Details of the Target

General Information of Target

Target ID LDTP05435
Target Name Activin receptor type-1 (ACVR1)
Gene Name ACVR1
Gene ID 90
Synonyms
ACVRLK2; Activin receptor type-1; EC 2.7.11.30; Activin receptor type I; ACTR-I; Activin receptor-like kinase 2; ALK-2; Serine/threonine-protein kinase receptor R1; SKR1; TGF-B superfamily receptor type I; TSR-I
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MVDGVMILPVLIMIALPSPSMEDEKPKVNPKLYMCVCEGLSCGNEDHCEGQQCFSSLSIN
DGFHVYQKGCFQVYEQGKMTCKTPPSPGQAVECCQGDWCNRNITAQLPTKGKSFPGTQNF
HLEVGLIILSVVFAVCLLACLLGVALRKFKRRNQERLNPRDVEYGTIEGLITTNVGDSTL
ADLLDHSCTSGSGSGLPFLVQRTVARQITLLECVGKGRYGEVWRGSWQGENVAVKIFSSR
DEKSWFRETELYNTVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTL
DTVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCCIADLGLAVM
HSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVDIWAFGLVLWEVARRMVS
NGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQRPNIPNRWFSDPTLTSLAKLMKECWYQ
NPSARLTALRIKKTLTKIDNSLDKLKTDC
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, TKL Ser/Thr protein kinase family, TGFB receptor subfamily
Subcellular location
Membrane
Function
Bone morphogenetic protein (BMP) type I receptor that is involved in a wide variety of biological processes, including bone, heart, cartilage, nervous, and reproductive system development and regulation. As a type I receptor, forms heterotetrameric receptor complexes with the type II receptors AMHR2, ACVR2A or ACVR2B. Upon binding of ligands such as BMP7 or GDF2/BMP9 to the heteromeric complexes, type II receptors transphosphorylate ACVR1 intracellular domain. In turn, ACVR1 kinase domain is activated and subsequently phosphorylates SMAD1/5/8 proteins that transduce the signal. In addition to its role in mediating BMP pathway-specific signaling, suppresses TGFbeta/activin pathway signaling by interfering with the binding of activin to its type II receptor. Besides canonical SMAD signaling, can activate non-canonical pathways such as p38 mitogen-activated protein kinases/MAPKs. May promote the expression of HAMP, potentially via its interaction with BMP6.
TTD ID
T12091
Uniprot ID
Q04771
DrugMap ID
TTJNBQA
Ensemble ID
ENST00000263640.7
HGNC ID
HGNC:171
ChEMBL ID
CHEMBL5903

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		12.56  LDD0402  [1]
IPM
 Probe Info  		N.A.  LDD0241  [2]
BTD
 Probe Info  		C449(0.82)  LDD2120  [3]
DBIA
 Probe Info  		C477(1.22)  LDD0531  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C477(1.22)  LDD0531  [4]
 LDCM0215  AC10 HEK-293T C449(0.96); C477(1.04); C213(1.04); C188(1.30)  LDD1508  [5]
 LDCM0226  AC11 HEK-293T C449(0.94); C477(0.82); C213(1.04); C188(0.96)  LDD1509  [5]
 LDCM0230  AC113 HCT 116 C477(2.16)  LDD0547  [4]
 LDCM0231  AC114 HCT 116 C477(0.84)  LDD0548  [4]
 LDCM0232  AC115 HCT 116 C477(1.42)  LDD0549  [4]
 LDCM0233  AC116 HCT 116 C477(1.44)  LDD0550  [4]
 LDCM0234  AC117 HCT 116 C477(1.08)  LDD0551  [4]
 LDCM0235  AC118 HCT 116 C477(1.55)  LDD0552  [4]
 LDCM0236  AC119 HCT 116 C477(1.29)  LDD0553  [4]
 LDCM0237  AC12 HEK-293T C449(0.95); C477(0.94); C213(1.09); C188(0.98)  LDD1510  [5]
 LDCM0238  AC120 HCT 116 C477(1.30)  LDD0555  [4]
 LDCM0239  AC121 HCT 116 C477(1.14)  LDD0556  [4]
 LDCM0240  AC122 HCT 116 C477(0.82)  LDD0557  [4]
 LDCM0241  AC123 HCT 116 C477(1.19)  LDD0558  [4]
 LDCM0242  AC124 HCT 116 C477(1.76)  LDD0559  [4]
 LDCM0243  AC125 HCT 116 C477(0.93)  LDD0560  [4]
 LDCM0244  AC126 HCT 116 C477(1.06)  LDD0561  [4]
 LDCM0245  AC127 HCT 116 C477(1.05)  LDD0562  [4]
 LDCM0259  AC14 HEK-293T C449(0.91); C477(1.14); C213(1.03); C188(1.00)  LDD1512  [5]
 LDCM0263  AC143 HCT 116 C477(0.66)  LDD0580  [4]
 LDCM0264  AC144 HCT 116 C477(1.04)  LDD0581  [4]
 LDCM0265  AC145 HCT 116 C477(1.37)  LDD0582  [4]
 LDCM0266  AC146 HCT 116 C477(1.51)  LDD0583  [4]
 LDCM0267  AC147 HCT 116 C477(1.89)  LDD0584  [4]
 LDCM0268  AC148 HCT 116 C477(3.37)  LDD0585  [4]
 LDCM0269  AC149 HCT 116 C477(1.25)  LDD0586  [4]
 LDCM0270  AC15 HEK-293T C449(0.95); C477(0.94); C213(1.00); C188(0.89)  LDD1513  [5]
 LDCM0271  AC150 HCT 116 C477(1.12)  LDD0588  [4]
 LDCM0272  AC151 HCT 116 C477(1.15)  LDD0589  [4]
 LDCM0273  AC152 HCT 116 C477(1.18)  LDD0590  [4]
 LDCM0274  AC153 HCT 116 C477(1.47)  LDD0591  [4]
 LDCM0621  AC154 HCT 116 C477(1.04)  LDD2158  [4]
 LDCM0622  AC155 HCT 116 C477(1.49)  LDD2159  [4]
 LDCM0623  AC156 HCT 116 C477(1.16)  LDD2160  [4]
 LDCM0624  AC157 HCT 116 C477(1.53)  LDD2161  [4]
 LDCM0276  AC17 HEK-293T C449(1.00); C477(0.86); C213(1.04); C188(0.89)  LDD1515  [5]
 LDCM0277  AC18 HEK-293T C449(0.98); C477(1.00); C213(1.01); C188(0.89)  LDD1516  [5]
 LDCM0278  AC19 HEK-293T C449(1.03); C477(0.94); C213(0.98); C188(0.73)  LDD1517  [5]
 LDCM0279  AC2 HCT 116 C477(1.21)  LDD0596  [4]
 LDCM0280  AC20 HEK-293T C449(1.00); C477(0.84); C213(0.97); C188(1.23)  LDD1519  [5]
 LDCM0281  AC21 HEK-293T C449(0.93); C477(0.96); C213(0.95); C188(0.87)  LDD1520  [5]
 LDCM0282  AC22 HEK-293T C449(0.81); C477(1.11); C213(1.00); C188(0.81)  LDD1521  [5]
 LDCM0283  AC23 HEK-293T C449(0.92); C477(0.96); C213(0.93); C188(0.88)  LDD1522  [5]
 LDCM0284  AC24 HEK-293T C449(0.98); C477(1.04); C213(1.05); C188(0.91)  LDD1523  [5]
 LDCM0285  AC25 HCT 116 C477(0.53)  LDD0602  [4]
 LDCM0286  AC26 HCT 116 C477(0.44)  LDD0603  [4]
 LDCM0287  AC27 HCT 116 C477(0.43)  LDD0604  [4]
 LDCM0288  AC28 HCT 116 C477(0.47)  LDD0605  [4]
 LDCM0289  AC29 HCT 116 C477(0.41)  LDD0606  [4]
 LDCM0290  AC3 HCT 116 C477(1.36)  LDD0607  [4]
 LDCM0291  AC30 HCT 116 C477(0.38)  LDD0608  [4]
 LDCM0292  AC31 HCT 116 C477(0.40)  LDD0609  [4]
 LDCM0293  AC32 HCT 116 C477(0.31)  LDD0610  [4]
 LDCM0294  AC33 HCT 116 C477(0.33)  LDD0611  [4]
 LDCM0295  AC34 HCT 116 C477(0.33)  LDD0612  [4]
 LDCM0296  AC35 HEK-293T C449(0.91); C477(0.90); C213(0.95); C188(0.81)  LDD1535  [5]
 LDCM0297  AC36 HEK-293T C449(1.02); C477(0.84); C213(0.98); C188(0.87)  LDD1536  [5]
 LDCM0298  AC37 HEK-293T C449(0.87); C477(1.01); C213(0.97); C188(1.03)  LDD1537  [5]
 LDCM0299  AC38 HEK-293T C449(0.97); C477(1.10); C213(0.96); C188(0.78)  LDD1538  [5]
 LDCM0300  AC39 HEK-293T C449(0.94); C477(0.91); C213(1.01); C188(0.97)  LDD1539  [5]
 LDCM0301  AC4 HCT 116 C477(1.31)  LDD0618  [4]
 LDCM0302  AC40 HEK-293T C449(0.97); C477(1.08); C213(1.09); C188(0.81)  LDD1541  [5]
 LDCM0303  AC41 HEK-293T C449(0.97); C477(0.73); C213(1.08); C188(1.10)  LDD1542  [5]
 LDCM0304  AC42 HEK-293T C449(0.96); C477(1.06); C213(1.11); C188(1.21)  LDD1543  [5]
 LDCM0305  AC43 HEK-293T C449(0.96); C477(1.09); C213(1.08); C188(0.97)  LDD1544  [5]
 LDCM0306  AC44 HEK-293T C449(0.96); C477(0.94); C213(1.05); C188(0.99)  LDD1545  [5]
 LDCM0307  AC45 HEK-293T C449(0.96); C477(0.95); C213(0.95); C188(1.07)  LDD1546  [5]
 LDCM0308  AC46 HEK-293T C449(0.93); C477(0.95); C213(1.04); C188(1.08)  LDD1547  [5]
 LDCM0309  AC47 HEK-293T C449(0.92); C477(0.93); C213(1.05); C188(0.80)  LDD1548  [5]
 LDCM0310  AC48 HEK-293T C449(0.99); C477(1.25); C213(1.04); C188(1.02)  LDD1549  [5]
 LDCM0311  AC49 HEK-293T C449(0.96); C477(0.93); C213(0.93); C188(1.10)  LDD1550  [5]
 LDCM0312  AC5 HCT 116 C477(1.28)  LDD0629  [4]
 LDCM0313  AC50 HEK-293T C449(0.98); C477(1.11); C213(1.06); C188(1.40)  LDD1552  [5]
 LDCM0314  AC51 HEK-293T C449(1.01); C477(0.84); C213(1.04); C188(0.69)  LDD1553  [5]
 LDCM0315  AC52 HEK-293T C449(0.95); C477(0.99); C213(0.99); C188(1.18)  LDD1554  [5]
 LDCM0316  AC53 HEK-293T C449(0.97); C477(0.92); C213(0.92); C188(1.65)  LDD1555  [5]
 LDCM0317  AC54 HEK-293T C449(0.94); C477(1.11); C213(0.99); C188(0.69)  LDD1556  [5]
 LDCM0318  AC55 HEK-293T C449(1.00); C477(0.88); C213(0.97); C188(0.90)  LDD1557  [5]
 LDCM0319  AC56 HEK-293T C449(0.99); C477(1.06); C213(1.03); C188(1.08)  LDD1558  [5]
 LDCM0320  AC57 HEK-293T C449(0.91); C477(0.69); C213(1.07); C188(0.87)  LDD1559  [5]
 LDCM0321  AC58 HEK-293T C449(0.93); C477(1.09); C213(1.07); C188(1.20)  LDD1560  [5]
 LDCM0322  AC59 HEK-293T C449(0.96); C477(1.07); C213(1.09); C188(0.85)  LDD1561  [5]
 LDCM0323  AC6 HEK-293T C449(0.90); C477(0.94); C213(1.03); C188(0.83)  LDD1562  [5]
 LDCM0324  AC60 HEK-293T C449(1.01); C477(0.92); C213(1.04); C188(1.35)  LDD1563  [5]
 LDCM0325  AC61 HEK-293T C449(0.93); C477(1.10); C213(1.01); C188(1.06)  LDD1564  [5]
 LDCM0326  AC62 HEK-293T C449(0.91); C477(1.04); C213(1.07); C188(0.94)  LDD1565  [5]
 LDCM0327  AC63 HEK-293T C449(0.96); C477(0.96); C213(1.07); C188(0.91)  LDD1566  [5]
 LDCM0328  AC64 HEK-293T C449(0.98); C477(1.14); C213(1.05); C188(1.24)  LDD1567  [5]
 LDCM0334  AC7 HEK-293T C449(0.95); C477(0.89); C213(1.01); C188(0.96)  LDD1568  [5]
 LDCM0345  AC8 HEK-293T C449(0.89); C477(1.08); C213(1.19); C188(0.91)  LDD1569  [5]
 LDCM0248  AKOS034007472 HEK-293T C449(0.94); C477(1.07); C213(1.02); C188(0.81)  LDD1511  [5]
 LDCM0356  AKOS034007680 HEK-293T C449(0.94); C477(0.76); C213(1.04); C188(0.97)  LDD1570  [5]
 LDCM0275  AKOS034007705 HEK-293T C449(0.96); C477(1.08); C213(1.09); C188(1.06)  LDD1514  [5]
 LDCM0156  Aniline NCI-H1299 11.36  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C477(1.03)  LDD2171  [4]
 LDCM0367  CL1 HEK-293T C449(0.98); C213(1.11); C188(0.81)  LDD1571  [5]
 LDCM0368  CL10 HEK-293T C449(1.02); C477(1.70); C213(1.35); C188(1.55)  LDD1572  [5]
 LDCM0369  CL100 HCT 116 C477(1.05)  LDD0686  [4]
 LDCM0370  CL101 HEK-293T C449(0.96); C213(1.01); C188(1.10)  LDD1574  [5]
 LDCM0371  CL102 HEK-293T C449(1.06); C477(1.03); C213(1.01); C188(1.46)  LDD1575  [5]
 LDCM0372  CL103 HEK-293T C449(0.99); C477(1.05); C213(0.97); C188(1.04)  LDD1576  [5]
 LDCM0373  CL104 HEK-293T C449(0.98); C477(0.95); C213(0.97); C188(1.29)  LDD1577  [5]
 LDCM0374  CL105 HEK-293T C449(1.01); C213(0.96); C188(1.24)  LDD1578  [5]
 LDCM0375  CL106 HEK-293T C449(0.95); C477(1.03); C213(0.97); C188(1.07)  LDD1579  [5]
 LDCM0376  CL107 HEK-293T C449(0.97); C477(1.03); C213(1.03); C188(1.27)  LDD1580  [5]
 LDCM0377  CL108 HEK-293T C449(0.96); C477(0.96); C213(0.87); C188(1.18)  LDD1581  [5]
 LDCM0378  CL109 HEK-293T C449(1.01); C213(0.97); C188(1.38)  LDD1582  [5]
 LDCM0379  CL11 HEK-293T C449(1.00); C477(0.99); C213(1.36); C188(1.10)  LDD1583  [5]
 LDCM0380  CL110 HEK-293T C449(0.92); C477(1.05); C213(1.01); C188(0.95)  LDD1584  [5]
 LDCM0381  CL111 HEK-293T C449(0.94); C477(0.85); C213(1.08); C188(0.93)  LDD1585  [5]
 LDCM0382  CL112 HCT 116 C477(0.58)  LDD0699  [4]
 LDCM0383  CL113 HCT 116 C477(0.35)  LDD0700  [4]
 LDCM0384  CL114 HCT 116 C477(0.50)  LDD0701  [4]
 LDCM0385  CL115 HCT 116 C477(0.38)  LDD0702  [4]
 LDCM0386  CL116 HCT 116 C477(0.39)  LDD0703  [4]
 LDCM0387  CL117 HEK-293T C449(1.04); C213(1.02); C188(1.13)  LDD1591  [5]
 LDCM0388  CL118 HEK-293T C449(0.96); C477(0.92); C213(1.04); C188(1.13)  LDD1592  [5]
 LDCM0389  CL119 HEK-293T C449(0.99); C477(0.88); C213(1.02); C188(1.04)  LDD1593  [5]
 LDCM0390  CL12 HEK-293T C449(0.98); C477(1.23); C213(1.34); C188(0.85)  LDD1594  [5]
 LDCM0391  CL120 HEK-293T C449(0.91); C477(0.87); C213(0.87); C188(1.22)  LDD1595  [5]
 LDCM0392  CL121 HEK-293T C449(1.01); C213(1.02); C188(0.81)  LDD1596  [5]
 LDCM0393  CL122 HEK-293T C449(0.95); C477(1.02); C213(1.09); C188(1.10)  LDD1597  [5]
 LDCM0394  CL123 HEK-293T C449(1.06); C477(0.96); C213(1.17); C188(0.98)  LDD1598  [5]
 LDCM0395  CL124 HEK-293T C449(0.95); C477(0.96); C213(1.04); C188(1.07)  LDD1599  [5]
 LDCM0396  CL125 HEK-293T C449(0.97); C213(1.08); C188(1.31)  LDD1600  [5]
 LDCM0397  CL126 HEK-293T C449(1.06); C477(0.93); C213(1.11); C188(0.83)  LDD1601  [5]
 LDCM0398  CL127 HEK-293T C449(0.98); C477(0.99); C213(1.19); C188(1.22)  LDD1602  [5]
 LDCM0399  CL128 HEK-293T C449(0.92); C477(0.95); C213(0.89); C188(1.38)  LDD1603  [5]
 LDCM0400  CL13 HEK-293T C449(1.04); C213(1.15); C188(1.01)  LDD1604  [5]
 LDCM0401  CL14 HEK-293T C449(0.97); C477(1.03); C213(1.06); C188(1.10)  LDD1605  [5]
 LDCM0402  CL15 HEK-293T C449(1.02); C477(1.18); C213(1.09); C188(0.99)  LDD1606  [5]
 LDCM0403  CL16 HEK-293T C449(0.95); C477(0.91); C213(0.86); C188(1.26)  LDD1607  [5]
 LDCM0404  CL17 HEK-293T C449(0.96); C477(1.62); C213(0.89); C188(1.07)  LDD1608  [5]
 LDCM0405  CL18 HEK-293T C449(0.97); C477(1.16); C213(1.03); C188(1.26)  LDD1609  [5]
 LDCM0406  CL19 HEK-293T C449(0.93); C477(0.91); C213(1.12); C188(0.90)  LDD1610  [5]
 LDCM0407  CL2 HEK-293T C449(0.94); C477(1.07); C213(1.08); C188(1.16)  LDD1611  [5]
 LDCM0408  CL20 HEK-293T C449(1.07); C477(1.13); C213(1.07); C188(1.09)  LDD1612  [5]
 LDCM0409  CL21 HEK-293T C449(0.98); C477(1.22); C213(1.14); C188(0.91)  LDD1613  [5]
 LDCM0410  CL22 HEK-293T C449(0.96); C477(1.24); C213(1.35); C188(1.32)  LDD1614  [5]
 LDCM0411  CL23 HEK-293T C449(1.01); C477(1.12); C213(1.26); C188(1.10)  LDD1615  [5]
 LDCM0412  CL24 HEK-293T C449(0.97); C477(1.38); C213(1.32); C188(1.09)  LDD1616  [5]
 LDCM0413  CL25 HEK-293T C449(1.00); C213(1.14); C188(1.12)  LDD1617  [5]
 LDCM0414  CL26 HEK-293T C449(1.01); C477(0.93); C213(1.00); C188(1.25)  LDD1618  [5]
 LDCM0415  CL27 HEK-293T C449(1.03); C477(0.95); C213(1.01); C188(1.14)  LDD1619  [5]
 LDCM0416  CL28 HEK-293T C449(0.96); C477(0.88); C213(1.09); C188(0.97)  LDD1620  [5]
 LDCM0417  CL29 HEK-293T C449(0.95); C477(1.47); C213(1.15); C188(1.39)  LDD1621  [5]
 LDCM0418  CL3 HEK-293T C449(0.99); C477(1.04); C213(0.94); C188(1.67)  LDD1622  [5]
 LDCM0419  CL30 HEK-293T C449(0.97); C477(1.12); C213(1.15); C188(1.16)  LDD1623  [5]
 LDCM0420  CL31 HCT 116 C477(0.39)  LDD0737  [4]
 LDCM0421  CL32 HCT 116 C477(0.81)  LDD0738  [4]
 LDCM0422  CL33 HCT 116 C477(0.43)  LDD0739  [4]
 LDCM0423  CL34 HCT 116 C477(0.31)  LDD0740  [4]
 LDCM0424  CL35 HCT 116 C477(0.26)  LDD0741  [4]
 LDCM0425  CL36 HCT 116 C477(0.27)  LDD0742  [4]
 LDCM0426  CL37 HCT 116 C477(0.27)  LDD0743  [4]
 LDCM0428  CL39 HCT 116 C477(0.36)  LDD0745  [4]
 LDCM0429  CL4 HEK-293T C449(1.02); C477(1.20); C213(1.09); C188(2.46)  LDD1633  [5]
 LDCM0430  CL40 HCT 116 C477(0.33)  LDD0747  [4]
 LDCM0431  CL41 HCT 116 C477(0.50)  LDD0748  [4]
 LDCM0432  CL42 HCT 116 C477(0.31)  LDD0749  [4]
 LDCM0433  CL43 HCT 116 C477(0.27)  LDD0750  [4]
 LDCM0434  CL44 HCT 116 C477(0.40)  LDD0751  [4]
 LDCM0435  CL45 HCT 116 C477(0.34)  LDD0752  [4]
 LDCM0436  CL46 HCT 116 C477(1.17)  LDD0753  [4]
 LDCM0437  CL47 HCT 116 C477(1.23)  LDD0754  [4]
 LDCM0438  CL48 HCT 116 C477(1.20)  LDD0755  [4]
 LDCM0439  CL49 HCT 116 C477(0.61)  LDD0756  [4]
 LDCM0440  CL5 HEK-293T C449(1.03); C477(1.10); C213(1.02); C188(0.85)  LDD1644  [5]
 LDCM0441  CL50 HCT 116 C477(1.11)  LDD0758  [4]
 LDCM0442  CL51 HCT 116 C477(1.35)  LDD0759  [4]
 LDCM0443  CL52 HCT 116 C477(0.91)  LDD0760  [4]
 LDCM0444  CL53 HCT 116 C477(0.90)  LDD0761  [4]
 LDCM0445  CL54 HCT 116 C477(1.24)  LDD0762  [4]
 LDCM0446  CL55 HCT 116 C477(1.13)  LDD0763  [4]
 LDCM0447  CL56 HCT 116 C477(0.80)  LDD0764  [4]
 LDCM0448  CL57 HCT 116 C477(1.12)  LDD0765  [4]
 LDCM0449  CL58 HCT 116 C477(0.99)  LDD0766  [4]
 LDCM0450  CL59 HCT 116 C477(0.89)  LDD0767  [4]
 LDCM0451  CL6 HEK-293T C449(0.97); C477(1.12); C213(1.17); C188(1.22)  LDD1654  [5]
 LDCM0452  CL60 HCT 116 C477(0.78)  LDD0769  [4]
 LDCM0453  CL61 HEK-293T C449(0.97); C213(1.09); C188(1.25)  LDD1656  [5]
 LDCM0454  CL62 HEK-293T C449(0.93); C477(0.90); C213(1.02); C188(1.16)  LDD1657  [5]
 LDCM0455  CL63 HEK-293T C449(1.00); C477(1.07); C213(1.03); C188(1.17)  LDD1658  [5]
 LDCM0456  CL64 HEK-293T C449(1.03); C477(1.21); C213(0.89); C188(1.32)  LDD1659  [5]
 LDCM0457  CL65 HEK-293T C449(0.90); C477(0.96); C213(0.89); C188(0.96)  LDD1660  [5]
 LDCM0458  CL66 HEK-293T C449(0.97); C477(1.13); C213(1.17); C188(1.26)  LDD1661  [5]
 LDCM0459  CL67 HEK-293T C449(1.00); C477(1.03); C213(1.08); C188(0.65)  LDD1662  [5]
 LDCM0460  CL68 HEK-293T C449(1.01); C477(1.07); C213(1.06); C188(1.15)  LDD1663  [5]
 LDCM0461  CL69 HEK-293T C449(0.97); C477(1.11); C213(1.06); C188(0.85)  LDD1664  [5]
 LDCM0462  CL7 HEK-293T C449(0.94); C477(0.92); C213(1.18); C188(1.00)  LDD1665  [5]
 LDCM0463  CL70 HEK-293T C449(0.84); C477(1.15); C213(1.20); C188(1.67)  LDD1666  [5]
 LDCM0464  CL71 HEK-293T C449(1.01); C477(1.06); C213(1.14); C188(0.89)  LDD1667  [5]
 LDCM0465  CL72 HEK-293T C449(0.93); C477(1.21); C213(1.19); C188(0.99)  LDD1668  [5]
 LDCM0466  CL73 HEK-293T C449(0.95); C213(1.03); C188(1.00)  LDD1669  [5]
 LDCM0467  CL74 HEK-293T C449(0.97); C477(0.87); C213(1.08); C188(1.04)  LDD1670  [5]
 LDCM0469  CL76 HEK-293T C449(0.94); C477(1.14); C213(1.11); C188(1.13)  LDD1672  [5]
 LDCM0470  CL77 HEK-293T C449(0.86); C477(0.94); C213(0.88); C188(1.13)  LDD1673  [5]
 LDCM0471  CL78 HEK-293T C449(0.95); C477(1.12); C213(1.07); C188(1.36)  LDD1674  [5]
 LDCM0472  CL79 HEK-293T C449(1.01); C477(0.98); C213(1.02); C188(0.90)  LDD1675  [5]
 LDCM0473  CL8 HEK-293T C449(1.08); C477(1.37); C213(1.45); C188(1.28)  LDD1676  [5]
 LDCM0474  CL80 HEK-293T C449(1.03); C477(1.07); C213(1.10); C188(1.13)  LDD1677  [5]
 LDCM0475  CL81 HEK-293T C449(0.94); C477(1.08); C213(1.06); C188(1.18)  LDD1678  [5]
 LDCM0476  CL82 HEK-293T C449(1.01); C477(1.06); C213(1.08); C188(0.83)  LDD1679  [5]
 LDCM0477  CL83 HEK-293T C449(1.05); C477(1.06); C213(1.20); C188(0.97)  LDD1680  [5]
 LDCM0478  CL84 HEK-293T C449(0.94); C477(1.22); C213(1.14); C188(1.04)  LDD1681  [5]
 LDCM0479  CL85 HEK-293T C449(1.01); C213(1.14); C188(1.47)  LDD1682  [5]
 LDCM0480  CL86 HEK-293T C449(1.15); C477(1.07); C213(1.16); C188(0.94)  LDD1683  [5]
 LDCM0481  CL87 HEK-293T C449(0.92); C477(1.10); C213(1.12); C188(1.35)  LDD1684  [5]
 LDCM0482  CL88 HEK-293T C449(0.90); C477(1.11); C213(1.00); C188(1.60)  LDD1685  [5]
 LDCM0483  CL89 HEK-293T C449(0.97); C477(1.03); C213(0.96); C188(0.96)  LDD1686  [5]
 LDCM0484  CL9 HEK-293T C449(0.94); C477(1.12); C213(1.14); C188(1.05)  LDD1687  [5]
 LDCM0485  CL90 HEK-293T C449(1.05); C477(1.25); C213(1.22); C188(1.25)  LDD1688  [5]
 LDCM0486  CL91 HCT 116 C477(1.24)  LDD0803  [4]
 LDCM0487  CL92 HCT 116 C477(1.06)  LDD0804  [4]
 LDCM0488  CL93 HCT 116 C477(0.95)  LDD0805  [4]
 LDCM0489  CL94 HCT 116 C477(0.99)  LDD0806  [4]
 LDCM0490  CL95 HCT 116 C477(1.50)  LDD0807  [4]
 LDCM0491  CL96 HCT 116 C477(1.35)  LDD0808  [4]
 LDCM0492  CL97 HCT 116 C477(1.31)  LDD0809  [4]
 LDCM0493  CL98 HCT 116 C477(1.41)  LDD0810  [4]
 LDCM0494  CL99 HCT 116 C477(1.31)  LDD0811  [4]
 LDCM0495  E2913 HEK-293T C449(0.96); C477(1.02); C213(1.24); C188(1.07)  LDD1698  [5]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C449(3.04)  LDD1702  [3]
 LDCM0468  Fragment33 HEK-293T C449(1.02); C477(1.00); C213(1.10); C188(1.28)  LDD1671  [5]
 LDCM0427  Fragment51 HCT 116 C477(0.43)  LDD0744  [4]
 LDCM0022  KB02 HEK-293T C449(0.90)  LDD1492  [5]
 LDCM0023  KB03 HEK-293T C449(0.95)  LDD1497  [5]
 LDCM0024  KB05 HMCB C213(2.78)  LDD3312  [6]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C449(0.82)  LDD2120  [3]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C449(0.93)  LDD2128  [3]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C449(0.81)  LDD2140  [3]
 LDCM0021  THZ1 HCT 116 C477(1.03)  LDD2173  [4]

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
Ephrin type-A receptor 6 (EPHA6) Tyr protein kinase family Q9UF33

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 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Incb00928 Small molecular drug D50OLM
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tp-0184 Small molecular drug DNI28K
Investigative
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atp Small molecular drug DB00171
Dorsomorphin Small molecular drug DB08597
Ldn-214117 Small molecular drug D06CMG
Ml347 Small molecular drug D0RF7O
Pmid23639540c13a Small molecular drug D0PP6Y
Pmid23639540c13d Small molecular drug D0F2MP
Pmid23639540c13r Small molecular drug D05NEC
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid27774822-compound-figure10compound12 Small molecular drug D0A8BV
Pmid27774822-compound-figure10compound4 Small molecular drug D0AE0M

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 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 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 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
5 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
6 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