Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T02719 | Target Info | |||
| Target Name | Metabotropic glutamate receptor 3 (mGluR3) | ||||
| Synonyms | mGLUR3; Group III metabotropic glutamate receptor; GPRC1C | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | GRM3 | ||||
| Biochemical Class | GPCR glutamate | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | [3H]LY341495 | Ligand Info | |||
| Canonical SMILES | C1C(C1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O | ||||
| InChI | 1S/C20H19NO5/c21-20(19(24)25,15-9-13(15)18(22)23)10-14-11-5-1-3-7-16(11)26-17-8-4-2-6-12(14)17/h1-8,13-15H,9-10,21H2,(H,22,23)(H,24,25)/t13-,15-,20-/m0/s1 | ||||
| InChIKey | VLZBRVJVCCNPRJ-KPHUOKFYSA-N | ||||
| PubChem Compound ID | 9819927 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 7WI6 Cryo-EM structure of LY341495/NAM-bound mGlu3 | ||||||
| Method | Electron microscopy | Resolution | 3.71 Å | Mutation | No | [1] |
| PDB Sequence |
REIKIEGDLV
40 LGGLFPINEK50 RINEDRGIQR68 LEAMLFAIDE78 INKDDYLLPG88 VKLGVHILDT 98 CSRDTYALEQ108 SLEFVRASLL141 IAGVIGGSYS151 SVSIQVANLL161 RLFQIPQISY 171 ASTSAKLSDK181 SRYDYFARTV191 PPDFYQAKAM201 AEILRFFNWT211 YVSTVASEGD 221 YGETGIEAFE231 QEARLRNICI241 ATAEKVGSYD257 SVIRELLQKP267 NARVVVLFMR 277 SDDSRELIAA287 ASRANASFTW297 VASDGWGAQE307 SIIKGSEHVA317 YGAITLELAS 327 QPVRQFDRYF337 QSLNPYNNHR347 NPWFRDFWEQ357 KFQCSLRVCD374 KHLAIDSSNY 384 EQESKIMFVV394 NAVYAMAHAL404 HKMQRTLCPN414 TTKLCDAMKI424 LDGKKLYKDY 434 LLKINFTAPF444 NPNKDADSIV454 KFDTFGDGMG464 RYNVFNFQNV474 GGKYSYLKVG 484 HWAETLSLDV494 NSIHWSRNSV504 PTSQCSDPCA514 PNEMKNMQPG524 DVCCWICIPC 534 EPYEYLADEF544 TCMDCGSGQW554 PTADLTGCYD564 LPEDYIRWED574 AWAIGPVTIA 584 CLGFMCTCMV594 VTVFIKHNNT604 PLVKASGREL614 CYILLFGVGL624 SYCMTFFFIA 634 KPSPVICALR644 RLGLGSSFAI654 CYSALLTKTN664 CSSQVFICLG694 LILVQIVMVS 704 VWLILEAPGT714 RRYTLAEKRE724 TVILKCNVKD734 SSMLISLTYD744 VILVILCTVY 754 AFPENFNEAK769 FIGFTMYTTC779 IIWLAFLPIF789 YVTSSDYRVQ799 TTTMCISVSL 809 SGFVVLGCLF819 APK
|
|||||
|
|
||||||
| PDB ID: 7WI8 Cryo-EM structure of inactive mGlu3 bound to LY341495 | ||||||
| Method | Electron microscopy | Resolution | 4.17 Å | Mutation | No | [1] |
| PDB Sequence |
REIKIEGDLV
40 LGGLFPINER59 INEDRGIQRL69 EAMLFAIDEI79 NKDDYLLPGV89 KLGVHILDTC 99 SRDTYALEQS109 LEFVRASLLI142 AGVIGGSYSS152 VSIQVANLLR162 LFQIPQISYA 172 STSAKLSDKS182 RYDYFARTVP192 PDFYQAKAMA202 EILRFFNWTY212 VSTVASEGDY 222 GETGIEAFEQ232 EARLRNICIA242 TAEKVGSYDS258 VIRELLQKPN268 ARVVVLFMRS 278 DDSRELIAAA288 SRANASFTWV298 ASDGWGAQES308 IIKGSEHVAY318 GAITLELASQ 328 PVRQFDRYFQ338 SLNPYNNHRN348 PWFRDFWEQK358 FQCSLLAIDS381 SNYEQESKIM 391 FVVNAVYAMA401 HALHKMQRTL411 CPNTTKLCDA421 MKILDGKKLY431 KDYLLKINFT 441 APFNPNKDAD451 SIVKFDTFGD461 GMGRYNVFNF471 QNVGGKYSYL481 KVGHWAETLS 491 LDVNSIHWSR501 NSVPTSQCSD511 PCAPNEMKNM521 QPGDVCCWIC531 IPCEPYEYLA 541 DEFTCMDCGS551 GQWPTADLTG561 CYDLPEDYIR571 WEDAWAIGPV581 TIACLGFMCT 591 CMVVTVFIKH601 NNTPLVKASG611 RELCYILLFG621 VGLSYCMTFF631 FIAKPSPVIC 641 ALRRLGLGSS651 FAICYSALLT661 KTNCIARQVF690 ICLGLILVQI700 VMVSVWLILE 710 APGTRRYTLA720 EKRETVILKC730 NVKDSSMLIS740 LTYDVILVIL750 CTVYAFKTRK 760 CPENFNEAKF770 IGFTMYTTCI780 IWLAFLPIFY790 VTSSDYRVQT800 TTMCISVSLS 810 GFVVLGCLFA820 PKV
|
|||||
|
|
||||||
| PDB ID: 3SM9 Crystal Structure of Metabotropic glutamate receptor 3 precursor in presence of LY341495 antagonist | ||||||
| Method | X-ray diffraction | Resolution | 2.26 Å | Mutation | No | [2] |
| PDB Sequence |
RREIKIEGDL
14 VLGGLFPINE24 KGTTEECGRI35 NEDRGIQRLE45 AMLFAIDEIN55 KDDYLLPGVK 65 LGVHILDTCS75 RDTYALEQSL85 EFVRASLLIA118 GVIGGSYSSV128 SIQVANLLRL 138 FQIPQISYAS148 TSAKLSDKSR158 YDYFARTVPP168 DFYQAKAMAE178 ILRFFNWTYV 188 STVASEGDYG198 ETGIEAFEQE208 ARLRNISIAT218 AEKVGRIRKS230 YDSVIRELLQ 240 KPNARVVVLF250 MRSDDSRELI260 AAASRANASF270 TWVASDGWGA280 QESIIKGSEH 290 VAYGAITLEL300 ASQPVRQFDR310 YFQSLNPYNN320 HRNPWFRDFW330 EQKFQCSLQN 343 HRRVCDKHLA353 IDSSNYEQES363 KIMFVVNAVY373 AMAHALHKMQ383 RTLCPNTTKL 393 CDAMKILDGK403 KLYKDYLLKI413 NFTAPFNDSI428 VKFDTFGDGM438 GRYNVFNFQN 448 VGGKYSYLKV458 GHWAETLSLD468 VNSIHWS
|
|||||
|
|
||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis of the activation of metabotropic glutamate receptor 3. Cell Res. 2022 Jul;32(7):695-698. | ||||
| REF 2 | Crystal Structure of Metabotropic glutamate receptor 3 precursor in presence of LY341495 antagonist | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.