Details of the Target

General Information of Target

Target ID LDTP05528
Target Name Apoptosis regulator BAX (BAX)
Gene Name BAX
Gene ID 581
Synonyms
BCL2L4; Apoptosis regulator BAX; Bcl-2-like protein 4; Bcl2-L-4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDGSGEQPRGGGPTSSEQIMKTGALLLQGFIQDRAGRMGGEAPELALDPVPQDASTKKLS
ECLKRIGDELDSNMELQRMIAAVDTDSPREVFFRVAADMFSDGNFNWGRVVALFYFASKL
VLKALCTKVPELIRTIMGWTLDFLRERLLGWIQDQGGWDGLLSYFGTPTWQTVTIFVAGV
LTASLTIWKKMG
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Bcl-2 family
Subcellular location
Cytoplasm; Mitochondrion outer membrane
Function
Plays a role in the mitochondrial apoptotic process. Under normal conditions, BAX is largely cytosolic via constant retrotranslocation from mitochondria to the cytosol mediated by BCL2L1/Bcl-xL, which avoids accumulation of toxic BAX levels at the mitochondrial outer membrane (MOM). Under stress conditions, undergoes a conformation change that causes translocation to the mitochondrion membrane, leading to the release of cytochrome c that then triggers apoptosis . Promotes activation of CASP3, and thereby apoptosis .
TTD ID
T89251
Uniprot ID
Q07812
DrugMap ID
TTQ57WJ
Ensemble ID
ENST00000293288.12
HGNC ID
HGNC:959
ChEMBL ID
CHEMBL5318

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 Deletion: p.E41GfsTer32 .
HCT15 SNV: p.L144I .
RH30 Substitution: p.Q32P .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		10.35  LDD0402  [1]
FBPP2
 Probe Info  		3.69  LDD0324  [2]
CY-1
 Probe Info  		100.00  LDD0243  [3]
BTD
 Probe Info  		C62(0.06)  LDD1700  [4]
Alkyne-RA190
 Probe Info  		2.79  LDD0299  [5]
DBIA
 Probe Info  		C62(1.05)  LDD1507  [6]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [7]
TFBX
 Probe Info  		N.A.  LDD0027  [8]
WYneN
 Probe Info  		N.A.  LDD0021  [9]
WYneO
 Probe Info  		N.A.  LDD0022  [9]
IPM
 Probe Info  		N.A.  LDD0005  [9]
STPyne
 Probe Info  		N.A.  LDD0009  [9]
1c-yne
 Probe Info  		K57(0.00); K21(0.00)  LDD0228  [10]
AOyne
 Probe Info  		15.00  LDD0443  [11]
NAIA_5
 Probe Info  		N.A.  LDD2223  [12]
PAL-AfBPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C278
 Probe Info  		48.17  LDD1948  [13]
C362
 Probe Info  		29.24  LDD2023  [13]
C407
 Probe Info  		11.16  LDD2064  [13]
FFF probe11
 Probe Info  		9.29  LDD0471  [14]
FFF probe13
 Probe Info  		20.00  LDD0475  [14]
FFF probe14
 Probe Info  		20.00  LDD0477  [14]
JN0003
 Probe Info  		20.00  LDD0469  [14]
KIRA6 AfBP
 Probe Info  		N.A.  LDD0378  [15]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C62(0.71)  LDD2112  [4]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C62(0.80)  LDD2117  [4]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C62(1.39)  LDD2103  [4]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C62(0.82)  LDD2132  [4]
 LDCM0214  AC1 HEK-293T C62(1.05)  LDD1507  [6]
 LDCM0215  AC10 HEK-293T C62(1.21)  LDD1508  [6]
 LDCM0237  AC12 HEK-293T C62(1.04)  LDD1510  [6]
 LDCM0259  AC14 HEK-293T C62(1.08)  LDD1512  [6]
 LDCM0270  AC15 HEK-293T C62(1.06)  LDD1513  [6]
 LDCM0276  AC17 HEK-293T C62(1.10)  LDD1515  [6]
 LDCM0277  AC18 HEK-293T C62(1.07)  LDD1516  [6]
 LDCM0279  AC2 HEK-293T C62(1.29)  LDD1518  [6]
 LDCM0280  AC20 HEK-293T C62(1.15)  LDD1519  [6]
 LDCM0281  AC21 HEK-293T C62(1.01); C126(0.90)  LDD1520  [6]
 LDCM0282  AC22 HEK-293T C62(1.10)  LDD1521  [6]
 LDCM0283  AC23 HEK-293T C62(1.06)  LDD1522  [6]
 LDCM0284  AC24 HEK-293T C62(1.03)  LDD1523  [6]
 LDCM0285  AC25 HEK-293T C62(1.02)  LDD1524  [6]
 LDCM0286  AC26 HEK-293T C62(1.12)  LDD1525  [6]
 LDCM0288  AC28 HEK-293T C62(1.13)  LDD1527  [6]
 LDCM0289  AC29 HEK-293T C62(1.07); C126(1.01)  LDD1528  [6]
 LDCM0291  AC30 HEK-293T C62(1.09)  LDD1530  [6]
 LDCM0292  AC31 HEK-293T C62(1.06)  LDD1531  [6]
 LDCM0293  AC32 HEK-293T C62(1.06)  LDD1532  [6]
 LDCM0294  AC33 HEK-293T C62(1.08)  LDD1533  [6]
 LDCM0295  AC34 HEK-293T C62(1.26)  LDD1534  [6]
 LDCM0297  AC36 HEK-293T C62(1.15)  LDD1536  [6]
 LDCM0298  AC37 HEK-293T C62(1.07); C126(0.99)  LDD1537  [6]
 LDCM0299  AC38 HEK-293T C62(1.10)  LDD1538  [6]
 LDCM0300  AC39 HEK-293T C62(1.04)  LDD1539  [6]
 LDCM0301  AC4 HEK-293T C62(1.15)  LDD1540  [6]
 LDCM0302  AC40 HEK-293T C62(1.12)  LDD1541  [6]
 LDCM0303  AC41 HEK-293T C62(1.00)  LDD1542  [6]
 LDCM0304  AC42 HEK-293T C62(1.08)  LDD1543  [6]
 LDCM0306  AC44 HEK-293T C62(1.00)  LDD1545  [6]
 LDCM0307  AC45 HEK-293T C62(0.97); C126(1.06)  LDD1546  [6]
 LDCM0308  AC46 HEK-293T C62(0.98)  LDD1547  [6]
 LDCM0309  AC47 HEK-293T C62(1.15)  LDD1548  [6]
 LDCM0310  AC48 HEK-293T C62(1.01)  LDD1549  [6]
 LDCM0311  AC49 HEK-293T C62(1.01)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C62(1.14); C126(0.94)  LDD1551  [6]
 LDCM0313  AC50 HEK-293T C62(1.19)  LDD1552  [6]
 LDCM0315  AC52 HEK-293T C62(1.02)  LDD1554  [6]
 LDCM0316  AC53 HEK-293T C62(1.06); C126(1.02)  LDD1555  [6]
 LDCM0317  AC54 HEK-293T C62(1.02)  LDD1556  [6]
 LDCM0318  AC55 HEK-293T C62(1.13)  LDD1557  [6]
 LDCM0319  AC56 HEK-293T C62(1.08)  LDD1558  [6]
 LDCM0320  AC57 HEK-293T C62(1.05)  LDD1559  [6]
 LDCM0321  AC58 HEK-293T C62(1.16)  LDD1560  [6]
 LDCM0323  AC6 HEK-293T C62(1.09)  LDD1562  [6]
 LDCM0324  AC60 HEK-293T C62(1.12)  LDD1563  [6]
 LDCM0325  AC61 HEK-293T C62(1.04); C126(0.88)  LDD1564  [6]
 LDCM0326  AC62 HEK-293T C62(1.04)  LDD1565  [6]
 LDCM0327  AC63 HEK-293T C62(1.12)  LDD1566  [6]
 LDCM0328  AC64 HEK-293T C62(1.09)  LDD1567  [6]
 LDCM0334  AC7 HEK-293T C62(1.17)  LDD1568  [6]
 LDCM0345  AC8 HEK-293T C62(1.10)  LDD1569  [6]
 LDCM0545  Acetamide MDA-MB-231 C62(0.67)  LDD2138  [4]
 LDCM0520  AKOS000195272 MDA-MB-231 C62(0.60)  LDD2113  [4]
 LDCM0248  AKOS034007472 HEK-293T C62(0.99); C126(0.95)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C62(1.04)  LDD1570  [6]
 LDCM0275  AKOS034007705 HEK-293T C62(1.05)  LDD1514  [6]
 LDCM0156  Aniline NCI-H1299 10.90  LDD0403  [1]
 LDCM0498  BS-3668 MDA-MB-231 C62(0.79)  LDD2091  [4]
 LDCM0367  CL1 HEK-293T C62(1.14)  LDD1571  [6]
 LDCM0368  CL10 HEK-293T C62(0.64)  LDD1572  [6]
 LDCM0369  CL100 HEK-293T C62(1.14)  LDD1573  [6]
 LDCM0370  CL101 HEK-293T C62(1.21)  LDD1574  [6]
 LDCM0371  CL102 HEK-293T C62(1.17)  LDD1575  [6]
 LDCM0372  CL103 HEK-293T C62(1.22)  LDD1576  [6]
 LDCM0373  CL104 HEK-293T C62(1.16)  LDD1577  [6]
 LDCM0374  CL105 HEK-293T C62(1.11)  LDD1578  [6]
 LDCM0375  CL106 HEK-293T C62(1.09)  LDD1579  [6]
 LDCM0376  CL107 HEK-293T C62(1.22)  LDD1580  [6]
 LDCM0377  CL108 HEK-293T C62(0.99)  LDD1581  [6]
 LDCM0378  CL109 HEK-293T C62(1.07)  LDD1582  [6]
 LDCM0379  CL11 HEK-293T C62(0.64)  LDD1583  [6]
 LDCM0380  CL110 HEK-293T C62(1.08)  LDD1584  [6]
 LDCM0381  CL111 HEK-293T C62(1.09)  LDD1585  [6]
 LDCM0382  CL112 HEK-293T C62(1.02)  LDD1586  [6]
 LDCM0383  CL113 HEK-293T C62(1.22)  LDD1587  [6]
 LDCM0384  CL114 HEK-293T C62(1.22)  LDD1588  [6]
 LDCM0385  CL115 HEK-293T C62(1.16)  LDD1589  [6]
 LDCM0386  CL116 HEK-293T C62(1.11)  LDD1590  [6]
 LDCM0387  CL117 HEK-293T C62(1.06)  LDD1591  [6]
 LDCM0388  CL118 HEK-293T C62(1.10)  LDD1592  [6]
 LDCM0389  CL119 HEK-293T C62(1.11)  LDD1593  [6]
 LDCM0390  CL12 HEK-293T C62(0.65)  LDD1594  [6]
 LDCM0391  CL120 HEK-293T C62(1.01)  LDD1595  [6]
 LDCM0392  CL121 HEK-293T C62(1.13)  LDD1596  [6]
 LDCM0393  CL122 HEK-293T C62(1.12)  LDD1597  [6]
 LDCM0394  CL123 HEK-293T C62(1.13)  LDD1598  [6]
 LDCM0395  CL124 HEK-293T C62(0.94)  LDD1599  [6]
 LDCM0396  CL125 HEK-293T C62(1.47)  LDD1600  [6]
 LDCM0397  CL126 HEK-293T C62(1.22)  LDD1601  [6]
 LDCM0398  CL127 HEK-293T C62(1.24)  LDD1602  [6]
 LDCM0399  CL128 HEK-293T C62(1.06)  LDD1603  [6]
 LDCM0400  CL13 HEK-293T C62(1.12)  LDD1604  [6]
 LDCM0401  CL14 HEK-293T C62(1.11)  LDD1605  [6]
 LDCM0402  CL15 HEK-293T C62(1.15)  LDD1606  [6]
 LDCM0403  CL16 HEK-293T C62(1.05)  LDD1607  [6]
 LDCM0404  CL17 HEK-293T C62(0.86)  LDD1608  [6]
 LDCM0405  CL18 HEK-293T C62(1.00)  LDD1609  [6]
 LDCM0407  CL2 HEK-293T C62(1.26)  LDD1611  [6]
 LDCM0408  CL20 HEK-293T C62(0.72)  LDD1612  [6]
 LDCM0409  CL21 HEK-293T C62(0.60); C126(0.97)  LDD1613  [6]
 LDCM0410  CL22 HEK-293T C62(0.59)  LDD1614  [6]
 LDCM0411  CL23 HEK-293T C62(0.67)  LDD1615  [6]
 LDCM0412  CL24 HEK-293T C62(0.59)  LDD1616  [6]
 LDCM0413  CL25 HEK-293T C62(1.37)  LDD1617  [6]
 LDCM0414  CL26 HEK-293T C62(1.11)  LDD1618  [6]
 LDCM0415  CL27 HEK-293T C62(1.11)  LDD1619  [6]
 LDCM0416  CL28 HEK-293T C62(1.02)  LDD1620  [6]
 LDCM0417  CL29 HEK-293T C62(1.02)  LDD1621  [6]
 LDCM0418  CL3 HEK-293T C62(1.29)  LDD1622  [6]
 LDCM0419  CL30 HEK-293T C62(0.93)  LDD1623  [6]
 LDCM0421  CL32 HEK-293T C62(0.80)  LDD1625  [6]
 LDCM0422  CL33 HEK-293T C62(0.65); C126(1.18)  LDD1626  [6]
 LDCM0423  CL34 HEK-293T C62(0.67)  LDD1627  [6]
 LDCM0424  CL35 HEK-293T C62(0.59)  LDD1628  [6]
 LDCM0425  CL36 HEK-293T C62(0.60)  LDD1629  [6]
 LDCM0426  CL37 HEK-293T C62(1.30)  LDD1630  [6]
 LDCM0428  CL39 HEK-293T C62(1.07)  LDD1632  [6]
 LDCM0429  CL4 HEK-293T C62(1.29)  LDD1633  [6]
 LDCM0430  CL40 HEK-293T C62(1.04)  LDD1634  [6]
 LDCM0431  CL41 HEK-293T C62(0.96)  LDD1635  [6]
 LDCM0432  CL42 HEK-293T C62(0.88)  LDD1636  [6]
 LDCM0434  CL44 HEK-293T C62(0.76)  LDD1638  [6]
 LDCM0435  CL45 HEK-293T C62(0.61); C126(0.94)  LDD1639  [6]
 LDCM0436  CL46 HEK-293T C62(0.63)  LDD1640  [6]
 LDCM0437  CL47 HEK-293T C62(0.59)  LDD1641  [6]
 LDCM0438  CL48 HEK-293T C62(0.63)  LDD1642  [6]
 LDCM0439  CL49 HEK-293T C62(1.33)  LDD1643  [6]
 LDCM0440  CL5 HEK-293T C62(1.00)  LDD1644  [6]
 LDCM0441  CL50 HEK-293T C62(1.11)  LDD1645  [6]
 LDCM0443  CL52 HEK-293T C62(1.07)  LDD1646  [6]
 LDCM0444  CL53 HEK-293T C62(0.99)  LDD1647  [6]
 LDCM0445  CL54 HEK-293T C62(0.98)  LDD1648  [6]
 LDCM0447  CL56 HEK-293T C62(0.72)  LDD1650  [6]
 LDCM0448  CL57 HEK-293T C62(0.63); C126(0.99)  LDD1651  [6]
 LDCM0449  CL58 HEK-293T C62(0.58)  LDD1652  [6]
 LDCM0450  CL59 HEK-293T C62(0.62)  LDD1653  [6]
 LDCM0451  CL6 HEK-293T C62(1.12)  LDD1654  [6]
 LDCM0452  CL60 HEK-293T C62(0.61)  LDD1655  [6]
 LDCM0453  CL61 HEK-293T C62(1.40)  LDD1656  [6]
 LDCM0454  CL62 HEK-293T C62(1.21)  LDD1657  [6]
 LDCM0455  CL63 HEK-293T C62(1.19)  LDD1658  [6]
 LDCM0456  CL64 HEK-293T C62(1.00)  LDD1659  [6]
 LDCM0457  CL65 HEK-293T C62(0.89)  LDD1660  [6]
 LDCM0458  CL66 HEK-293T C62(0.89)  LDD1661  [6]
 LDCM0460  CL68 HEK-293T C62(0.78)  LDD1663  [6]
 LDCM0461  CL69 HEK-293T C62(0.64); C126(0.99)  LDD1664  [6]
 LDCM0463  CL70 HEK-293T C62(0.62)  LDD1666  [6]
 LDCM0464  CL71 HEK-293T C62(0.65)  LDD1667  [6]
 LDCM0465  CL72 HEK-293T C62(0.61)  LDD1668  [6]
 LDCM0466  CL73 HEK-293T C62(1.28)  LDD1669  [6]
 LDCM0467  CL74 HEK-293T C62(1.30)  LDD1670  [6]
 LDCM0469  CL76 HEK-293T C62(0.92)  LDD1672  [6]
 LDCM0470  CL77 HEK-293T C62(0.94)  LDD1673  [6]
 LDCM0471  CL78 HEK-293T C62(1.03)  LDD1674  [6]
 LDCM0473  CL8 HEK-293T C62(0.95)  LDD1676  [6]
 LDCM0474  CL80 HEK-293T C62(0.82)  LDD1677  [6]
 LDCM0475  CL81 HEK-293T C62(0.68); C126(0.97)  LDD1678  [6]
 LDCM0476  CL82 HEK-293T C62(0.72)  LDD1679  [6]
 LDCM0477  CL83 HEK-293T C62(0.68)  LDD1680  [6]
 LDCM0478  CL84 HEK-293T C62(0.69)  LDD1681  [6]
 LDCM0479  CL85 HEK-293T C62(1.66)  LDD1682  [6]
 LDCM0480  CL86 HEK-293T C62(1.49)  LDD1683  [6]
 LDCM0481  CL87 HEK-293T C62(1.45)  LDD1684  [6]
 LDCM0482  CL88 HEK-293T C62(1.38)  LDD1685  [6]
 LDCM0483  CL89 HEK-293T C62(1.04)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C62(0.67); C126(1.03)  LDD1687  [6]
 LDCM0485  CL90 HEK-293T C62(1.06)  LDD1688  [6]
 LDCM0487  CL92 HEK-293T C62(0.84)  LDD1690  [6]
 LDCM0488  CL93 HEK-293T C62(0.77); C126(1.05)  LDD1691  [6]
 LDCM0489  CL94 HEK-293T C62(0.68)  LDD1692  [6]
 LDCM0490  CL95 HEK-293T C62(0.85)  LDD1693  [6]
 LDCM0491  CL96 HEK-293T C62(0.92)  LDD1694  [6]
 LDCM0492  CL97 HEK-293T C62(1.30)  LDD1695  [6]
 LDCM0493  CL98 HEK-293T C62(1.20)  LDD1696  [6]
 LDCM0494  CL99 HEK-293T C62(1.17)  LDD1697  [6]
 LDCM0495  E2913 HEK-293T C62(1.13)  LDD1698  [6]
 LDCM0468  Fragment33 HEK-293T C62(1.24)  LDD1671  [6]
 LDCM0427  Fragment51 HEK-293T C62(1.06)  LDD1631  [6]
 LDCM0024  KB05 T cell C126(20.00)  LDD1709  [16]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C62(0.57)  LDD2102  [4]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C62(0.97)  LDD2089  [4]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C62(0.93)  LDD2092  [4]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C62(0.05)  LDD2093  [4]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C62(1.56)  LDD2094  [4]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C62(0.12); C126(0.46)  LDD2096  [4]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C62(0.46)  LDD2097  [4]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C62(1.28)  LDD2098  [4]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C62(0.10)  LDD2099  [4]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C62(0.39)  LDD2100  [4]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C62(0.44)  LDD2101  [4]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C62(0.68)  LDD2104  [4]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C62(1.67)  LDD2105  [4]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C62(0.24)  LDD2106  [4]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C62(0.57)  LDD2107  [4]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C62(0.17)  LDD2109  [4]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C62(0.81)  LDD2110  [4]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C62(0.33)  LDD2114  [4]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C62(0.43)  LDD2115  [4]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C62(0.22)  LDD2118  [4]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C62(0.94)  LDD2120  [4]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C62(0.58)  LDD2123  [4]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C62(0.17); C126(1.15)  LDD2124  [4]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C62(0.04)  LDD2125  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C62(0.35)  LDD2127  [4]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C62(1.02)  LDD2128  [4]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C62(0.06)  LDD2129  [4]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C62(0.53)  LDD2134  [4]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C62(0.22)  LDD2135  [4]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C62(0.68)  LDD2137  [4]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C62(0.06)  LDD1700  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C62(0.09)  LDD2140  [4]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C62(0.46)  LDD2141  [4]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C62(0.96)  LDD2143  [4]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C62(2.14)  LDD2145  [4]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C62(0.77)  LDD2146  [4]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C62(0.58)  LDD2148  [4]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C62(0.73)  LDD2150  [4]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C62(0.14)  LDD2151  [4]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C62(4.08)  LDD2153  [4]
 LDCM0131  RA190 MM1.R 2.79  LDD0299  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
X-ray repair cross-complementing protein 6 (XRCC6) Ku70 family P12956
E3 ubiquitin-protein ligase RNF144B (RNF144B) RBR family Q7Z419
Transporter and channel
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apoptosis regulator BAX (BAX) Bcl-2 family Q07812
Apoptosis regulator Bcl-2 (BCL2) Bcl-2 family P10415
Bcl-2 homologous antagonist/killer (BAK1) Bcl-2 family Q16611
Bcl-2-like protein 11 (BCL2L11) Bcl-2 family O43521
Bcl-2-like protein 2 (BCL2L2) Bcl-2 family Q92843
Potassium voltage-gated channel subfamily A member 3 (KCNA3) Potassium channel family P22001
Serine/threonine-protein kinase/endoribonuclease IRE1 (ERN1) Ser/Thr protein kinase family O75460
Alpha-synuclein (SNCA) Synuclein family P37840
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bcl-2-like protein 10 (BCL2L10) Bcl-2 family Q9HD36
Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) Bcl-2 family Q07820
Humanin (MT-RNR2) Humanin family Q8IVG9
Apoptosis-associated speck-like protein containing a CARD (PYCARD) . Q9ULZ3
BH3-interacting domain death agonist (BID) . P55957
Heat shock factor 2-binding protein (HSF2BP) . O75031
Protein Bop (RTL10) . Q7L3V2
UV radiation resistance-associated gene protein (UVRAG) . Q9P2Y5

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Thymoquinone Small molecular drug DY4OZ6
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tak-901 Small molecular drug DB12756

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 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
3 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.
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 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.
6 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
7 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
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 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
10 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
11 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.
12 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
13 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
14 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.
15 Kinase Photoaffinity Labeling Reveals Low Selectivity Profile of the IRE1 Targeting Imidazopyrazine-Based KIRA6 Inhibitor. ACS Chem Biol. 2020 Dec 18;15(12):3106-3111. doi: 10.1021/acschembio.0c00802. Epub 2020 Dec 8.
Mass spectrometry data entry: PXD022628
16 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.