Details of the Target

General Information of Target

Target ID LDTP05537
Target Name Activated CDC42 kinase 1 (TNK2)
Gene Name TNK2
Gene ID 10188
Synonyms
ACK1; Activated CDC42 kinase 1; ACK-1; EC 2.7.10.2; EC 2.7.11.1; Tyrosine kinase non-receptor protein 2
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MQPEEGTGWLLELLSEVQLQQYFLRLRDDLNVTRLSHFEYVKNEDLEKIGMGRPGQRRLW
EAVKRRKALCKRKSWMSKVFSGKRLEAEFPPHHSQSTFRKTSPAPGGPAGEGPLQSLTCL
IGEKDLRLLEKLGDGSFGVVRRGEWDAPSGKTVSVAVKCLKPDVLSQPEAMDDFIREVNA
MHSLDHRNLIRLYGVVLTPPMKMVTELAPLGSLLDRLRKHQGHFLLGTLSRYAVQVAEGM
GYLESKRFIHRDLAARNLLLATRDLVKIGDFGLMRALPQNDDHYVMQEHRKVPFAWCAPE
SLKTRTFSHASDTWMFGVTLWEMFTYGQEPWIGLNGSQILHKIDKEGERLPRPEDCPQDI
YNVMVQCWAHKPEDRPTFVALRDFLLEAQPTDMRALQDFEEPDKLHIQMNDVITVIEGRA
ENYWWRGQNTRTLCVGPFPRNVVTSVAGLSAQDISQPLQNSFIHTGHGDSDPRHCWGFPD
RIDELYLGNPMDPPDLLSVELSTSRPPQHLGGVKKPTYDPVSEDQDPLSSDFKRLGLRKP
GLPRGLWLAKPSARVPGTKASRGSGAEVTLIDFGEEPVVPALRPCAPSLAQLAMDACSLL
DETPPQSPTRALPRPLHPTPVVDWDARPLPPPPAYDDVAQDEDDFEICSINSTLVGAGVP
AGPSQGQTNYAFVPEQARPPPPLEDNLFLPPQGGGKPPSSAQTAEIFQALQQECMRQLQA
PAGSPAPSPSPGGDDKPQVPPRVPIPPRPTRPHVQLSPAPPGEEETSQWPGPASPPRVPP
REPLSPQGSRTPSPLVPPGSSPLPPRLSSSPGKTMPTTQSFASDPKYATPQVIQAPGPRA
GPCILPIVRDGKKVSSTHYYLLPERPSYLERYQRFLREAQSPEEPTPLPVPLLLPPPSTP
APAAPTATVRPMPQAALDPKANFSTNNSNPGARPPPPRATARLPQRGCPGDGPEAGRPAD
KIQMAMVHGVTTEECQAALQCHGWSVQRAAQYLKVEQLFGLGLRPRGECHKVLEMFDWNL
EQAGCHLLGSWGPAHHKR
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family
Subcellular location
Cell membrane
Function
Non-receptor tyrosine-protein and serine/threonine-protein kinase that is implicated in cell spreading and migration, cell survival, cell growth and proliferation. Transduces extracellular signals to cytosolic and nuclear effectors. Phosphorylates AKT1, AR, MCF2, WASL and WWOX. Implicated in trafficking and clathrin-mediated endocytosis through binding to epidermal growth factor receptor (EGFR) and clathrin. Binds to both poly- and mono-ubiquitin and regulates ligand-induced degradation of EGFR, thereby contributing to the accumulation of EGFR at the limiting membrane of early endosomes. Downstream effector of CDC42 which mediates CDC42-dependent cell migration via phosphorylation of BCAR1. May be involved both in adult synaptic function and plasticity and in brain development. Activates AKT1 by phosphorylating it on 'Tyr-176'. Phosphorylates AR on 'Tyr-267' and 'Tyr-363' thereby promoting its recruitment to androgen-responsive enhancers (AREs). Phosphorylates WWOX on 'Tyr-287'. Phosphorylates MCF2, thereby enhancing its activity as a guanine nucleotide exchange factor (GEF) toward Rho family proteins. Contributes to the control of AXL receptor levels. Confers metastatic properties on cancer cells and promotes tumor growth by negatively regulating tumor suppressor such as WWOX and positively regulating pro-survival factors such as AKT1 and AR. Phosphorylates WASP.
TTD ID
T63220
Uniprot ID
Q07912
DrugMap ID
TTIET93
Ensemble ID
ENST00000333602.14
HGNC ID
HGNC:19297
ChEMBL ID
CHEMBL4599

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
DBIA
 Probe Info  		C882(4.33); C458(2.21)  LDD3311  [1]
BTD
 Probe Info  		C159(1.18)  LDD1700  [2]
IA-alkyne
 Probe Info  		C843(5.80)  LDD1703  [3]
NAIA_4
 Probe Info  		N.A.  LDD2226  [4]
NAIA_5
 Probe Info  		N.A.  LDD2225  [4]
IPM
 Probe Info  		C434(0.00); C843(0.00)  LDD0147  [5]
TFBX
 Probe Info  		N.A.  LDD0148  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C159(0.90)  LDD2095  [2]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C159(1.12)  LDD2117  [2]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C159(1.06)  LDD2152  [2]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C159(0.66)  LDD2132  [2]
 LDCM0214  AC1 HEK-293T C434(1.00); C843(1.20); C159(0.91); C948(1.14)  LDD1507  [6]
 LDCM0215  AC10 HEK-293T C434(0.99); C843(0.86); C159(1.07)  LDD1508  [6]
 LDCM0226  AC11 HEK-293T C434(0.99); C843(0.90)  LDD1509  [6]
 LDCM0237  AC12 HEK-293T C843(1.04); C159(1.11); C948(1.06)  LDD1510  [6]
 LDCM0259  AC14 HEK-293T C434(0.83); C843(1.16); C948(0.91)  LDD1512  [6]
 LDCM0270  AC15 HEK-293T C434(1.39); C843(1.17); C948(0.79)  LDD1513  [6]
 LDCM0276  AC17 HEK-293T C434(0.88); C843(1.19); C159(1.02); C948(1.21)  LDD1515  [6]
 LDCM0277  AC18 HEK-293T C434(1.08); C843(1.41); C159(1.13)  LDD1516  [6]
 LDCM0278  AC19 HEK-293T C434(1.38); C843(1.21)  LDD1517  [6]
 LDCM0279  AC2 HEK-293T C434(1.23); C843(0.80); C159(1.25)  LDD1518  [6]
 LDCM0280  AC20 HEK-293T C843(1.06); C159(1.08); C948(1.00)  LDD1519  [6]
 LDCM0281  AC21 HEK-293T C434(0.73); C843(0.84); C159(0.98); C948(0.91)  LDD1520  [6]
 LDCM0282  AC22 HEK-293T C434(0.83); C843(0.72); C948(0.82)  LDD1521  [6]
 LDCM0283  AC23 HEK-293T C434(1.06); C843(1.10); C948(1.08)  LDD1522  [6]
 LDCM0284  AC24 HEK-293T C434(0.88); C843(1.08); C948(0.95)  LDD1523  [6]
 LDCM0285  AC25 HEK-293T C434(0.97); C843(1.13); C159(0.94); C948(1.10)  LDD1524  [6]
 LDCM0286  AC26 HEK-293T C434(1.00); C843(1.16); C159(0.93)  LDD1525  [6]
 LDCM0287  AC27 HEK-293T C434(1.02); C843(1.13)  LDD1526  [6]
 LDCM0288  AC28 HEK-293T C843(1.07); C159(0.95); C948(1.00)  LDD1527  [6]
 LDCM0289  AC29 HEK-293T C434(0.84); C843(1.06); C159(0.81); C948(1.09)  LDD1528  [6]
 LDCM0290  AC3 HEK-293T C434(0.89); C843(1.03)  LDD1529  [6]
 LDCM0291  AC30 HEK-293T C434(1.04); C843(1.19); C948(1.08)  LDD1530  [6]
 LDCM0292  AC31 HEK-293T C434(1.15); C843(0.96); C948(0.95)  LDD1531  [6]
 LDCM0293  AC32 HEK-293T C434(0.97); C843(0.77); C948(1.00)  LDD1532  [6]
 LDCM0294  AC33 HEK-293T C434(0.89); C843(1.10); C159(0.82); C948(1.34)  LDD1533  [6]
 LDCM0295  AC34 HEK-293T C434(1.11); C843(1.09); C159(0.95)  LDD1534  [6]
 LDCM0296  AC35 HEK-293T C434(0.87); C843(1.15)  LDD1535  [6]
 LDCM0297  AC36 HEK-293T C843(1.11); C159(1.18); C948(0.92)  LDD1536  [6]
 LDCM0298  AC37 HEK-293T C434(1.02); C843(1.01); C159(0.97); C948(1.09)  LDD1537  [6]
 LDCM0299  AC38 HEK-293T C434(1.29); C843(1.03); C948(0.79)  LDD1538  [6]
 LDCM0300  AC39 HEK-293T C434(1.01); C843(1.15); C948(1.04)  LDD1539  [6]
 LDCM0301  AC4 HEK-293T C843(1.01); C159(0.98); C948(0.92)  LDD1540  [6]
 LDCM0302  AC40 HEK-293T C434(1.20); C843(0.79); C948(1.12)  LDD1541  [6]
 LDCM0303  AC41 HEK-293T C434(0.90); C843(1.43); C159(0.83); C948(1.19)  LDD1542  [6]
 LDCM0304  AC42 HEK-293T C434(0.80); C843(1.17); C159(1.11)  LDD1543  [6]
 LDCM0305  AC43 HEK-293T C434(1.00); C843(1.03)  LDD1544  [6]
 LDCM0306  AC44 HEK-293T C843(0.92); C159(1.15); C948(0.93)  LDD1545  [6]
 LDCM0307  AC45 HEK-293T C434(1.02); C843(1.00); C159(0.93); C948(1.15)  LDD1546  [6]
 LDCM0308  AC46 HEK-293T C434(0.95); C843(0.97); C948(0.95)  LDD1547  [6]
 LDCM0309  AC47 HEK-293T C434(1.06); C843(1.13); C948(0.70)  LDD1548  [6]
 LDCM0310  AC48 HEK-293T C434(1.10); C843(1.09); C948(0.94)  LDD1549  [6]
 LDCM0311  AC49 HEK-293T C434(1.10); C843(1.01); C159(0.96); C948(1.09)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C434(0.83); C843(0.81); C159(1.05); C948(1.05)  LDD1551  [6]
 LDCM0313  AC50 HEK-293T C434(1.05); C843(1.02); C159(1.08)  LDD1552  [6]
 LDCM0314  AC51 HEK-293T C434(1.00); C843(0.90)  LDD1553  [6]
 LDCM0315  AC52 HEK-293T C843(1.23); C159(1.15); C948(1.11)  LDD1554  [6]
 LDCM0316  AC53 HEK-293T C434(1.16); C843(1.22); C159(0.98); C948(1.07)  LDD1555  [6]
 LDCM0317  AC54 HEK-293T C434(0.82); C843(1.03); C948(0.90)  LDD1556  [6]
 LDCM0318  AC55 HEK-293T C434(0.92); C843(1.21); C948(0.87)  LDD1557  [6]
 LDCM0319  AC56 HEK-293T C434(0.82); C843(0.95); C948(1.00)  LDD1558  [6]
 LDCM0320  AC57 HEK-293T C434(0.87); C843(1.12); C159(1.05); C948(1.15)  LDD1559  [6]
 LDCM0321  AC58 HEK-293T C434(1.46); C843(1.10); C159(1.07)  LDD1560  [6]
 LDCM0322  AC59 HEK-293T C434(0.81); C843(1.08)  LDD1561  [6]
 LDCM0323  AC6 HEK-293T C434(0.92); C843(0.94); C948(1.04)  LDD1562  [6]
 LDCM0324  AC60 HEK-293T C843(1.12); C159(1.15); C948(0.94)  LDD1563  [6]
 LDCM0325  AC61 HEK-293T C434(1.07); C843(0.78); C159(1.09); C948(0.95)  LDD1564  [6]
 LDCM0326  AC62 HEK-293T C434(0.94); C843(0.91); C948(0.91)  LDD1565  [6]
 LDCM0327  AC63 HEK-293T C434(0.96); C843(0.98); C948(0.81)  LDD1566  [6]
 LDCM0328  AC64 HEK-293T C434(0.92); C843(0.80); C948(0.95)  LDD1567  [6]
 LDCM0334  AC7 HEK-293T C434(1.14); C843(1.00); C948(0.89)  LDD1568  [6]
 LDCM0345  AC8 HEK-293T C434(1.20); C843(1.08); C948(1.07)  LDD1569  [6]
 LDCM0520  AKOS000195272 MDA-MB-231 C159(1.05)  LDD2113  [2]
 LDCM0248  AKOS034007472 HEK-293T C434(0.98); C843(1.59); C159(1.18); C948(1.07)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C434(0.79); C843(0.94); C159(0.89); C948(1.10)  LDD1570  [6]
 LDCM0275  AKOS034007705 HEK-293T C434(1.06); C843(0.81); C948(1.00)  LDD1514  [6]
 LDCM0498  BS-3668 MDA-MB-231 C159(0.23)  LDD2091  [2]
 LDCM0367  CL1 HEK-293T C434(1.01); C843(1.18); C159(1.07)  LDD1571  [6]
 LDCM0368  CL10 HEK-293T C434(0.91); C843(1.62); C948(1.28)  LDD1572  [6]
 LDCM0369  CL100 HEK-293T C843(0.89)  LDD1573  [6]
 LDCM0370  CL101 HEK-293T C434(0.86); C843(1.10); C159(0.84)  LDD1574  [6]
 LDCM0371  CL102 HEK-293T C434(0.97); C843(1.15)  LDD1575  [6]
 LDCM0372  CL103 HEK-293T C434(1.09); C843(1.00); C948(1.06)  LDD1576  [6]
 LDCM0373  CL104 HEK-293T C843(0.97)  LDD1577  [6]
 LDCM0374  CL105 HEK-293T C434(1.18); C843(0.99); C159(0.94)  LDD1578  [6]
 LDCM0375  CL106 HEK-293T C434(0.87); C843(0.98)  LDD1579  [6]
 LDCM0376  CL107 HEK-293T C434(1.07); C843(1.04); C948(1.11)  LDD1580  [6]
 LDCM0377  CL108 HEK-293T C843(0.86)  LDD1581  [6]
 LDCM0378  CL109 HEK-293T C434(0.92); C843(1.15); C159(0.83)  LDD1582  [6]
 LDCM0379  CL11 HEK-293T C434(0.99); C843(1.52); C948(0.81)  LDD1583  [6]
 LDCM0380  CL110 HEK-293T C434(1.07); C843(0.91)  LDD1584  [6]
 LDCM0381  CL111 HEK-293T C434(0.97); C843(1.18); C948(1.06)  LDD1585  [6]
 LDCM0382  CL112 HEK-293T C843(1.03)  LDD1586  [6]
 LDCM0383  CL113 HEK-293T C434(1.09); C843(1.09); C159(1.11)  LDD1587  [6]
 LDCM0384  CL114 HEK-293T C434(1.29); C843(1.15)  LDD1588  [6]
 LDCM0385  CL115 HEK-293T C434(1.04); C843(1.13); C948(1.11)  LDD1589  [6]
 LDCM0386  CL116 HEK-293T C843(0.88)  LDD1590  [6]
 LDCM0387  CL117 HEK-293T C434(0.95); C843(1.10); C159(0.95)  LDD1591  [6]
 LDCM0388  CL118 HEK-293T C434(0.88); C843(1.17)  LDD1592  [6]
 LDCM0389  CL119 HEK-293T C434(1.04); C843(0.96); C948(1.06)  LDD1593  [6]
 LDCM0390  CL12 HEK-293T C434(1.12); C843(0.89); C948(1.02)  LDD1594  [6]
 LDCM0391  CL120 HEK-293T C843(0.96)  LDD1595  [6]
 LDCM0392  CL121 HEK-293T C434(1.03); C843(0.88); C159(0.92)  LDD1596  [6]
 LDCM0393  CL122 HEK-293T C434(0.94); C843(1.25)  LDD1597  [6]
 LDCM0394  CL123 HEK-293T C434(0.93); C843(1.01); C948(1.06)  LDD1598  [6]
 LDCM0395  CL124 HEK-293T C843(0.91)  LDD1599  [6]
 LDCM0396  CL125 HEK-293T C434(0.92); C843(1.02); C159(1.05)  LDD1600  [6]
 LDCM0397  CL126 HEK-293T C434(0.99); C843(1.16)  LDD1601  [6]
 LDCM0398  CL127 HEK-293T C434(0.96); C843(1.11); C948(1.08)  LDD1602  [6]
 LDCM0399  CL128 HEK-293T C843(0.90)  LDD1603  [6]
 LDCM0400  CL13 HEK-293T C434(1.33); C843(1.02); C159(1.07)  LDD1604  [6]
 LDCM0401  CL14 HEK-293T C434(1.15); C843(1.06)  LDD1605  [6]
 LDCM0402  CL15 HEK-293T C434(0.87); C843(0.86); C948(1.09)  LDD1606  [6]
 LDCM0403  CL16 HEK-293T C843(0.78)  LDD1607  [6]
 LDCM0404  CL17 HEK-293T C434(0.95); C843(0.93); C159(1.06); C948(0.98)  LDD1608  [6]
 LDCM0405  CL18 HEK-293T C434(1.01); C843(1.04); C159(0.99)  LDD1609  [6]
 LDCM0406  CL19 HEK-293T C434(0.94); C843(1.23)  LDD1610  [6]
 LDCM0407  CL2 HEK-293T C434(1.09); C843(1.09)  LDD1611  [6]
 LDCM0408  CL20 HEK-293T C843(1.06); C159(1.36); C948(1.12)  LDD1612  [6]
 LDCM0409  CL21 HEK-293T C434(1.21); C843(0.99); C159(0.99); C948(1.13)  LDD1613  [6]
 LDCM0410  CL22 HEK-293T C434(0.91); C843(1.66); C948(0.91)  LDD1614  [6]
 LDCM0411  CL23 HEK-293T C434(1.18); C843(1.42); C948(0.81)  LDD1615  [6]
 LDCM0412  CL24 HEK-293T C434(1.30); C843(0.80); C948(1.21)  LDD1616  [6]
 LDCM0413  CL25 HEK-293T C434(0.90); C843(1.08); C159(1.09)  LDD1617  [6]
 LDCM0414  CL26 HEK-293T C434(1.05); C843(0.88)  LDD1618  [6]
 LDCM0415  CL27 HEK-293T C434(1.19); C843(0.86); C948(0.97)  LDD1619  [6]
 LDCM0416  CL28 HEK-293T C843(0.80)  LDD1620  [6]
 LDCM0417  CL29 HEK-293T C434(1.00); C843(0.83); C159(0.74); C948(1.18)  LDD1621  [6]
 LDCM0418  CL3 HEK-293T C434(0.91); C843(1.14); C948(0.99)  LDD1622  [6]
 LDCM0419  CL30 HEK-293T C434(1.19); C843(1.11); C159(1.19)  LDD1623  [6]
 LDCM0420  CL31 HEK-293T C434(1.03); C843(1.16)  LDD1624  [6]
 LDCM0421  CL32 HEK-293T C843(1.20); C159(1.00); C948(0.92)  LDD1625  [6]
 LDCM0422  CL33 HEK-293T C434(0.77); C843(1.20); C159(1.08); C948(1.10)  LDD1626  [6]
 LDCM0423  CL34 HEK-293T C434(1.15); C843(1.37); C948(0.85)  LDD1627  [6]
 LDCM0424  CL35 HEK-293T C434(1.25); C843(1.54); C948(0.79)  LDD1628  [6]
 LDCM0425  CL36 HEK-293T C434(1.23); C843(0.84); C948(0.92)  LDD1629  [6]
 LDCM0426  CL37 HEK-293T C434(1.62); C843(1.02); C159(0.89)  LDD1630  [6]
 LDCM0428  CL39 HEK-293T C434(1.02); C843(0.85); C948(1.07)  LDD1632  [6]
 LDCM0429  CL4 HEK-293T C843(0.80)  LDD1633  [6]
 LDCM0430  CL40 HEK-293T C843(0.82)  LDD1634  [6]
 LDCM0431  CL41 HEK-293T C434(1.10); C843(1.00); C159(0.95); C948(1.09)  LDD1635  [6]
 LDCM0432  CL42 HEK-293T C434(0.82); C843(1.36); C159(1.05)  LDD1636  [6]
 LDCM0433  CL43 HEK-293T C434(1.01); C843(1.17)  LDD1637  [6]
 LDCM0434  CL44 HEK-293T C843(1.15); C159(0.94); C948(0.83)  LDD1638  [6]
 LDCM0435  CL45 HEK-293T C434(0.88); C843(0.94); C159(1.01); C948(1.28)  LDD1639  [6]
 LDCM0436  CL46 HEK-293T C434(0.93); C843(1.55); C948(0.97)  LDD1640  [6]
 LDCM0437  CL47 HEK-293T C434(0.91); C843(1.29); C948(0.70)  LDD1641  [6]
 LDCM0438  CL48 HEK-293T C434(0.91); C843(1.01); C948(1.10)  LDD1642  [6]
 LDCM0439  CL49 HEK-293T C434(0.91); C843(0.97); C159(0.86)  LDD1643  [6]
 LDCM0440  CL5 HEK-293T C434(1.14); C843(1.17); C159(0.82); C948(1.29)  LDD1644  [6]
 LDCM0441  CL50 HEK-293T C434(1.05); C843(0.93)  LDD1645  [6]
 LDCM0443  CL52 HEK-293T C843(0.79)  LDD1646  [6]
 LDCM0444  CL53 HEK-293T C434(1.05); C843(1.08); C159(0.84); C948(1.09)  LDD1647  [6]
 LDCM0445  CL54 HEK-293T C434(1.05); C843(0.96); C159(1.11)  LDD1648  [6]
 LDCM0446  CL55 HEK-293T C434(1.32); C843(1.25)  LDD1649  [6]
 LDCM0447  CL56 HEK-293T C843(1.10); C159(1.15); C948(1.07)  LDD1650  [6]
 LDCM0448  CL57 HEK-293T C434(0.74); C843(1.05); C159(1.01); C948(1.51)  LDD1651  [6]
 LDCM0449  CL58 HEK-293T C434(1.02); C843(1.33); C948(0.96)  LDD1652  [6]
 LDCM0450  CL59 HEK-293T C434(1.38); C843(1.21); C948(0.99)  LDD1653  [6]
 LDCM0451  CL6 HEK-293T C434(0.89); C843(0.90); C159(1.08)  LDD1654  [6]
 LDCM0452  CL60 HEK-293T C434(0.85); C843(0.70); C948(1.01)  LDD1655  [6]
 LDCM0453  CL61 HEK-293T C434(0.87); C843(0.94); C159(0.97)  LDD1656  [6]
 LDCM0454  CL62 HEK-293T C434(1.22); C843(1.05)  LDD1657  [6]
 LDCM0455  CL63 HEK-293T C434(0.94); C843(1.09); C948(1.04)  LDD1658  [6]
 LDCM0456  CL64 HEK-293T C843(1.01)  LDD1659  [6]
 LDCM0457  CL65 HEK-293T C434(1.03); C843(1.62); C159(0.90); C948(1.18)  LDD1660  [6]
 LDCM0458  CL66 HEK-293T C434(0.90); C843(1.23); C159(1.31)  LDD1661  [6]
 LDCM0459  CL67 HEK-293T C434(0.96); C843(1.21)  LDD1662  [6]
 LDCM0460  CL68 HEK-293T C843(1.26); C159(1.06); C948(1.18)  LDD1663  [6]
 LDCM0461  CL69 HEK-293T C434(0.74); C843(0.93); C159(0.92); C948(1.14)  LDD1664  [6]
 LDCM0462  CL7 HEK-293T C434(1.43); C843(1.37)  LDD1665  [6]
 LDCM0463  CL70 HEK-293T C434(0.89); C843(1.53); C948(0.91)  LDD1666  [6]
 LDCM0464  CL71 HEK-293T C434(0.96); C843(1.28); C948(1.06)  LDD1667  [6]
 LDCM0465  CL72 HEK-293T C434(1.07); C843(0.71); C948(1.12)  LDD1668  [6]
 LDCM0466  CL73 HEK-293T C434(1.68); C843(1.09); C159(1.09)  LDD1669  [6]
 LDCM0467  CL74 HEK-293T C434(0.83); C843(1.52)  LDD1670  [6]
 LDCM0469  CL76 HEK-293T C843(1.52)  LDD1672  [6]
 LDCM0470  CL77 HEK-293T C434(0.77); C843(0.86); C159(1.04); C948(1.24)  LDD1673  [6]
 LDCM0471  CL78 HEK-293T C434(0.96); C843(0.91); C159(1.20)  LDD1674  [6]
 LDCM0472  CL79 HEK-293T C434(0.89); C843(1.30)  LDD1675  [6]
 LDCM0473  CL8 HEK-293T C843(1.14); C159(1.12); C948(1.03)  LDD1676  [6]
 LDCM0474  CL80 HEK-293T C843(1.03); C159(0.98); C948(0.98)  LDD1677  [6]
 LDCM0475  CL81 HEK-293T C434(1.05); C843(0.96); C159(0.91); C948(1.04)  LDD1678  [6]
 LDCM0476  CL82 HEK-293T C434(1.57); C843(1.24); C948(0.96)  LDD1679  [6]
 LDCM0477  CL83 HEK-293T C434(0.95); C843(1.15); C948(1.00)  LDD1680  [6]
 LDCM0478  CL84 HEK-293T C434(0.99); C843(0.62); C948(1.06)  LDD1681  [6]
 LDCM0479  CL85 HEK-293T C434(0.89); C843(1.08); C159(1.11)  LDD1682  [6]
 LDCM0480  CL86 HEK-293T C434(0.96); C843(1.24)  LDD1683  [6]
 LDCM0481  CL87 HEK-293T C434(1.23); C843(0.93); C948(1.05)  LDD1684  [6]
 LDCM0482  CL88 HEK-293T C843(0.76)  LDD1685  [6]
 LDCM0483  CL89 HEK-293T C434(1.11); C843(0.93); C159(0.99); C948(1.17)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C434(1.39); C843(1.01); C159(1.10); C948(1.12)  LDD1687  [6]
 LDCM0485  CL90 HEK-293T C434(1.10); C843(1.26); C159(1.02)  LDD1688  [6]
 LDCM0486  CL91 HEK-293T C434(0.80); C843(1.19)  LDD1689  [6]
 LDCM0487  CL92 HEK-293T C843(1.08); C159(0.96); C948(1.18)  LDD1690  [6]
 LDCM0488  CL93 HEK-293T C434(0.88); C843(1.32); C159(0.92); C948(1.15)  LDD1691  [6]
 LDCM0489  CL94 HEK-293T C434(0.83); C843(1.35); C948(1.12)  LDD1692  [6]
 LDCM0490  CL95 HEK-293T C434(0.96); C843(1.39); C948(1.28)  LDD1693  [6]
 LDCM0491  CL96 HEK-293T C434(0.99); C843(0.88); C948(1.21)  LDD1694  [6]
 LDCM0492  CL97 HEK-293T C434(1.23); C843(1.06); C159(1.08)  LDD1695  [6]
 LDCM0493  CL98 HEK-293T C434(1.01); C843(1.24)  LDD1696  [6]
 LDCM0494  CL99 HEK-293T C434(1.01); C843(1.09); C948(1.19)  LDD1697  [6]
 LDCM0495  E2913 HEK-293T C434(1.00); C843(0.91); C948(1.22)  LDD1698  [6]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C843(4.77); C434(1.33)  LDD1702  [2]
 LDCM0468  Fragment33 HEK-293T C434(0.95); C843(0.78); C948(0.99)  LDD1671  [6]
 LDCM0427  Fragment51 HEK-293T C434(1.01); C843(1.02)  LDD1631  [6]
 LDCM0022  KB02 T cell C843(5.80)  LDD1703  [3]
 LDCM0023  KB03 MDA-MB-231 C434(3.24)  LDD1701  [2]
 LDCM0024  KB05 G361 C882(4.33); C458(2.21)  LDD3311  [1]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C159(0.63)  LDD2096  [2]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C159(0.96)  LDD2101  [2]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C159(0.79)  LDD2107  [2]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C159(0.56)  LDD2109  [2]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C159(0.78)  LDD2111  [2]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C159(0.69)  LDD2115  [2]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C159(1.27)  LDD2116  [2]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C159(1.00)  LDD2118  [2]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C159(2.63)  LDD2119  [2]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C159(0.88)  LDD2120  [2]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C159(0.65)  LDD2122  [2]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C159(0.60)  LDD2123  [2]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C159(0.66)  LDD2124  [2]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C159(0.53)  LDD2125  [2]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C159(1.33)  LDD2126  [2]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C159(0.67)  LDD2127  [2]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C159(1.04)  LDD2128  [2]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C159(1.06)  LDD2129  [2]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C159(0.78)  LDD2135  [2]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C159(0.99)  LDD2136  [2]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C159(1.18)  LDD1700  [2]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C159(0.45)  LDD2140  [2]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C159(1.13)  LDD2143  [2]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C159(2.50)  LDD2144  [2]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C159(0.87)  LDD2146  [2]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C159(0.98)  LDD2149  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Galactose-1-phosphate uridylyltransferase (GALT) Galactose-1-phosphate uridylyltransferase type 1 family P07902
Serine/threonine-protein kinase Nek6 (NEK6) NEK Ser/Thr protein kinase family Q9HC98
Activated CDC42 kinase 1 (TNK2) Tyr protein kinase family Q07912
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Clathrin heavy chain 1 (CLTC) Clathrin heavy chain family Q00610
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Aquaporin-1 (AQP1) MIP/aquaporin (TC 1.A.8) family P29972
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Breast cancer anti-estrogen resistance protein 1 (BCAR1) CAS family P56945
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
2-(3-amino-3-carboxypropyl)histidine synthase subunit 2 (DPH2) DPH1/DPH2 family Q9BQC3
Notch homolog 2 N-terminal-like protein A (NOTCH2NLA) NOTCH family Q7Z3S9
Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) PI3K p85 subunit family Q92569
SH2 domain-containing protein 1A (SH2D1A) . O60880
SH2 domain-containing protein 1B (SH2D1B) . O14796

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Entrectinib Small molecular drug DB11986
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atp Small molecular drug DB00171
Debromohymenialdisine Small molecular drug DB04367
Pmid17280833c30 Small molecular drug D0D5KZ
Patented
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bdbm50379214 Small molecular drug D04SWX
Us8481733, 106 Small molecular drug D0SZ3I
Us8481733, 118 Small molecular drug D0T9JA
Us8481733, 95 Small molecular drug D0PX1D

References

1 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
2 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
3 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.
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 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