Details of the Target

General Information of Target

Target ID LDTP00622
Target Name Histone deacetylase 3 (HDAC3)
Gene Name HDAC3
Gene ID 8841
Synonyms
Histone deacetylase 3; HD3; EC 3.5.1.98; Protein deacetylase HDAC3; EC 3.5.1.-; Protein deacylase HDAC3; EC 3.5.1.-; RPD3-2; SMAP45
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAKTVAYFYDPDVGNFHYGAGHPMKPHRLALTHSLVLHYGLYKKMIVFKPYQASQHDMCR
FHSEDYIDFLQRVSPTNMQGFTKSLNAFNVGDDCPVFPGLFEFCSRYTGASLQGATQLNN
KICDIAINWAGGLHHAKKFEASGFCYVNDIVIGILELLKYHPRVLYIDIDIHHGDGVQEA
FYLTDRVMTVSFHKYGNYFFPGTGDMYEVGAESGRYYCLNVPLRDGIDDQSYKHLFQPVI
NQVVDFYQPTCIVLQCGADSLGCDRLGCFNLSIRGHGECVEYVKSFNIPLLVLGGGGYTV
RNVARCWTYETSLLVEEAISEELPYSEYFEYFAPDFTLHPDVSTRIENQNSRQYLDQIRQ
TIFENLKMLNHAPSVQIHDVPADLLTYDRTDEADAEERGPEENYSRPEAPNEFYDGDHDN
DKESDVEI
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Histone deacetylase family, HD type 1 subfamily
Subcellular location
Nucleus
Function
Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4), and some other non-histone substrates. Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Participates in the BCL6 transcriptional repressor activity by deacetylating the H3 'Lys-27' (H3K27) on enhancer elements, antagonizing EP300 acetyltransferase activity and repressing proximal gene expression. Acts as a molecular chaperone for shuttling phosphorylated NR2C1 to PML bodies for sumoylation. Contributes, together with XBP1 isoform 1, to the activation of NFE2L2-mediated HMOX1 transcription factor gene expression in a PI(3)K/mTORC2/Akt-dependent signaling pathway leading to endothelial cell (EC) survival under disturbed flow/oxidative stress. Regulates both the transcriptional activation and repression phases of the circadian clock in a deacetylase activity-independent manner. During the activation phase, promotes the accumulation of ubiquitinated BMAL1 at the E-boxes and during the repression phase, blocks FBXL3-mediated CRY1/2 ubiquitination and promotes the interaction of CRY1 and BMAL1. The NCOR1-HDAC3 complex regulates the circadian expression of the core clock gene BMAL1 and the genes involved in lipid metabolism in the liver. Also functions as a deacetylase for non-histone targets, such as KAT5, MEF2D, MAPK14, RARA and STAT3. Serves as a corepressor of RARA, mediating its deacetylation and repression, leading to inhibition of RARE DNA element binding. In association with RARA, plays a role in the repression of microRNA-10a and thereby in the inflammatory response. In addition to protein deacetylase activity, also acts as a protein-lysine deacylase by recognizing other acyl groups: catalyzes removal of (2E)-butenoyl (crotonyl) and 2-hydroxyisobutanoyl (2-hydroxyisobutyryl) acyl groups from lysine residues, leading to protein decrotonylation and de-2-hydroxyisobutyrylation, respectively. Catalyzes decrotonylation of MAPRE1/EB1.
TTD ID
T05090
Uniprot ID
O15379
DrugMap ID
TT4YWTO
Ensemble ID
ENST00000305264.8
HGNC ID
HGNC:4854
ChEMBL ID
CHEMBL1829

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HT115 SNV: p.D421Y DBIA    Probe Info 
MEC1 SNV: p.F48L DBIA    Probe Info 
SHP77 Substitution: p.D391N DBIA    Probe Info 

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  		12.29  LDD0402  [1]
SAHA-CA-4PAP
 Probe Info  		20.00  LDD0269  [2]
BTD
 Probe Info  		C279(0.92)  LDD2093  [3]
DBIA
 Probe Info  		C94(6.23)  LDD0204  [4]
IPM
 Probe Info  		C218(0.96)  LDD1702  [3]
4-Iodoacetamidophenylacetylene
 Probe Info  		C279(0.00); C268(0.00); C218(0.00)  LDD0038  [5]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [6]
Lodoacetamide azide
 Probe Info  		C279(0.00); C123(0.00); C268(0.00); C218(0.00)  LDD0037  [5]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [7]
Acrolein
 Probe Info  		N.A.  LDD0217  [8]
Methacrolein
 Probe Info  		N.A.  LDD0218  [8]
AOyne
 Probe Info  		15.00  LDD0443  [9]
NAIA_5
 Probe Info  		N.A.  LDD2223  [10]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
SAHA-CA-8PAP
 Probe Info  		N.A.  LDD0362  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C279(1.74)  LDD2152  [3]
 LDCM0214  AC1 HEK-293T C279(1.05); C218(0.87); C123(0.98); C268(1.04)  LDD1507  [11]
 LDCM0215  AC10 HEK-293T C218(0.96); C123(0.97); C268(0.95); C59(1.04)  LDD1508  [11]
 LDCM0226  AC11 HEK-293T C279(1.03); C218(1.00); C123(0.98); C268(1.00)  LDD1509  [11]
 LDCM0237  AC12 HEK-293T C279(1.03); C218(0.98); C123(1.05); C268(1.08)  LDD1510  [11]
 LDCM0259  AC14 HEK-293T C279(0.92); C218(0.98); C123(0.88); C268(0.90)  LDD1512  [11]
 LDCM0270  AC15 HEK-293T C279(0.96); C218(1.00); C123(0.96); C268(0.94)  LDD1513  [11]
 LDCM0276  AC17 HEK-293T C279(0.99); C218(0.97); C123(1.01); C268(1.14)  LDD1515  [11]
 LDCM0277  AC18 HEK-293T C218(0.85); C123(1.05); C268(0.90); C59(1.00)  LDD1516  [11]
 LDCM0278  AC19 HEK-293T C279(1.06); C218(1.05); C123(1.19); C268(1.23)  LDD1517  [11]
 LDCM0279  AC2 HEK-293T C218(0.97); C123(0.97); C268(0.99); C59(1.04)  LDD1518  [11]
 LDCM0280  AC20 HEK-293T C279(1.00); C218(0.92); C123(0.99); C268(1.09)  LDD1519  [11]
 LDCM0281  AC21 HEK-293T C279(1.02); C218(1.02); C123(0.98); C268(1.04)  LDD1520  [11]
 LDCM0282  AC22 HEK-293T C279(0.91); C218(0.97); C123(0.96); C268(0.91)  LDD1521  [11]
 LDCM0283  AC23 HEK-293T C279(0.91); C218(0.99); C123(1.03); C268(1.00)  LDD1522  [11]
 LDCM0284  AC24 HEK-293T C218(1.03); C123(0.95); C268(0.99); C59(0.90)  LDD1523  [11]
 LDCM0285  AC25 HEK-293T C279(1.04); C218(0.90); C123(0.97); C268(0.96)  LDD1524  [11]
 LDCM0286  AC26 HEK-293T C218(0.87); C123(0.97); C268(0.95); C59(0.87)  LDD1525  [11]
 LDCM0287  AC27 HEK-293T C279(1.14); C218(0.99); C123(1.09); C268(1.01)  LDD1526  [11]
 LDCM0288  AC28 HEK-293T C279(0.96); C218(0.90); C123(0.98); C268(0.95)  LDD1527  [11]
 LDCM0289  AC29 HEK-293T C279(1.01); C218(1.05); C123(0.98); C268(0.94)  LDD1528  [11]
 LDCM0290  AC3 HEK-293T C279(0.95); C218(0.93); C123(1.10); C268(0.95)  LDD1529  [11]
 LDCM0291  AC30 HEK-293T C279(0.87); C218(0.96); C123(1.13); C268(0.99)  LDD1530  [11]
 LDCM0292  AC31 HEK-293T C279(0.89); C218(0.93); C123(0.93); C268(0.97)  LDD1531  [11]
 LDCM0293  AC32 HEK-293T C218(0.99); C123(1.03); C268(0.99); C59(0.99)  LDD1532  [11]
 LDCM0294  AC33 HEK-293T C279(0.95); C218(1.01); C123(1.03); C268(1.01)  LDD1533  [11]
 LDCM0295  AC34 HEK-293T C218(0.96); C123(0.98); C268(0.94); C59(1.04)  LDD1534  [11]
 LDCM0296  AC35 HEK-293T C279(1.27); C218(1.04); C123(1.05); C268(0.93)  LDD1535  [11]
 LDCM0297  AC36 HEK-293T C279(1.00); C218(0.99); C123(1.09); C268(0.85)  LDD1536  [11]
 LDCM0298  AC37 HEK-293T C279(1.00); C218(1.07); C123(0.96); C268(0.95)  LDD1537  [11]
 LDCM0299  AC38 HEK-293T C279(0.90); C218(0.95); C123(1.03); C268(0.85)  LDD1538  [11]
 LDCM0300  AC39 HEK-293T C279(0.91); C218(0.98); C123(0.96); C268(0.99)  LDD1539  [11]
 LDCM0301  AC4 HEK-293T C279(1.02); C218(0.98); C123(0.99); C268(0.89)  LDD1540  [11]
 LDCM0302  AC40 HEK-293T C218(0.92); C123(1.13); C268(0.99); C59(1.00)  LDD1541  [11]
 LDCM0303  AC41 HEK-293T C279(1.05); C218(0.97); C123(1.04); C268(1.06)  LDD1542  [11]
 LDCM0304  AC42 HEK-293T C218(0.93); C123(0.98); C268(0.95); C59(1.12)  LDD1543  [11]
 LDCM0305  AC43 HEK-293T C279(1.11); C218(1.00); C123(1.03); C268(0.97)  LDD1544  [11]
 LDCM0306  AC44 HEK-293T C279(0.98); C218(0.97); C123(0.99); C268(0.87)  LDD1545  [11]
 LDCM0307  AC45 HEK-293T C279(0.92); C218(0.95); C123(0.84); C268(0.94)  LDD1546  [11]
 LDCM0308  AC46 HEK-293T C279(0.90); C218(0.93); C123(1.06); C268(0.94)  LDD1547  [11]
 LDCM0309  AC47 HEK-293T C279(0.98); C218(0.92); C123(0.97); C268(0.92)  LDD1548  [11]
 LDCM0310  AC48 HEK-293T C218(1.01); C123(1.08); C268(0.95); C59(0.96)  LDD1549  [11]
 LDCM0311  AC49 HEK-293T C279(1.13); C218(0.96); C123(1.00); C268(1.03)  LDD1550  [11]
 LDCM0312  AC5 HEK-293T C279(1.05); C218(0.97); C123(1.03); C268(0.85)  LDD1551  [11]
 LDCM0313  AC50 HEK-293T C218(0.96); C123(0.97); C268(0.91); C59(1.15)  LDD1552  [11]
 LDCM0314  AC51 HEK-293T C279(0.89); C218(1.03); C123(1.05); C268(1.01)  LDD1553  [11]
 LDCM0315  AC52 HEK-293T C279(1.07); C218(0.89); C123(0.98); C268(1.07)  LDD1554  [11]
 LDCM0316  AC53 HEK-293T C279(0.99); C218(1.01); C123(1.11); C268(0.93)  LDD1555  [11]
 LDCM0317  AC54 HEK-293T C279(1.02); C218(1.02); C123(0.98); C268(0.92)  LDD1556  [11]
 LDCM0318  AC55 HEK-293T C279(1.03); C218(0.93); C123(0.98); C268(1.00)  LDD1557  [11]
 LDCM0319  AC56 HEK-293T C218(1.03); C123(1.08); C268(0.99); C59(0.93)  LDD1558  [11]
 LDCM0320  AC57 HEK-293T C279(1.07); C218(1.04); C123(1.07); C268(0.99)  LDD1559  [11]
 LDCM0321  AC58 HEK-293T C218(0.90); C123(0.95); C268(0.95); C59(0.90)  LDD1560  [11]
 LDCM0322  AC59 HEK-293T C279(1.12); C218(1.03); C123(0.99); C268(1.01)  LDD1561  [11]
 LDCM0323  AC6 HEK-293T C279(1.00); C218(0.98); C123(0.95); C268(1.02)  LDD1562  [11]
 LDCM0324  AC60 HEK-293T C279(1.00); C218(0.86); C123(0.94); C268(0.96)  LDD1563  [11]
 LDCM0325  AC61 HEK-293T C279(1.02); C218(0.99); C123(1.19); C268(0.89)  LDD1564  [11]
 LDCM0326  AC62 HEK-293T C279(1.00); C218(0.91); C123(1.17); C268(0.94)  LDD1565  [11]
 LDCM0327  AC63 HEK-293T C279(1.01); C218(0.97); C123(1.02); C268(1.07)  LDD1566  [11]
 LDCM0328  AC64 HEK-293T C218(1.01); C123(0.93); C268(0.92); C59(0.93)  LDD1567  [11]
 LDCM0334  AC7 HEK-293T C279(0.98); C218(0.93); C123(0.99); C268(0.95)  LDD1568  [11]
 LDCM0345  AC8 HEK-293T C218(1.01); C123(1.04); C268(0.92); C59(0.92)  LDD1569  [11]
 LDCM0248  AKOS034007472 HEK-293T C279(1.03); C218(1.04); C123(0.96); C268(0.95)  LDD1511  [11]
 LDCM0356  AKOS034007680 HEK-293T C279(1.01); C218(0.96); C123(1.07); C268(0.99)  LDD1570  [11]
 LDCM0275  AKOS034007705 HEK-293T C218(1.04); C123(0.98); C268(0.90); C59(1.06)  LDD1514  [11]
 LDCM0102  BDHI 8 Jurkat C94(6.23)  LDD0204  [4]
 LDCM0367  CL1 HEK-293T C279(1.10); C218(0.97); C123(1.09); C268(1.00)  LDD1571  [11]
 LDCM0368  CL10 HEK-293T C279(1.07); C218(1.29); C123(1.75); C268(1.08)  LDD1572  [11]
 LDCM0369  CL100 HEK-293T C218(0.96); C123(0.95); C268(0.96); C59(0.97)  LDD1573  [11]
 LDCM0370  CL101 HEK-293T C279(1.05); C218(0.96); C123(1.00); C268(1.00)  LDD1574  [11]
 LDCM0371  CL102 HEK-293T C279(0.93); C218(0.96); C123(1.00); C268(0.94)  LDD1575  [11]
 LDCM0372  CL103 HEK-293T C279(0.99); C218(1.02); C123(0.91)  LDD1576  [11]
 LDCM0373  CL104 HEK-293T C218(1.02); C123(0.90); C268(0.98); C59(1.02)  LDD1577  [11]
 LDCM0374  CL105 HEK-293T C279(1.05); C218(0.93); C123(1.04); C268(0.89)  LDD1578  [11]
 LDCM0375  CL106 HEK-293T C279(0.93); C218(0.99); C123(0.97); C268(0.92)  LDD1579  [11]
 LDCM0376  CL107 HEK-293T C279(0.92); C218(0.97); C123(0.94)  LDD1580  [11]
 LDCM0377  CL108 HEK-293T C218(0.99); C123(0.96); C268(1.02); C59(0.94)  LDD1581  [11]
 LDCM0378  CL109 HEK-293T C279(0.98); C218(1.01); C123(1.06); C268(0.98)  LDD1582  [11]
 LDCM0379  CL11 HEK-293T C279(1.05); C218(1.39); C123(1.13); C268(1.54)  LDD1583  [11]
 LDCM0380  CL110 HEK-293T C279(1.05); C218(0.99); C123(0.98); C268(1.04)  LDD1584  [11]
 LDCM0381  CL111 HEK-293T C279(0.93); C218(0.91); C123(0.97)  LDD1585  [11]
 LDCM0382  CL112 HEK-293T C218(0.97); C123(0.94); C268(0.99); C59(0.92)  LDD1586  [11]
 LDCM0383  CL113 HEK-293T C279(0.99); C218(1.04); C123(0.94); C268(0.99)  LDD1587  [11]
 LDCM0384  CL114 HEK-293T C279(0.96); C218(1.06); C123(1.05); C268(0.96)  LDD1588  [11]
 LDCM0385  CL115 HEK-293T C279(1.06); C218(1.00); C123(0.98)  LDD1589  [11]
 LDCM0386  CL116 HEK-293T C218(0.90); C123(0.95); C268(1.02); C59(1.05)  LDD1590  [11]
 LDCM0387  CL117 HEK-293T C279(1.08); C218(1.04); C123(1.06); C268(1.03)  LDD1591  [11]
 LDCM0388  CL118 HEK-293T C279(0.90); C218(1.02); C123(0.98); C268(0.96)  LDD1592  [11]
 LDCM0389  CL119 HEK-293T C279(0.99); C218(0.97); C123(0.91)  LDD1593  [11]
 LDCM0390  CL12 HEK-293T C218(1.35); C123(1.07); C268(1.13); C59(1.25)  LDD1594  [11]
 LDCM0391  CL120 HEK-293T C218(0.99); C123(0.92); C268(0.97); C59(1.20)  LDD1595  [11]
 LDCM0392  CL121 HEK-293T C279(1.02); C218(0.98); C123(1.10); C268(0.99)  LDD1596  [11]
 LDCM0393  CL122 HEK-293T C279(0.92); C218(1.04); C123(0.95); C268(0.97)  LDD1597  [11]
 LDCM0394  CL123 HEK-293T C279(0.99); C218(0.92); C123(1.03)  LDD1598  [11]
 LDCM0395  CL124 HEK-293T C218(0.98); C123(0.93); C268(1.00); C59(1.02)  LDD1599  [11]
 LDCM0396  CL125 HEK-293T C279(1.10); C218(0.98); C123(1.10); C268(0.96)  LDD1600  [11]
 LDCM0397  CL126 HEK-293T C279(0.96); C218(1.00); C123(1.08); C268(0.91)  LDD1601  [11]
 LDCM0398  CL127 HEK-293T C279(0.95); C218(1.00); C123(1.02)  LDD1602  [11]
 LDCM0399  CL128 HEK-293T C218(0.89); C123(1.04); C268(0.98); C59(0.85)  LDD1603  [11]
 LDCM0400  CL13 HEK-293T C279(1.03); C218(1.00); C123(1.14); C268(0.99)  LDD1604  [11]
 LDCM0401  CL14 HEK-293T C279(0.98); C218(1.25); C123(0.93); C268(0.96)  LDD1605  [11]
 LDCM0402  CL15 HEK-293T C279(1.11); C218(1.23); C123(1.07)  LDD1606  [11]
 LDCM0403  CL16 HEK-293T C218(1.10); C123(0.96); C268(0.91); C59(1.08)  LDD1607  [11]
 LDCM0404  CL17 HEK-293T C279(1.19); C218(1.20); C123(1.15); C268(0.97)  LDD1608  [11]
 LDCM0405  CL18 HEK-293T C218(1.10); C123(0.98); C268(0.89); C59(1.31)  LDD1609  [11]
 LDCM0406  CL19 HEK-293T C279(1.10); C218(1.27); C123(1.04); C268(0.98)  LDD1610  [11]
 LDCM0407  CL2 HEK-293T C279(1.02); C218(1.28); C123(0.97); C268(1.02)  LDD1611  [11]
 LDCM0408  CL20 HEK-293T C279(1.11); C218(1.16); C123(0.96); C268(1.09)  LDD1612  [11]
 LDCM0409  CL21 HEK-293T C279(1.22); C218(1.28); C123(1.35); C268(1.01)  LDD1613  [11]
 LDCM0410  CL22 HEK-293T C279(1.06); C218(1.31); C123(1.03); C268(1.02)  LDD1614  [11]
 LDCM0411  CL23 HEK-293T C279(1.05); C218(1.21); C123(1.03); C268(1.54)  LDD1615  [11]
 LDCM0412  CL24 HEK-293T C218(1.41); C123(1.01); C268(1.03); C59(1.35)  LDD1616  [11]
 LDCM0413  CL25 HEK-293T C279(1.12); C218(1.03); C123(1.09); C268(1.06)  LDD1617  [11]
 LDCM0414  CL26 HEK-293T C279(0.97); C218(0.98); C123(0.94); C268(0.93)  LDD1618  [11]
 LDCM0415  CL27 HEK-293T C279(1.07); C218(1.05); C123(0.99)  LDD1619  [11]
 LDCM0416  CL28 HEK-293T C218(0.95); C123(0.90); C268(1.01); C59(1.16)  LDD1620  [11]
 LDCM0417  CL29 HEK-293T C279(1.06); C218(1.02); C123(0.94); C268(1.12)  LDD1621  [11]
 LDCM0418  CL3 HEK-293T C279(1.02); C218(1.21); C123(0.98)  LDD1622  [11]
 LDCM0419  CL30 HEK-293T C218(1.07); C123(0.97); C268(0.97); C59(1.36)  LDD1623  [11]
 LDCM0420  CL31 HEK-293T C279(0.99); C218(1.18); C123(1.06); C268(1.07)  LDD1624  [11]
 LDCM0421  CL32 HEK-293T C279(1.14); C218(1.04); C123(0.92); C268(1.04)  LDD1625  [11]
 LDCM0422  CL33 HEK-293T C279(1.23); C218(1.14); C123(1.16); C268(1.10)  LDD1626  [11]
 LDCM0423  CL34 HEK-293T C279(1.21); C218(1.15); C123(0.90); C268(1.09)  LDD1627  [11]
 LDCM0424  CL35 HEK-293T C279(1.08); C218(1.34); C123(1.05); C268(1.42)  LDD1628  [11]
 LDCM0425  CL36 HEK-293T C218(1.29); C123(1.11); C268(1.03); C59(1.48)  LDD1629  [11]
 LDCM0426  CL37 HEK-293T C279(1.08); C218(1.03); C123(1.11); C268(0.97)  LDD1630  [11]
 LDCM0428  CL39 HEK-293T C279(1.04); C218(0.92); C123(0.99)  LDD1632  [11]
 LDCM0429  CL4 HEK-293T C218(1.03); C123(1.00); C268(0.94); C59(1.11)  LDD1633  [11]
 LDCM0430  CL40 HEK-293T C218(1.05); C123(0.93); C268(0.97); C59(1.21)  LDD1634  [11]
 LDCM0431  CL41 HEK-293T C279(1.02); C218(0.98); C123(0.98); C268(1.07)  LDD1635  [11]
 LDCM0432  CL42 HEK-293T C218(1.01); C123(0.97); C268(1.00); C59(1.08)  LDD1636  [11]
 LDCM0433  CL43 HEK-293T C279(1.05); C218(1.15); C123(0.99); C268(1.01)  LDD1637  [11]
 LDCM0434  CL44 HEK-293T C279(1.08); C218(1.09); C123(1.03); C268(1.11)  LDD1638  [11]
 LDCM0435  CL45 HEK-293T C279(1.09); C218(1.10); C123(1.04); C268(0.93)  LDD1639  [11]
 LDCM0436  CL46 HEK-293T C279(1.03); C218(1.17); C123(0.95); C268(1.11)  LDD1640  [11]
 LDCM0437  CL47 HEK-293T C279(1.07); C218(1.37); C123(0.97); C268(1.29)  LDD1641  [11]
 LDCM0438  CL48 HEK-293T C218(1.18); C123(1.08); C268(1.04); C59(1.14)  LDD1642  [11]
 LDCM0439  CL49 HEK-293T C279(1.09); C218(1.01); C123(1.07); C268(0.94)  LDD1643  [11]
 LDCM0440  CL5 HEK-293T C279(1.17); C218(1.09); C123(1.17); C268(1.04)  LDD1644  [11]
 LDCM0441  CL50 HEK-293T C279(1.05); C218(1.08); C123(0.98); C268(0.90)  LDD1645  [11]
 LDCM0443  CL52 HEK-293T C218(1.04); C123(0.93); C268(0.97); C59(1.15)  LDD1646  [11]
 LDCM0444  CL53 HEK-293T C279(1.17); C218(1.06); C123(1.06); C268(1.05)  LDD1647  [11]
 LDCM0445  CL54 HEK-293T C218(1.03); C123(1.09); C268(0.97); C59(1.16)  LDD1648  [11]
 LDCM0446  CL55 HEK-293T C279(1.39); C218(1.18); C123(1.06); C268(1.05)  LDD1649  [11]
 LDCM0447  CL56 HEK-293T C279(1.03); C218(1.15); C123(1.08); C268(0.98)  LDD1650  [11]
 LDCM0448  CL57 HEK-293T C279(1.14); C218(1.14); C123(1.11); C268(1.04)  LDD1651  [11]
 LDCM0449  CL58 HEK-293T C279(1.18); C218(1.13); C123(1.14); C268(1.00)  LDD1652  [11]
 LDCM0450  CL59 HEK-293T C279(1.10); C218(1.22); C123(1.05); C268(1.35)  LDD1653  [11]
 LDCM0451  CL6 HEK-293T C218(0.99); C123(1.13); C268(0.90); C59(1.48)  LDD1654  [11]
 LDCM0452  CL60 HEK-293T C218(1.27); C123(1.05); C268(0.97); C59(1.07)  LDD1655  [11]
 LDCM0453  CL61 HEK-293T C279(1.06); C218(0.90); C123(1.01); C268(0.96)  LDD1656  [11]
 LDCM0454  CL62 HEK-293T C279(0.97); C218(1.04); C123(0.90); C268(0.89)  LDD1657  [11]
 LDCM0455  CL63 HEK-293T C279(0.96); C218(0.98); C123(0.89)  LDD1658  [11]
 LDCM0456  CL64 HEK-293T C218(1.00); C123(0.94); C268(0.96); C59(1.29)  LDD1659  [11]
 LDCM0457  CL65 HEK-293T C279(1.03); C218(1.01); C123(1.07); C268(0.97)  LDD1660  [11]
 LDCM0458  CL66 HEK-293T C218(0.96); C123(0.98); C268(0.99); C59(1.14)  LDD1661  [11]
 LDCM0459  CL67 HEK-293T C279(1.07); C218(1.22); C123(0.97); C268(1.05)  LDD1662  [11]
 LDCM0460  CL68 HEK-293T C279(1.12); C218(1.08); C123(1.03); C268(1.02)  LDD1663  [11]
 LDCM0461  CL69 HEK-293T C279(1.07); C218(1.14); C123(1.00); C268(0.95)  LDD1664  [11]
 LDCM0462  CL7 HEK-293T C279(1.31); C218(1.10); C123(1.13); C268(0.96)  LDD1665  [11]
 LDCM0463  CL70 HEK-293T C279(1.08); C218(1.11); C123(0.95); C268(0.98)  LDD1666  [11]
 LDCM0464  CL71 HEK-293T C279(1.11); C218(1.22); C123(0.97); C268(1.10)  LDD1667  [11]
 LDCM0465  CL72 HEK-293T C218(1.17); C123(1.06); C268(1.02); C59(1.42)  LDD1668  [11]
 LDCM0466  CL73 HEK-293T C279(1.08); C218(0.97); C123(1.10); C268(0.94)  LDD1669  [11]
 LDCM0467  CL74 HEK-293T C279(0.90); C218(1.01); C123(0.95); C268(0.90)  LDD1670  [11]
 LDCM0469  CL76 HEK-293T C218(1.00); C123(0.97); C268(0.98); C59(1.16)  LDD1672  [11]
 LDCM0470  CL77 HEK-293T C279(1.06); C218(1.05); C123(1.13); C268(0.98)  LDD1673  [11]
 LDCM0471  CL78 HEK-293T C218(1.05); C123(1.01); C268(0.87); C59(1.17)  LDD1674  [11]
 LDCM0472  CL79 HEK-293T C279(1.29); C218(1.11); C123(1.01); C268(1.01)  LDD1675  [11]
 LDCM0473  CL8 HEK-293T C279(1.52); C218(1.31); C123(1.93); C268(1.30)  LDD1676  [11]
 LDCM0474  CL80 HEK-293T C279(1.15); C218(0.91); C123(1.01); C268(1.02)  LDD1677  [11]
 LDCM0475  CL81 HEK-293T C279(1.12); C218(1.17); C123(0.98); C268(0.95)  LDD1678  [11]
 LDCM0476  CL82 HEK-293T C279(0.98); C218(1.16); C123(0.92); C268(0.96)  LDD1679  [11]
 LDCM0477  CL83 HEK-293T C279(1.17); C218(1.20); C123(1.01); C268(1.04)  LDD1680  [11]
 LDCM0478  CL84 HEK-293T C218(1.14); C123(1.36); C268(1.02); C59(1.19)  LDD1681  [11]
 LDCM0479  CL85 HEK-293T C279(1.06); C218(0.96); C123(1.24); C268(0.93)  LDD1682  [11]
 LDCM0480  CL86 HEK-293T C279(0.95); C218(0.99); C123(0.98); C268(0.92)  LDD1683  [11]
 LDCM0481  CL87 HEK-293T C279(1.03); C218(0.92); C123(1.03)  LDD1684  [11]
 LDCM0482  CL88 HEK-293T C218(0.94); C123(1.02); C268(0.97); C59(1.08)  LDD1685  [11]
 LDCM0483  CL89 HEK-293T C279(1.14); C218(0.99); C123(1.14); C268(0.98)  LDD1686  [11]
 LDCM0484  CL9 HEK-293T C279(1.24); C218(1.25); C123(0.99); C268(1.01)  LDD1687  [11]
 LDCM0485  CL90 HEK-293T C218(1.13); C123(1.34); C268(1.12); C59(2.07)  LDD1688  [11]
 LDCM0486  CL91 HEK-293T C279(1.49); C218(1.06); C123(1.11); C268(0.99)  LDD1689  [11]
 LDCM0487  CL92 HEK-293T C279(1.08); C218(1.13); C123(1.06); C268(0.87)  LDD1690  [11]
 LDCM0488  CL93 HEK-293T C279(1.10); C218(1.14); C123(1.04); C268(1.02)  LDD1691  [11]
 LDCM0489  CL94 HEK-293T C279(0.98); C218(1.07); C123(1.32); C268(0.94)  LDD1692  [11]
 LDCM0490  CL95 HEK-293T C279(1.43); C218(1.08); C123(1.27); C268(1.12)  LDD1693  [11]
 LDCM0491  CL96 HEK-293T C218(1.08); C123(1.08); C268(0.98); C59(0.97)  LDD1694  [11]
 LDCM0492  CL97 HEK-293T C279(1.12); C218(0.99); C123(1.08); C268(1.00)  LDD1695  [11]
 LDCM0493  CL98 HEK-293T C279(0.96); C218(1.01); C123(0.96); C268(0.94)  LDD1696  [11]
 LDCM0494  CL99 HEK-293T C279(1.01); C218(0.93); C123(1.01)  LDD1697  [11]
 LDCM0495  E2913 HEK-293T C279(1.09); C218(1.02); C123(0.94)  LDD1698  [11]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C218(0.96)  LDD1702  [3]
 LDCM0468  Fragment33 HEK-293T C279(1.03); C218(0.99); C123(0.97)  LDD1671  [11]
 LDCM0427  Fragment51 HEK-293T C279(0.91); C218(1.00); C123(0.92); C268(0.93)  LDD1631  [11]
 LDCM0107  IAA HeLa N.A.  LDD0221  [8]
 LDCM0022  KB02 HEK-293T C59(0.84); C218(1.01); C123(0.94); C268(1.01)  LDD1492  [11]
 LDCM0023  KB03 Jurkat C94(17.98); C218(39.56)  LDD0209  [4]
 LDCM0024  KB05 COLO792 C280(2.08); C124(3.15)  LDD3310  [12]
 LDCM0109  NEM HeLa N.A.  LDD0223  [8]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C279(0.92)  LDD2093  [3]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C279(1.47)  LDD2119  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C279(1.09)  LDD2146  [3]
 LDCM0627  NUDT7-COV-1 HEK-293T C268(0.55)  LDD2206  [13]
 LDCM0131  RA190 MM1.R C94(1.72)  LDD0304  [14]
 LDCM0096  SAHA K562 20.00  LDD0269  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Lysine-specific histone demethylase 1A (KDM1A) Flavin monoamine oxidase family O60341
Phosphoglycerate kinase 1 (PGK1) Phosphoglycerate kinase family P00558
Serine/threonine-protein phosphatase 4 catalytic subunit (PPP4C) PPP phosphatase family P60510
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
G1/S-specific cyclin-D1 (CCND1) Cyclin family P24385
Transcription factor
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear receptor corepressor 1 (NCOR1) N-CoR nuclear receptor corepressors family O75376
Nuclear receptor corepressor 2 (NCOR2) N-CoR nuclear receptor corepressors family Q9Y618
Nuclear receptor subfamily 0 group B member 2 (NR0B2) Nuclear hormone receptor family Q15466
Methyl-CpG-binding domain protein 1 (MBD1) . Q9UIS9
Myc proto-oncogene protein (MYC) . P01106
Trans-acting T-cell-specific transcription factor GATA-3 (GATA3) . P23771
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
A-kinase anchor protein 8 (AKAP8) AKAP95 family O43823
A-kinase anchor protein 8-like (AKAP8L) AKAP95 family Q9ULX6
Polycomb protein SUZ12 (SUZ12) VEFS (VRN2-EMF2-FIS2-SU(Z)12) family Q15022
DCC-interacting protein 13-alpha (APPL1) . Q9UKG1
G protein pathway suppressor 2 (GPS2) . Q13227
Lethal(3)malignant brain tumor-like protein 2 (L3MBTL2) . Q969R5
Melanoma-associated antigen 2 (MAGEA2; MAGEA2B) . P43356
Nuclear receptor-interacting protein 1 (NRIP1) . P48552

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Decitabine Small molecular drug DB01262
Phenylbutyric Acid Small molecular drug DB06819
Propanoic Acid Small molecular drug DB03766
Romidepsin Small molecular drug DB06176
Valproic Acid Small molecular drug DB00313
Vorinostat Small molecular drug DB02546
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Chr-3996 Small molecular drug D06TKI
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abexinostat Small molecular drug DB12565
Droxinostat Small molecular drug D00VXM
Mocetinostat Small molecular drug DB11830
Pracinostat Small molecular drug DB05223
Rgfp966 Small molecular drug D00HXX
Patented
Click To Hide/Show 16 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Diaryl Amine Derivative 4 Small molecular drug D0XN2W
Pmid29671355-compound-11 Small molecular drug D0EH2K
Pmid29671355-compound-21 Small molecular drug D0LP1K
Pmid29671355-compound-25 Small molecular drug D0RA0D
Pmid29671355-compound-31 Small molecular drug D0DI9S
Pmid29671355-compound-43 Small molecular drug D0BP8I
Pmid29671355-compound-44 Small molecular drug D0N2DK
Pmid29671355-compound-55 Small molecular drug D0OU0J
Pmid29671355-compound-56 Small molecular drug D0CH8Q
Pmid29671355-compound-57 Small molecular drug D0UD9R
Pmid29671355-compound-59 Small molecular drug D0C9NX
Pmid29671355-compound-61 Small molecular drug D0JB4S
Pmid29671355-compound-62 Small molecular drug D07WAT
Pmid29671355-compound-67 Small molecular drug D0M0RE
Pmid29671355-compound-8 Small molecular drug D0LN1T
Pmid29671355-compound-9 Small molecular drug D0Q1QY

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 Streamlined Target Deconvolution Approach Utilizing a Single Photoreactive Chloroalkane Capture Tag. ACS Chem Biol. 2021 Feb 19;16(2):404-413. doi: 10.1021/acschembio.0c00987. Epub 2021 Feb 5.
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 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.
5 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
6 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
7 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
8 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.
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 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
11 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
12 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
13 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
14 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.