLQI 508 SLGRMLLDIL518 KFLFIYCLVL528 LAFANGLNQL538 YFYYETRAID548 EPNNCKGIRC 558 EKQNNAFSTL568 FETLQSLFWS578 VFGLLNLYVT588 NVKARHEFTE598 FVGATMFGTY 608 NVISLVVLLN618 MLIAMMNNSY628 QLIADHADIE638 WKFARTKLWM648 SYFDEGGTLP 658 PPFNIISLIQ709 NQHYQEVIRN719 LVKRYVAAMI729 RNSKTTEENF743 KELKQDISSF 753 RYEVLDLLG
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| PDB ID: 7D4Q Structure of human TRPC5 in complex with HC-070 | ||||||
| Method | Electron microscopy | Resolution | 2.74 Å | Mutation | No | [2] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYTQFSEFTP 141 DITPIMLAAH151 TNNYEIIKLL161 VQKRVTIPRP171 HQIRCNCVEC181 VSSSEVDSLR 191 HSRSRLNIYK201 ALASPSLIAL211 SSEDPILTAF221 RLGWELKELS231 KVENEFKAEY 241 EELSQQCKLF251 AKDLLDQARS261 SRELEIILNH271 RDDLAKLKVA293 IKYHQKEFVA 303 QPNCQQLLAT313 LWYDGFPGWR323 RKHWVVKLLT333 CMTIGFLFPM343 LSIAYLISPR 353 SNLGLFIKKP363 FIKFICHTAS373 YLTFLFMLLL383 ASQDLHVQGP398 PPTVVEWMIL 408 PWVLGFIWGE418 IKEMWDGGFT428 EYIHDWWNLM438 DFAMNSLYLA448 TISLKIVAYV 458 KYNGSRPREE468 WEMWHPTLIA478 EALFAISNIL488 SSLRLISLFT498 ANSHLGPLQI 508 SLGRMLLDIL518 KFLFIYCLVL528 LAFANGLNQL538 YFYYETRAID548 EPNNCKGIRC 558 EKQNNAFSTL568 FETLQSLFWS578 VFGLLNLYVT588 NVKARHEFTE598 FVGATMFGTY 608 NVISLVVLLN618 MLIAMMNNSY628 QLIADHADIE638 WKFARTKLWM648 SYFDEGGTLP 658 PPFNIISLIQ709 NQHYQEVIRN719 LVKRYVAAMI729 RNSKTTEENF743 KELKQDISSF 753 RYEVLDLL
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| PDB ID: 7E4T Human TRPC5 apo state structure at 3 angstrom | ||||||
| Method | Electron microscopy | Resolution | 3.00 Å | Mutation | No | [2] |
| PDB Sequence |
RIPLQIVRAE
26 TELSAEEKAF36 LNAVEKGDYA46 TVKQALQEAE56 IYYNVNINCM66 DPLGRSALLI 76 AIENENLEIM86 ELLLNHSVYV96 GDALLYAIRK106 EVVGAVELLL116 SYQFSEFTPD 142 ITPIMLAAHT152 NNYEIIKLLV162 QKRVTIPRPH172 QIRCNCVECV182 SSSEVDSLRH 192 SRSRLNIYKA202 LASPSLIALS212 SEDPILTAFR222 LGWELKELSK232 VENEFKAEYE 242 ELSQQCKLFA252 KDLLDQARSS262 RELEIILNHR272 DDLAKLKVAI294 KYHQKEFVAQ 304 PNCQQLLATL314 WYDGFPGWRR324 KHWVVKLLTC334 MTIGFLFPML344 SIAYLISPRS 354 NLGLFIKKPF364 IKFICHTASY374 LTFLFMLLLA384 SQDLHVQGPP399 PTVVEWMILP 409 WVLGFIWGEI419 KEMWDGGFTE429 YIHDWWNLMD439 FAMNSLYLAT449 ISLKIVAYVK 459 YNGSRPREEW469 EMWHPTLIAE479 ALFAISNILS489 SLRLISLFTA499 NSHLGPLQIS 509 LGRMLLDILK519 FLFIYCLVLL529 AFANGLNQLY539 FYYETRAIDE549 PNNCKGIRCE 559 KQNNAFSTLF569 ETLQSLFWSV579 FGLLNLYVTN589 VKARHEFTEF599 VGATMFGTYN 609 VISLVVLLNM619 LIAMMNNSYQ629 LIADHADIEW639 KFARTKLWMS649 YFDEGGTLPP 659 PFNIISLIQN710 QHYQEVIRNL720 VKRYVAAMIR730 NTEENFKELK747 QDISSFRYEV 757 LDLL
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural identification of riluzole-binding site on human TRPC5. Cell Discov. 2022 Jul 12;8(1):67. | ||||
| REF 2 | Structural basis for human TRPC5 channel inhibition by two distinct inhibitors. Elife. 2021 Mar 8;10:e63429. | ||||
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