Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94255 | Target Info | |||
| Target Name | Long transient receptor potential channel 4 (TRPM4) | ||||
| Synonyms | hTRPM4; Transient receptor potential cation channel subfamily M member 4; Melastatin-4; LTrpC4; LTrpC-4; Calcium-activated non-selective cation channel 1 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | TRPM4 | ||||
| Biochemical Class | Transient receptor potential catioin channel | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Decavanadate | Ligand Info | |||||
| Structure Description | Cryo-EM structure of a human TRPM4 channel in complex with calcium and decavanadate | PDB:5WP6 | ||||
| Method | Electron microscopy | Resolution | 3.80 Å | Mutation | No | [1] |
| PDB Sequence |
EQSWIPKIFK
16 KKTCHTTEKP71 TDAYGELDFT81 GAGRKHSNFL91 RLSDRTDPAA101 VYSLVTRTWG 111 FRAPNLVVSV121 LGGSGGPVLQ131 TWLQDLLRRG141 LVRAAQSTGA151 WIVTGGLHTG 161 IGRHVGVAVR171 DHQMASTGGT181 KVVAMGVAPW191 GVVRNRDTLI201 NPKGSFPARY 211 RWRGVQFPLD226 YNYSAFFLVD236 DGTHGCLGGE246 NRFRLRLESY256 ISQQKTGVGG 266 TGIDIPVLLL276 LIDGDEKMLT286 RIENATQAQL296 PCLLVAGSGG306 AADCLAETLE 316 DTRQGEARDR334 IRRFFPKGDL344 EVLQAQVERI354 MTRKELLTVY364 SSEDGSEEFE 374 TIVLKALVKA384 CGSYLDELRL399 AVAWNRVDIA409 QSELFRGDIQ419 WRSFHLEASL 429 MDALLNDRPE439 FVRLLISHGL449 SLGHFLTPMR459 LAQLYSAAPS469 NSLIRNLLDQ 479 APWSDLLLWA566 LLLNRAQMAM576 YFWEMGSNAV586 SSALGACLLL596 RVMARLEPDA 606 EEAARRKDLA616 FKFEGMGVDL626 FGECYRSSEV636 RAARLLLRRC646 PLWGDATCLQ 656 LAMQADARAF666 FAQDGVQSLL676 TQKWWGDMAS686 TTPIWALVLA696 FFCPPLIYTR 706 LITFRRCLRR771 WFHFWGAPVT781 IFMGNVVSYL791 LFLLLFSRVL801 LVDFQPAPPG 811 SLELLLYFWA821 FTLLCEELRQ831 GLSGGSLASG843 GPGPGHASLS853 QRLRLYLADS 863 WNQCDLVALT873 CFLLGVGCRL883 TPGLYHLGRT893 VLCIDFMVFT903 VRLLHIFTVN 913 KQLGPKIVIV923 SKMMKDVFFF933 LFFLGVWLVA943 YGVATEGLLR953 PRDSDFPSIL 963 RRVFYRPYLQ973 IFGQIPQEDM983 DVALMEHSNC993 SSEPGFWAHP1003 PGAQAGTCVS 1013 QYANWLVVLL1023 LVIFLLVANI1033 LLVNLLIAMF1043 SYTFGKVQGN1053 SDLYWKAQRY 1063 RLIREFHSRP1073 ALAPPFIVIS1083 HLRLLLRQAL1106 EHFRVYLSKE1116 AERKLLTWES 1126 VHKENFLLAR1136 ARDKRESDSE1146 RLKRTSQKVD1156 LALKQLGHIR1166 EYEQRLKVLE 1176 REVQQCSRVL1186 GWVAEAL
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| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Human TRPM4 ion channel in lipid nanodiscs in a calcium-bound state | PDB:6BQV | ||||
| Method | Electron microscopy | Resolution | 3.10 Å | Mutation | No | [2] |
| PDB Sequence |
TGAGRHSNFL
91 RLSDRTDPAA101 VYSLVTRTWG111 FRAPNLVVSV121 LGGSGGPVLQ131 TWLQDLLRRG 141 LVRAAQSTGA151 WIVTGGLHTG161 IGRHVGVAVR171 DHQMASTGGT181 KVVAMGVAPW 191 GVVRNRDTLI201 NPKGSFPARY211 RWVQFPLDYN228 YSAFFLVDDL243 GGENRFRLRL 253 ESYISQQKTG263 VGGTGIDIPV273 LLLLIDGDEK283 MLTRIENATQ293 AQLPCLLVAG 303 SGGAADCLAE313 TLEDTLGEAR332 DRIRRFFPKG342 DLEVLQAQVE352 RIMTRKELLT 362 VYSSEDGSEE372 FETIVLKALV382 KACGEASAYL394 DELRLAVAWN404 RVDIAQSELF 414 RGDIQWRSFH424 LEASLMDALL434 NDRPEFVRLL444 ISHGLSLGHF454 LTPMRLAQLY 464 SAAPSNSLIR474 NLLDQASVGH505 VLRMLLGPWS560 DLLLWALLLN570 RAQMAMYFWE 580 MGSNAVSSAL590 GACLLLRVMA600 RLEPDAEEAA610 RRKDLAFKFE620 GMGVDLFGEC 630 YRSSEVRAAR640 LLLRRCPLWG650 DATCLQLAMQ660 ADARAFFAQD670 GVQSLLTQKW 680 WGDMASTTPI690 WALVLAFFCP700 PLIYTRLITF710 RRCLRRWFHF775 WGAPVTIFMG 785 NVVSYLLFLL795 LFSRVLLVDF805 QPAPPGSLEL815 LLYFWAFTLL825 CEELRQGLSG 835 SGGPGPGHAS851 LSQRLRLYLA861 DSWNQCDLVA871 LTCFLLGVGC881 RLTPGLYHLG 891 RTVLCIDFMV901 FTVRLLHIFT911 VNKQLGPKIV921 IVSKMMKDVF931 FFLFFLGVWL 941 VAYGVATEGL951 LRPRDSDFPS961 ILRRVFYRPY971 LQIFGQIPQE981 DMDVALMEHS 991 NCSSEPGFWA1001 HPPGAQAGTC1011 VSQYANWLVV1021 LLLVIFLLVA1031 NILLVNLLIA 1041 MFSYTFGKVQ1051 GNSDLYWKAQ1061 RYRLIREFHS1071 RPALAPPFIV1081 ISHLRLLLRQ 1091 LCREHFRVYL1113 SKEAERKLLT1123 WESVHKENFL1133 LARARDKRES1143 DSERLKRTSQ 1153 KVDLALKQLG1163 HIREYEQRLK1173 VL
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TRP680
3.324
ILE690
3.678
LEU693
4.817
VAL694
3.642
PHE698
4.100
VAL780
4.018
PHE783
3.172
MET784
3.926
VAL787
3.748
VAL788
3.682
LEU791
3.380
LEU792
4.318
LEU795
3.649
TRP864
4.008
VAL904
4.245
LEU907
3.655
HIS908
3.590
PHE910
4.110
VAL912
4.500
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Electron cryo-microscopy structure of a human TRPM4 channel. Nature. 2017 Dec 14;552(7684):200-204. | ||||
| REF 2 | Structure of the human TRPM4 ion channel in a lipid nanodisc. Science. 2018 Jan 12;359(6372):228-232. | ||||
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