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5TZR

GPR40 in complex with partial agonist MK-8666

Functional Information from GO Data
ChainGOidnamespacecontents
A0003796molecular_functionlysozyme activity
A0003824molecular_functioncatalytic activity
A0004930molecular_functionG protein-coupled receptor activity
A0007186biological_processG protein-coupled receptor signaling pathway
A0009253biological_processpeptidoglycan catabolic process
A0016020cellular_componentmembrane
A0016787molecular_functionhydrolase activity
A0016798molecular_functionhydrolase activity, acting on glycosyl bonds
A0016998biological_processcell wall macromolecule catabolic process
A0030430cellular_componenthost cell cytoplasm
A0031640biological_processkilling of cells of another organism
A0042742biological_processdefense response to bacterium
A0044659biological_processviral release from host cell by cytolysis
Functional Information from PDB Data
site_idAC1
Number of Residues4
Detailsbinding site for residue NA A 2401
ChainResidue
ASER1036
APHE1114
ASER1117
AHOH2549

site_idAC2
Number of Residues13
Detailsbinding site for residue MK6 A 2402
ChainResidue
AGLY139
APHE142
ALEU158
ATRP174
AARG183
ATYR2240
AARG2258
AHOH2551
APRO80
AALA83
APHE87
ATYR91
ALEU138

site_idAC3
Number of Residues3
Detailsbinding site for residue MLI A 2403
ChainResidue
AGLU1011
AGLY1030
AGLN1105

site_idAC4
Number of Residues3
Detailsbinding site for residue OLC A 2404
ChainResidue
ALEU188
APHE2248
AOLC2408

site_idAC5
Number of Residues7
Detailsbinding site for residue OLC A 2405
ChainResidue
APHE9
APRO40
ATYR44
AALA102
AALA103
ALEU189
ALEU190

site_idAC6
Number of Residues1
Detailsbinding site for residue OLC A 2407
ChainResidue
AOLC2408

site_idAC7
Number of Residues3
Detailsbinding site for residue OLC A 2408
ChainResidue
ATHR31
AOLC2404
AOLC2407

site_idAC8
Number of Residues2
Detailsbinding site for residue OLC A 2409
ChainResidue
ATRP2224
AGLY2227

site_idAC9
Number of Residues1
Detailsbinding site for residue OLC A 2410
ChainResidue
AGLN6

site_idAD1
Number of Residues4
Detailsbinding site for residue OLC A 2411
ChainResidue
AVAL64
APRO73
ALEU78
ALEU106

site_idAD2
Number of Residues1
Detailsbinding site for residue 1PE A 2412
ChainResidue
ATYR2250

site_idAD3
Number of Residues8
Detailsbinding site for residue 1PE A 2413
ChainResidue
AGLY1023
ATYR1024
ATYR1025
ALYS1035
APRO1037
ALYS1135
AARG1137
AASN1140

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues22
DetailsTransmembrane: {"description":"Helical; Name=1","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues9
DetailsTopological domain: {"description":"Cytoplasmic","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues22
DetailsTransmembrane: {"description":"Helical; Name=2","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI4
Number of Residues56
DetailsTopological domain: {"description":"Extracellular","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI5
Number of Residues21
DetailsTransmembrane: {"description":"Helical; Name=3","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI6
Number of Residues20
DetailsTransmembrane: {"description":"Helical; Name=4","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI7
Number of Residues21
DetailsTransmembrane: {"description":"Helical; Name=5","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI8
Number of Residues24
DetailsTransmembrane: {"description":"Helical; Name=6","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI9
Number of Residues22
DetailsTransmembrane: {"description":"Helical; Name=7","evidences":[{"evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"25043059","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI10
Number of Residues2
DetailsSite: {"description":"Important for receptor activation","evidences":[{"source":"PubMed","id":"19068482","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI11
Number of Residues1
DetailsGlycosylation: {"description":"N-linked (GlcNAc...) asparagine","evidences":[{"evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI12
Number of Residues1
DetailsActive site: {"description":"Proton donor/acceptor","evidences":[{"source":"HAMAP-Rule","id":"MF_04110","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"3382407","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"7831309","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"8266098","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI13
Number of Residues1
DetailsActive site: {"description":"Proton donor/acceptor","evidences":[{"source":"HAMAP-Rule","id":"MF_04110","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"1892846","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"3382407","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"7831309","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"8266098","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI14
Number of Residues2
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"8266098","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI15
Number of Residues2
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"7831309","evidenceCode":"ECO:0000303"}]}
ChainResidueDetails

Catalytic Information from CSA
site_idMCSA1
Number of Residues2
DetailsM-CSA 921
ChainResidueDetails
AGLU1011proton shuttle (general acid/base)
AASP1020covalent catalysis

247536

PDB entries from 2026-01-14

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