General Information of Target

Target ID LDTP02016
Target Name Glucocorticoid receptor (NR3C1)
Gene Name NR3C1
Gene ID 2908
Synonyms
GRL; Glucocorticoid receptor; GR; Nuclear receptor subfamily 3 group C member 1
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MDSKESLTPGREENPSSVLAQERGDVMDFYKTLRGGATVKVSASSPSLAVASQSDSKQRR
LLVDFPKGSVSNAQQPDLSKAVSLSMGLYMGETETKVMGNDLGFPQQGQISLSSGETDLK
LLEESIANLNRSTSVPENPKSSASTAVSAAPTEKEFPKTHSDVSSEQQHLKGQTGTNGGN
VKLYTTDQSTFDILQDLEFSSGSPGKETNESPWRSDLLIDENCLLSPLAGEDDSFLLEGN
SNEDCKPLILPDTKPKIKDNGDLVLSSPSNVTLPQVKTEKEDFIELCTPGVIKQEKLGTV
YCQASFPGANIIGNKMSAISVHGVSTSGGQMYHYDMNTASLSQQQDQKPIFNVIPPIPVG
SENWNRCQGSGDDNLTSLGTLNFPGRTVFSNGYSSPSMRPDVSSPPSSSSTATTGPPPKL
CLVCSDEASGCHYGVLTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRYRK
CLQAGMNLEARKTKKKIKGIQQATTGVSQETSENPGNKTIVPATLPQLTPTLVSLLEVIE
PEVLYAGYDSSVPDSTWRIMTTLNMLGGRQVIAAVKWAKAIPGFRNLHLDDQMTLLQYSW
MFLMAFALGWRSYRQSSANLLCFAPDLIINEQRMTLPCMYDQCKHMLYVSSELHRLQVSY
EEYLCMKTLLLLSSVPKDGLKSQELFDEIRMTYIKELGKAIVKREGNSSQNWQRFYQLTK
LLDSMHEVVENLLNYCFQTFLDKTMSIEFPEMLAEIITNQIPKYSNGNIKKLLFHQK
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR3 subfamily
Subcellular location
Cytoplasm; Nucleus
Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling. Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth.; [Isoform Alpha]: Has transcriptional activation and repression activity. Mediates glucocorticoid-induced apoptosis. Promotes accurate chromosome segregation during mitosis. May act as a tumor suppressor. May play a negative role in adipogenesis through the regulation of lipolytic and antilipogenic gene expression.; [Isoform Beta]: Acts as a dominant negative inhibitor of isoform Alpha. Has intrinsic transcriptional activity independent of isoform Alpha when both isoforms are coexpressed. Loses this transcription modulator function on its own. Has no hormone-binding activity. May play a role in controlling glucose metabolism by maintaining insulin sensitivity. Reduces hepatic gluconeogenesis through down-regulation of PEPCK in an isoform Alpha-dependent manner. Directly regulates STAT1 expression in isoform Alpha-independent manner.; [Isoform Alpha-2]: Has lower transcriptional activation activity than isoform Alpha. Exerts a dominant negative effect on isoform Alpha trans-repression mechanism.; [Isoform GR-P]: Increases activity of isoform Alpha.; [Isoform Alpha-B]: More effective than isoform Alpha in transcriptional activation, but not repression activity.; [Isoform 10]: Has transcriptional activation activity.; [Isoform Alpha-C1]: Has transcriptional activation activity.; [Isoform Alpha-C2]: Has transcriptional activation activity.; [Isoform Alpha-C3]: Has highest transcriptional activation activity of all isoforms created by alternative initiation. Has transcriptional repression activity. Mediates glucocorticoid-induced apoptosis.; [Isoform Alpha-D1]: Has transcriptional activation activity.; [Isoform Alpha-D2]: Has transcriptional activation activity.; [Isoform Alpha-D3]: Has lowest transcriptional activation activity of all isoforms created by alternative initiation. Has transcriptional repression activity.
TTD ID
T40016
Uniprot ID
P04150
DrugMap ID
TTYRL6O
Ensemble ID
ENST00000231509.7
HGNC ID
HGNC:7978
ChEMBL ID
CHEMBL2034

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CCK81 Insertion: p.L772TfsTer27 .
HCC15 SNV: p.R11I DBIA    Probe Info 
HCT116 SNV: p.C302Ter .
HT SNV: p.Y334Ter .
JURKAT SNV: p.R477H .
MEWO SNV: p.L664F DBIA    Probe Info 
NCIH1793 Substitution: p.A146F DBIA    Probe Info 
REH SNV: p.Q527Ter DBIA    Probe Info 
SUPT1 SNV: p.G506Ter DBIA    Probe Info 
SW948 SNV: p.S709C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 22 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
15.00  LDD0402  [1]
N1
 Probe Info 
100.00  LDD0242  [2]
STPyne
 Probe Info 
K695(8.33)  LDD0277  [3]
BTD
 Probe Info 
C463(0.97)  LDD2136  [4]
Sulforaphane-probe2
 Probe Info 
1.97  LDD0160  [5]
NAIA_5
 Probe Info 
C287(0.32)  LDD2227  [6]
AHL-Pu-1
 Probe Info 
C622(3.44)  LDD0168  [7]
DBIA
 Probe Info 
C638(20.00); C643(20.00); C622(5.32); C302(2.63)  LDD0080  [8]
IA-alkyne
 Probe Info 
C463(0.00); C287(0.00)  LDD0162  [9]
Lodoacetamide azide
 Probe Info 
C457(0.00); C463(0.00); C481(0.00)  LDD0037  [10]
IPM
 Probe Info 
N.A.  LDD0025  [11]
JW-RF-010
 Probe Info 
N.A.  LDD0026  [11]
NAIA_4
 Probe Info 
C287(0.00); C302(0.00); C367(0.00)  LDD2226  [6]
TFBX
 Probe Info 
C302(0.00); C665(0.00); C622(0.00)  LDD0027  [11]
WYneN
 Probe Info 
N.A.  LDD0021  [12]
WYneO
 Probe Info 
N.A.  LDD0022  [12]
PF-06672131
 Probe Info 
N.A.  LDD0017  [13]
Acrolein
 Probe Info 
H160(0.00); C287(0.00)  LDD0217  [14]
Crotonaldehyde
 Probe Info 
N.A.  LDD0219  [14]
W1
 Probe Info 
N.A.  LDD0236  [15]
AOyne
 Probe Info 
15.00  LDD0443  [16]
HHS-482
 Probe Info 
Y764(0.93)  LDD2239  [17]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C159
 Probe Info 
8.11  LDD1839  [18]
C383
 Probe Info 
10.85  LDD2042  [18]
FFF probe11
 Probe Info 
20.00  LDD0471  [19]
A-DA
 Probe Info 
2.64  LDD0141  [20]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C622(3.44)  LDD0168  [7]
 LDCM0026  4SU-RNA+native RNA HEK-293T C736(2.10)  LDD0169  [7]
 LDCM0214  AC1 HEK-293T C481(0.85); C287(1.05); C367(1.24); C302(1.06)  LDD1507  [21]
 LDCM0215  AC10 HEK-293T C481(1.03); C287(1.05); C367(1.20); C622(0.97)  LDD1508  [21]
 LDCM0226  AC11 HEK-293T C481(1.03); C287(1.09); C367(1.01); C302(0.95)  LDD1509  [21]
 LDCM0237  AC12 HEK-293T C481(1.08); C287(1.09); C367(1.01); C665(1.03)  LDD1510  [21]
 LDCM0259  AC14 HEK-293T C481(1.04); C287(1.01); C367(1.10); C665(0.95)  LDD1512  [21]
 LDCM0270  AC15 HEK-293T C481(1.05); C287(1.02); C367(1.08); C665(0.97)  LDD1513  [21]
 LDCM0276  AC17 HEK-293T C481(0.96); C287(0.99); C367(1.09); C302(1.01)  LDD1515  [21]
 LDCM0277  AC18 HEK-293T C481(1.04); C287(1.01); C367(1.24); C622(0.94)  LDD1516  [21]
 LDCM0278  AC19 HEK-293T C481(1.14); C287(1.43); C367(1.17); C302(1.23)  LDD1517  [21]
 LDCM0279  AC2 HEK-293T C481(1.01); C287(1.10); C367(1.21); C622(1.07)  LDD1518  [21]
 LDCM0280  AC20 HEK-293T C481(1.06); C287(1.05); C367(1.01); C665(0.98)  LDD1519  [21]
 LDCM0281  AC21 HEK-293T C481(0.96); C287(0.91); C367(0.97); C622(0.95)  LDD1520  [21]
 LDCM0282  AC22 HEK-293T C481(0.94); C287(1.09); C367(1.09); C665(0.87)  LDD1521  [21]
 LDCM0283  AC23 HEK-293T C481(0.99); C287(0.97); C367(0.92); C665(0.89)  LDD1522  [21]
 LDCM0284  AC24 HEK-293T C481(0.97); C287(1.00); C367(1.04); C622(1.11)  LDD1523  [21]
 LDCM0285  AC25 HEK-293T C481(0.91); C287(1.01); C367(0.98); C302(0.92)  LDD1524  [21]
 LDCM0286  AC26 HEK-293T C481(0.97); C287(1.01); C367(1.26); C622(1.01)  LDD1525  [21]
 LDCM0287  AC27 HEK-293T C481(1.05); C287(0.95); C367(1.12); C302(0.92)  LDD1526  [21]
 LDCM0288  AC28 HEK-293T C481(1.04); C287(1.02); C367(1.06); C665(1.09)  LDD1527  [21]
 LDCM0289  AC29 HEK-293T C481(0.96); C287(1.01); C367(0.94); C622(0.92)  LDD1528  [21]
 LDCM0290  AC3 HEK-293T C481(0.93); C287(1.07); C367(1.01); C302(0.92)  LDD1529  [21]
 LDCM0291  AC30 HEK-293T C481(0.98); C287(1.04); C367(1.11); C665(0.91)  LDD1530  [21]
 LDCM0292  AC31 HEK-293T C481(1.11); C287(1.04); C367(1.07); C665(1.03)  LDD1531  [21]
 LDCM0293  AC32 HEK-293T C481(0.95); C287(0.93); C367(0.93); C622(0.98)  LDD1532  [21]
 LDCM0294  AC33 HEK-293T C481(0.92); C287(0.95); C367(0.99); C302(0.96)  LDD1533  [21]
 LDCM0295  AC34 HEK-293T C481(1.05); C287(1.00); C367(1.11); C622(1.08)  LDD1534  [21]
 LDCM0296  AC35 HEK-293T C481(1.03); C287(1.03); C367(1.00); C302(0.87)  LDD1535  [21]
 LDCM0297  AC36 HEK-293T C481(1.10); C287(1.00); C367(1.00); C665(1.00)  LDD1536  [21]
 LDCM0298  AC37 HEK-293T C481(1.05); C287(0.96); C367(0.95); C622(1.07)  LDD1537  [21]
 LDCM0299  AC38 HEK-293T C481(1.08); C287(1.01); C367(1.29); C665(0.94)  LDD1538  [21]
 LDCM0300  AC39 HEK-293T C481(1.05); C287(1.00); C367(1.08); C665(0.93)  LDD1539  [21]
 LDCM0301  AC4 HEK-293T C481(0.99); C287(1.01); C367(1.04); C665(0.89)  LDD1540  [21]
 LDCM0302  AC40 HEK-293T C481(1.04); C287(1.06); C367(1.08); C622(1.00)  LDD1541  [21]
 LDCM0303  AC41 HEK-293T C481(0.90); C287(1.03); C367(1.11); C302(1.01)  LDD1542  [21]
 LDCM0304  AC42 HEK-293T C481(1.10); C287(1.11); C367(1.19); C622(1.10)  LDD1543  [21]
 LDCM0305  AC43 HEK-293T C481(1.03); C287(1.06); C367(1.11); C302(0.94)  LDD1544  [21]
 LDCM0306  AC44 HEK-293T C481(1.06); C287(1.03); C367(1.10); C665(1.03)  LDD1545  [21]
 LDCM0307  AC45 HEK-293T C481(1.02); C287(0.96); C367(0.98); C622(0.94)  LDD1546  [21]
 LDCM0308  AC46 HEK-293T C481(1.00); C287(1.02); C367(1.09); C665(0.94)  LDD1547  [21]
 LDCM0309  AC47 HEK-293T C481(1.06); C287(1.03); C367(1.00); C665(1.01)  LDD1548  [21]
 LDCM0310  AC48 HEK-293T C481(1.19); C287(1.00); C367(1.29); C622(0.97)  LDD1549  [21]
 LDCM0311  AC49 HEK-293T C481(0.90); C287(1.03); C367(1.18); C302(1.00)  LDD1550  [21]
 LDCM0312  AC5 HEK-293T C481(1.02); C287(1.04); C367(0.75); C622(1.04)  LDD1551  [21]
 LDCM0313  AC50 HEK-293T C481(1.10); C287(1.06); C367(1.46); C622(1.11)  LDD1552  [21]
 LDCM0314  AC51 HEK-293T C481(1.06); C287(1.20); C367(1.07); C302(0.96)  LDD1553  [21]
 LDCM0315  AC52 HEK-293T C481(1.06); C287(1.13); C367(1.12); C665(0.97)  LDD1554  [21]
 LDCM0316  AC53 HEK-293T C481(1.03); C287(1.05); C367(0.98); C622(0.97)  LDD1555  [21]
 LDCM0317  AC54 HEK-293T C481(1.06); C287(1.00); C367(1.22); C665(0.94)  LDD1556  [21]
 LDCM0318  AC55 HEK-293T C481(1.04); C287(1.02); C367(1.15); C665(0.96)  LDD1557  [21]
 LDCM0319  AC56 HEK-293T C481(1.03); C287(0.99); C367(1.16); C622(1.01)  LDD1558  [21]
 LDCM0320  AC57 HEK-293T C481(0.91); C287(1.00); C367(1.15); C302(1.01)  LDD1559  [21]
 LDCM0321  AC58 HEK-293T C481(1.04); C287(1.07); C367(1.21); C622(1.10)  LDD1560  [21]
 LDCM0322  AC59 HEK-293T C481(0.98); C287(0.98); C367(1.03); C302(0.87)  LDD1561  [21]
 LDCM0323  AC6 HEK-293T C481(0.99); C287(1.05); C367(1.28); C665(0.99)  LDD1562  [21]
 LDCM0324  AC60 HEK-293T C481(1.01); C287(1.01); C367(1.03); C665(0.92)  LDD1563  [21]
 LDCM0325  AC61 HEK-293T C481(0.98); C287(1.06); C367(0.98); C622(0.90)  LDD1564  [21]
 LDCM0326  AC62 HEK-293T C481(0.99); C287(1.04); C367(1.14); C665(0.92)  LDD1565  [21]
 LDCM0327  AC63 HEK-293T C481(1.00); C287(0.95); C367(1.07); C665(0.98)  LDD1566  [21]
 LDCM0328  AC64 HEK-293T C481(1.02); C287(1.00); C367(1.01); C622(1.06)  LDD1567  [21]
 LDCM0334  AC7 HEK-293T C481(0.94); C287(0.97); C367(0.97); C665(1.06)  LDD1568  [21]
 LDCM0345  AC8 HEK-293T C481(0.99); C287(1.10); C367(1.04); C622(0.89)  LDD1569  [21]
 LDCM0248  AKOS034007472 HEK-293T C481(1.01); C287(0.99); C367(0.99); C622(1.08)  LDD1511  [21]
 LDCM0356  AKOS034007680 HEK-293T C481(0.93); C287(1.00); C367(1.10); C302(1.00)  LDD1570  [21]
 LDCM0275  AKOS034007705 HEK-293T C481(1.09); C287(0.96); C367(1.21); C622(1.05)  LDD1514  [21]
 LDCM0156  Aniline NCI-H1299 N.A.  LDD0404  [1]
 LDCM0108  Chloroacetamide HeLa C287(0.00); H160(0.00); H169(0.00); C622(0.00)  LDD0222  [14]
 LDCM0632  CL-Sc Hep-G2 C287(0.32)  LDD2227  [6]
 LDCM0367  CL1 HEK-293T C481(1.02); C287(1.01); C367(1.02); C665(0.97)  LDD1571  [21]
 LDCM0368  CL10 HEK-293T C481(1.00); C287(1.01); C367(1.25); C665(1.21)  LDD1572  [21]
 LDCM0369  CL100 HEK-293T C481(0.98); C287(1.09); C302(0.94)  LDD1573  [21]
 LDCM0370  CL101 HEK-293T C481(1.03); C287(0.99); C367(1.10); C665(0.94)  LDD1574  [21]
 LDCM0371  CL102 HEK-293T C481(1.01); C287(0.98); C622(0.96); C302(0.92)  LDD1575  [21]
 LDCM0372  CL103 HEK-293T C481(0.89); C287(1.06); C622(1.20); C302(1.04)  LDD1576  [21]
 LDCM0373  CL104 HEK-293T C481(1.12); C287(1.09); C302(0.87)  LDD1577  [21]
 LDCM0374  CL105 HEK-293T C481(1.01); C287(1.02); C367(1.05); C665(0.89)  LDD1578  [21]
 LDCM0375  CL106 HEK-293T C481(1.09); C287(1.06); C622(0.92); C302(0.77)  LDD1579  [21]
 LDCM0376  CL107 HEK-293T C481(0.94); C287(1.03); C622(1.12); C302(1.01)  LDD1580  [21]
 LDCM0377  CL108 HEK-293T C481(0.98); C287(1.09); C302(0.92)  LDD1581  [21]
 LDCM0378  CL109 HEK-293T C481(0.95); C287(1.02); C367(0.95); C665(0.93)  LDD1582  [21]
 LDCM0379  CL11 HEK-293T C481(1.19); C287(0.97); C367(1.08); C665(1.00)  LDD1583  [21]
 LDCM0380  CL110 HEK-293T C481(0.96); C287(1.16); C622(1.16); C302(0.85)  LDD1584  [21]
 LDCM0381  CL111 HEK-293T C481(0.92); C287(0.98); C622(1.01); C302(0.89)  LDD1585  [21]
 LDCM0382  CL112 HEK-293T C481(0.95); C287(1.10); C302(0.90)  LDD1586  [21]
 LDCM0383  CL113 HEK-293T C481(1.04); C287(1.02); C367(1.10); C665(1.03)  LDD1587  [21]
 LDCM0384  CL114 HEK-293T C481(1.02); C287(1.08); C622(1.01); C302(0.81)  LDD1588  [21]
 LDCM0385  CL115 HEK-293T C481(1.18); C287(1.02); C622(1.16); C302(1.06)  LDD1589  [21]
 LDCM0386  CL116 HEK-293T C481(1.10); C287(1.17); C302(0.97)  LDD1590  [21]
 LDCM0387  CL117 HEK-293T C481(1.03); C287(1.01); C367(0.96); C665(0.96)  LDD1591  [21]
 LDCM0388  CL118 HEK-293T C481(1.12); C287(1.13); C622(1.17); C302(0.93)  LDD1592  [21]
 LDCM0389  CL119 HEK-293T C481(0.92); C287(1.01); C622(1.05); C302(0.98)  LDD1593  [21]
 LDCM0390  CL12 HEK-293T C481(0.98); C287(0.99); C367(1.01); C622(0.96)  LDD1594  [21]
 LDCM0391  CL120 HEK-293T C481(0.95); C287(1.10); C302(0.98)  LDD1595  [21]
 LDCM0392  CL121 HEK-293T C481(1.05); C287(1.02); C367(1.10); C665(0.94)  LDD1596  [21]
 LDCM0393  CL122 HEK-293T C481(1.06); C287(1.09); C622(0.89); C302(0.77)  LDD1597  [21]
 LDCM0394  CL123 HEK-293T C481(0.92); C287(1.00); C622(1.08); C302(0.93)  LDD1598  [21]
 LDCM0395  CL124 HEK-293T C481(1.02); C287(1.05); C302(1.02)  LDD1599  [21]
 LDCM0396  CL125 HEK-293T C481(0.99); C287(1.06); C367(1.02); C665(0.94)  LDD1600  [21]
 LDCM0397  CL126 HEK-293T C481(0.99); C287(1.04); C622(1.12); C302(0.87)  LDD1601  [21]
 LDCM0398  CL127 HEK-293T C481(0.99); C287(0.96); C622(0.96); C302(1.06)  LDD1602  [21]
 LDCM0399  CL128 HEK-293T C481(1.03); C287(1.11); C302(1.00)  LDD1603  [21]
 LDCM0400  CL13 HEK-293T C481(1.06); C287(1.12); C367(0.89); C665(0.87)  LDD1604  [21]
 LDCM0401  CL14 HEK-293T C481(1.17); C287(1.13); C622(0.89); C302(0.76)  LDD1605  [21]
 LDCM0402  CL15 HEK-293T C481(1.13); C287(1.05); C622(1.10); C302(1.02)  LDD1606  [21]
 LDCM0403  CL16 HEK-293T C481(1.20); C287(1.12); C302(0.88)  LDD1607  [21]
 LDCM0404  CL17 HEK-293T C481(0.93); C287(0.96); C367(1.17); C302(0.96)  LDD1608  [21]
 LDCM0405  CL18 HEK-293T C481(1.16); C287(0.95); C367(1.23); C622(1.09)  LDD1609  [21]
 LDCM0406  CL19 HEK-293T C481(1.18); C287(1.07); C367(1.16); C302(0.87)  LDD1610  [21]
 LDCM0407  CL2 HEK-293T C481(1.14); C287(1.13); C622(1.24); C302(0.78)  LDD1611  [21]
 LDCM0408  CL20 HEK-293T C481(1.22); C287(1.16); C367(1.07); C665(1.14)  LDD1612  [21]
 LDCM0409  CL21 HEK-293T C481(0.99); C287(1.06); C367(0.97); C622(0.98)  LDD1613  [21]
 LDCM0410  CL22 HEK-293T C481(1.12); C287(1.04); C367(1.25); C665(1.25)  LDD1614  [21]
 LDCM0411  CL23 HEK-293T C481(1.30); C287(0.97); C367(1.13); C665(0.98)  LDD1615  [21]
 LDCM0412  CL24 HEK-293T C481(1.08); C287(0.99); C367(1.18); C622(1.02)  LDD1616  [21]
 LDCM0413  CL25 HEK-293T C481(1.00); C287(0.92); C367(0.98); C665(0.95)  LDD1617  [21]
 LDCM0414  CL26 HEK-293T C481(1.10); C287(1.14); C622(0.91); C302(0.96)  LDD1618  [21]
 LDCM0415  CL27 HEK-293T C481(0.80); C287(1.02); C622(1.13); C302(1.00)  LDD1619  [21]
 LDCM0416  CL28 HEK-293T C481(1.03); C287(1.04); C302(1.00)  LDD1620  [21]
 LDCM0417  CL29 HEK-293T C481(0.95); C287(0.95); C367(1.05); C302(0.88)  LDD1621  [21]
 LDCM0418  CL3 HEK-293T C481(1.07); C287(0.97); C622(1.22); C302(0.99)  LDD1622  [21]
 LDCM0419  CL30 HEK-293T C481(1.08); C287(1.04); C367(1.14); C622(0.96)  LDD1623  [21]
 LDCM0420  CL31 HEK-293T C481(1.11); C287(1.27); C367(0.99); C302(0.85)  LDD1624  [21]
 LDCM0421  CL32 HEK-293T C481(1.18); C287(1.18); C367(1.08); C665(1.04)  LDD1625  [21]
 LDCM0422  CL33 HEK-293T C481(0.90); C287(0.97); C367(1.04); C622(0.67)  LDD1626  [21]
 LDCM0423  CL34 HEK-293T C481(1.04); C287(1.12); C367(1.25); C665(1.12)  LDD1627  [21]
 LDCM0424  CL35 HEK-293T C481(1.14); C287(1.00); C367(1.05); C665(1.09)  LDD1628  [21]
 LDCM0425  CL36 HEK-293T C481(0.95); C287(1.05); C367(0.98); C622(0.88)  LDD1629  [21]
 LDCM0426  CL37 HEK-293T C481(1.02); C287(0.97); C367(1.08); C665(1.01)  LDD1630  [21]
 LDCM0428  CL39 HEK-293T C481(0.82); C287(0.96); C622(1.00); C302(0.91)  LDD1632  [21]
 LDCM0429  CL4 HEK-293T C481(1.06); C287(1.06); C302(0.96)  LDD1633  [21]
 LDCM0430  CL40 HEK-293T C481(1.05); C287(1.13); C302(0.93)  LDD1634  [21]
 LDCM0431  CL41 HEK-293T C481(0.92); C287(1.05); C367(1.09); C302(0.92)  LDD1635  [21]
 LDCM0432  CL42 HEK-293T C481(1.11); C287(1.25); C367(1.22); C622(0.99)  LDD1636  [21]
 LDCM0433  CL43 HEK-293T C481(1.06); C287(0.93); C367(0.94); C302(0.83)  LDD1637  [21]
 LDCM0434  CL44 HEK-293T C481(1.07); C287(1.11); C367(1.04); C665(0.94)  LDD1638  [21]
 LDCM0435  CL45 HEK-293T C481(0.95); C287(1.02); C367(1.28); C622(1.07)  LDD1639  [21]
 LDCM0436  CL46 HEK-293T C481(1.09); C287(1.05); C367(1.16); C665(1.16)  LDD1640  [21]
 LDCM0437  CL47 HEK-293T C481(1.17); C287(1.02); C367(1.13); C665(1.05)  LDD1641  [21]
 LDCM0438  CL48 HEK-293T C481(0.92); C287(1.06); C367(1.15); C622(0.92)  LDD1642  [21]
 LDCM0439  CL49 HEK-293T C481(1.00); C287(1.03); C367(1.07); C665(1.09)  LDD1643  [21]
 LDCM0440  CL5 HEK-293T C481(0.99); C287(1.06); C367(1.17); C302(0.99)  LDD1644  [21]
 LDCM0441  CL50 HEK-293T C481(1.10); C287(1.04); C622(0.87); C302(0.91)  LDD1645  [21]
 LDCM0443  CL52 HEK-293T C481(1.12); C287(1.17); C302(0.97)  LDD1646  [21]
 LDCM0444  CL53 HEK-293T C481(0.85); C287(1.08); C367(0.99); C302(0.93)  LDD1647  [21]
 LDCM0445  CL54 HEK-293T C481(1.03); C287(1.08); C367(1.21); C622(1.14)  LDD1648  [21]
 LDCM0446  CL55 HEK-293T C481(1.12); C287(1.14); C367(1.02); C302(0.80)  LDD1649  [21]
 LDCM0447  CL56 HEK-293T C481(1.15); C287(1.04); C367(1.07); C665(0.94)  LDD1650  [21]
 LDCM0448  CL57 HEK-293T C481(0.97); C287(1.20); C367(1.02); C622(0.91)  LDD1651  [21]
 LDCM0449  CL58 HEK-293T C481(1.11); C287(1.12); C367(1.07); C665(1.18)  LDD1652  [21]
 LDCM0450  CL59 HEK-293T C481(1.33); C287(1.02); C367(1.11); C665(0.91)  LDD1653  [21]
 LDCM0451  CL6 HEK-293T C481(1.16); C287(1.11); C367(1.26); C622(1.08)  LDD1654  [21]
 LDCM0452  CL60 HEK-293T C481(0.99); C287(0.98); C367(1.03); C622(1.00)  LDD1655  [21]
 LDCM0453  CL61 HEK-293T C481(1.03); C287(1.06); C367(1.05); C665(0.91)  LDD1656  [21]
 LDCM0454  CL62 HEK-293T C481(1.07); C287(1.13); C622(0.97); C302(0.84)  LDD1657  [21]
 LDCM0455  CL63 HEK-293T C481(1.03); C287(1.03); C622(1.20); C302(1.00)  LDD1658  [21]
 LDCM0456  CL64 HEK-293T C481(0.98); C287(1.16); C302(0.95)  LDD1659  [21]
 LDCM0457  CL65 HEK-293T C481(0.96); C287(1.06); C367(1.05); C302(0.93)  LDD1660  [21]
 LDCM0458  CL66 HEK-293T C481(1.08); C287(1.08); C367(1.28); C622(1.04)  LDD1661  [21]
 LDCM0459  CL67 HEK-293T C481(1.09); C287(1.02); C367(1.07); C302(0.82)  LDD1662  [21]
 LDCM0460  CL68 HEK-293T C481(1.17); C287(1.06); C367(1.07); C665(0.99)  LDD1663  [21]
 LDCM0461  CL69 HEK-293T C481(1.03); C287(0.98); C367(0.97); C622(0.92)  LDD1664  [21]
 LDCM0462  CL7 HEK-293T C481(1.17); C287(1.13); C367(1.05); C302(0.89)  LDD1665  [21]
 LDCM0463  CL70 HEK-293T C481(1.13); C287(1.04); C367(1.35); C665(1.08)  LDD1666  [21]
 LDCM0464  CL71 HEK-293T C481(1.15); C287(1.03); C367(1.12); C665(1.08)  LDD1667  [21]
 LDCM0465  CL72 HEK-293T C481(1.08); C287(1.01); C367(1.05); C622(1.02)  LDD1668  [21]
 LDCM0466  CL73 HEK-293T C481(0.93); C287(0.95); C367(1.05); C665(0.95)  LDD1669  [21]
 LDCM0467  CL74 HEK-293T C481(1.06); C287(0.96); C622(1.05); C302(0.72)  LDD1670  [21]
 LDCM0469  CL76 HEK-293T C481(1.00); C287(1.15); C302(0.97)  LDD1672  [21]
 LDCM0470  CL77 HEK-293T C481(0.87); C287(0.99); C367(1.05); C302(0.91)  LDD1673  [21]
 LDCM0471  CL78 HEK-293T C481(1.08); C287(1.08); C367(1.27); C622(0.98)  LDD1674  [21]
 LDCM0472  CL79 HEK-293T C481(1.06); C287(1.15); C367(0.97); C302(0.77)  LDD1675  [21]
 LDCM0473  CL8 HEK-293T C481(1.08); C287(0.98); C367(1.00); C665(1.20)  LDD1676  [21]
 LDCM0474  CL80 HEK-293T C481(1.10); C287(1.03); C367(1.11); C665(0.99)  LDD1677  [21]
 LDCM0475  CL81 HEK-293T C481(1.08); C287(1.04); C367(0.98); C622(0.97)  LDD1678  [21]
 LDCM0476  CL82 HEK-293T C481(1.08); C287(1.00); C367(1.14); C665(1.13)  LDD1679  [21]
 LDCM0477  CL83 HEK-293T C481(1.11); C287(0.94); C367(1.10); C665(1.07)  LDD1680  [21]
 LDCM0478  CL84 HEK-293T C481(0.90); C287(0.94); C367(1.12); C622(0.96)  LDD1681  [21]
 LDCM0479  CL85 HEK-293T C481(0.95); C287(1.01); C367(1.08); C665(1.07)  LDD1682  [21]
 LDCM0480  CL86 HEK-293T C481(1.09); C287(1.07); C622(1.01); C302(0.88)  LDD1683  [21]
 LDCM0481  CL87 HEK-293T C481(1.09); C287(0.99); C622(1.19); C302(1.06)  LDD1684  [21]
 LDCM0482  CL88 HEK-293T C481(1.04); C287(1.09); C302(0.97)  LDD1685  [21]
 LDCM0483  CL89 HEK-293T C481(0.95); C287(1.03); C367(1.05); C302(0.99)  LDD1686  [21]
 LDCM0484  CL9 HEK-293T C481(1.07); C287(1.09); C367(0.94); C622(0.90)  LDD1687  [21]
 LDCM0485  CL90 HEK-293T C481(0.73); C287(1.13); C367(1.25); C622(1.11)  LDD1688  [21]
 LDCM0486  CL91 HEK-293T C481(1.10); C287(1.05); C367(1.07); C302(0.89)  LDD1689  [21]
 LDCM0487  CL92 HEK-293T C481(1.04); C287(1.01); C367(0.94); C665(1.06)  LDD1690  [21]
 LDCM0488  CL93 HEK-293T C481(0.99); C287(1.04); C367(1.02); C622(0.89)  LDD1691  [21]
 LDCM0489  CL94 HEK-293T C481(1.04); C287(1.09); C367(0.98); C665(1.06)  LDD1692  [21]
 LDCM0490  CL95 HEK-293T C481(0.97); C287(0.91); C367(1.22); C665(1.14)  LDD1693  [21]
 LDCM0491  CL96 HEK-293T C481(0.96); C287(0.99); C367(1.00); C622(0.82)  LDD1694  [21]
 LDCM0492  CL97 HEK-293T C481(0.94); C287(1.00); C367(0.99); C665(0.86)  LDD1695  [21]
 LDCM0493  CL98 HEK-293T C481(1.03); C287(1.00); C622(0.86); C302(0.86)  LDD1696  [21]
 LDCM0494  CL99 HEK-293T C481(0.84); C287(0.90); C622(1.10); C302(1.07)  LDD1697  [21]
 LDCM0495  E2913 HEK-293T C481(0.91); C287(0.97); C622(1.10); C302(0.97)  LDD1698  [21]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C457(1.08)  LDD1702  [4]
 LDCM0625  F8 Ramos C302(1.11); C367(1.00)  LDD2187  [22]
 LDCM0572  Fragment10 MDA-MB-231 C302(4.12)  LDD1389  [23]
 LDCM0573  Fragment11 Ramos C302(1.46)  LDD1392  [23]
 LDCM0574  Fragment12 Ramos C302(1.33)  LDD1394  [23]
 LDCM0575  Fragment13 Ramos C367(0.50)  LDD2192  [22]
 LDCM0576  Fragment14 Ramos C302(2.19)  LDD1398  [23]
 LDCM0577  Fragment15 Ramos C302(0.89)  LDD1400  [23]
 LDCM0580  Fragment21 Ramos C302(1.91); C367(0.28)  LDD2195  [22]
 LDCM0581  Fragment22 Ramos C302(0.87)  LDD1407  [23]
 LDCM0582  Fragment23 Ramos C302(4.71)  LDD1409  [23]
 LDCM0578  Fragment27 MDA-MB-231 C302(1.30)  LDD1401  [23]
 LDCM0586  Fragment28 Ramos C302(0.47); C367(0.98)  LDD2198  [22]
 LDCM0588  Fragment30 Ramos C302(0.87); C367(0.50)  LDD2199  [22]
 LDCM0589  Fragment31 Ramos C302(1.10); C367(0.49)  LDD2200  [22]
 LDCM0590  Fragment32 Ramos C302(1.00)  LDD2201  [22]
 LDCM0468  Fragment33 HEK-293T C481(1.09); C287(1.00); C622(1.12); C302(1.00)  LDD1671  [21]
 LDCM0593  Fragment35 Ramos C302(0.91)  LDD1430  [23]
 LDCM0595  Fragment37 Ramos C302(0.87)  LDD1432  [23]
 LDCM0596  Fragment38 Ramos C302(1.31); C367(0.29)  LDD2203  [22]
 LDCM0601  Fragment43 MDA-MB-231 C302(1.47)  LDD1441  [23]
 LDCM0427  Fragment51 HEK-293T C481(1.11); C287(1.07); C622(1.03); C302(0.87)  LDD1631  [21]
 LDCM0610  Fragment52 Ramos C302(1.80)  LDD1453  [23]
 LDCM0614  Fragment56 Ramos C302(0.78)  LDD2205  [22]
 LDCM0569  Fragment7 Ramos C302(1.69)  LDD2186  [22]
 LDCM0571  Fragment9 Ramos C302(0.87)  LDD2188  [22]
 LDCM0107  IAA HeLa H169(0.00); H160(0.00)  LDD0221  [14]
 LDCM0022  KB02 HCT 116 C638(20.00); C643(20.00); C622(5.32); C302(2.63)  LDD0080  [8]
 LDCM0023  KB03 HCT 116 C638(20.00); C643(20.00); C622(20.00); C302(2.23)  LDD0081  [8]
 LDCM0024  KB05 HCT 116 C638(20.00); C643(20.00); C622(8.02); C302(3.47)  LDD0082  [8]
 LDCM0109  NEM HeLa N.A.  LDD0223  [14]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C463(0.97)  LDD2136  [4]
 LDCM0081  Rofecoxib A-549 2.64  LDD0141  [20]
 LDCM0170  Structure8 Ramos 5.45  LDD0433  [24]
 LDCM0003  Sulforaphane MDA-MB-231 1.97  LDD0160  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-alpha (HSP90AA1) Heat shock protein 90 family P07900
RAC-alpha serine/threonine-protein kinase (AKT1) AGC Ser/Thr protein kinase family P31749
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Septin-6 (SEPTIN6) Septin GTPase family Q14141
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hepatocyte nuclear factor 4-alpha (HNF4A) Nuclear hormone receptor family P41235
Retinoic acid receptor RXR-beta (RXRB) Nuclear hormone receptor family P28702
Transcription factor SOX-14 (SOX14) . O95416
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
T-cell surface glycoprotein CD4 (CD4) . P01730
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
TATA element modulatory factor (TMF1) . P82094
Uncharacterized protein KIAA0408 (KIAA0408) . Q6ZU52

The Drug(s) Related To This Target

Approved
Click To Hide/Show 68 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alclometasone Small molecular drug DB00240
Amcinonide Small molecular drug DB00288
Beclomethasone Dipropionate Small molecular drug DB00394
Betamethasone Small molecular drug D0CW1P
Betamethasone Benzoate Small molecular drug D06CWH
Betamethasone Valerate Small molecular drug D03SXE
Budesonide Small molecular drug D0Y7IU
Ciclesonide Small molecular drug DB01410
Clobetasol Propionate Small molecular drug DB01013
Clocortolone Small molecular drug DB00838
Cortisone Acetate Small molecular drug DB01380
Deflazacort Small molecular drug D09WYX
Desonide Small molecular drug DB01260
Desoximetasone Small molecular drug DB00547
Dexamethasone Small molecular drug D0IT2G
Dexamethasone Sodium Phosphate Small molecular drug D0NA8U
Diflorasone Small molecular drug DB00223
Difluprednate Small molecular drug DB06781
Drospirenone Small molecular drug DB01395
Fludrocortisone Small molecular drug DB00687
Flumethasone Small molecular drug DB00663
Flunisolide Small molecular drug D0FM2P
Fluocinolone Acetonide Small molecular drug D02QJH
Fluocinolone Acetonide Small molecular drug DB00591
Fluocinonide Small molecular drug DB01047
Fluorometholone Small molecular drug D0P0HT
Fluoxymesterone Small molecular drug DB01185
Flurandrenolide Small molecular drug DB00846
Fluticasone Small molecular drug D0LC6K
Fluticasone Furoate Small molecular drug DB08906
Fluticasone Propionate Small molecular drug DB00588
Gestrinone Small molecular drug DB11619
Gw685698x Small molecular drug D0Y7JU
Hydrocortamate Small molecular drug D05RXI
Hydrocortisone Small molecular drug D0KR5B
Levonorgestrel Small molecular drug DB00367
Loteprednol Etabonate Small molecular drug DB14596
Medrysone Small molecular drug DB00253
Megestrol Acetate Small molecular drug DB00351
Meprednisone Small molecular drug D0I5DS
Methylprednisolone Small molecular drug D08PIQ
Mifepristone Small molecular drug D0Z4EI
Mometasone Small molecular drug D03HYX
Norethisterone Small molecular drug DB00717
Prednicarbate Small molecular drug DB01130
Prednisolone Small molecular drug D0D1SG
Prednisone Small molecular drug D0IL7L
Progesterone Small molecular drug DB00396
Rimexolone Small molecular drug DB00896
Spironolactone Small molecular drug DB00421
Triamcinolone Small molecular drug D03BLF
Ulipristal Small molecular drug DB08867
Ulobetasol Small molecular drug DB00596
Betamethasone Phosphate . DB14669
Clobetasone . DB13158
Dexamethasone Acetate . DB14649
Difluocortolone . DB09095
Hydrocortisone Acetate . DB14539
Hydrocortisone Butyrate . DB14540
Hydrocortisone Cypionate . DB14541
Hydrocortisone Phosphate . DB14542
Hydrocortisone Probutate . DB14543
Hydrocortisone Valerate . DB14544
Mometasone Furoate . DB14512
Prednisolone Acetate . DB15566
Prednisolone Phosphate . DB14631
Segesterone Acetate . DB14583
Tixocortol . DB09091
Phase 3
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mapracorat Small molecular drug D01IUS
Cort-125134 . D03WNG
Fst-201 . D00TPW
Phase 2
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bay 86-5044 Small molecular drug D0L3HU
Etiprednol Dicloacetate Small molecular drug D0OR8W
Org 34517/34850 Small molecular drug D0E2WF
Org-34517 Small molecular drug D05MDJ
De-110 . D0I1DZ
Gw-870086-x . D06XSB
Ionis-gccrrx . D01HYQ
Las-41002 . D05RXW
Tpi-1020 . D0T5TU
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ibi-20089 . D0J6UV
Ncx-1015 . D0OS8C
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aldosterone Small molecular drug DB04630
B-octylglucoside Small molecular drug D02UVH
Hexane-1,6-diol Small molecular drug D0O0ZU
Hexane-16-diol Small molecular drug DB02210
Onapristone Small molecular drug DB12637
Paramethasone Small molecular drug DB01384
Cortivazol . DB13003
Hydrocortisone Aceponate . DB14538
Discontinued
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd-5423 Small molecular drug D09UFV
Gsk870086 . D01NUG
Nm-135 . D03RCP
Org-34116 . D0I7EX
Pf-251802 . D03CHE
Wc-3027 . D0G2CQ

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 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
3 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
4 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
5 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279
6 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
7 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
8 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.
9 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
10 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
11 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
12 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
13 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
14 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
15 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.
16 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.
17 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
18 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
19 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
20 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.
21 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
22 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
23 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
24 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.