Details of the Target

General Information of Target

Target ID LDTP03823
Target Name TGF-beta receptor type-1 (TGFBR1)
Gene Name TGFBR1
Gene ID 7046
Synonyms
ALK5; SKR4; TGF-beta receptor type-1; TGFR-1; EC 2.7.11.30; Activin A receptor type II-like protein kinase of 53kD; Activin receptor-like kinase 5; ALK-5; ALK5; Serine/threonine-protein kinase receptor R4; SKR4; TGF-beta type I receptor; Transforming growth factor-beta receptor type I; TGF-beta receptor type I; TbetaR-I
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE
TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG
LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER
SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS
ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI
HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA
ARLTALRIKKTLSQLSQQEGIKM
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, TGFB receptor subfamily
Subcellular location
Cell membrane
Function
Transmembrane serine/threonine kinase forming with the TGF-beta type II serine/threonine kinase receptor, TGFBR2, 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 is thus regulating 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 the 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. For instance, TGFBR1 induces TRAF6 autoubiquitination which in turn results in MAP3K7 ubiquitination and activation to trigger apoptosis. Also regulates epithelial to mesenchymal transition through a SMAD-independent signaling pathway through PARD6A phosphorylation and activation.
TTD ID
T53389
Uniprot ID
P36897
DrugMap ID
TTP4520
Ensemble ID
ENST00000374990.6
HGNC ID
HGNC:11772
ChEMBL ID
CHEMBL4439

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL27 SNV: p.N45S .
CALU1 SNV: p.R82T DBIA    Probe Info 
EGI1 Deletion: p.E228del .
HCC44 SNV: p.K449N .
JHH1 SNV: p.D363H .
LS513 SNV: p.D333H; p.R413Ter .
NCIH2172 SNV: p.Y295F .
RL952 SNV: p.P112L .
SNGM SNV: p.Y99Ter .
SW480 SNV: p.E447G .

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  		K490(1.60)  LDD0277  [1]
DBIA
 Probe Info  		C465(5.73)  LDD3336  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [3]
NAIA_4
 Probe Info  		N.A.  LDD2226  [4]
IPM
 Probe Info  		C461(0.00); C86(0.00); C446(0.00)  LDD0147  [5]
TFBX
 Probe Info  		N.A.  LDD0148  [5]
AOyne
 Probe Info  		14.50  LDD0443  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C461(0.97); C446(1.20); C86(1.02); C415(1.30)  LDD1507  [7]
 LDCM0215  AC10 HEK-293T C461(1.00); C446(1.18); C86(0.97); C106(1.05)  LDD1508  [7]
 LDCM0226  AC11 HEK-293T C461(0.99); C446(1.10); C86(1.05); C348(1.40)  LDD1509  [7]
 LDCM0237  AC12 HEK-293T C461(0.98); C86(1.00); C348(1.04)  LDD1510  [7]
 LDCM0259  AC14 HEK-293T C461(1.01); C446(1.19); C86(0.95); C348(0.96)  LDD1512  [7]
 LDCM0270  AC15 HEK-293T C461(1.02); C446(1.13); C86(0.99); C415(0.92)  LDD1513  [7]
 LDCM0276  AC17 HEK-293T C461(0.97); C446(1.11); C86(1.11); C415(1.10)  LDD1515  [7]
 LDCM0277  AC18 HEK-293T C461(1.03); C446(1.07); C86(1.02); C106(0.95)  LDD1516  [7]
 LDCM0278  AC19 HEK-293T C461(0.93); C446(1.07); C86(1.21); C348(1.32)  LDD1517  [7]
 LDCM0279  AC2 HEK-293T C461(0.98); C446(1.18); C86(0.97); C106(0.85)  LDD1518  [7]
 LDCM0280  AC20 HEK-293T C461(1.01); C86(0.99); C348(1.00)  LDD1519  [7]
 LDCM0281  AC21 HEK-293T C461(1.01); C446(1.08); C415(0.86); C348(1.04)  LDD1520  [7]
 LDCM0282  AC22 HEK-293T C461(0.98); C446(1.11); C86(0.95); C348(0.86)  LDD1521  [7]
 LDCM0283  AC23 HEK-293T C461(0.98); C446(1.13); C86(0.95); C415(1.39)  LDD1522  [7]
 LDCM0284  AC24 HEK-293T C461(1.03); C86(0.93); C415(1.15); C348(1.28)  LDD1523  [7]
 LDCM0285  AC25 HEK-293T C461(0.98); C446(1.25); C86(1.06); C415(1.20)  LDD1524  [7]
 LDCM0286  AC26 HEK-293T C461(0.98); C446(1.12); C86(0.96); C106(0.85)  LDD1525  [7]
 LDCM0287  AC27 HEK-293T C461(0.96); C446(1.09); C86(1.05); C348(0.93)  LDD1526  [7]
 LDCM0288  AC28 HEK-293T C461(1.02); C86(1.02); C348(1.15)  LDD1527  [7]
 LDCM0289  AC29 HEK-293T C461(1.01); C446(1.04); C415(1.01); C348(0.91)  LDD1528  [7]
 LDCM0290  AC3 HEK-293T C461(0.94); C446(1.09); C86(1.00); C348(1.13)  LDD1529  [7]
 LDCM0291  AC30 HEK-293T C461(0.97); C446(1.04); C86(1.03); C348(0.87)  LDD1530  [7]
 LDCM0292  AC31 HEK-293T C461(0.93); C446(1.07); C86(1.05); C415(1.22)  LDD1531  [7]
 LDCM0293  AC32 HEK-293T C461(0.92); C86(0.95); C415(1.26); C348(0.95)  LDD1532  [7]
 LDCM0294  AC33 HEK-293T C461(1.02); C446(1.16); C86(1.10); C415(1.78)  LDD1533  [7]
 LDCM0295  AC34 HEK-293T C461(0.96); C446(1.34); C86(0.97); C106(1.04)  LDD1534  [7]
 LDCM0296  AC35 HEK-293T C461(0.93); C446(1.07); C86(0.88); C348(1.13)  LDD1535  [7]
 LDCM0297  AC36 HEK-293T C461(1.04); C86(1.01); C348(1.09)  LDD1536  [7]
 LDCM0298  AC37 HEK-293T C461(1.02); C446(1.01); C415(0.94); C348(0.97)  LDD1537  [7]
 LDCM0299  AC38 HEK-293T C461(0.99); C446(1.10); C86(0.97); C348(0.84)  LDD1538  [7]
 LDCM0300  AC39 HEK-293T C461(0.98); C446(1.08); C86(0.98); C415(1.30)  LDD1539  [7]
 LDCM0301  AC4 HEK-293T C461(1.02); C86(1.06); C348(0.82)  LDD1540  [7]
 LDCM0302  AC40 HEK-293T C461(0.90); C86(0.96); C415(1.12); C348(1.01)  LDD1541  [7]
 LDCM0303  AC41 HEK-293T C461(1.03); C446(1.19); C86(1.13); C415(1.26)  LDD1542  [7]
 LDCM0304  AC42 HEK-293T C461(1.09); C446(1.22); C86(1.03); C106(0.97)  LDD1543  [7]
 LDCM0305  AC43 HEK-293T C461(0.98); C446(1.14); C86(1.00); C348(1.16)  LDD1544  [7]
 LDCM0306  AC44 HEK-293T C461(1.03); C86(1.01); C348(1.10)  LDD1545  [7]
 LDCM0307  AC45 HEK-293T C461(1.05); C446(1.09); C415(1.13); C348(1.01)  LDD1546  [7]
 LDCM0308  AC46 HEK-293T C461(0.89); C446(1.04); C86(0.90); C348(1.05)  LDD1547  [7]
 LDCM0309  AC47 HEK-293T C461(0.99); C446(1.12); C86(1.05); C415(1.33)  LDD1548  [7]
 LDCM0310  AC48 HEK-293T C461(0.95); C86(0.97); C415(1.47); C348(1.33)  LDD1549  [7]
 LDCM0311  AC49 HEK-293T C461(0.99); C446(1.14); C86(1.02); C415(1.46)  LDD1550  [7]
 LDCM0312  AC5 HEK-293T C461(0.95); C446(1.08); C415(0.84); C348(0.93)  LDD1551  [7]
 LDCM0313  AC50 HEK-293T C461(0.98); C446(1.23); C86(0.97); C106(1.08)  LDD1552  [7]
 LDCM0314  AC51 HEK-293T C461(0.96); C446(1.07); C86(0.93); C348(0.95)  LDD1553  [7]
 LDCM0315  AC52 HEK-293T C461(0.95); C86(1.01); C348(0.90)  LDD1554  [7]
 LDCM0316  AC53 HEK-293T C461(0.98); C446(1.03); C415(0.86); C348(1.03)  LDD1555  [7]
 LDCM0317  AC54 HEK-293T C461(0.98); C446(1.11); C86(0.95); C348(0.91)  LDD1556  [7]
 LDCM0318  AC55 HEK-293T C461(0.95); C446(1.03); C86(0.98); C415(0.99)  LDD1557  [7]
 LDCM0319  AC56 HEK-293T C461(0.94); C86(0.95); C415(1.23); C348(0.94)  LDD1558  [7]
 LDCM0320  AC57 HEK-293T C461(1.00); C446(1.20); C86(1.07); C415(1.04)  LDD1559  [7]
 LDCM0321  AC58 HEK-293T C461(0.96); C446(1.09); C86(1.03); C106(0.86)  LDD1560  [7]
 LDCM0322  AC59 HEK-293T C461(1.02); C446(1.10); C86(0.95); C348(1.04)  LDD1561  [7]
 LDCM0323  AC6 HEK-293T C461(0.94); C446(1.11); C86(1.06); C348(0.89)  LDD1562  [7]
 LDCM0324  AC60 HEK-293T C461(0.96); C86(1.01); C348(0.87)  LDD1563  [7]
 LDCM0325  AC61 HEK-293T C461(0.98); C446(1.12); C415(1.04); C348(1.00)  LDD1564  [7]
 LDCM0326  AC62 HEK-293T C461(0.94); C446(1.16); C86(1.01); C348(0.95)  LDD1565  [7]
 LDCM0327  AC63 HEK-293T C461(0.96); C446(1.13); C86(1.02); C415(0.83)  LDD1566  [7]
 LDCM0328  AC64 HEK-293T C461(1.00); C86(0.96); C415(1.16); C348(1.04)  LDD1567  [7]
 LDCM0334  AC7 HEK-293T C461(0.93); C446(1.13); C86(1.00); C415(0.69)  LDD1568  [7]
 LDCM0345  AC8 HEK-293T C461(0.90); C86(0.95); C415(1.47); C348(0.92)  LDD1569  [7]
 LDCM0248  AKOS034007472 HEK-293T C461(1.02); C446(1.03); C415(0.89); C348(0.96)  LDD1511  [7]
 LDCM0356  AKOS034007680 HEK-293T C461(1.00); C446(1.25); C86(1.08); C415(1.35)  LDD1570  [7]
 LDCM0275  AKOS034007705 HEK-293T C461(0.91); C86(0.87); C415(1.49); C348(0.96)  LDD1514  [7]
 LDCM0367  CL1 HEK-293T C461(1.09); C446(1.33); C86(0.94); C415(1.03)  LDD1571  [7]
 LDCM0368  CL10 HEK-293T C461(1.27); C446(0.95); C86(1.06); C348(0.72)  LDD1572  [7]
 LDCM0369  CL100 HEK-293T C461(1.03); C446(1.24)  LDD1573  [7]
 LDCM0370  CL101 HEK-293T C461(1.04); C446(1.20); C86(1.05); C415(1.11)  LDD1574  [7]
 LDCM0371  CL102 HEK-293T C461(1.19); C446(1.15); C415(1.03); C348(1.17)  LDD1575  [7]
 LDCM0372  CL103 HEK-293T C461(0.99); C446(1.21); C86(0.97); C415(1.20)  LDD1576  [7]
 LDCM0373  CL104 HEK-293T C461(1.09); C446(1.14)  LDD1577  [7]
 LDCM0374  CL105 HEK-293T C461(1.03); C446(1.16); C86(0.93); C415(0.83)  LDD1578  [7]
 LDCM0375  CL106 HEK-293T C461(1.14); C446(1.05); C415(0.98); C348(0.96)  LDD1579  [7]
 LDCM0376  CL107 HEK-293T C461(0.99); C446(1.04); C86(1.00); C415(0.85)  LDD1580  [7]
 LDCM0377  CL108 HEK-293T C461(1.07); C446(1.17)  LDD1581  [7]
 LDCM0378  CL109 HEK-293T C461(1.08); C446(1.08); C86(0.90); C415(1.08)  LDD1582  [7]
 LDCM0379  CL11 HEK-293T C461(1.28); C446(0.78); C86(1.00); C415(1.16)  LDD1583  [7]
 LDCM0380  CL110 HEK-293T C461(1.42); C446(1.18); C415(1.09); C348(0.97)  LDD1584  [7]
 LDCM0381  CL111 HEK-293T C461(1.08); C446(1.09); C86(0.96); C415(1.11)  LDD1585  [7]
 LDCM0382  CL112 HEK-293T C461(1.09); C446(1.43)  LDD1586  [7]
 LDCM0383  CL113 HEK-293T C461(0.98); C446(1.22); C86(0.88); C415(1.10)  LDD1587  [7]
 LDCM0384  CL114 HEK-293T C461(1.20); C446(1.22); C415(0.96); C348(1.00)  LDD1588  [7]
 LDCM0385  CL115 HEK-293T C461(1.01); C446(1.10); C86(0.92); C415(1.22)  LDD1589  [7]
 LDCM0386  CL116 HEK-293T C461(0.92); C446(1.31)  LDD1590  [7]
 LDCM0387  CL117 HEK-293T C461(0.99); C446(1.19); C86(0.92); C415(1.05)  LDD1591  [7]
 LDCM0388  CL118 HEK-293T C461(1.04); C446(1.05); C415(1.25); C348(1.00)  LDD1592  [7]
 LDCM0389  CL119 HEK-293T C461(1.00); C446(1.11); C86(0.93); C415(1.09)  LDD1593  [7]
 LDCM0390  CL12 HEK-293T C461(1.09); C86(1.09); C415(1.69); C348(0.79)  LDD1594  [7]
 LDCM0391  CL120 HEK-293T C461(0.95); C446(1.25)  LDD1595  [7]
 LDCM0392  CL121 HEK-293T C461(1.03); C446(1.25); C86(0.93); C415(1.00)  LDD1596  [7]
 LDCM0393  CL122 HEK-293T C461(1.06); C446(1.09); C415(1.16); C348(1.14)  LDD1597  [7]
 LDCM0394  CL123 HEK-293T C461(1.20); C446(1.02); C86(1.04); C415(1.02)  LDD1598  [7]
 LDCM0395  CL124 HEK-293T C461(1.15); C446(1.24)  LDD1599  [7]
 LDCM0396  CL125 HEK-293T C461(0.98); C446(1.25); C86(1.03); C415(0.83)  LDD1600  [7]
 LDCM0397  CL126 HEK-293T C461(1.01); C446(1.19); C415(1.05); C348(1.03)  LDD1601  [7]
 LDCM0398  CL127 HEK-293T C461(0.96); C446(1.17); C86(0.94); C415(0.88)  LDD1602  [7]
 LDCM0399  CL128 HEK-293T C461(0.96); C446(1.34)  LDD1603  [7]
 LDCM0400  CL13 HEK-293T C461(0.99); C446(1.40); C86(0.88); C415(1.03)  LDD1604  [7]
 LDCM0401  CL14 HEK-293T C461(1.03); C446(1.05); C415(1.04); C348(1.08)  LDD1605  [7]
 LDCM0402  CL15 HEK-293T C461(1.30); C446(1.11); C86(1.23); C415(0.74)  LDD1606  [7]
 LDCM0403  CL16 HEK-293T C461(1.04); C446(1.12)  LDD1607  [7]
 LDCM0404  CL17 HEK-293T C461(1.25); C446(1.17); C86(1.11); C415(1.42)  LDD1608  [7]
 LDCM0405  CL18 HEK-293T C461(0.99); C446(1.01); C86(0.95); C106(0.87)  LDD1609  [7]
 LDCM0406  CL19 HEK-293T C461(1.05); C446(0.95); C86(0.94); C348(1.00)  LDD1610  [7]
 LDCM0407  CL2 HEK-293T C461(1.01); C446(1.26); C415(1.06); C348(0.96)  LDD1611  [7]
 LDCM0408  CL20 HEK-293T C461(1.05); C86(1.05); C348(1.09)  LDD1612  [7]
 LDCM0409  CL21 HEK-293T C461(1.38); C446(0.83); C415(1.13); C348(1.02)  LDD1613  [7]
 LDCM0410  CL22 HEK-293T C461(1.12); C446(0.81); C86(0.99); C348(0.83)  LDD1614  [7]
 LDCM0411  CL23 HEK-293T C461(1.28); C446(0.70); C86(1.01); C415(1.34)  LDD1615  [7]
 LDCM0412  CL24 HEK-293T C461(1.01); C86(1.02); C415(1.69); C348(0.90)  LDD1616  [7]
 LDCM0413  CL25 HEK-293T C461(1.07); C446(1.29); C86(0.96); C415(0.90)  LDD1617  [7]
 LDCM0414  CL26 HEK-293T C461(1.00); C446(1.10); C415(0.93); C348(1.08)  LDD1618  [7]
 LDCM0415  CL27 HEK-293T C461(0.92); C446(1.08); C86(1.00); C415(1.13)  LDD1619  [7]
 LDCM0416  CL28 HEK-293T C461(1.01); C446(1.13)  LDD1620  [7]
 LDCM0417  CL29 HEK-293T C461(0.94); C446(1.04); C86(1.02); C415(1.13)  LDD1621  [7]
 LDCM0418  CL3 HEK-293T C461(1.02); C446(1.17); C86(1.09); C415(1.11)  LDD1622  [7]
 LDCM0419  CL30 HEK-293T C461(0.97); C446(0.98); C86(0.97); C106(0.92)  LDD1623  [7]
 LDCM0420  CL31 HEK-293T C461(1.04); C446(0.92); C86(1.08); C348(1.31)  LDD1624  [7]
 LDCM0421  CL32 HEK-293T C461(1.09); C86(1.10); C348(0.94)  LDD1625  [7]
 LDCM0422  CL33 HEK-293T C461(1.29); C446(0.83); C415(1.16); C348(1.06)  LDD1626  [7]
 LDCM0423  CL34 HEK-293T C461(1.12); C446(0.78); C86(1.05); C348(0.90)  LDD1627  [7]
 LDCM0424  CL35 HEK-293T C461(1.15); C446(0.75); C86(1.05); C415(1.09)  LDD1628  [7]
 LDCM0425  CL36 HEK-293T C461(1.14); C86(1.04); C415(1.55); C348(0.91)  LDD1629  [7]
 LDCM0426  CL37 HEK-293T C461(1.09); C446(1.23); C86(0.87); C415(1.11)  LDD1630  [7]
 LDCM0428  CL39 HEK-293T C461(1.04); C446(1.15); C86(1.11); C415(1.17)  LDD1632  [7]
 LDCM0429  CL4 HEK-293T C461(1.13); C446(1.11)  LDD1633  [7]
 LDCM0430  CL40 HEK-293T C461(1.00); C446(1.17)  LDD1634  [7]
 LDCM0431  CL41 HEK-293T C461(1.18); C446(1.04); C86(1.14); C415(1.24)  LDD1635  [7]
 LDCM0432  CL42 HEK-293T C461(1.05); C446(0.82); C86(0.92); C106(0.94)  LDD1636  [7]
 LDCM0433  CL43 HEK-293T C461(1.01); C446(0.88); C86(0.98); C348(1.19)  LDD1637  [7]
 LDCM0434  CL44 HEK-293T C461(1.11); C86(1.08); C348(0.92)  LDD1638  [7]
 LDCM0435  CL45 HEK-293T C461(1.26); C446(0.88); C415(1.34); C348(1.17)  LDD1639  [7]
 LDCM0436  CL46 HEK-293T C461(1.23); C446(0.83); C86(1.10); C348(0.83)  LDD1640  [7]
 LDCM0437  CL47 HEK-293T C461(1.21); C446(0.81); C86(1.11); C415(1.15)  LDD1641  [7]
 LDCM0438  CL48 HEK-293T C461(1.11); C86(1.01); C415(1.52); C348(0.71)  LDD1642  [7]
 LDCM0439  CL49 HEK-293T C461(0.99); C446(1.28); C86(0.94); C415(0.82)  LDD1643  [7]
 LDCM0440  CL5 HEK-293T C461(1.00); C446(1.15); C86(1.08); C415(1.34)  LDD1644  [7]
 LDCM0441  CL50 HEK-293T C461(1.01); C446(1.15); C415(1.12); C348(1.01)  LDD1645  [7]
 LDCM0443  CL52 HEK-293T C461(1.12); C446(1.17)  LDD1646  [7]
 LDCM0444  CL53 HEK-293T C461(1.36); C446(1.15); C86(1.21); C415(1.15)  LDD1647  [7]
 LDCM0445  CL54 HEK-293T C461(1.13); C446(0.96); C86(0.96); C106(0.89)  LDD1648  [7]
 LDCM0446  CL55 HEK-293T C461(1.03); C446(0.91); C86(0.96); C348(0.98)  LDD1649  [7]
 LDCM0447  CL56 HEK-293T C461(1.01); C86(1.04); C348(0.93)  LDD1650  [7]
 LDCM0448  CL57 HEK-293T C461(1.18); C446(0.92); C415(1.09); C348(0.91)  LDD1651  [7]
 LDCM0449  CL58 HEK-293T C461(0.98); C446(0.77); C86(0.98); C348(0.95)  LDD1652  [7]
 LDCM0450  CL59 HEK-293T C461(1.25); C446(0.69); C86(1.12); C415(1.11)  LDD1653  [7]
 LDCM0451  CL6 HEK-293T C461(1.31); C446(1.10); C86(1.01); C106(0.91)  LDD1654  [7]
 LDCM0452  CL60 HEK-293T C461(1.30); C86(0.93); C415(2.40); C348(0.94)  LDD1655  [7]
 LDCM0453  CL61 HEK-293T C461(0.93); C446(1.23); C86(0.95); C415(0.79)  LDD1656  [7]
 LDCM0454  CL62 HEK-293T C461(1.03); C446(1.12); C415(1.09); C348(0.97)  LDD1657  [7]
 LDCM0455  CL63 HEK-293T C461(0.92); C446(1.06); C86(0.96); C415(1.09)  LDD1658  [7]
 LDCM0456  CL64 HEK-293T C461(1.24); C446(1.16)  LDD1659  [7]
 LDCM0457  CL65 HEK-293T C461(0.99); C446(1.11); C86(1.09); C415(1.34)  LDD1660  [7]
 LDCM0458  CL66 HEK-293T C461(1.09); C446(1.07); C86(1.03); C106(1.03)  LDD1661  [7]
 LDCM0459  CL67 HEK-293T C461(1.01); C446(0.93); C86(0.98); C348(1.04)  LDD1662  [7]
 LDCM0460  CL68 HEK-293T C461(1.12); C86(1.10); C348(1.07)  LDD1663  [7]
 LDCM0461  CL69 HEK-293T C461(1.12); C446(0.81); C415(1.35); C348(1.04)  LDD1664  [7]
 LDCM0462  CL7 HEK-293T C461(1.05); C446(0.85); C86(0.93); C348(1.08)  LDD1665  [7]
 LDCM0463  CL70 HEK-293T C461(0.99); C446(0.75); C86(0.94); C348(0.93)  LDD1666  [7]
 LDCM0464  CL71 HEK-293T C461(1.12); C446(0.72); C86(1.07); C415(1.28)  LDD1667  [7]
 LDCM0465  CL72 HEK-293T C461(1.07); C86(1.00); C415(1.58); C348(1.34)  LDD1668  [7]
 LDCM0466  CL73 HEK-293T C461(1.13); C446(1.40); C86(0.91); C415(1.04)  LDD1669  [7]
 LDCM0467  CL74 HEK-293T C461(1.06); C446(1.15); C415(0.96); C348(0.96)  LDD1670  [7]
 LDCM0469  CL76 HEK-293T C461(1.01); C446(1.27)  LDD1672  [7]
 LDCM0470  CL77 HEK-293T C461(1.37); C446(1.15); C86(1.05); C415(1.19)  LDD1673  [7]
 LDCM0471  CL78 HEK-293T C461(1.05); C446(1.08); C86(0.95); C106(0.99)  LDD1674  [7]
 LDCM0472  CL79 HEK-293T C461(1.01); C446(0.99); C86(1.02); C348(1.04)  LDD1675  [7]
 LDCM0473  CL8 HEK-293T C461(1.48); C86(1.29); C348(0.98)  LDD1676  [7]
 LDCM0474  CL80 HEK-293T C461(1.10); C86(1.04); C348(1.16)  LDD1677  [7]
 LDCM0475  CL81 HEK-293T C461(1.07); C446(0.85); C415(1.41); C348(1.11)  LDD1678  [7]
 LDCM0476  CL82 HEK-293T C461(1.04); C446(0.85); C86(0.97); C348(0.77)  LDD1679  [7]
 LDCM0477  CL83 HEK-293T C461(1.19); C446(0.80); C86(1.09); C415(1.19)  LDD1680  [7]
 LDCM0478  CL84 HEK-293T C461(1.12); C86(1.08); C415(1.47); C348(0.80)  LDD1681  [7]
 LDCM0479  CL85 HEK-293T C461(0.99); C446(1.37); C86(0.90); C415(0.80)  LDD1682  [7]
 LDCM0480  CL86 HEK-293T C461(1.04); C446(1.21); C415(0.97); C348(0.99)  LDD1683  [7]
 LDCM0481  CL87 HEK-293T C461(1.06); C446(1.27); C86(0.98); C415(1.36)  LDD1684  [7]
 LDCM0482  CL88 HEK-293T C461(1.03); C446(1.26)  LDD1685  [7]
 LDCM0483  CL89 HEK-293T C461(1.07); C446(1.23); C86(1.10); C415(1.12)  LDD1686  [7]
 LDCM0484  CL9 HEK-293T C461(1.19); C446(0.83); C415(1.36); C348(1.09)  LDD1687  [7]
 LDCM0485  CL90 HEK-293T C461(1.52); C446(1.22); C86(1.06); C106(0.97)  LDD1688  [7]
 LDCM0486  CL91 HEK-293T C461(1.10); C446(0.99); C86(1.03); C348(1.20)  LDD1689  [7]
 LDCM0487  CL92 HEK-293T C461(1.23); C86(1.05); C348(1.31)  LDD1690  [7]
 LDCM0488  CL93 HEK-293T C461(1.21); C446(0.94); C415(1.52); C348(1.14)  LDD1691  [7]
 LDCM0489  CL94 HEK-293T C461(1.02); C446(0.82); C86(0.92); C348(0.91)  LDD1692  [7]
 LDCM0490  CL95 HEK-293T C461(1.25); C446(1.00); C86(1.22); C415(1.01)  LDD1693  [7]
 LDCM0491  CL96 HEK-293T C461(1.21); C86(1.04); C415(1.29); C348(0.86)  LDD1694  [7]
 LDCM0492  CL97 HEK-293T C461(1.14); C446(1.19); C86(0.95); C415(0.99)  LDD1695  [7]
 LDCM0493  CL98 HEK-293T C461(1.12); C446(1.10); C415(0.99); C348(1.08)  LDD1696  [7]
 LDCM0494  CL99 HEK-293T C461(0.95); C446(1.14); C86(1.05); C415(1.20)  LDD1697  [7]
 LDCM0495  E2913 HEK-293T C461(0.91); C446(1.12); C86(1.07); C415(1.11)  LDD1698  [7]
 LDCM0468  Fragment33 HEK-293T C461(1.06); C446(1.08); C86(0.92); C415(1.17)  LDD1671  [7]
 LDCM0427  Fragment51 HEK-293T C461(1.06); C446(1.13); C415(0.89); C348(0.90)  LDD1631  [7]
 LDCM0022  KB02 HEK-293T C86(0.96); C461(0.80); C415(0.89)  LDD1492  [7]
 LDCM0023  KB03 HEK-293T C86(1.00); C461(0.96); C415(0.73)  LDD1497  [7]
 LDCM0024  KB05 MONO-MAC-6 C465(5.73)  LDD3336  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Peptidyl-prolyl cis-trans isomerase FKBP1A (FKBP1A) FKBP-type PPIase family P62942
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
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 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Leucine-rich alpha-2-glycoprotein (LRG1) . P02750

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ly2157299 Small molecular drug D06TFI
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Metelimumab Antibody D06FAA
Tew-7197 . D0MR0B
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pf-06952229 Small molecular drug DQ5Y6Z
Tp-0184 Small molecular drug DNI28K
Ly3200882 . D06BGZ
P-2745 . D02USG
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sb-431542 Small molecular drug D0C7WP
Investigative
Click To Hide/Show 28 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
2-phenyl-n-(Pyridin-4-yl)Quinazolin-4-amine Small molecular drug D0V3OJ
4-(3-pyridin-2-yl-1h-pyrazol-4-yl)Quinoline Small molecular drug DB03921
4-pyridin-2-yl-5-quinolin-2-yl-thiazol-2-ylamine Small molecular drug D07ZMW
4-pyridin-2-yl-5-quinolin-4-yl-thiazol-2-ylamine Small molecular drug D0XL7C
4-pyridin-3-yl-5-quinolin-4-yl-thiazol-2-ylamine Small molecular drug D0H5CE
5''-quinolin-4-yl-[2,4'bithiazolyl-2''-ylamine Small molecular drug D05BMP
Gw-788388 Small molecular drug D0C3AD
Hts-466284 Small molecular drug D0XB4P
In-1130 Small molecular drug D0K6YK
In-1166 Small molecular drug D0H6ZP
Ldn-214117 Small molecular drug D06CMG
Ly2109761 Small molecular drug D06KKN
Pmid16539403c15b Small molecular drug D06BDC
Pmid23639540c13d Small molecular drug D0F2MP
Pmid23639540c13r Small molecular drug D05NEC
Sb-505124 Small molecular drug D0Q5UH
Sb-525334 Small molecular drug D03ANS
Sd-208 Small molecular drug D0V8AC
2-(6-methylpyridin-2-yl)-n-pyridin-4-ylquinazolin-4-amine . DB07267
3-(4-fluorophenyl)-2-(6-methylpyridin-2-yl)-56-dihydro-4h-pyrrolo[12-b]Pyrazole . DB04480
Ace-435 . D0S5TT
Drp-049 . D0I4VX
N-1h-indazol-5-yl-2-(6-methylpyridin-2-yl)Quinazolin-4-amine . DB08450
N-[4-(5-fluoro-6-methylpyridin-2-yl)-5-quinoxalin-6-yl-1h-imidazol-2-yl]Acetamide . DB07152
Naphthyridine Inhibitor . DB04434
Ptl-101 . D0J6JC
Tgf-beta Shield . D0QJ4Y
Wilvent . D00ZFC
Discontinued
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lf-984 . D0ID0R
Sm-16 . D0I4LB

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 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
4 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
5 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
6 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.
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