Details of the Target

General Information of Target

Target ID LDTP03838
Target Name TGF-beta receptor type-2 (TGFBR2)
Gene Name TGFBR2
Gene ID 7048
Synonyms
TGF-beta receptor type-2; TGFR-2; EC 2.7.11.30; TGF-beta type II receptor; Transforming growth factor-beta receptor type II; TGF-beta receptor type II; TbetaR-II
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MGRGLLRGLWPLHIVLWTRIASTIPPHVQKSVNNDMIVTDNNGAVKFPQLCKFCDVRFST
CDNQKSCMSNCSITSICEKPQEVCVAVWRKNDENITLETVCHDPKLPYHDFILEDAASPK
CIMKEKKKPGETFFMCSCSSDECNDNIIFSEEYNTSNPDLLLVIFQVTGISLLPPLGVAI
SVIIIFYCYRVNRQQKLSSTWETGKTRKLMEFSEHCAIILEDDRSDISSTCANNINHNTE
LLPIELDTLVGKGRFAEVYKAKLKQNTSEQFETVAVKIFPYEEYASWKTEKDIFSDINLK
HENILQFLTAEERKTELGKQYWLITAFHAKGNLQEYLTRHVISWEDLRKLGSSLARGIAH
LHSDHTPCGRPKMPIVHRDLKSSNILVKNDLTCCLCDFGLSLRLDPTLSVDDLANSGQVG
TARYMAPEVLESRMNLENVESFKQTDVYSMALVLWEMTSRCNAVGEVKDYEPPFGSKVRE
HPCVESMKDNVLRDRGRPEIPSFWLNHQGIQMVCETLTECWDHDPEARLTAQCVAERFSE
LEHLDRLSGRSCSEEKIPEDGSLNTTK
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, TGFB receptor subfamily
Subcellular location
Secreted; Cell membrane
Function
Transmembrane serine/threonine kinase forming with the TGF-beta type I serine/threonine kinase receptor, TGFBR1, the non-promiscuous receptor for the TGF-beta cytokines TGFB1, TGFB2 and TGFB3. Transduces the TGFB1, TGFB2 and TGFB3 signal from the cell surface to the cytoplasm and thus regulates a plethora of physiological and pathological processes including cell cycle arrest in epithelial and hematopoietic cells, control of mesenchymal cell proliferation and differentiation, wound healing, extracellular matrix production, immunosuppression and carcinogenesis. The formation of the receptor complex composed of 2 TGFBR1 and 2 TGFBR2 molecules symmetrically bound to the cytokine dimer results in the phosphorylation and activation of TGFBR1 by the constitutively active TGFBR2. Activated TGFBR1 phosphorylates SMAD2 which dissociates from the receptor and interacts with SMAD4. The SMAD2-SMAD4 complex is subsequently translocated to the nucleus where it modulates the transcription of the TGF-beta-regulated genes. This constitutes the canonical SMAD-dependent TGF-beta signaling cascade. Also involved in non-canonical, SMAD-independent TGF-beta signaling pathways.; [Isoform 1]: Has transforming growth factor beta-activated receptor activity.; [Isoform 2]: Has transforming growth factor beta-activated receptor activity.; [Isoform 3]: Binds TGFB1, TGFB2 and TGFB3 in the picomolar affinity range without the participation of additional receptors. Blocks activation of SMAD2 and SMAD3 by TGFB1.
TTD ID
T49989
Uniprot ID
P37173
DrugMap ID
TTZE3P7
Ensemble ID
ENST00000295754.10
HGNC ID
HGNC:11773
ChEMBL ID
CHEMBL4267

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.L452P .
HKGZCC Deletion: p.K260VfsTer19 .
HT115 SNV: p.S441P; p.R497Ter .
KMCH1 Insertion: p.S66YfsTer4 .
OCUM1 SNV: p.R537C .
OVCAR5 Insertion: p.P129AfsTer3
SNV: p.N384S		 DBIA    Probe Info 
RKO Deletion: p.K128AfsTer3 .
SNU1 Deletion: p.K128AfsTer3; p.S409WfsTer21 .
SUPT1 SNV: p.P243S .
TE4 SNV: p.P371L .
VMRCRCW Deletion: p.I180YfsTer18 .
WM1552C Insertion: p.P129AfsTer3 DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K488(1.04)  LDD0277  [1]
IPM
 Probe Info  		C533(0.00); C483(0.00)  LDD0241  [2]
DBIA
 Probe Info  		C558(2.53)  LDD3316  [3]
BTD
 Probe Info  		C533(0.88)  LDD2117  [4]
NAIA_4
 Probe Info  		C461(0.00); C483(0.00); 0.00  LDD2226  [5]
TFBX
 Probe Info  		N.A.  LDD0148  [6]
W1
 Probe Info  		C533(0.00); C483(0.00)  LDD0236  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C533(0.88)  LDD2117  [4]
 LDCM0214  AC1 HEK-293T C483(0.99); C533(1.15); C461(0.88)  LDD1507  [7]
 LDCM0215  AC10 HEK-293T C533(0.94); C461(1.07)  LDD1508  [7]
 LDCM0226  AC11 HEK-293T C533(1.10); C461(1.07)  LDD1509  [7]
 LDCM0237  AC12 HEK-293T C533(1.03); C461(1.10)  LDD1510  [7]
 LDCM0259  AC14 HEK-293T C483(1.04); C533(1.03)  LDD1512  [7]
 LDCM0270  AC15 HEK-293T C483(1.03); C533(0.94); C461(1.07)  LDD1513  [7]
 LDCM0276  AC17 HEK-293T C483(0.94); C533(1.02); C461(1.06)  LDD1515  [7]
 LDCM0277  AC18 HEK-293T C533(0.95); C461(0.95)  LDD1516  [7]
 LDCM0278  AC19 HEK-293T C533(1.16); C461(1.12)  LDD1517  [7]
 LDCM0279  AC2 HEK-293T C533(0.94); C461(0.88)  LDD1518  [7]
 LDCM0280  AC20 HEK-293T C533(0.96); C461(1.05)  LDD1519  [7]
 LDCM0281  AC21 HEK-293T C483(1.00); C533(0.94)  LDD1520  [7]
 LDCM0282  AC22 HEK-293T C483(1.04); C533(1.07)  LDD1521  [7]
 LDCM0283  AC23 HEK-293T C483(0.94); C533(1.01); C461(1.09)  LDD1522  [7]
 LDCM0284  AC24 HEK-293T C533(1.00); C461(1.01)  LDD1523  [7]
 LDCM0285  AC25 HEK-293T C483(1.06); C533(0.99); C461(1.06)  LDD1524  [7]
 LDCM0286  AC26 HEK-293T C533(0.99); C461(1.03)  LDD1525  [7]
 LDCM0287  AC27 HEK-293T C533(1.19); C461(1.01)  LDD1526  [7]
 LDCM0288  AC28 HEK-293T C533(1.03); C461(1.08)  LDD1527  [7]
 LDCM0289  AC29 HEK-293T C483(1.07); C533(0.92)  LDD1528  [7]
 LDCM0290  AC3 HEK-293T C533(1.00); C461(0.96)  LDD1529  [7]
 LDCM0291  AC30 HEK-293T C483(1.07); C533(0.96)  LDD1530  [7]
 LDCM0292  AC31 HEK-293T C483(1.01); C533(1.05); C461(1.06)  LDD1531  [7]
 LDCM0293  AC32 HEK-293T C533(1.07); C461(1.05)  LDD1532  [7]
 LDCM0294  AC33 HEK-293T C483(0.92); C533(0.97); C461(0.99)  LDD1533  [7]
 LDCM0295  AC34 HEK-293T C533(1.00); C461(0.96)  LDD1534  [7]
 LDCM0296  AC35 HEK-293T C533(1.14); C461(1.06)  LDD1535  [7]
 LDCM0297  AC36 HEK-293T C533(0.99); C461(1.03)  LDD1536  [7]
 LDCM0298  AC37 HEK-293T C483(1.01); C533(0.82)  LDD1537  [7]
 LDCM0299  AC38 HEK-293T C483(1.12); C533(0.97)  LDD1538  [7]
 LDCM0300  AC39 HEK-293T C483(1.04); C533(1.00); C461(1.11)  LDD1539  [7]
 LDCM0301  AC4 HEK-293T C533(1.03); C461(0.90)  LDD1540  [7]
 LDCM0302  AC40 HEK-293T C533(1.07); C461(1.15)  LDD1541  [7]
 LDCM0303  AC41 HEK-293T C483(1.06); C533(1.05); C461(1.08)  LDD1542  [7]
 LDCM0304  AC42 HEK-293T C533(1.03); C461(1.02)  LDD1543  [7]
 LDCM0305  AC43 HEK-293T C533(1.07); C461(1.07)  LDD1544  [7]
 LDCM0306  AC44 HEK-293T C533(1.08); C461(1.07)  LDD1545  [7]
 LDCM0307  AC45 HEK-293T C483(1.11); C533(0.71)  LDD1546  [7]
 LDCM0308  AC46 HEK-293T C483(1.11); C533(0.93)  LDD1547  [7]
 LDCM0309  AC47 HEK-293T C483(1.03); C533(1.02); C461(1.08)  LDD1548  [7]
 LDCM0310  AC48 HEK-293T C533(1.00); C461(1.16)  LDD1549  [7]
 LDCM0311  AC49 HEK-293T C483(0.99); C533(0.92); C461(1.07)  LDD1550  [7]
 LDCM0312  AC5 HEK-293T C483(1.00); C533(0.78)  LDD1551  [7]
 LDCM0313  AC50 HEK-293T C533(0.94); C461(1.06)  LDD1552  [7]
 LDCM0314  AC51 HEK-293T C533(1.05); C461(1.08)  LDD1553  [7]
 LDCM0315  AC52 HEK-293T C533(0.99); C461(1.08)  LDD1554  [7]
 LDCM0316  AC53 HEK-293T C483(1.05); C533(1.02)  LDD1555  [7]
 LDCM0317  AC54 HEK-293T C483(1.18); C533(0.94)  LDD1556  [7]
 LDCM0318  AC55 HEK-293T C483(1.01); C533(0.98); C461(1.10)  LDD1557  [7]
 LDCM0319  AC56 HEK-293T C533(0.98); C461(1.05)  LDD1558  [7]
 LDCM0320  AC57 HEK-293T C483(0.94); C533(1.11); C461(0.97)  LDD1559  [7]
 LDCM0321  AC58 HEK-293T C533(1.06); C461(0.99)  LDD1560  [7]
 LDCM0322  AC59 HEK-293T C533(1.01); C461(1.02)  LDD1561  [7]
 LDCM0323  AC6 HEK-293T C483(1.06); C533(1.05)  LDD1562  [7]
 LDCM0324  AC60 HEK-293T C533(1.09); C461(1.05)  LDD1563  [7]
 LDCM0325  AC61 HEK-293T C483(1.03); C533(1.17)  LDD1564  [7]
 LDCM0326  AC62 HEK-293T C483(1.11); C533(0.94)  LDD1565  [7]
 LDCM0327  AC63 HEK-293T C483(1.00); C533(1.02); C461(1.05)  LDD1566  [7]
 LDCM0328  AC64 HEK-293T C533(1.09); C461(1.01)  LDD1567  [7]
 LDCM0334  AC7 HEK-293T C483(1.04); C533(1.05); C461(0.98)  LDD1568  [7]
 LDCM0345  AC8 HEK-293T C533(1.10); C461(1.00)  LDD1569  [7]
 LDCM0248  AKOS034007472 HEK-293T C483(1.02); C533(0.70)  LDD1511  [7]
 LDCM0356  AKOS034007680 HEK-293T C483(1.07); C533(0.97); C461(1.09)  LDD1570  [7]
 LDCM0275  AKOS034007705 HEK-293T C533(1.02); C461(1.15)  LDD1514  [7]
 LDCM0367  CL1 HEK-293T C483(1.18); C533(0.92); C461(1.04)  LDD1571  [7]
 LDCM0368  CL10 HEK-293T C483(1.39); C533(1.17)  LDD1572  [7]
 LDCM0369  CL100 HEK-293T C533(1.09)  LDD1573  [7]
 LDCM0370  CL101 HEK-293T C483(0.97); C533(0.78); C461(1.07)  LDD1574  [7]
 LDCM0371  CL102 HEK-293T C533(1.06); C461(1.18)  LDD1575  [7]
 LDCM0372  CL103 HEK-293T C533(0.95)  LDD1576  [7]
 LDCM0373  CL104 HEK-293T C533(1.08)  LDD1577  [7]
 LDCM0374  CL105 HEK-293T C483(0.99); C533(0.89); C461(1.04)  LDD1578  [7]
 LDCM0375  CL106 HEK-293T C533(0.85); C461(1.05)  LDD1579  [7]
 LDCM0376  CL107 HEK-293T C533(0.86)  LDD1580  [7]
 LDCM0377  CL108 HEK-293T C533(0.96)  LDD1581  [7]
 LDCM0378  CL109 HEK-293T C483(1.01); C533(1.04); C461(1.01)  LDD1582  [7]
 LDCM0379  CL11 HEK-293T C483(1.45); C533(1.16); C461(1.30)  LDD1583  [7]
 LDCM0380  CL110 HEK-293T C533(1.01); C461(1.13)  LDD1584  [7]
 LDCM0381  CL111 HEK-293T C533(0.95)  LDD1585  [7]
 LDCM0382  CL112 HEK-293T C533(1.00)  LDD1586  [7]
 LDCM0383  CL113 HEK-293T C483(0.94); C533(0.83); C461(1.08)  LDD1587  [7]
 LDCM0384  CL114 HEK-293T C533(1.10); C461(1.24)  LDD1588  [7]
 LDCM0385  CL115 HEK-293T C533(0.97)  LDD1589  [7]
 LDCM0386  CL116 HEK-293T C533(1.01)  LDD1590  [7]
 LDCM0387  CL117 HEK-293T C483(1.05); C533(0.83); C461(1.02)  LDD1591  [7]
 LDCM0388  CL118 HEK-293T C533(0.93); C461(1.27)  LDD1592  [7]
 LDCM0389  CL119 HEK-293T C533(0.88)  LDD1593  [7]
 LDCM0390  CL12 HEK-293T C533(1.07); C461(1.36)  LDD1594  [7]
 LDCM0391  CL120 HEK-293T C533(1.03)  LDD1595  [7]
 LDCM0392  CL121 HEK-293T C483(0.93); C533(0.71); C461(1.12)  LDD1596  [7]
 LDCM0393  CL122 HEK-293T C533(0.87); C461(1.26)  LDD1597  [7]
 LDCM0394  CL123 HEK-293T C533(1.02)  LDD1598  [7]
 LDCM0395  CL124 HEK-293T C533(1.05)  LDD1599  [7]
 LDCM0396  CL125 HEK-293T C483(0.89); C533(0.81); C461(1.03)  LDD1600  [7]
 LDCM0397  CL126 HEK-293T C533(0.91); C461(1.14)  LDD1601  [7]
 LDCM0398  CL127 HEK-293T C533(1.02)  LDD1602  [7]
 LDCM0399  CL128 HEK-293T C533(1.02)  LDD1603  [7]
 LDCM0400  CL13 HEK-293T C483(1.04); C533(0.99); C461(1.09)  LDD1604  [7]
 LDCM0401  CL14 HEK-293T C533(0.93); C461(1.41)  LDD1605  [7]
 LDCM0402  CL15 HEK-293T C533(0.93)  LDD1606  [7]
 LDCM0403  CL16 HEK-293T C533(0.99)  LDD1607  [7]
 LDCM0404  CL17 HEK-293T C483(1.21); C533(1.13); C461(1.13)  LDD1608  [7]
 LDCM0405  CL18 HEK-293T C533(0.88); C461(1.26)  LDD1609  [7]
 LDCM0406  CL19 HEK-293T C533(1.05); C461(1.15)  LDD1610  [7]
 LDCM0407  CL2 HEK-293T C533(0.94); C461(1.18)  LDD1611  [7]
 LDCM0408  CL20 HEK-293T C533(1.02); C461(1.30)  LDD1612  [7]
 LDCM0409  CL21 HEK-293T C483(1.56); C533(1.00)  LDD1613  [7]
 LDCM0410  CL22 HEK-293T C483(1.56); C533(0.99)  LDD1614  [7]
 LDCM0411  CL23 HEK-293T C483(1.39); C533(0.99); C461(1.33)  LDD1615  [7]
 LDCM0412  CL24 HEK-293T C533(1.11); C461(1.27)  LDD1616  [7]
 LDCM0413  CL25 HEK-293T C483(0.93); C533(0.81); C461(1.02)  LDD1617  [7]
 LDCM0414  CL26 HEK-293T C533(0.94); C461(1.10)  LDD1618  [7]
 LDCM0415  CL27 HEK-293T C533(0.95)  LDD1619  [7]
 LDCM0416  CL28 HEK-293T C533(1.02)  LDD1620  [7]
 LDCM0417  CL29 HEK-293T C483(1.02); C533(0.92); C461(1.03)  LDD1621  [7]
 LDCM0418  CL3 HEK-293T C533(0.88)  LDD1622  [7]
 LDCM0419  CL30 HEK-293T C533(0.88); C461(1.05)  LDD1623  [7]
 LDCM0420  CL31 HEK-293T C533(1.13); C461(1.14)  LDD1624  [7]
 LDCM0421  CL32 HEK-293T C533(1.00); C461(1.35)  LDD1625  [7]
 LDCM0422  CL33 HEK-293T C483(1.44); C533(0.91)  LDD1626  [7]
 LDCM0423  CL34 HEK-293T C483(1.35); C533(0.95)  LDD1627  [7]
 LDCM0424  CL35 HEK-293T C483(1.39); C533(0.98); C461(1.32)  LDD1628  [7]
 LDCM0425  CL36 HEK-293T C533(1.07); C461(1.30)  LDD1629  [7]
 LDCM0426  CL37 HEK-293T C483(0.89); C533(0.94); C461(0.95)  LDD1630  [7]
 LDCM0428  CL39 HEK-293T C533(0.92)  LDD1632  [7]
 LDCM0429  CL4 HEK-293T C533(0.98)  LDD1633  [7]
 LDCM0430  CL40 HEK-293T C533(1.02)  LDD1634  [7]
 LDCM0431  CL41 HEK-293T C483(1.01); C533(1.13); C461(1.12)  LDD1635  [7]
 LDCM0432  CL42 HEK-293T C533(0.89); C461(1.08)  LDD1636  [7]
 LDCM0433  CL43 HEK-293T C533(1.03); C461(1.09)  LDD1637  [7]
 LDCM0434  CL44 HEK-293T C533(1.01); C461(1.31)  LDD1638  [7]
 LDCM0435  CL45 HEK-293T C483(1.46); C533(1.25)  LDD1639  [7]
 LDCM0436  CL46 HEK-293T C483(1.17); C533(0.98)  LDD1640  [7]
 LDCM0437  CL47 HEK-293T C483(1.45); C533(1.03); C461(1.26)  LDD1641  [7]
 LDCM0438  CL48 HEK-293T C533(0.91); C461(1.21)  LDD1642  [7]
 LDCM0439  CL49 HEK-293T C483(0.93); C533(0.54); C461(1.02)  LDD1643  [7]
 LDCM0440  CL5 HEK-293T C483(0.98); C533(1.16); C461(1.02)  LDD1644  [7]
 LDCM0441  CL50 HEK-293T C533(0.85); C461(1.15)  LDD1645  [7]
 LDCM0443  CL52 HEK-293T C533(1.05)  LDD1646  [7]
 LDCM0444  CL53 HEK-293T C483(1.16); C533(1.13); C461(1.14)  LDD1647  [7]
 LDCM0445  CL54 HEK-293T C533(1.06); C461(1.29)  LDD1648  [7]
 LDCM0446  CL55 HEK-293T C533(1.00); C461(1.19)  LDD1649  [7]
 LDCM0447  CL56 HEK-293T C533(1.04); C461(1.32)  LDD1650  [7]
 LDCM0448  CL57 HEK-293T C483(1.56); C533(0.97)  LDD1651  [7]
 LDCM0449  CL58 HEK-293T C483(1.22); C533(1.13)  LDD1652  [7]
 LDCM0450  CL59 HEK-293T C483(1.45); C533(0.99); C461(1.43)  LDD1653  [7]
 LDCM0451  CL6 HEK-293T C533(1.03); C461(1.05)  LDD1654  [7]
 LDCM0452  CL60 HEK-293T C533(1.10); C461(1.50)  LDD1655  [7]
 LDCM0453  CL61 HEK-293T C483(0.80); C533(0.80); C461(1.01)  LDD1656  [7]
 LDCM0454  CL62 HEK-293T C533(0.84); C461(1.21)  LDD1657  [7]
 LDCM0455  CL63 HEK-293T C533(0.79)  LDD1658  [7]
 LDCM0456  CL64 HEK-293T C533(1.12)  LDD1659  [7]
 LDCM0457  CL65 HEK-293T C483(1.07); C533(1.05); C461(0.99)  LDD1660  [7]
 LDCM0458  CL66 HEK-293T C533(1.07); C461(1.36)  LDD1661  [7]
 LDCM0459  CL67 HEK-293T C533(1.12); C461(1.19)  LDD1662  [7]
 LDCM0460  CL68 HEK-293T C533(0.94); C461(1.27)  LDD1663  [7]
 LDCM0461  CL69 HEK-293T C483(1.26); C533(0.62)  LDD1664  [7]
 LDCM0462  CL7 HEK-293T C533(1.06); C461(1.13)  LDD1665  [7]
 LDCM0463  CL70 HEK-293T C483(1.34); C533(1.01)  LDD1666  [7]
 LDCM0464  CL71 HEK-293T C483(1.39); C533(1.09); C461(1.27)  LDD1667  [7]
 LDCM0465  CL72 HEK-293T C533(1.09); C461(1.50)  LDD1668  [7]
 LDCM0466  CL73 HEK-293T C483(0.91); C533(0.78); C461(0.85)  LDD1669  [7]
 LDCM0467  CL74 HEK-293T C533(0.86); C461(1.11)  LDD1670  [7]
 LDCM0469  CL76 HEK-293T C533(1.04)  LDD1672  [7]
 LDCM0470  CL77 HEK-293T C483(1.06); C533(1.13); C461(1.11)  LDD1673  [7]
 LDCM0471  CL78 HEK-293T C533(1.00); C461(1.24)  LDD1674  [7]
 LDCM0472  CL79 HEK-293T C533(1.20); C461(1.17)  LDD1675  [7]
 LDCM0473  CL8 HEK-293T C533(1.57); C461(1.51)  LDD1676  [7]
 LDCM0474  CL80 HEK-293T C533(0.98); C461(1.23)  LDD1677  [7]
 LDCM0475  CL81 HEK-293T C483(1.25); C533(0.64)  LDD1678  [7]
 LDCM0476  CL82 HEK-293T C483(1.49); C533(0.93)  LDD1679  [7]
 LDCM0477  CL83 HEK-293T C483(1.29); C533(1.04); C461(1.24)  LDD1680  [7]
 LDCM0478  CL84 HEK-293T C533(0.94); C461(1.32)  LDD1681  [7]
 LDCM0479  CL85 HEK-293T C483(0.86); C533(1.20); C461(0.99)  LDD1682  [7]
 LDCM0480  CL86 HEK-293T C533(0.79); C461(1.12)  LDD1683  [7]
 LDCM0481  CL87 HEK-293T C533(0.91)  LDD1684  [7]
 LDCM0482  CL88 HEK-293T C533(1.12)  LDD1685  [7]
 LDCM0483  CL89 HEK-293T C483(1.01); C533(1.02); C461(1.06)  LDD1686  [7]
 LDCM0484  CL9 HEK-293T C483(1.36); C533(0.70)  LDD1687  [7]
 LDCM0485  CL90 HEK-293T C533(1.34); C461(1.27)  LDD1688  [7]
 LDCM0486  CL91 HEK-293T C533(1.15); C461(1.12)  LDD1689  [7]
 LDCM0487  CL92 HEK-293T C533(1.26); C461(1.27)  LDD1690  [7]
 LDCM0488  CL93 HEK-293T C483(1.25); C533(0.90)  LDD1691  [7]
 LDCM0489  CL94 HEK-293T C483(1.42); C533(0.98)  LDD1692  [7]
 LDCM0490  CL95 HEK-293T C483(1.50); C533(1.15); C461(1.47)  LDD1693  [7]
 LDCM0491  CL96 HEK-293T C533(0.99); C461(1.25)  LDD1694  [7]
 LDCM0492  CL97 HEK-293T C483(1.00); C533(0.93); C461(1.02)  LDD1695  [7]
 LDCM0493  CL98 HEK-293T C533(1.10); C461(1.09)  LDD1696  [7]
 LDCM0494  CL99 HEK-293T C533(0.88)  LDD1697  [7]
 LDCM0495  E2913 HEK-293T C533(0.95)  LDD1698  [7]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C533(4.03); C483(1.53)  LDD1702  [4]
 LDCM0468  Fragment33 HEK-293T C533(0.94)  LDD1671  [7]
 LDCM0427  Fragment51 HEK-293T C533(0.84); C461(0.98)  LDD1631  [7]
 LDCM0022  KB02 HEK-293T C533(1.00)  LDD1492  [7]
 LDCM0023  KB03 HEK-293T C533(1.12)  LDD1497  [7]
 LDCM0024  KB05 MEL167 C558(2.53)  LDD3316  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C533(0.71)  LDD2125  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C533(1.18)  LDD2127  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C533(0.90)  LDD2136  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C533(0.78)  LDD2140  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 16 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adenylate kinase 2, mitochondrial (AK2) Adenylate kinase family P54819
Histone-lysine N-methyltransferase SUV39H1 (SUV39H1) Histone-lysine methyltransferase family O43463
ATP-dependent RNA helicase DDX19B (DDX19B) DEAD box helicase family Q9UMR2
Deoxyribonuclease-1-like 1 (DNASE1L1) DNase I family P49184
Isocitrate dehydrogenase [NADP] cytoplasmic (IDH1) Isocitrate and isopropylmalate dehydrogenases family O75874
Dihydropyrimidinase-related protein 4 (DPYSL4) Hydantoinase/dihydropyrimidinase family O14531
Phospholipid phosphatase-related protein type 1 (PLPPR1) PA-phosphatase related phosphoesterase family Q8TBJ4
Ubiquitin carboxyl-terminal hydrolase 25 (USP25) Peptidase C19 family Q9UHP3
Kell blood group glycoprotein (KEL) Peptidase M13 family P23276
Kallikrein-8 (KLK8) Peptidase S1 family O60259
Proprotein convertase subtilisin/kexin type 7 (PCSK7) Peptidase S8 family Q16549
GPI mannosyltransferase 2 (PIGV) PIGV family Q9NUD9
26S proteasome non-ATPase regulatory subunit 2 (PSMD2) Proteasome subunit S2 family Q13200
Dolichyl-diphosphooligosaccharide--protein glycosyltransferase subunit STT3A (STT3A) STT3 family P46977
Tripartite motif-containing protein 43 (TRIM43) TRIM/RBCC family Q96BQ3
Ataxin-3 (ATXN3) . P54252
Transporter and channel
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Choline transporter-like protein 5 (SLC44A5) CTL (choline transporter-like) family Q8NCS7
Huntingtin (HTT) Huntingtin family P42858
Integrin alpha-V (ITGAV) Integrin alpha chain family P06756
Major facilitator superfamily domain-containing protein 10 (MFSD10) Major facilitator superfamily Q14728
Nuclear protein localization protein 4 homolog (NPLOC4) NPL4 family Q8TAT6
Peroxisome proliferator-activated receptor alpha (PPARA) Nuclear hormone receptor family Q07869
Cadherin-1 (CDH1) . P12830
Transcription factor
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein C-ets-2 (ETS2) ETS family P15036
Myoneurin (MYNN) Krueppel C2H2-type zinc-finger protein family Q9NPC7
Transcription factor Sp6 (SP6) Sp1 C2H2-type zinc-finger protein family Q3SY56
Transcriptional repressor protein YY1 (YY1) YY transcription factor family P25490
Myc proto-oncogene protein (MYC) . P01106
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transforming growth factor beta-1 proprotein (TGFB1) TGF-beta family P01137
Other
Click To Hide/Show 26 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ataxin-1 (ATXN1) ATXN1 family P54253
Death domain-associated protein 6 (DAXX) DAXX family Q9UER7
Large ribosomal subunit protein eL43 (RPL37A) Eukaryotic ribosomal protein eL43 family P61513
Protein VCF1 (VCF1) FAM104 family Q969W3
Guanine nucleotide-binding protein G(o) subunit alpha (GNAO1) G-alpha family P09471
Pre-mRNA-splicing factor ISY1 homolog (ISY1) ISY1 family Q9ULR0
Mediator of RNA polymerase II transcription subunit 12 (MED12) Mediator complex subunit 12 family Q93074
Neuronal membrane glycoprotein M6-a (GPM6A) Myelin proteolipid protein family P51674
Pleiotrophin (PTN) Pleiotrophin family P21246
RNA-binding protein 5 (RBM5) RBM5/RBM10 family P52756
Alpha-sarcoglycan (SGCA) Sarcoglycan alpha/epsilon family Q16586
T-complex protein 1 subunit zeta (CCT6A) TCP-1 chaperonin family P40227
Transforming growth factor beta-3 proprotein (TGFB3) TGF-beta family P10600
UPF0500 protein C1orf216 (C1orf216) UPF0500 family Q8TAB5
ADP-ribosylation factor GTPase-activating protein 3 (ARFGAP3) . Q9NP61
Bromo adjacent homology domain-containing 1 protein (BAHD1) . Q8TBE0
INO80 complex subunit C (INO80C) . Q6PI98
Killer cell lectin-like receptor subfamily G member 1 (KLRG1) . Q96E93
Kinetochore-associated protein NSL1 homolog (NSL1) . Q96IY1
Leucine-rich alpha-2-glycoprotein (LRG1) . P02750
Ligand of Numb protein X 2 (LNX2) . Q8N448
Mitochondrial antiviral-signaling protein (MAVS) . Q7Z434
Rab-interacting lysosomal protein (RILP) . Q96NA2
SERPINE1 mRNA-binding protein 1 (SERBP1) . Q8NC51
Signal peptide, CUB and EGF-like domain-containing protein 3 (SCUBE3) . Q8IX30
TRAF3-interacting JNK-activating modulator (TRAF3IP3) . Q9Y228

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Foreskin Fibroblast (Neonatal) . DB10770
Foreskin Keratinocyte (Neonatal) . DB10772
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tgf-br2 Mab Antibody D0P7KU
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ly2109761 Small molecular drug D06KKN
Pmid16539403c15b Small molecular drug D06BDC
Pmid23639540c13a Small molecular drug D0PP6Y
Pmid23639540c13d Small molecular drug D0F2MP

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 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.
3 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
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 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
6 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
7 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