Details of the Target

General Information of Target

Target ID LDTP03322
Target Name Bromodomain-containing protein 2 (BRD2)
Gene Name BRD2
Gene ID 6046
Synonyms
KIAA9001; RING3; Bromodomain-containing protein 2; O27.1.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLQNVTPHNKLPGEGNAGLLGLGPEAAAPGKRIRKPSLLYEGFESPTMASVPALQLTPAN
PPPPEVSNPKKPGRVTNQLQYLHKVVMKALWKHQFAWPFRQPVDAVKLGLPDYHKIIKQP
MDMGTIKRRLENNYYWAASECMQDFNTMFTNCYIYNKPTDDIVLMAQTLEKIFLQKVASM
PQEEQELVVTIPKNSHKKGAKLAALQGSVTSAHQVPAVSSVSHTALYTPPPEIPTTVLNI
PHPSVISSPLLKSLHSAGPPLLAVTAAPPAQPLAKKKGVKRKADTTTPTPTAILAPGSPA
SPPGSLEPKAARLPPMRRESGRPIKPPRKDLPDSQQQHQSSKKGKLSEQLKHCNGILKEL
LSKKHAAYAWPFYKPVDASALGLHDYHDIIKHPMDLSTVKRKMENRDYRDAQEFAADVRL
MFSNCYKYNPPDHDVVAMARKLQDVFEFRYAKMPDEPLEPGPLPVSTAMPPGLAKSSSES
SSEESSSESSSEEEEEEDEEDEEEEESESSDSEEERAHRLAELQEQLRAVHEQLAALSQG
PISKPKRKREKKEKKKKRKAEKHRGRAGADEDDKGPRAPRPPQPKKSKKASGSGGGSAAL
GPSGFGPSGGSGTKLPKKATKTAPPALPTGYDSEEEEESRPMSYDEKRQLSLDINKLPGE
KLGRVVHIIQAREPSLRDSNPEEIEIDFETLKPSTLRELERYVLSCLRKKPRKPYTIKKP
VGKTKEELALEKKRELEKRLQDVSGQLNSTKKPPKKANEKTESSSAQQVAVSRLSASSSS
SDSSSSSSSSSSSDTSDSDSG
Target Type
Clinical trial
Target Bioclass
Other
Subcellular location
Nucleus
Function
Chromatin reader protein that specifically recognizes and binds histone H4 acetylated at 'Lys-5' and 'Lys-12' (H4K5ac and H4K12ac, respectively), thereby controlling gene expression and remodeling chromatin structures . Recruits transcription factors and coactivators to target gene sites, and activates RNA polymerase II machinery for transcriptional elongation. Plays a key role in genome compartmentalization via its association with CTCF and cohesin: recruited to chromatin by CTCF and promotes formation of topologically associating domains (TADs) via its ability to bind acetylated histones, contributing to CTCF boundary formation and enhancer insulation. Also recognizes and binds acetylated non-histone proteins, such as STAT3. Involved in inflammatory response by regulating differentiation of naive CD4(+) T-cells into T-helper Th17: recognizes and binds STAT3 acetylated at 'Lys-87', promoting STAT3 recruitment to chromatin. In addition to acetylated lysines, also recognizes and binds lysine residues on histones that are both methylated and acetylated on the same side chain to form N6-acetyl-N6-methyllysine (Kacme), an epigenetic mark of active chromatin associated with increased transcriptional initiation. Specifically binds histone H4 acetyl-methylated at 'Lys-5' and 'Lys-12' (H4K5acme and H4K12acme, respectively).
TTD ID
T86399
Uniprot ID
P25440
DrugMap ID
TTNISW6
Ensemble ID
ENST00000374825.9
HGNC ID
HGNC:1103
ChEMBL ID
CHEMBL1293289

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.R577M DBIA    Probe Info 
HCC1806 SNV: p.K756E DBIA    Probe Info 
HCC1937 Substitution: p.A49C DBIA    Probe Info 
HEC1 SNV: p.P658H DBIA    Probe Info 
HT SNV: p.N748S .
HUH1 Insertion: p.E41MfsTer46 DBIA    Probe Info 
IGROV1 Deletion: p.F145LfsTer20 DBIA    Probe Info 
Ishikawa (Heraklio) 02 ER SNV: p.W97Ter DBIA    Probe Info 
JM1 SNV: p.W136Ter DBIA    Probe Info 
MEC1 Substitution: p.A49C DBIA    Probe Info 
MFE296 Substitution: p.A49C DBIA    Probe Info 
OVK18 Insertion: p.E505dup DBIA    Probe Info 
SKMEL5 Substitution: p.A49C DBIA    Probe Info 
TOV21G SNV: p.P616H DBIA    Probe Info 
U2OS Substitution: p.A49C photo_BS    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 14 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
ONAyne
 Probe Info  		K661(0.56)  LDD0274  [1]
DBIA
 Probe Info  		C741(0.95)  LDD3313  [2]
BTD
 Probe Info  		C706(1.13)  LDD2093  [3]
IPM
 Probe Info  		C706(0.55)  LDD1701  [3]
m-APA
 Probe Info  		N.A.  LDD2233  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		C425(0.00); C706(0.00); C353(0.00)  LDD0038  [5]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [6]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [5]
NHS
 Probe Info  		N.A.  LDD0010  [7]
TFBX
 Probe Info  		C425(0.00); C706(0.00)  LDD0148  [8]
Acrolein
 Probe Info  		N.A.  LDD0217  [9]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [9]
Methacrolein
 Probe Info  		N.A.  LDD0218  [9]
W1
 Probe Info  		N.A.  LDD0236  [10]
PAL-AfBPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C193
 Probe Info  		5.13  LDD1869  [11]
FFF probe2
 Probe Info  		11.16  LDD0463  [12]
FFF probe6
 Probe Info  		6.14  LDD0467  [12]
8df
 Probe Info  		3.27  LDD0250  [13]
8ef
 Probe Info  		6.15  LDD0251  [13]
photo_BS
 Probe Info  		2.03  LDD0412  [14]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C706(0.87)  LDD1507  [15]
 LDCM0215  AC10 HEK-293T C706(0.96)  LDD1508  [15]
 LDCM0226  AC11 HEK-293T C706(0.98)  LDD1509  [15]
 LDCM0237  AC12 HEK-293T C706(0.99)  LDD1510  [15]
 LDCM0259  AC14 HEK-293T C706(0.88)  LDD1512  [15]
 LDCM0270  AC15 HEK-293T C706(0.95)  LDD1513  [15]
 LDCM0276  AC17 HEK-293T C706(0.82)  LDD1515  [15]
 LDCM0277  AC18 HEK-293T C706(0.85)  LDD1516  [15]
 LDCM0278  AC19 HEK-293T C706(0.87)  LDD1517  [15]
 LDCM0279  AC2 HEK-293T C706(1.02)  LDD1518  [15]
 LDCM0280  AC20 HEK-293T C706(0.93)  LDD1519  [15]
 LDCM0281  AC21 HEK-293T C706(1.36)  LDD1520  [15]
 LDCM0282  AC22 HEK-293T C706(0.91)  LDD1521  [15]
 LDCM0283  AC23 HEK-293T C706(1.08)  LDD1522  [15]
 LDCM0284  AC24 HEK-293T C706(0.99)  LDD1523  [15]
 LDCM0285  AC25 HEK-293T C706(1.00)  LDD1524  [15]
 LDCM0286  AC26 HEK-293T C706(0.78)  LDD1525  [15]
 LDCM0287  AC27 HEK-293T C706(1.24)  LDD1526  [15]
 LDCM0288  AC28 HEK-293T C706(0.96)  LDD1527  [15]
 LDCM0289  AC29 HEK-293T C706(1.08)  LDD1528  [15]
 LDCM0290  AC3 HEK-293T C706(0.92)  LDD1529  [15]
 LDCM0291  AC30 HEK-293T C706(0.99)  LDD1530  [15]
 LDCM0292  AC31 HEK-293T C706(0.97)  LDD1531  [15]
 LDCM0293  AC32 HEK-293T C706(1.05)  LDD1532  [15]
 LDCM0294  AC33 HEK-293T C706(1.01)  LDD1533  [15]
 LDCM0295  AC34 HEK-293T C706(1.05)  LDD1534  [15]
 LDCM0296  AC35 HEK-293T C706(1.15)  LDD1535  [15]
 LDCM0297  AC36 HEK-293T C706(0.96)  LDD1536  [15]
 LDCM0298  AC37 HEK-293T C706(1.22)  LDD1537  [15]
 LDCM0299  AC38 HEK-293T C706(1.09)  LDD1538  [15]
 LDCM0300  AC39 HEK-293T C706(1.07)  LDD1539  [15]
 LDCM0301  AC4 HEK-293T C706(1.00)  LDD1540  [15]
 LDCM0302  AC40 HEK-293T C706(1.18)  LDD1541  [15]
 LDCM0303  AC41 HEK-293T C706(1.03)  LDD1542  [15]
 LDCM0304  AC42 HEK-293T C706(0.88)  LDD1543  [15]
 LDCM0305  AC43 HEK-293T C706(1.19)  LDD1544  [15]
 LDCM0306  AC44 HEK-293T C706(0.99)  LDD1545  [15]
 LDCM0307  AC45 HEK-293T C706(1.04)  LDD1546  [15]
 LDCM0308  AC46 HEK-293T C706(1.03)  LDD1547  [15]
 LDCM0309  AC47 HEK-293T C706(1.09)  LDD1548  [15]
 LDCM0310  AC48 HEK-293T C706(1.05)  LDD1549  [15]
 LDCM0311  AC49 HEK-293T C706(0.85)  LDD1550  [15]
 LDCM0312  AC5 HEK-293T C706(1.12)  LDD1551  [15]
 LDCM0313  AC50 HEK-293T C706(0.90)  LDD1552  [15]
 LDCM0314  AC51 HEK-293T C706(1.16)  LDD1553  [15]
 LDCM0315  AC52 HEK-293T C706(1.04)  LDD1554  [15]
 LDCM0316  AC53 HEK-293T C706(1.11)  LDD1555  [15]
 LDCM0317  AC54 HEK-293T C706(0.97)  LDD1556  [15]
 LDCM0318  AC55 HEK-293T C706(1.22)  LDD1557  [15]
 LDCM0319  AC56 HEK-293T C706(1.17)  LDD1558  [15]
 LDCM0320  AC57 HEK-293T C706(0.86)  LDD1559  [15]
 LDCM0321  AC58 HEK-293T C706(0.92)  LDD1560  [15]
 LDCM0322  AC59 HEK-293T C706(0.87)  LDD1561  [15]
 LDCM0323  AC6 HEK-293T C706(0.98)  LDD1562  [15]
 LDCM0324  AC60 HEK-293T C706(0.99)  LDD1563  [15]
 LDCM0325  AC61 HEK-293T C706(0.97)  LDD1564  [15]
 LDCM0326  AC62 HEK-293T C706(0.87)  LDD1565  [15]
 LDCM0327  AC63 HEK-293T C706(0.94)  LDD1566  [15]
 LDCM0328  AC64 HEK-293T C706(1.02)  LDD1567  [15]
 LDCM0334  AC7 HEK-293T C706(0.98)  LDD1568  [15]
 LDCM0345  AC8 HEK-293T C706(0.99)  LDD1569  [15]
 LDCM0248  AKOS034007472 HEK-293T C706(0.88)  LDD1511  [15]
 LDCM0356  AKOS034007680 HEK-293T C706(0.76)  LDD1570  [15]
 LDCM0275  AKOS034007705 HEK-293T C706(0.98)  LDD1514  [15]
 LDCM0092  Amine 8 HL-60 3.27  LDD0250  [13]
 LDCM0160  Bromosprine HEK-293T 2.03  LDD0412  [14]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [9]
 LDCM0367  CL1 HEK-293T C706(0.78)  LDD1571  [15]
 LDCM0368  CL10 HEK-293T C706(0.74)  LDD1572  [15]
 LDCM0369  CL100 HEK-293T C706(0.99)  LDD1573  [15]
 LDCM0370  CL101 HEK-293T C706(0.76)  LDD1574  [15]
 LDCM0371  CL102 HEK-293T C706(1.04)  LDD1575  [15]
 LDCM0372  CL103 HEK-293T C706(0.86)  LDD1576  [15]
 LDCM0373  CL104 HEK-293T C706(1.20)  LDD1577  [15]
 LDCM0374  CL105 HEK-293T C706(0.91)  LDD1578  [15]
 LDCM0375  CL106 HEK-293T C706(1.00)  LDD1579  [15]
 LDCM0376  CL107 HEK-293T C706(1.36)  LDD1580  [15]
 LDCM0377  CL108 HEK-293T C706(0.86)  LDD1581  [15]
 LDCM0378  CL109 HEK-293T C706(0.66)  LDD1582  [15]
 LDCM0379  CL11 HEK-293T C706(0.75)  LDD1583  [15]
 LDCM0380  CL110 HEK-293T C706(0.95)  LDD1584  [15]
 LDCM0381  CL111 HEK-293T C706(1.24)  LDD1585  [15]
 LDCM0382  CL112 HEK-293T C706(0.85)  LDD1586  [15]
 LDCM0383  CL113 HEK-293T C706(0.77)  LDD1587  [15]
 LDCM0384  CL114 HEK-293T C706(0.78)  LDD1588  [15]
 LDCM0385  CL115 HEK-293T C706(1.13)  LDD1589  [15]
 LDCM0386  CL116 HEK-293T C706(1.24)  LDD1590  [15]
 LDCM0387  CL117 HEK-293T C706(0.89)  LDD1591  [15]
 LDCM0388  CL118 HEK-293T C706(0.90)  LDD1592  [15]
 LDCM0389  CL119 HEK-293T C706(0.95)  LDD1593  [15]
 LDCM0390  CL12 HEK-293T C706(0.80)  LDD1594  [15]
 LDCM0391  CL120 HEK-293T C706(1.57)  LDD1595  [15]
 LDCM0392  CL121 HEK-293T C706(0.77)  LDD1596  [15]
 LDCM0393  CL122 HEK-293T C706(1.07)  LDD1597  [15]
 LDCM0394  CL123 HEK-293T C706(0.92)  LDD1598  [15]
 LDCM0395  CL124 HEK-293T C706(1.18)  LDD1599  [15]
 LDCM0396  CL125 HEK-293T C706(0.91)  LDD1600  [15]
 LDCM0397  CL126 HEK-293T C706(0.96)  LDD1601  [15]
 LDCM0398  CL127 HEK-293T C706(1.08)  LDD1602  [15]
 LDCM0399  CL128 HEK-293T C706(1.27)  LDD1603  [15]
 LDCM0400  CL13 HEK-293T C706(0.64)  LDD1604  [15]
 LDCM0401  CL14 HEK-293T C706(0.97)  LDD1605  [15]
 LDCM0402  CL15 HEK-293T C706(0.70)  LDD1606  [15]
 LDCM0403  CL16 HEK-293T C706(1.21)  LDD1607  [15]
 LDCM0404  CL17 HEK-293T C706(0.68)  LDD1608  [15]
 LDCM0405  CL18 HEK-293T C706(0.83)  LDD1609  [15]
 LDCM0406  CL19 HEK-293T C706(1.14)  LDD1610  [15]
 LDCM0407  CL2 HEK-293T C706(0.89)  LDD1611  [15]
 LDCM0408  CL20 HEK-293T C706(1.05)  LDD1612  [15]
 LDCM0409  CL21 HEK-293T C706(0.87)  LDD1613  [15]
 LDCM0410  CL22 HEK-293T C706(0.84)  LDD1614  [15]
 LDCM0411  CL23 HEK-293T C706(1.01)  LDD1615  [15]
 LDCM0412  CL24 HEK-293T C706(1.04)  LDD1616  [15]
 LDCM0413  CL25 HEK-293T C706(0.78)  LDD1617  [15]
 LDCM0414  CL26 HEK-293T C706(0.98)  LDD1618  [15]
 LDCM0415  CL27 HEK-293T C706(1.15)  LDD1619  [15]
 LDCM0416  CL28 HEK-293T C706(1.00)  LDD1620  [15]
 LDCM0417  CL29 HEK-293T C706(1.10)  LDD1621  [15]
 LDCM0418  CL3 HEK-293T C706(0.92)  LDD1622  [15]
 LDCM0419  CL30 HEK-293T C706(0.83)  LDD1623  [15]
 LDCM0420  CL31 HEK-293T C706(0.95)  LDD1624  [15]
 LDCM0421  CL32 HEK-293T C706(1.02)  LDD1625  [15]
 LDCM0422  CL33 HEK-293T C706(0.86)  LDD1626  [15]
 LDCM0423  CL34 HEK-293T C706(0.77)  LDD1627  [15]
 LDCM0424  CL35 HEK-293T C706(0.99)  LDD1628  [15]
 LDCM0425  CL36 HEK-293T C706(0.80)  LDD1629  [15]
 LDCM0426  CL37 HEK-293T C706(0.91)  LDD1630  [15]
 LDCM0428  CL39 HEK-293T C706(0.94)  LDD1632  [15]
 LDCM0429  CL4 HEK-293T C706(1.48)  LDD1633  [15]
 LDCM0430  CL40 HEK-293T C706(1.65)  LDD1634  [15]
 LDCM0431  CL41 HEK-293T C706(0.67)  LDD1635  [15]
 LDCM0432  CL42 HEK-293T C706(0.99)  LDD1636  [15]
 LDCM0433  CL43 HEK-293T C706(0.99)  LDD1637  [15]
 LDCM0434  CL44 HEK-293T C706(0.92)  LDD1638  [15]
 LDCM0435  CL45 HEK-293T C706(0.94)  LDD1639  [15]
 LDCM0436  CL46 HEK-293T C706(0.71)  LDD1640  [15]
 LDCM0437  CL47 HEK-293T C706(0.95)  LDD1641  [15]
 LDCM0438  CL48 HEK-293T C706(0.88)  LDD1642  [15]
 LDCM0439  CL49 HEK-293T C706(0.94)  LDD1643  [15]
 LDCM0440  CL5 HEK-293T C706(0.69)  LDD1644  [15]
 LDCM0441  CL50 HEK-293T C706(1.12)  LDD1645  [15]
 LDCM0443  CL52 HEK-293T C706(1.11)  LDD1646  [15]
 LDCM0444  CL53 HEK-293T C706(0.73)  LDD1647  [15]
 LDCM0445  CL54 HEK-293T C706(0.96)  LDD1648  [15]
 LDCM0446  CL55 HEK-293T C706(1.35)  LDD1649  [15]
 LDCM0447  CL56 HEK-293T C706(1.00)  LDD1650  [15]
 LDCM0448  CL57 HEK-293T C706(0.81)  LDD1651  [15]
 LDCM0449  CL58 HEK-293T C706(0.90)  LDD1652  [15]
 LDCM0450  CL59 HEK-293T C706(1.02)  LDD1653  [15]
 LDCM0451  CL6 HEK-293T C706(0.93)  LDD1654  [15]
 LDCM0452  CL60 HEK-293T C706(0.98)  LDD1655  [15]
 LDCM0453  CL61 HEK-293T C706(0.98)  LDD1656  [15]
 LDCM0454  CL62 HEK-293T C706(1.12)  LDD1657  [15]
 LDCM0455  CL63 HEK-293T C706(1.06)  LDD1658  [15]
 LDCM0456  CL64 HEK-293T C706(0.92)  LDD1659  [15]
 LDCM0457  CL65 HEK-293T C706(0.81)  LDD1660  [15]
 LDCM0458  CL66 HEK-293T C706(0.75)  LDD1661  [15]
 LDCM0459  CL67 HEK-293T C706(1.04)  LDD1662  [15]
 LDCM0460  CL68 HEK-293T C706(1.04)  LDD1663  [15]
 LDCM0461  CL69 HEK-293T C706(1.04)  LDD1664  [15]
 LDCM0462  CL7 HEK-293T C706(1.07)  LDD1665  [15]
 LDCM0463  CL70 HEK-293T C706(0.95)  LDD1666  [15]
 LDCM0464  CL71 HEK-293T C706(0.86)  LDD1667  [15]
 LDCM0465  CL72 HEK-293T C706(1.05)  LDD1668  [15]
 LDCM0466  CL73 HEK-293T C706(0.94)  LDD1669  [15]
 LDCM0467  CL74 HEK-293T C706(0.98)  LDD1670  [15]
 LDCM0469  CL76 HEK-293T C706(1.29)  LDD1672  [15]
 LDCM0470  CL77 HEK-293T C706(0.71)  LDD1673  [15]
 LDCM0471  CL78 HEK-293T C706(1.02)  LDD1674  [15]
 LDCM0472  CL79 HEK-293T C706(1.13)  LDD1675  [15]
 LDCM0473  CL8 HEK-293T C706(0.67)  LDD1676  [15]
 LDCM0474  CL80 HEK-293T C706(0.95)  LDD1677  [15]
 LDCM0475  CL81 HEK-293T C706(0.87)  LDD1678  [15]
 LDCM0476  CL82 HEK-293T C706(0.89)  LDD1679  [15]
 LDCM0477  CL83 HEK-293T C706(1.01)  LDD1680  [15]
 LDCM0478  CL84 HEK-293T C706(1.05)  LDD1681  [15]
 LDCM0479  CL85 HEK-293T C706(0.81)  LDD1682  [15]
 LDCM0480  CL86 HEK-293T C706(1.03)  LDD1683  [15]
 LDCM0481  CL87 HEK-293T C706(1.03)  LDD1684  [15]
 LDCM0482  CL88 HEK-293T C706(1.17)  LDD1685  [15]
 LDCM0483  CL89 HEK-293T C706(0.79)  LDD1686  [15]
 LDCM0484  CL9 HEK-293T C706(1.06)  LDD1687  [15]
 LDCM0485  CL90 HEK-293T C706(0.78)  LDD1688  [15]
 LDCM0486  CL91 HEK-293T C706(1.34)  LDD1689  [15]
 LDCM0487  CL92 HEK-293T C706(0.94)  LDD1690  [15]
 LDCM0488  CL93 HEK-293T C706(1.17)  LDD1691  [15]
 LDCM0489  CL94 HEK-293T C706(0.82)  LDD1692  [15]
 LDCM0490  CL95 HEK-293T C706(0.76)  LDD1693  [15]
 LDCM0491  CL96 HEK-293T C706(0.97)  LDD1694  [15]
 LDCM0492  CL97 HEK-293T C706(0.80)  LDD1695  [15]
 LDCM0493  CL98 HEK-293T C706(1.19)  LDD1696  [15]
 LDCM0494  CL99 HEK-293T C706(0.89)  LDD1697  [15]
 LDCM0182  Compound 18 HEK-293T 6.68  LDD0501  [12]
 LDCM0181  Compound 41 HEK-293T 6.43  LDD0502  [12]
 LDCM0495  E2913 HEK-293T C706(0.99)  LDD1698  [15]
 LDCM0468  Fragment33 HEK-293T C706(0.88)  LDD1671  [15]
 LDCM0427  Fragment51 HEK-293T C706(0.90)  LDD1631  [15]
 LDCM0107  IAA HeLa N.A.  LDD0221  [9]
 LDCM0022  KB02 HEK-293T C706(0.95)  LDD1492  [15]
 LDCM0023  KB03 HEK-293T C706(0.97)  LDD1497  [15]
 LDCM0024  KB05 Hs 936.T C741(0.95)  LDD3313  [2]
 LDCM0109  NEM HeLa N.A.  LDD0227  [9]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C706(1.13)  LDD2093  [3]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C353(0.73)  LDD2109  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Runt-related transcription factor 3 (RUNX3) . Q13761
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone H4 (H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16) Histone H4 family P62805

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Otx-015 Small molecular drug D02YNI
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abbv-744 . D05ICT
Investigative
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bic1 Small molecular drug D0T3AT
Et Bromodomain Inhibitor Small molecular drug D08SEK
Gw841819x Small molecular drug D03LIP
I-bet151 Small molecular drug D0WU1S
Me Bromodomain Inhibitor Small molecular drug D09QOB
Pmid21851057c4d Small molecular drug D0H3TC
Pmid24000170c36 Small molecular drug D0C2XT
Pmid24000170c38 Small molecular drug D0Q2GK
Xd14 Small molecular drug D07FGY
Patented
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid26924192-compound-102 Small molecular drug D03RPJ
Pmid26924192-compound-103 Small molecular drug D05XXS
Pmid26924192-compound-104 Small molecular drug D03NWT
Pmid26924192-compound-105 Small molecular drug D0NN4U
Pmid26924192-compound-106 Small molecular drug D0AE6Y
Pyrrolo-pyrrolone Derivative 1 Small molecular drug D0YM3G

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 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
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 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
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 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
8 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
9 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.
10 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.
11 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
12 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.
13 One-Step Synthesis of Photoaffinity Probes for Live-Cell MS-Based Proteomics. Chemistry. 2021 Dec 20;27(71):17880-17888. doi: 10.1002/chem.202102036. Epub 2021 Sep 14.
14 Chemical Proteomic Profiling of Bromodomains Enables the Wide-Spectrum Evaluation of Bromodomain Inhibitors in Living Cells. J Am Chem Soc. 2019 Jul 24;141(29):11497-11505. doi: 10.1021/jacs.9b02738. Epub 2019 Jul 9.
15 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