Details of the Target

General Information of Target

Target ID LDTP03774
Target Name G protein-coupled receptor kinase 3 (GRK3)
Gene Name GRK3
Gene ID 157
Synonyms
ADRBK2; BARK2; G protein-coupled receptor kinase 3; EC 2.7.11.15; Beta-adrenergic receptor kinase 2; Beta-ARK-2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MADLEAVLADVSYLMAMEKSKATPAARASKRIVLPEPSIRSVMQKYLAERNEITFDKIFN
QKIGFLLFKDFCLNEINEAVPQVKFYEEIKEYEKLDNEEDRLCRSRQIYDAYIMKELLSC
SHPFSKQAVEHVQSHLSKKQVTSTLFQPYIEEICESLRGDIFQKFMESDKFTRFCQWKNV
ELNIHLTMNEFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMTYAFHTPDKLCFILDLMNGGDLHYHLSQHGVFSEKEMRFYATE
IILGLEHMHNRFVVYRDLKPANILLDEHGHARISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGTAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTVNVELPDTFSPE
LKSLLEGLLQRDVSKRLGCHGGGSQEVKEHSFFKGVDWQHVYLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDCDQELYKNFPLVISERWQQEVTETVYEAVNADTDKIEARK
RAKNKQLGHEEDYALGKDCIMHGYMLKLGNPFLTQWQRRYFYLFPNRLEWRGEGESRQNL
LTMEQILSVEETQIKDKKCILFRIKGGKQFVLQCESDPEFVQWKKELNETFKEAQRLLRR
APKFLNKPRSGTVELPKPSLCHRNSNGL
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, GPRK subfamily
Subcellular location
Postsynapse
Function Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.
TTD ID
T57174
Uniprot ID
P35626
DrugMap ID
TT5A4DX
Ensemble ID
ENST00000324198.11
HGNC ID
HGNC:290
ChEMBL ID
CHEMBL1075166

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info  		N.A.  LDD0241  [1]
DBIA
 Probe Info  		C103(10.44)  LDD0209  [2]
4-Iodoacetamidophenylacetylene
 Probe Info  		C72(0.00); C120(0.00); C154(0.00); C379(0.00)  LDD0038  [3]
IA-alkyne
 Probe Info  		C120(0.00); C379(0.00); C501(0.00); C681(0.00)  LDD0036  [3]
Lodoacetamide azide
 Probe Info  		C559(0.00); C120(0.00); C379(0.00); C501(0.00)  LDD0037  [3]
NAIA_4
 Probe Info  		N.A.  LDD2226  [4]
NAIA_5
 Probe Info  		N.A.  LDD2225  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0226  AC11 HEK-293T C120(0.77)  LDD1509  [5]
 LDCM0237  AC12 HEK-293T C120(1.09)  LDD1510  [5]
 LDCM0278  AC19 HEK-293T C120(0.97)  LDD1517  [5]
 LDCM0280  AC20 HEK-293T C120(1.14)  LDD1519  [5]
 LDCM0281  AC21 HEK-293T C154(1.25)  LDD1520  [5]
 LDCM0287  AC27 HEK-293T C120(0.89)  LDD1526  [5]
 LDCM0288  AC28 HEK-293T C120(0.98)  LDD1527  [5]
 LDCM0289  AC29 HEK-293T C154(1.09)  LDD1528  [5]
 LDCM0290  AC3 HEK-293T C120(1.01)  LDD1529  [5]
 LDCM0296  AC35 HEK-293T C120(0.75)  LDD1535  [5]
 LDCM0297  AC36 HEK-293T C120(1.20)  LDD1536  [5]
 LDCM0298  AC37 HEK-293T C154(1.24)  LDD1537  [5]
 LDCM0301  AC4 HEK-293T C120(1.15)  LDD1540  [5]
 LDCM0305  AC43 HEK-293T C120(0.80)  LDD1544  [5]
 LDCM0306  AC44 HEK-293T C120(0.86)  LDD1545  [5]
 LDCM0307  AC45 HEK-293T C154(0.99)  LDD1546  [5]
 LDCM0312  AC5 HEK-293T C154(1.29)  LDD1551  [5]
 LDCM0314  AC51 HEK-293T C120(0.83)  LDD1553  [5]
 LDCM0315  AC52 HEK-293T C120(0.84)  LDD1554  [5]
 LDCM0316  AC53 HEK-293T C154(1.37)  LDD1555  [5]
 LDCM0322  AC59 HEK-293T C120(0.90)  LDD1561  [5]
 LDCM0324  AC60 HEK-293T C120(1.02)  LDD1563  [5]
 LDCM0325  AC61 HEK-293T C154(0.97)  LDD1564  [5]
 LDCM0248  AKOS034007472 HEK-293T C154(1.11)  LDD1511  [5]
 LDCM0369  CL100 HEK-293T C120(0.93)  LDD1573  [5]
 LDCM0373  CL104 HEK-293T C120(0.87)  LDD1577  [5]
 LDCM0377  CL108 HEK-293T C120(0.99)  LDD1581  [5]
 LDCM0382  CL112 HEK-293T C120(0.97)  LDD1586  [5]
 LDCM0386  CL116 HEK-293T C120(0.94)  LDD1590  [5]
 LDCM0391  CL120 HEK-293T C120(0.96)  LDD1595  [5]
 LDCM0395  CL124 HEK-293T C120(0.74)  LDD1599  [5]
 LDCM0399  CL128 HEK-293T C120(0.77)  LDD1603  [5]
 LDCM0403  CL16 HEK-293T C120(0.68)  LDD1607  [5]
 LDCM0406  CL19 HEK-293T C120(0.81)  LDD1610  [5]
 LDCM0408  CL20 HEK-293T C120(0.98)  LDD1612  [5]
 LDCM0409  CL21 HEK-293T C154(1.26)  LDD1613  [5]
 LDCM0416  CL28 HEK-293T C120(0.85)  LDD1620  [5]
 LDCM0420  CL31 HEK-293T C120(0.66)  LDD1624  [5]
 LDCM0421  CL32 HEK-293T C120(0.80)  LDD1625  [5]
 LDCM0422  CL33 HEK-293T C154(1.06)  LDD1626  [5]
 LDCM0429  CL4 HEK-293T C120(0.82)  LDD1633  [5]
 LDCM0430  CL40 HEK-293T C120(1.07)  LDD1634  [5]
 LDCM0433  CL43 HEK-293T C120(0.80)  LDD1637  [5]
 LDCM0434  CL44 HEK-293T C120(0.89)  LDD1638  [5]
 LDCM0435  CL45 HEK-293T C154(1.13)  LDD1639  [5]
 LDCM0443  CL52 HEK-293T C120(0.82)  LDD1646  [5]
 LDCM0446  CL55 HEK-293T C120(0.80)  LDD1649  [5]
 LDCM0447  CL56 HEK-293T C120(0.87)  LDD1650  [5]
 LDCM0448  CL57 HEK-293T C154(0.99)  LDD1651  [5]
 LDCM0456  CL64 HEK-293T C120(0.86)  LDD1659  [5]
 LDCM0459  CL67 HEK-293T C120(0.75)  LDD1662  [5]
 LDCM0460  CL68 HEK-293T C120(1.08)  LDD1663  [5]
 LDCM0461  CL69 HEK-293T C154(1.09)  LDD1664  [5]
 LDCM0462  CL7 HEK-293T C120(0.77)  LDD1665  [5]
 LDCM0469  CL76 HEK-293T C120(0.92)  LDD1672  [5]
 LDCM0472  CL79 HEK-293T C120(0.69)  LDD1675  [5]
 LDCM0473  CL8 HEK-293T C120(0.82)  LDD1676  [5]
 LDCM0474  CL80 HEK-293T C120(1.03)  LDD1677  [5]
 LDCM0475  CL81 HEK-293T C154(1.38)  LDD1678  [5]
 LDCM0482  CL88 HEK-293T C120(0.79)  LDD1685  [5]
 LDCM0484  CL9 HEK-293T C154(1.07)  LDD1687  [5]
 LDCM0486  CL91 HEK-293T C120(0.71)  LDD1689  [5]
 LDCM0487  CL92 HEK-293T C120(0.95)  LDD1690  [5]
 LDCM0488  CL93 HEK-293T C154(1.10)  LDD1691  [5]
 LDCM0022  KB02 22RV1 C340(1.54)  LDD2243  [6]
 LDCM0023  KB03 Jurkat C103(10.44)  LDD0209  [2]
 LDCM0024  KB05 HMCB C340(1.56)  LDD3312  [6]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Beta-adrenergic receptor kinase 1 (GRK2) AGC Ser/Thr protein kinase family P25098

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atp Small molecular drug DB00171
Pmid21596927c101 Small molecular drug D0U8UK

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
3 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
5 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
6 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840