Details of the Target

General Information of Target

Target ID LDTP14207
Target Name Adhesion G-protein coupled receptor G1 (ADGRG1)
Gene Name ADGRG1
Gene ID 9289
Synonyms
GPR56; TM7LN4; TM7XN1; Adhesion G-protein coupled receptor G1; G-protein coupled receptor 56; Protein TM7XN1) [Cleaved into: ADGRG1 N-terminal fragment; ADGRG1 NT; GPR56 N-terminal fragment; GPR56 NT; GPR56(N); GPR56 extracellular subunit; GPR56 subunit alpha; ADGRG1 C-terminal fragment; ADGRG1 CT; GPR56 C-terminal fragment; GPR56 CT; GPR56(C); GPR56 seven-transmembrane subunit; GPR56 7TM; GPR56 subunit beta)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKFLIFAFFGGVHLLSLCSGKAICKNGISKRTFEEIKEEIASCGDVAKAIINLAVYGKAQ
NRSYERLALLVDTVGPRLSGSKNLEKAIQIMYQNLQQDGLEKVHLEPVRIPHWERGEESA
VMLEPRIHKIAILGLGSSIGTPPEGITAEVLVVTSFDELQRRASEARGKIVVYNQPYINY
SRTVQYRTQGAVEAAKVGALASLIRSVASFSIYSPHTGIQEYQDGVPKIPTACITVEDAE
MMSRMASHGIKIVIQLKMGAKTYPDTDSFNTVAEITGSKYPEQVVLVSGHLDSWDVGQGA
MDDGGGAFISWEALSLIKDLGLRPKRTLRLVLWTAEEQGGVGAFQYYQLHKVNISNYSLV
MESDAGTFLPTGLQFTGSEKARAIMEEVMSLLQPLNITQVLSHGEGTDINFWIQAGVPGA
SLLDDLYKYFFFHHSHGDTMTVMDPKQMNVAAAVWAVVSYVVADMEEMLPRS
Target Bioclass
GPCR
Family
G-protein coupled receptor 2 family, LN-TM7 subfamily
Subcellular location
Secreted; Membrane raft; Cell membrane
Function
Receptor involved in cell adhesion and probably in cell-cell interactions. Mediates cell matrix adhesion in developing neurons and hematopoietic stem cells. Receptor for collagen III/COL3A1 in the developing brain and involved in regulation of cortical development, specifically in maintenance of the pial basement membrane integrity and in cortical lamination. Binding to the COL3A1 ligand inhibits neuronal migration and activates the RhoA pathway by coupling to GNA13 and possibly GNA12. Plays a role in the maintenance of hematopoietic stem cells and/or leukemia stem cells in bone marrow niche. Plays a critical role in cancer progression by inhibiting VEGFA production threreby inhibiting angiogenesis through a signaling pathway mediated by PRKCA. Plays an essential role in testis development.; [ADGRG1 N-terminal fragment]: Plays a critical role in cancer progression by activating VEGFA production and angiogenesis through a signaling pathway mediated by PRKCA.
Uniprot ID
Q9Y653
Ensemble ID
ENST00000388813.9
HGNC ID
HGNC:4512
ChEMBL ID
CHEMBL4523929

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K195(7.94); K215(5.00)  LDD0277  [1]
OPA-S-S-alkyne
 Probe Info  		K49(1.54); K107(2.31); K215(4.06)  LDD3494  [2]
BTD
 Probe Info  		C434(1.05)  LDD2090  [3]
DBIA
 Probe Info  		C562(1.01)  LDD0531  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C434(0.93)  LDD2103  [3]
 LDCM0214  AC1 HCT 116 C562(1.01)  LDD0531  [4]
 LDCM0279  AC2 HCT 116 C562(1.07)  LDD0596  [4]
 LDCM0290  AC3 HCT 116 C562(1.05)  LDD0607  [4]
 LDCM0301  AC4 HCT 116 C562(1.17)  LDD0618  [4]
 LDCM0308  AC46 HCT 116 C562(0.93)  LDD0625  [4]
 LDCM0309  AC47 HCT 116 C562(1.11)  LDD0626  [4]
 LDCM0310  AC48 HCT 116 C562(1.07)  LDD0627  [4]
 LDCM0311  AC49 HCT 116 C562(1.13)  LDD0628  [4]
 LDCM0312  AC5 HCT 116 C562(0.98)  LDD0629  [4]
 LDCM0313  AC50 HCT 116 C562(1.01)  LDD0630  [4]
 LDCM0314  AC51 HCT 116 C562(1.02)  LDD0631  [4]
 LDCM0315  AC52 HCT 116 C562(0.96)  LDD0632  [4]
 LDCM0316  AC53 HCT 116 C562(1.26)  LDD0633  [4]
 LDCM0317  AC54 HCT 116 C562(1.09)  LDD0634  [4]
 LDCM0318  AC55 HCT 116 C562(1.11)  LDD0635  [4]
 LDCM0319  AC56 HCT 116 C562(1.05)  LDD0636  [4]
 LDCM0367  CL1 HCT 116 C562(0.99)  LDD0684  [4]
 LDCM0368  CL10 HCT 116 C562(0.97)  LDD0685  [4]
 LDCM0369  CL100 HCT 116 C562(1.19)  LDD0686  [4]
 LDCM0379  CL11 HCT 116 C562(0.96)  LDD0696  [4]
 LDCM0390  CL12 HCT 116 C562(0.90)  LDD0707  [4]
 LDCM0392  CL121 HCT 116 C562(0.79)  LDD0709  [4]
 LDCM0393  CL122 HCT 116 C562(1.10)  LDD0710  [4]
 LDCM0394  CL123 HCT 116 C562(1.25)  LDD0711  [4]
 LDCM0395  CL124 HCT 116 C562(1.11)  LDD0712  [4]
 LDCM0400  CL13 HCT 116 C562(0.88)  LDD0717  [4]
 LDCM0401  CL14 HCT 116 C562(1.00)  LDD0718  [4]
 LDCM0402  CL15 HCT 116 C562(0.99)  LDD0719  [4]
 LDCM0407  CL2 HCT 116 C562(0.94)  LDD0724  [4]
 LDCM0418  CL3 HCT 116 C562(0.90)  LDD0735  [4]
 LDCM0420  CL31 HCT 116 C562(0.84)  LDD0737  [4]
 LDCM0421  CL32 HCT 116 C562(0.91)  LDD0738  [4]
 LDCM0422  CL33 HCT 116 C562(1.17)  LDD0739  [4]
 LDCM0423  CL34 HCT 116 C562(0.93)  LDD0740  [4]
 LDCM0424  CL35 HCT 116 C562(0.93)  LDD0741  [4]
 LDCM0425  CL36 HCT 116 C562(1.06)  LDD0742  [4]
 LDCM0426  CL37 HCT 116 C562(1.17)  LDD0743  [4]
 LDCM0428  CL39 HCT 116 C562(1.07)  LDD0745  [4]
 LDCM0429  CL4 HCT 116 C562(1.00)  LDD0746  [4]
 LDCM0430  CL40 HCT 116 C562(0.77)  LDD0747  [4]
 LDCM0431  CL41 HCT 116 C562(1.10)  LDD0748  [4]
 LDCM0432  CL42 HCT 116 C562(0.93)  LDD0749  [4]
 LDCM0433  CL43 HCT 116 C562(1.18)  LDD0750  [4]
 LDCM0434  CL44 HCT 116 C562(1.04)  LDD0751  [4]
 LDCM0435  CL45 HCT 116 C562(1.09)  LDD0752  [4]
 LDCM0436  CL46 HCT 116 C562(0.90)  LDD0753  [4]
 LDCM0437  CL47 HCT 116 C562(0.84)  LDD0754  [4]
 LDCM0438  CL48 HCT 116 C562(0.83)  LDD0755  [4]
 LDCM0439  CL49 HCT 116 C562(0.83)  LDD0756  [4]
 LDCM0440  CL5 HCT 116 C562(0.90)  LDD0757  [4]
 LDCM0441  CL50 HCT 116 C562(0.95)  LDD0758  [4]
 LDCM0442  CL51 HCT 116 C562(0.83)  LDD0759  [4]
 LDCM0443  CL52 HCT 116 C562(0.92)  LDD0760  [4]
 LDCM0444  CL53 HCT 116 C562(0.84)  LDD0761  [4]
 LDCM0445  CL54 HCT 116 C562(0.88)  LDD0762  [4]
 LDCM0446  CL55 HCT 116 C562(0.80)  LDD0763  [4]
 LDCM0447  CL56 HCT 116 C562(0.87)  LDD0764  [4]
 LDCM0448  CL57 HCT 116 C562(0.84)  LDD0765  [4]
 LDCM0449  CL58 HCT 116 C562(0.91)  LDD0766  [4]
 LDCM0450  CL59 HCT 116 C562(0.91)  LDD0767  [4]
 LDCM0451  CL6 HCT 116 C562(0.86)  LDD0768  [4]
 LDCM0452  CL60 HCT 116 C562(0.86)  LDD0769  [4]
 LDCM0462  CL7 HCT 116 C562(1.04)  LDD0779  [4]
 LDCM0473  CL8 HCT 116 C562(1.19)  LDD0790  [4]
 LDCM0484  CL9 HCT 116 C562(1.08)  LDD0801  [4]
 LDCM0486  CL91 HCT 116 C562(1.40)  LDD0803  [4]
 LDCM0487  CL92 HCT 116 C562(1.22)  LDD0804  [4]
 LDCM0488  CL93 HCT 116 C562(1.26)  LDD0805  [4]
 LDCM0489  CL94 HCT 116 C562(0.94)  LDD0806  [4]
 LDCM0490  CL95 HCT 116 C562(0.95)  LDD0807  [4]
 LDCM0491  CL96 HCT 116 C562(1.02)  LDD0808  [4]
 LDCM0492  CL97 HCT 116 C562(1.30)  LDD0809  [4]
 LDCM0493  CL98 HCT 116 C562(1.16)  LDD0810  [4]
 LDCM0494  CL99 HCT 116 C562(1.00)  LDD0811  [4]
 LDCM0427  Fragment51 HCT 116 C562(1.12)  LDD0744  [4]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C434(1.32)  LDD2102  [3]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C434(1.05)  LDD2090  [3]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C434(0.78)  LDD2092  [3]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C434(0.96)  LDD2094  [3]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C434(1.49)  LDD2098  [3]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C434(1.02)  LDD2105  [3]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C434(1.49)  LDD2147  [3]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C434(1.57)  LDD2153  [3]

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 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
4 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.