Details of the Target

General Information of Target

Target ID LDTP14273
Target Name Casein kinase I isoform gamma-3 (CSNK1G3)
Gene Name CSNK1G3
Gene ID 1456
Synonyms
Casein kinase I isoform gamma-3; CKI-gamma 3; EC 2.7.11.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MMNKLYIGNLSPAVTADDLRQLFGDRKLPLAGQVLLKSGYAFVDYPDQNWAIRAIETLSG
KVELHGKIMEVDYSVSKKLRSRKIQIRNIPPHLQWEVLDGLLAQYGTVENVEQVNTDTET
AVVNVTYATREEAKIAMEKLSGHQFENYSFKISYIPDEEVSSPSPPQRAQRGDHSSREQG
HAPGGTSQARQIDFPLRILVPTQFVGAIIGKEGLTIKNITKQTQSRVDIHRKENSGAAEK
PVTIHATPEGTSEACRMILEIMQKEADETKLAEEIPLKILAHNGLVGRLIGKEGRNLKKI
EHETGTKITISSLQDLSIYNPERTITVKGTVEACASAEIEIMKKLREAFENDMLAVNQQA
NLIPGLNLSALGIFSTGLSVLSPPAGPRGAPPAAPYHPFTTHSGYFSSLYPHHQFGPFPH
HHSYPEQEIVNLFIPTQAVGAIIGKKGAHIKQLARFAGASIKIAPAEGPDVSERMVIITG
PPEAQFKAQGRIFGKLKEENFFNPKEEVKLEAHIRVPSSTAGRVIGKGGKTVNELQNLTS
AEVIVPRDQTPDENEEVIVRIIGHFFASQTAQRKIREIVQQVKQQEQKYPQGVASQRSK
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CK1 Ser/Thr protein kinase family, Casein kinase I subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine-protein kinase. Casein kinases are operationally defined by their preferential utilization of acidic proteins such as caseins as substrates. It can phosphorylate a large number of proteins. Participates in Wnt signaling. Regulates fast synaptic transmission mediated by glutamate.
TTD ID
T29728
Uniprot ID
Q9Y6M4
DrugMap ID
TT34L5N
Ensemble ID
ENST00000345990.9
HGNC ID
HGNC:2456
ChEMBL ID
CHEMBL5084

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
DBIA
 Probe Info  		C51(6.72)  LDD0209  [2]
ATP probe
 Probe Info  		N.A.  LDD0199  [3]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [4]
TFBX
 Probe Info  		N.A.  LDD0027  [4]
WYneO
 Probe Info  		N.A.  LDD0022  [5]
ENE
 Probe Info  		N.A.  LDD0006  [5]
IPM
 Probe Info  		N.A.  LDD0005  [5]
SF
 Probe Info  		Y68(0.00); Y87(0.00)  LDD0028  [6]
STPyne
 Probe Info  		N.A.  LDD0009  [5]
YN-1
 Probe Info  		N.A.  LDD0447  [7]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [8]
AOyne
 Probe Info  		11.60  LDD0443  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C277(0.96); C51(1.37); C108(1.10)  LDD1507  [10]
 LDCM0215  AC10 HEK-293T C277(1.07); C51(0.92); C130(0.92)  LDD1508  [10]
 LDCM0226  AC11 HEK-293T C277(0.83); C51(0.97)  LDD1509  [10]
 LDCM0237  AC12 HEK-293T C51(0.98)  LDD1510  [10]
 LDCM0259  AC14 HEK-293T C277(1.03); C51(0.93)  LDD1512  [10]
 LDCM0270  AC15 HEK-293T C277(0.92); C51(0.88)  LDD1513  [10]
 LDCM0276  AC17 HEK-293T C277(0.75); C51(0.98); C108(0.87)  LDD1515  [10]
 LDCM0277  AC18 HEK-293T C277(1.29); C51(0.94); C130(0.98)  LDD1516  [10]
 LDCM0278  AC19 HEK-293T C277(0.47); C51(1.06)  LDD1517  [10]
 LDCM0279  AC2 HEK-293T C277(1.12); C51(0.88); C130(0.93)  LDD1518  [10]
 LDCM0280  AC20 HEK-293T C51(0.95)  LDD1519  [10]
 LDCM0281  AC21 HEK-293T C51(0.97)  LDD1520  [10]
 LDCM0282  AC22 HEK-293T C277(0.77); C51(0.97)  LDD1521  [10]
 LDCM0283  AC23 HEK-293T C277(1.02); C51(0.95)  LDD1522  [10]
 LDCM0284  AC24 HEK-293T C277(0.96); C51(0.96)  LDD1523  [10]
 LDCM0285  AC25 HEK-293T C277(2.00); C51(0.94); C108(1.11)  LDD1524  [10]
 LDCM0286  AC26 HEK-293T C277(1.28); C51(0.97); C130(0.98)  LDD1525  [10]
 LDCM0287  AC27 HEK-293T C277(0.72); C51(0.95)  LDD1526  [10]
 LDCM0288  AC28 HEK-293T C51(1.28)  LDD1527  [10]
 LDCM0289  AC29 HEK-293T C51(0.94)  LDD1528  [10]
 LDCM0290  AC3 HEK-293T C277(0.87); C51(0.98)  LDD1529  [10]
 LDCM0291  AC30 HEK-293T C277(0.96); C51(0.94)  LDD1530  [10]
 LDCM0292  AC31 HEK-293T C277(1.01); C51(0.90)  LDD1531  [10]
 LDCM0293  AC32 HEK-293T C277(0.82); C51(1.01)  LDD1532  [10]
 LDCM0294  AC33 HEK-293T C277(0.81); C51(0.97); C108(1.07)  LDD1533  [10]
 LDCM0295  AC34 HEK-293T C277(1.40); C51(0.97); C130(0.91)  LDD1534  [10]
 LDCM0296  AC35 HEK-293T C277(0.98); C51(1.01)  LDD1535  [10]
 LDCM0297  AC36 HEK-293T C51(0.97)  LDD1536  [10]
 LDCM0298  AC37 HEK-293T C51(0.97)  LDD1537  [10]
 LDCM0299  AC38 HEK-293T C277(0.91); C51(0.99)  LDD1538  [10]
 LDCM0300  AC39 HEK-293T C277(0.97); C51(0.97)  LDD1539  [10]
 LDCM0301  AC4 HEK-293T C51(0.96)  LDD1540  [10]
 LDCM0302  AC40 HEK-293T C277(1.11); C51(0.97)  LDD1541  [10]
 LDCM0303  AC41 HEK-293T C277(0.68); C51(0.92); C108(0.99)  LDD1542  [10]
 LDCM0304  AC42 HEK-293T C277(0.89); C51(1.01); C130(0.97)  LDD1543  [10]
 LDCM0305  AC43 HEK-293T C277(0.88); C51(1.02)  LDD1544  [10]
 LDCM0306  AC44 HEK-293T C51(0.96)  LDD1545  [10]
 LDCM0307  AC45 HEK-293T C51(1.00)  LDD1546  [10]
 LDCM0308  AC46 HEK-293T C277(0.85); C51(1.04)  LDD1547  [10]
 LDCM0309  AC47 HEK-293T C277(0.94); C51(0.93)  LDD1548  [10]
 LDCM0310  AC48 HEK-293T C277(0.85); C51(0.96)  LDD1549  [10]
 LDCM0311  AC49 HEK-293T C277(0.65); C51(0.92); C108(1.07)  LDD1550  [10]
 LDCM0312  AC5 HEK-293T C51(0.91)  LDD1551  [10]
 LDCM0313  AC50 HEK-293T C277(1.09); C51(0.95); C130(0.81)  LDD1552  [10]
 LDCM0314  AC51 HEK-293T C277(1.17); C51(0.95)  LDD1553  [10]
 LDCM0315  AC52 HEK-293T C51(0.97)  LDD1554  [10]
 LDCM0316  AC53 HEK-293T C51(0.99)  LDD1555  [10]
 LDCM0317  AC54 HEK-293T C277(0.87); C51(0.99)  LDD1556  [10]
 LDCM0318  AC55 HEK-293T C277(1.01); C51(0.97)  LDD1557  [10]
 LDCM0319  AC56 HEK-293T C277(1.06); C51(0.96)  LDD1558  [10]
 LDCM0320  AC57 HEK-293T C277(0.90); C51(1.03); C108(1.09)  LDD1559  [10]
 LDCM0321  AC58 HEK-293T C277(1.26); C51(0.93); C130(0.81)  LDD1560  [10]
 LDCM0322  AC59 HEK-293T C277(0.84); C51(0.98)  LDD1561  [10]
 LDCM0323  AC6 HEK-293T C277(0.86); C51(0.99)  LDD1562  [10]
 LDCM0324  AC60 HEK-293T C51(1.03)  LDD1563  [10]
 LDCM0325  AC61 HEK-293T C51(0.96)  LDD1564  [10]
 LDCM0326  AC62 HEK-293T C277(0.91); C51(0.96)  LDD1565  [10]
 LDCM0327  AC63 HEK-293T C277(1.09); C51(0.93)  LDD1566  [10]
 LDCM0328  AC64 HEK-293T C277(0.96); C51(0.98)  LDD1567  [10]
 LDCM0334  AC7 HEK-293T C277(0.85); C51(1.05)  LDD1568  [10]
 LDCM0345  AC8 HEK-293T C277(0.91); C51(0.96)  LDD1569  [10]
 LDCM0248  AKOS034007472 HEK-293T C51(0.95)  LDD1511  [10]
 LDCM0356  AKOS034007680 HEK-293T C277(0.96); C51(0.92); C108(1.04)  LDD1570  [10]
 LDCM0275  AKOS034007705 HEK-293T C277(1.04); C51(0.96)  LDD1514  [10]
 LDCM0156  Aniline NCI-H1299 11.94  LDD0403  [1]
 LDCM0367  CL1 HEK-293T C277(0.92)  LDD1571  [10]
 LDCM0368  CL10 HEK-293T C277(0.85); C51(1.26)  LDD1572  [10]
 LDCM0369  CL100 HEK-293T C51(0.97)  LDD1573  [10]
 LDCM0370  CL101 HEK-293T C277(0.78)  LDD1574  [10]
 LDCM0373  CL104 HEK-293T C51(0.99)  LDD1577  [10]
 LDCM0374  CL105 HEK-293T C277(0.81)  LDD1578  [10]
 LDCM0377  CL108 HEK-293T C51(1.03)  LDD1581  [10]
 LDCM0378  CL109 HEK-293T C277(1.29)  LDD1582  [10]
 LDCM0379  CL11 HEK-293T C277(0.81); C51(1.12)  LDD1583  [10]
 LDCM0382  CL112 HEK-293T C51(1.04)  LDD1586  [10]
 LDCM0383  CL113 HEK-293T C277(0.89)  LDD1587  [10]
 LDCM0386  CL116 HEK-293T C51(0.96)  LDD1590  [10]
 LDCM0387  CL117 HEK-293T C277(0.78)  LDD1591  [10]
 LDCM0390  CL12 HEK-293T C277(1.06); C51(1.01)  LDD1594  [10]
 LDCM0391  CL120 HEK-293T C51(1.00)  LDD1595  [10]
 LDCM0392  CL121 HEK-293T C277(0.82)  LDD1596  [10]
 LDCM0395  CL124 HEK-293T C51(0.97)  LDD1599  [10]
 LDCM0396  CL125 HEK-293T C277(1.06)  LDD1600  [10]
 LDCM0399  CL128 HEK-293T C51(1.00)  LDD1603  [10]
 LDCM0400  CL13 HEK-293T C277(0.87)  LDD1604  [10]
 LDCM0403  CL16 HEK-293T C51(0.98)  LDD1607  [10]
 LDCM0404  CL17 HEK-293T C277(1.16); C51(0.93); C108(1.34)  LDD1608  [10]
 LDCM0405  CL18 HEK-293T C277(1.34); C51(0.95); C130(1.04)  LDD1609  [10]
 LDCM0406  CL19 HEK-293T C277(0.69); C51(1.05)  LDD1610  [10]
 LDCM0408  CL20 HEK-293T C51(1.03)  LDD1612  [10]
 LDCM0409  CL21 HEK-293T C51(1.03)  LDD1613  [10]
 LDCM0410  CL22 HEK-293T C277(0.81); C51(1.12)  LDD1614  [10]
 LDCM0411  CL23 HEK-293T C277(0.92); C51(0.97)  LDD1615  [10]
 LDCM0412  CL24 HEK-293T C277(0.99); C51(1.03)  LDD1616  [10]
 LDCM0413  CL25 HEK-293T C277(0.68)  LDD1617  [10]
 LDCM0416  CL28 HEK-293T C51(1.04)  LDD1620  [10]
 LDCM0417  CL29 HEK-293T C277(0.98); C51(0.93); C108(1.02)  LDD1621  [10]
 LDCM0419  CL30 HEK-293T C277(0.98); C51(1.00); C130(0.93)  LDD1623  [10]
 LDCM0420  CL31 HEK-293T C277(1.22); C51(1.13)  LDD1624  [10]
 LDCM0421  CL32 HEK-293T C51(1.02)  LDD1625  [10]
 LDCM0422  CL33 HEK-293T C51(1.05)  LDD1626  [10]
 LDCM0423  CL34 HEK-293T C277(0.93); C51(1.06)  LDD1627  [10]
 LDCM0424  CL35 HEK-293T C277(0.98); C51(1.05)  LDD1628  [10]
 LDCM0425  CL36 HEK-293T C277(0.99); C51(1.04)  LDD1629  [10]
 LDCM0426  CL37 HEK-293T C277(0.72)  LDD1630  [10]
 LDCM0429  CL4 HEK-293T C51(0.98)  LDD1633  [10]
 LDCM0430  CL40 HEK-293T C51(1.02)  LDD1634  [10]
 LDCM0431  CL41 HEK-293T C277(0.99); C51(1.02); C108(1.02)  LDD1635  [10]
 LDCM0432  CL42 HEK-293T C277(1.20); C51(0.98); C130(0.98)  LDD1636  [10]
 LDCM0433  CL43 HEK-293T C277(0.69); C51(1.02)  LDD1637  [10]
 LDCM0434  CL44 HEK-293T C51(1.03)  LDD1638  [10]
 LDCM0435  CL45 HEK-293T C51(1.13)  LDD1639  [10]
 LDCM0436  CL46 HEK-293T C277(0.98); C51(1.09)  LDD1640  [10]
 LDCM0437  CL47 HEK-293T C277(1.09); C51(1.08)  LDD1641  [10]
 LDCM0438  CL48 HEK-293T C277(1.01); C51(1.03)  LDD1642  [10]
 LDCM0439  CL49 HEK-293T C277(0.91)  LDD1643  [10]
 LDCM0440  CL5 HEK-293T C277(1.05); C51(0.93); C108(1.10)  LDD1644  [10]
 LDCM0443  CL52 HEK-293T C51(1.01)  LDD1646  [10]
 LDCM0444  CL53 HEK-293T C277(0.96); C51(0.98); C108(1.17)  LDD1647  [10]
 LDCM0445  CL54 HEK-293T C277(1.08); C51(1.01); C130(0.87)  LDD1648  [10]
 LDCM0446  CL55 HEK-293T C277(1.01); C51(1.10)  LDD1649  [10]
 LDCM0447  CL56 HEK-293T C51(1.10)  LDD1650  [10]
 LDCM0448  CL57 HEK-293T C51(1.13)  LDD1651  [10]
 LDCM0449  CL58 HEK-293T C277(0.89); C51(1.10)  LDD1652  [10]
 LDCM0450  CL59 HEK-293T C277(1.07); C51(1.01)  LDD1653  [10]
 LDCM0451  CL6 HEK-293T C277(0.78); C51(0.91); C130(0.78)  LDD1654  [10]
 LDCM0452  CL60 HEK-293T C277(1.34); C51(1.07)  LDD1655  [10]
 LDCM0453  CL61 HEK-293T C277(1.30)  LDD1656  [10]
 LDCM0456  CL64 HEK-293T C51(1.03)  LDD1659  [10]
 LDCM0457  CL65 HEK-293T C277(0.75); C51(0.88); C108(1.11)  LDD1660  [10]
 LDCM0458  CL66 HEK-293T C277(1.04); C51(0.96); C130(1.05)  LDD1661  [10]
 LDCM0459  CL67 HEK-293T C277(1.30); C51(1.03)  LDD1662  [10]
 LDCM0460  CL68 HEK-293T C51(1.06)  LDD1663  [10]
 LDCM0461  CL69 HEK-293T C51(1.01)  LDD1664  [10]
 LDCM0462  CL7 HEK-293T C277(0.78); C51(1.00)  LDD1665  [10]
 LDCM0463  CL70 HEK-293T C277(0.97); C51(1.10)  LDD1666  [10]
 LDCM0464  CL71 HEK-293T C277(1.20); C51(1.03)  LDD1667  [10]
 LDCM0465  CL72 HEK-293T C277(1.48); C51(1.11)  LDD1668  [10]
 LDCM0466  CL73 HEK-293T C277(0.84)  LDD1669  [10]
 LDCM0469  CL76 HEK-293T C51(0.99)  LDD1672  [10]
 LDCM0470  CL77 HEK-293T C277(0.89); C51(0.98); C108(1.16)  LDD1673  [10]
 LDCM0471  CL78 HEK-293T C277(1.10); C51(0.94); C130(0.91)  LDD1674  [10]
 LDCM0472  CL79 HEK-293T C277(1.07); C51(0.98)  LDD1675  [10]
 LDCM0473  CL8 HEK-293T C51(1.03)  LDD1676  [10]
 LDCM0474  CL80 HEK-293T C51(1.01)  LDD1677  [10]
 LDCM0475  CL81 HEK-293T C51(1.01)  LDD1678  [10]
 LDCM0476  CL82 HEK-293T C277(0.82); C51(1.10)  LDD1679  [10]
 LDCM0477  CL83 HEK-293T C277(1.05); C51(1.08)  LDD1680  [10]
 LDCM0478  CL84 HEK-293T C277(0.77); C51(1.03)  LDD1681  [10]
 LDCM0479  CL85 HEK-293T C277(0.93)  LDD1682  [10]
 LDCM0482  CL88 HEK-293T C51(0.99)  LDD1685  [10]
 LDCM0483  CL89 HEK-293T C277(0.80); C51(0.99); C108(1.26)  LDD1686  [10]
 LDCM0484  CL9 HEK-293T C51(1.05)  LDD1687  [10]
 LDCM0485  CL90 HEK-293T C277(0.69); C51(1.01); C130(0.83)  LDD1688  [10]
 LDCM0486  CL91 HEK-293T C277(1.00); C51(1.01)  LDD1689  [10]
 LDCM0487  CL92 HEK-293T C51(0.99)  LDD1690  [10]
 LDCM0488  CL93 HEK-293T C51(1.12)  LDD1691  [10]
 LDCM0489  CL94 HEK-293T C277(0.89); C51(1.09)  LDD1692  [10]
 LDCM0490  CL95 HEK-293T C277(0.98); C51(1.16)  LDD1693  [10]
 LDCM0491  CL96 HEK-293T C277(1.04); C51(0.99)  LDD1694  [10]
 LDCM0492  CL97 HEK-293T C277(0.75)  LDD1695  [10]
 LDCM0022  KB02 HEK-293T C51(0.86); C277(0.77)  LDD1492  [10]
 LDCM0023  KB03 Jurkat C51(6.72)  LDD0209  [2]
 LDCM0024  KB05 HMCB C280(2.30)  LDD3312  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
MyoD family inhibitor (MDFI) MDFI family Q99750
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin-associated protein 10-10 (KRTAP10-10) KRTAP type 10 family P60014
Aspartate-rich protein 1 (DRICH1) . Q6PGQ1

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
K-00546 Small molecular drug DB07664
Pmid21982499c14k Small molecular drug D06UKS
Purvalanol A Small molecular drug DB04751
4-amino-2-[(3-chlorophenyl)Amino]-5-(4-fluorobenzoyl)-13-thiazol-3-ium . DB07489
{4-amino-2-[(4-methoxyphenyl)Amino]-13-thiazol-5-yl}(4-methoxyphenyl)Methanone . DB07488

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
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 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
4 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
5 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
6 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
7 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
8 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
9 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
10 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
11 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