General Information of Target

Target ID LDTP02868
Target Name Fumarylacetoacetase (FAH)
Gene Name FAH
Gene ID 2184
Synonyms
Fumarylacetoacetase; FAA; EC 3.7.1.2; Beta-diketonase; Fumarylacetoacetate hydrolase
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
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Sequence
MSFIPVAEDSDFPIHNLPYGVFSTRGDPRPRIGVAIGDQILDLSIIKHLFTGPVLSKHQD
VFNQPTLNSFMGLGQAAWKEARVFLQNLLSVSQARLRDDTELRKCAFISQASATMHLPAT
IGDYTDFYSSRQHATNVGIMFRDKENALMPNWLHLPVGYHGRASSVVVSGTPIRRPMGQM
KPDDSKPPVYGACKLLDMELEMAFFVGPGNRLGEPIPISKAHEHIFGMVLMNDWSARDIQ
KWEYVPLGPFLGKSFGTTVSPWVVPMDALMPFAVPNPKQDPRPLPYLCHDEPYTFDINLS
VNLKGEGMSQAATICKSNFKYMYWTMLQQLTHHSVNGCNLRPGDLLASGTISGPEPENFG
SMLELSWKGTKPIDLGNGQTRKFLLDGDEVIITGYCQGDGYRIGFGQCAGKVLPALLPS
Target Bioclass
Enzyme
Family
FAH family
Uniprot ID
P16930
Ensemble ID
ENST00000261755.9
HGNC ID
HGNC:3579

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.E101K DBIA    Probe Info 
HCT116 SNV: p.T350I .
HEC1 SNV: p.D184N DBIA    Probe Info 
HEC1B SNV: p.D184N .
IM95 Deletion: p.F205LfsTer2 .
Ishikawa (Heraklio) 02 ER Deletion: p.F205LfsTer2 .
LNCaP clone FGC SNV: p.S90F DBIA    Probe Info 
OV90 SNV: p.I216L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 18 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info 
4.37  LDD0215  [1]
TH211
 Probe Info 
Y244(20.00)  LDD0257  [2]
YN-1
 Probe Info 
100.00  LDD0444  [3]
STPyne
 Probe Info 
K241(0.91)  LDD2217  [4]
BTD
 Probe Info 
C408(1.79)  LDD1700  [5]
DBIA
 Probe Info 
C408(34.16)  LDD0209  [6]
HHS-482
 Probe Info 
Y244(1.61)  LDD0285  [7]
HHS-475
 Probe Info 
Y244(15.07)  LDD0264  [8]
IPM
 Probe Info 
C408(4.99)  LDD1701  [5]
HHS-465
 Probe Info 
Y244(0.68)  LDD2237  [9]
4-Iodoacetamidophenylacetylene
 Probe Info 
C105(0.00); C408(0.00); C315(0.00)  LDD0038  [10]
IA-alkyne
 Probe Info 
C408(0.00); C105(0.00); C315(0.00)  LDD0036  [10]
Lodoacetamide azide
 Probe Info 
C105(0.00); C315(0.00)  LDD0037  [10]
WYneO
 Probe Info 
N.A.  LDD0022  [11]
KY-26
 Probe Info 
N.A.  LDD0301  [12]
SF
 Probe Info 
N.A.  LDD0028  [13]
1c-yne
 Probe Info 
N.A.  LDD0228  [14]
NAIA_5
 Probe Info 
C105(0.00); C315(0.00)  LDD2223  [15]
PAL-AfBPP Probe
Click To Hide/Show 19 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C091
 Probe Info 
13.45  LDD1782  [16]
C108
 Probe Info 
12.64  LDD1795  [16]
C143
 Probe Info 
12.91  LDD1825  [16]
C158
 Probe Info 
20.82  LDD1838  [16]
C166
 Probe Info 
8.88  LDD1846  [16]
C204
 Probe Info 
30.27  LDD1879  [16]
C206
 Probe Info 
51.27  LDD1881  [16]
C264
 Probe Info 
21.56  LDD1935  [16]
C273
 Probe Info 
4.92  LDD1943  [16]
C301
 Probe Info 
6.06  LDD1970  [16]
C320
 Probe Info 
7.41  LDD1986  [16]
C339
 Probe Info 
6.06  LDD2002  [16]
C348
 Probe Info 
12.04  LDD2009  [16]
C403
 Probe Info 
16.56  LDD2061  [16]
FFF probe13
 Probe Info 
20.00  LDD0475  [17]
FFF probe14
 Probe Info 
20.00  LDD0477  [17]
FFF probe3
 Probe Info 
11.61  LDD0464  [17]
OEA-DA
 Probe Info 
20.00  LDD0046  [18]
STS-1
 Probe Info 
N.A.  LDD0068  [19]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C193(0.59)  LDD2142  [5]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C408(0.63)  LDD2095  [5]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C408(1.35)  LDD2130  [5]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C408(1.06)  LDD2117  [5]
 LDCM0215  AC10 HEK-293T C105(1.03)  LDD1508  [20]
 LDCM0226  AC11 HEK-293T C105(1.22); C288(1.45)  LDD1509  [20]
 LDCM0237  AC12 HEK-293T C288(0.89)  LDD1510  [20]
 LDCM0259  AC14 HEK-293T C288(1.05)  LDD1512  [20]
 LDCM0270  AC15 HEK-293T C288(0.95)  LDD1513  [20]
 LDCM0277  AC18 HEK-293T C105(0.96)  LDD1516  [20]
 LDCM0278  AC19 HEK-293T C105(1.10); C288(1.30)  LDD1517  [20]
 LDCM0279  AC2 HEK-293T C105(1.00)  LDD1518  [20]
 LDCM0280  AC20 HEK-293T C288(0.96)  LDD1519  [20]
 LDCM0281  AC21 HEK-293T C288(0.88)  LDD1520  [20]
 LDCM0282  AC22 HEK-293T C288(0.89)  LDD1521  [20]
 LDCM0283  AC23 HEK-293T C288(1.02)  LDD1522  [20]
 LDCM0284  AC24 HEK-293T C105(0.99); C288(1.12)  LDD1523  [20]
 LDCM0286  AC26 HEK-293T C105(1.03)  LDD1525  [20]
 LDCM0287  AC27 HEK-293T C105(1.11); C288(0.98)  LDD1526  [20]
 LDCM0288  AC28 HEK-293T C288(1.06)  LDD1527  [20]
 LDCM0289  AC29 HEK-293T C288(0.89)  LDD1528  [20]
 LDCM0290  AC3 HEK-293T C105(1.42); C288(1.35)  LDD1529  [20]
 LDCM0291  AC30 HEK-293T C288(0.95)  LDD1530  [20]
 LDCM0292  AC31 HEK-293T C288(0.92)  LDD1531  [20]
 LDCM0293  AC32 HEK-293T C105(0.99); C288(0.99)  LDD1532  [20]
 LDCM0295  AC34 HEK-293T C105(0.97)  LDD1534  [20]
 LDCM0296  AC35 HEK-293T C105(1.19); C288(0.99)  LDD1535  [20]
 LDCM0297  AC36 HEK-293T C288(1.10)  LDD1536  [20]
 LDCM0298  AC37 HEK-293T C288(1.02)  LDD1537  [20]
 LDCM0299  AC38 HEK-293T C288(1.09)  LDD1538  [20]
 LDCM0300  AC39 HEK-293T C288(0.99)  LDD1539  [20]
 LDCM0301  AC4 HEK-293T C288(1.00)  LDD1540  [20]
 LDCM0302  AC40 HEK-293T C105(0.98); C288(1.03)  LDD1541  [20]
 LDCM0304  AC42 HEK-293T C105(1.03)  LDD1543  [20]
 LDCM0305  AC43 HEK-293T C105(1.17); C288(1.37)  LDD1544  [20]
 LDCM0306  AC44 HEK-293T C288(1.04)  LDD1545  [20]
 LDCM0307  AC45 HEK-293T C288(0.92)  LDD1546  [20]
 LDCM0308  AC46 HEK-293T C288(0.99)  LDD1547  [20]
 LDCM0309  AC47 HEK-293T C288(1.01)  LDD1548  [20]
 LDCM0310  AC48 HEK-293T C105(1.13); C288(1.14)  LDD1549  [20]
 LDCM0312  AC5 HEK-293T C288(0.84)  LDD1551  [20]
 LDCM0313  AC50 HEK-293T C105(1.02)  LDD1552  [20]
 LDCM0314  AC51 HEK-293T C105(1.12); C288(1.69)  LDD1553  [20]
 LDCM0315  AC52 HEK-293T C288(1.19)  LDD1554  [20]
 LDCM0316  AC53 HEK-293T C288(0.78)  LDD1555  [20]
 LDCM0317  AC54 HEK-293T C288(0.98)  LDD1556  [20]
 LDCM0318  AC55 HEK-293T C288(0.94)  LDD1557  [20]
 LDCM0319  AC56 HEK-293T C105(1.18); C288(1.09)  LDD1558  [20]
 LDCM0321  AC58 HEK-293T C105(0.99)  LDD1560  [20]
 LDCM0322  AC59 HEK-293T C105(1.36); C288(0.80)  LDD1561  [20]
 LDCM0323  AC6 HEK-293T C288(0.97)  LDD1562  [20]
 LDCM0324  AC60 HEK-293T C288(0.92)  LDD1563  [20]
 LDCM0325  AC61 HEK-293T C288(0.67)  LDD1564  [20]
 LDCM0326  AC62 HEK-293T C288(0.97)  LDD1565  [20]
 LDCM0327  AC63 HEK-293T C288(0.88)  LDD1566  [20]
 LDCM0328  AC64 HEK-293T C105(0.97); C288(1.11)  LDD1567  [20]
 LDCM0334  AC7 HEK-293T C288(0.97)  LDD1568  [20]
 LDCM0345  AC8 HEK-293T C105(0.78); C288(1.00)  LDD1569  [20]
 LDCM0520  AKOS000195272 MDA-MB-231 C408(0.67)  LDD2113  [5]
 LDCM0248  AKOS034007472 HEK-293T C288(1.00)  LDD1511  [20]
 LDCM0275  AKOS034007705 HEK-293T C105(1.08); C288(1.07)  LDD1514  [20]
 LDCM0498  BS-3668 MDA-MB-231 C408(0.53)  LDD2091  [5]
 LDCM0367  CL1 HEK-293T C105(0.84)  LDD1571  [20]
 LDCM0368  CL10 HEK-293T C288(1.46)  LDD1572  [20]
 LDCM0369  CL100 HEK-293T C105(1.08); C288(0.96)  LDD1573  [20]
 LDCM0370  CL101 HEK-293T C105(0.90)  LDD1574  [20]
 LDCM0371  CL102 HEK-293T C105(1.04); C288(0.81)  LDD1575  [20]
 LDCM0373  CL104 HEK-293T C105(1.21); C288(0.84)  LDD1577  [20]
 LDCM0374  CL105 HEK-293T C105(0.97)  LDD1578  [20]
 LDCM0375  CL106 HEK-293T C105(1.14); C288(0.85)  LDD1579  [20]
 LDCM0377  CL108 HEK-293T C105(1.18); C288(1.34)  LDD1581  [20]
 LDCM0378  CL109 HEK-293T C105(0.89)  LDD1582  [20]
 LDCM0379  CL11 HEK-293T C288(1.31)  LDD1583  [20]
 LDCM0380  CL110 HEK-293T C105(1.00); C288(0.82)  LDD1584  [20]
 LDCM0382  CL112 HEK-293T C105(1.32); C288(1.43)  LDD1586  [20]
 LDCM0383  CL113 HEK-293T C105(0.96)  LDD1587  [20]
 LDCM0384  CL114 HEK-293T C105(0.85); C288(0.81)  LDD1588  [20]
 LDCM0386  CL116 HEK-293T C105(1.08); C288(1.01)  LDD1590  [20]
 LDCM0387  CL117 HEK-293T C105(0.97)  LDD1591  [20]
 LDCM0388  CL118 HEK-293T C105(0.84); C288(0.84)  LDD1592  [20]
 LDCM0390  CL12 HEK-293T C105(0.93); C288(1.34)  LDD1594  [20]
 LDCM0391  CL120 HEK-293T C105(0.99); C288(1.11)  LDD1595  [20]
 LDCM0392  CL121 HEK-293T C105(0.93)  LDD1596  [20]
 LDCM0393  CL122 HEK-293T C105(0.89); C288(0.89)  LDD1597  [20]
 LDCM0395  CL124 HEK-293T C105(1.01); C288(1.29)  LDD1599  [20]
 LDCM0396  CL125 HEK-293T C105(0.96)  LDD1600  [20]
 LDCM0397  CL126 HEK-293T C105(0.70); C288(0.95)  LDD1601  [20]
 LDCM0399  CL128 HEK-293T C105(0.93); C288(1.01)  LDD1603  [20]
 LDCM0400  CL13 HEK-293T C105(0.84)  LDD1604  [20]
 LDCM0401  CL14 HEK-293T C105(0.94); C288(1.00)  LDD1605  [20]
 LDCM0403  CL16 HEK-293T C105(0.97); C288(1.32)  LDD1607  [20]
 LDCM0405  CL18 HEK-293T C105(1.04)  LDD1609  [20]
 LDCM0406  CL19 HEK-293T C105(1.28); C288(1.44)  LDD1610  [20]
 LDCM0407  CL2 HEK-293T C105(1.06); C288(0.96)  LDD1611  [20]
 LDCM0408  CL20 HEK-293T C288(2.13)  LDD1612  [20]
 LDCM0409  CL21 HEK-293T C288(1.32)  LDD1613  [20]
 LDCM0410  CL22 HEK-293T C288(1.59)  LDD1614  [20]
 LDCM0411  CL23 HEK-293T C288(1.41)  LDD1615  [20]
 LDCM0412  CL24 HEK-293T C105(0.95); C288(1.44)  LDD1616  [20]
 LDCM0413  CL25 HEK-293T C105(0.81)  LDD1617  [20]
 LDCM0414  CL26 HEK-293T C105(1.05); C288(0.95)  LDD1618  [20]
 LDCM0416  CL28 HEK-293T C105(0.95); C288(1.07)  LDD1620  [20]
 LDCM0419  CL30 HEK-293T C105(0.96)  LDD1623  [20]
 LDCM0420  CL31 HEK-293T C105(1.03); C288(1.43)  LDD1624  [20]
 LDCM0421  CL32 HEK-293T C288(1.54)  LDD1625  [20]
 LDCM0422  CL33 HEK-293T C288(1.20)  LDD1626  [20]
 LDCM0423  CL34 HEK-293T C288(1.42)  LDD1627  [20]
 LDCM0424  CL35 HEK-293T C288(1.45)  LDD1628  [20]
 LDCM0425  CL36 HEK-293T C105(0.96); C288(1.29)  LDD1629  [20]
 LDCM0426  CL37 HEK-293T C105(0.87)  LDD1630  [20]
 LDCM0429  CL4 HEK-293T C105(1.04); C288(1.26)  LDD1633  [20]
 LDCM0430  CL40 HEK-293T C105(1.03); C288(0.90)  LDD1634  [20]
 LDCM0432  CL42 HEK-293T C105(0.99)  LDD1636  [20]
 LDCM0433  CL43 HEK-293T C105(1.20); C288(1.34)  LDD1637  [20]
 LDCM0434  CL44 HEK-293T C288(1.33)  LDD1638  [20]
 LDCM0435  CL45 HEK-293T C288(1.21)  LDD1639  [20]
 LDCM0436  CL46 HEK-293T C288(1.45)  LDD1640  [20]
 LDCM0437  CL47 HEK-293T C288(1.32)  LDD1641  [20]
 LDCM0438  CL48 HEK-293T C105(1.20); C288(1.27)  LDD1642  [20]
 LDCM0439  CL49 HEK-293T C105(1.09)  LDD1643  [20]
 LDCM0441  CL50 HEK-293T C105(0.92); C288(0.89)  LDD1645  [20]
 LDCM0443  CL52 HEK-293T C105(1.00); C288(1.05)  LDD1646  [20]
 LDCM0445  CL54 HEK-293T C105(1.09)  LDD1648  [20]
 LDCM0446  CL55 HEK-293T C105(1.33); C288(1.71)  LDD1649  [20]
 LDCM0447  CL56 HEK-293T C288(1.30)  LDD1650  [20]
 LDCM0448  CL57 HEK-293T C288(1.08)  LDD1651  [20]
 LDCM0449  CL58 HEK-293T C288(1.54)  LDD1652  [20]
 LDCM0450  CL59 HEK-293T C288(1.26)  LDD1653  [20]
 LDCM0451  CL6 HEK-293T C105(1.18)  LDD1654  [20]
 LDCM0452  CL60 HEK-293T C105(1.02); C288(1.42)  LDD1655  [20]
 LDCM0453  CL61 HEK-293T C105(0.95)  LDD1656  [20]
 LDCM0454  CL62 HEK-293T C105(1.08); C288(1.03)  LDD1657  [20]
 LDCM0456  CL64 HEK-293T C105(1.13); C288(2.03)  LDD1659  [20]
 LDCM0458  CL66 HEK-293T C105(1.12)  LDD1661  [20]
 LDCM0459  CL67 HEK-293T C105(1.16); C288(1.54)  LDD1662  [20]
 LDCM0460  CL68 HEK-293T C288(1.36)  LDD1663  [20]
 LDCM0461  CL69 HEK-293T C288(1.25)  LDD1664  [20]
 LDCM0462  CL7 HEK-293T C105(1.24); C288(1.80)  LDD1665  [20]
 LDCM0463  CL70 HEK-293T C288(1.39)  LDD1666  [20]
 LDCM0464  CL71 HEK-293T C288(1.18)  LDD1667  [20]
 LDCM0465  CL72 HEK-293T C105(1.09); C288(1.33)  LDD1668  [20]
 LDCM0466  CL73 HEK-293T C105(0.89)  LDD1669  [20]
 LDCM0467  CL74 HEK-293T C105(1.51); C288(1.00)  LDD1670  [20]
 LDCM0469  CL76 HEK-293T C105(1.04); C288(1.60)  LDD1672  [20]
 LDCM0471  CL78 HEK-293T C105(1.04)  LDD1674  [20]
 LDCM0472  CL79 HEK-293T C105(1.24); C288(1.67)  LDD1675  [20]
 LDCM0473  CL8 HEK-293T C288(1.08)  LDD1676  [20]
 LDCM0474  CL80 HEK-293T C288(1.21)  LDD1677  [20]
 LDCM0475  CL81 HEK-293T C288(1.13)  LDD1678  [20]
 LDCM0476  CL82 HEK-293T C288(1.17)  LDD1679  [20]
 LDCM0477  CL83 HEK-293T C288(1.16)  LDD1680  [20]
 LDCM0478  CL84 HEK-293T C105(0.95); C288(1.04)  LDD1681  [20]
 LDCM0479  CL85 HEK-293T C105(1.03)  LDD1682  [20]
 LDCM0480  CL86 HEK-293T C105(0.65); C288(0.99)  LDD1683  [20]
 LDCM0482  CL88 HEK-293T C105(1.04); C288(1.12)  LDD1685  [20]
 LDCM0484  CL9 HEK-293T C288(1.33)  LDD1687  [20]
 LDCM0485  CL90 HEK-293T C105(1.03)  LDD1688  [20]
 LDCM0486  CL91 HEK-293T C105(1.30); C288(1.51)  LDD1689  [20]
 LDCM0487  CL92 HEK-293T C288(1.10)  LDD1690  [20]
 LDCM0488  CL93 HEK-293T C288(1.09)  LDD1691  [20]
 LDCM0489  CL94 HEK-293T C288(1.26)  LDD1692  [20]
 LDCM0490  CL95 HEK-293T C288(0.94)  LDD1693  [20]
 LDCM0491  CL96 HEK-293T C105(0.94); C288(1.05)  LDD1694  [20]
 LDCM0492  CL97 HEK-293T C105(0.97)  LDD1695  [20]
 LDCM0493  CL98 HEK-293T C105(0.77); C288(0.86)  LDD1696  [20]
 LDCM0191  Compound 21 HEK-293T 5.48  LDD0508  [17]
 LDCM0190  Compound 34 HEK-293T 3.28  LDD0510  [17]
 LDCM0193  Compound 36 HEK-293T 4.68  LDD0511  [17]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C408(2.35)  LDD1702  [5]
 LDCM0427  Fragment51 HEK-293T C105(1.14); C288(0.79)  LDD1631  [20]
 LDCM0116  HHS-0101 DM93 Y244(15.07)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y244(9.98)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y244(5.38)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y244(20.00)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y244(12.94)  LDD0268  [8]
 LDCM0123  JWB131 DM93 Y244(1.61)  LDD0285  [7]
 LDCM0124  JWB142 DM93 Y244(0.44)  LDD0286  [7]
 LDCM0125  JWB146 DM93 Y244(2.42)  LDD0287  [7]
 LDCM0126  JWB150 DM93 Y244(1.25)  LDD0288  [7]
 LDCM0127  JWB152 DM93 Y244(6.96)  LDD0289  [7]
 LDCM0128  JWB198 DM93 Y244(1.37)  LDD0290  [7]
 LDCM0129  JWB202 DM93 Y244(0.43)  LDD0291  [7]
 LDCM0130  JWB211 DM93 Y244(1.50)  LDD0292  [7]
 LDCM0022  KB02 HEK-293T C105(0.94)  LDD1492  [20]
 LDCM0023  KB03 Jurkat C408(34.16)  LDD0209  [6]
 LDCM0024  KB05 G361 C315(1.17)  LDD3311  [21]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C408(0.69)  LDD2089  [5]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C408(1.63)  LDD2090  [5]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C408(1.10)  LDD2093  [5]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C408(1.01)  LDD2096  [5]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C193(0.86)  LDD2097  [5]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C408(0.26); C193(0.71)  LDD2098  [5]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C408(0.98)  LDD2101  [5]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C193(0.51)  LDD2106  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C408(1.02)  LDD2107  [5]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C408(0.73); C315(0.79)  LDD2109  [5]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C193(1.02)  LDD2114  [5]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C408(0.54)  LDD2115  [5]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C408(0.80); C315(0.99)  LDD2118  [5]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C408(2.10)  LDD2119  [5]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C408(0.69)  LDD2120  [5]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C408(0.70); C315(0.89)  LDD2122  [5]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C315(0.67)  LDD2124  [5]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C408(0.52); C315(0.65)  LDD2126  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C408(0.82); C315(1.04)  LDD2127  [5]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C408(1.20)  LDD2129  [5]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C408(0.61)  LDD2133  [5]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C408(0.43); C193(0.49)  LDD2134  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C408(0.81); C315(0.94)  LDD2136  [5]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C408(1.79)  LDD1700  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C408(0.85); C315(0.91)  LDD2140  [5]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C193(0.57)  LDD2141  [5]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C193(0.19)  LDD2145  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C408(0.46)  LDD2148  [5]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C408(0.84); C315(0.62)  LDD2149  [5]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C408(0.44)  LDD2150  [5]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C408(1.77)  LDD2153  [5]
 LDCM0131  RA190 MM1.R C315(1.35)  LDD0304  [22]

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
Transcription factor 4 (TCF4) . P15884
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin-associated protein 10-8 (KRTAP10-8) KRTAP type 10 family P60410
Keratin-associated protein 5-9 (KRTAP5-9) KRTAP type 5 family P26371
Keratin-associated protein 13-3 (KRTAP13-3) PMG family Q3SY46
Pleckstrin homology domain-containing family F member 2 (PLEKHF2) . Q9H8W4

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fumaric Acid Small molecular drug DB01677
4-[Hydroxy-[Methyl-phosphinoyl]]-3-oxo-butanoic Acid . DB01832
Acetoacetic Acid . DB01762

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
4 Global profiling of lysine reactivity and ligandability in the human proteome. Nat Chem. 2017 Dec;9(12):1181-1190. doi: 10.1038/nchem.2826. Epub 2017 Jul 31.
5 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
6 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.
7 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
8 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
9 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.
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 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
12 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
13 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
14 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.
15 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
16 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
17 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.
18 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
19 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
20 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
21 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
22 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.