Details of the Target

General Information of Target

Target ID LDTP04024
Target Name Glucagon-like peptide 1 receptor (GLP1R)
Gene Name GLP1R
Gene ID 2740
Synonyms
Glucagon-like peptide 1 receptor; GLP-1 receptor; GLP-1-R; GLP-1R
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDL
FCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPW
RDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIH
LNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAAN
YYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRN
SNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLL
GTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERW
RLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 2 family
Subcellular location
Cell membrane
Function
G-protein coupled receptor for glucagon-like peptide 1 (GLP-1). Ligand binding triggers activation of a signaling cascade that leads to the activation of adenylyl cyclase and increased intracellular cAMP levels. Plays a role in regulating insulin secretion in response to GLP-1.
TTD ID
T36075
Uniprot ID
P43220
DrugMap ID
TTVIMDE
Ensemble ID
ENST00000373256.5
HGNC ID
HGNC:4324
ChEMBL ID
CHEMBL1784

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
BTD
 Probe Info  		C341(0.89)  LDD2107  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C341(0.89)  LDD2107  [1]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C341(0.98)  LDD2136  [1]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C341(0.84)  LDD2137  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
Keratin-associated protein 1-1 (KRTAP1-1) KRTAP type 1 family Q07627
Keratin-associated protein 1-3 (KRTAP1-3) KRTAP type 1 family Q8IUG1
Keratin-associated protein 10-7 (KRTAP10-7) KRTAP type 10 family P60409
Keratin-associated protein 10-8 (KRTAP10-8) KRTAP type 10 family P60410
Keratin-associated protein 10-9 (KRTAP10-9) KRTAP type 10 family P60411
Keratin-associated protein 5-9 (KRTAP5-9) KRTAP type 5 family P26371
Notch homolog 2 N-terminal-like protein A (NOTCH2NLA) NOTCH family Q7Z3S9
Notch homolog 2 N-terminal-like protein C (NOTCH2NLC) NOTCH family P0DPK4
Keratin-associated protein 17-1 (KRTAP17-1) . Q9BYP8

The Drug(s) Related To This Target

Approved
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Glucagon BiotechDrug DB00040
Exenatide Small molecular drug D00YVF
Liraglutide Small molecular drug D03GOI
Lixisenatide Small molecular drug D05MKA
Pramlintide Small molecular drug D0C4AM
Semaglutide Small molecular drug D02ULU
Albiglutide . D0F1DY
Dulaglutide . D03NAW
Phase 3
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gma102 Antibody DK1MX0
Gma105 Antibody DO78YZ
Efpeglenatide . D05OZQ
Glp-1 . D08NXW
Latin T1d . D0H1UW
Taspoglutide . D0B1EQ
Tirzepatide . DA69JF
Phase 2
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bi 456906 Small molecular drug DX1U3C
Pf-06882961 Small molecular drug D5XV9K
Gtp-010 . D0O3DK
Ly-2428757 . D0U9LV
Ly2944876 . D08FMK
Oi338gt . D06QWM
Ormd-0901 . D05XXF
Pb-1023 . D03MSV
Tt-401 . D0Q8VM
Ttp-054 . D09FTJ
Ttp273 . D0DI1B
Uni-re-4 . D0G4QL
Phase 1
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ct 868 Small molecular drug DEC8O3
Cm3.1-ac100 . D08PCR
Cnto-3649 . D0W7SX
Cvx 096 . D0FC4R
Jnj-54728518 . D00TED
Nn-9926 . D08NIN
Og987sc . D0U9NN
Pf-4603629 . D00BZZ
Sar425899 . D02URD
Sar438335 . D0FY4L
Zp2929 . D0FW0B
Zyog1 . D0A0FB
Investigative
Click To Hide/Show 33 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gx-g6 Antibody D01TMK
Ac-3174 Small molecular drug D0NY1R
Betp Small molecular drug D03JQD
Ampe4l . D0D7YR
Cam-2036 . D0ED6E
Cnto-736 . D07MBQ
C[Asp22-lys26][Gly8]Glp-1(7-37)-nh2 . D0B3BS
C[Cpa19-lys26][Gly8]Glp-1(7-37)-nh2 . D0W8BP
C[Glu18-lys22][Gly8]Glp-1(7-37)-nh2 . D0B4WW
C[Glu19-lys23][Gly8]Glp-1(7-37)-nh2 . D0S2GY
C[Glu21-lys25][Gly8]Glp-1(7-37)-nh2 . D04LSW
C[Glu21-lys26][Gly8]Glp-1(7-37)-nh2 . D0W2EI
C[Glu22-lys26][Gly8]Glp-1(7-37)-nh2 . D08HSQ
C[Glu22-orn26][Gly8]Glp-1(7-37)-nh2 . D03YDP
C[Glu23-lys27][Gly8]Glp-1(7-37)-nh2 . D0M7LZ
C[Glu24-lys28][Gly8]Glp-1(7-37)-nh2 . D0R1NH
C[Glu26-lys30][Gly8]Glp-1(7-37)-nh2 . D04NUZ
C[Hglu22-lys26][Gly8]Glp-1(7-37)-nh2 . D0I7WD
F-18 Exendin-4 Derivative Pet Tracers . D0O0LF
Glp-17-(7-36) Derivative . D0XL7R
Glu20-lys24][Gly8][Glp-1(7-37)-nh2 . D0F2GY
Glucagon-like Peptide-1 Analog . D0Q4AR
Glutazumab . DB16697
Haegtftsdvssylegqaakefiawlvkgrg-nh2 . D02TKT
Haegtftsdvssylegqaakeifawlvkgr . D00UCX
Pgc Glp-1 . D0U2XB
Skl-18287 . D0D9KV
Sx-glp1 . D09RUJ
Zp-3022 . D0Z9WP
[123i] Iodobenzoyl 12-ex4 . D0O1DS
[Gly8, Aib22]Glp-1(7-37)-nh2 . D06PZJ
[Gly8,Glu22]Glp-1(7,37)-nh2 . D0BL8S
[Gly8]Glp-1(7-37)-nh2 . D0R2ZG
Discontinued
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cjc-1131 Small molecular drug D0L1JE
Azm-134 . D0I0TD
Cm-glp-1 . D00NSM
Ly-307161 . D0Q9HT
Ly-315902 . D0K5HD
Rg7685 . D0M4RX
Th-0318 . D0D2JD

References

1 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761