Details of the Target

General Information of Target

Target ID LDTP05453
Target Name Focal adhesion kinase 1 (PTK2)
Gene Name PTK2
Gene ID 5747
Synonyms
FAK; FAK1; Focal adhesion kinase 1; FADK 1; EC 2.7.10.2; Focal adhesion kinase-related nonkinase; FRNK; Protein phosphatase 1 regulatory subunit 71; PPP1R71; Protein-tyrosine kinase 2; p125FAK; pp125FAK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGD
ATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEW
KYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSY
WEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESI
LKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQ
TIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFII
RPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRE
RIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDH
PHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESK
RFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFT
SASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWA
YDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGY
PSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQE
IAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLS
RGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNE
GVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLA
LRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQM
LTAAHALAVDAKNLLDVIDQARLKMLGQTRPH
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, FAK subfamily
Subcellular location
Cell junction, focal adhesion
Function
Non-receptor protein-tyrosine kinase that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adhesions and cell protrusions, cell cycle progression, cell proliferation and apoptosis. Required for early embryonic development and placenta development. Required for embryonic angiogenesis, normal cardiomyocyte migration and proliferation, and normal heart development. Regulates axon growth and neuronal cell migration, axon branching and synapse formation; required for normal development of the nervous system. Plays a role in osteogenesis and differentiation of osteoblasts. Functions in integrin signal transduction, but also in signaling downstream of numerous growth factor receptors, G-protein coupled receptors (GPCR), EPHA2, netrin receptors and LDL receptors. Forms multisubunit signaling complexes with SRC and SRC family members upon activation; this leads to the phosphorylation of additional tyrosine residues, creating binding sites for scaffold proteins, effectors and substrates. Regulates numerous signaling pathways. Promotes activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascade. Promotes activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling cascade. Promotes localized and transient activation of guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs), and thereby modulates the activity of Rho family GTPases. Signaling via CAS family members mediates activation of RAC1. Phosphorylates NEDD9 following integrin stimulation. Recruits the ubiquitin ligase MDM2 to P53/TP53 in the nucleus, and thereby regulates P53/TP53 activity, P53/TP53 ubiquitination and proteasomal degradation. Phosphorylates SRC; this increases SRC kinase activity. Phosphorylates ACTN1, ARHGEF7, GRB7, RET and WASL. Promotes phosphorylation of PXN and STAT1; most likely PXN and STAT1 are phosphorylated by a SRC family kinase that is recruited to autophosphorylated PTK2/FAK1, rather than by PTK2/FAK1 itself. Promotes phosphorylation of BCAR1; GIT2 and SHC1; this requires both SRC and PTK2/FAK1. Promotes phosphorylation of BMX and PIK3R1. Isoform 6 (FRNK) does not contain a kinase domain and inhibits PTK2/FAK1 phosphorylation and signaling. Its enhanced expression can attenuate the nuclear accumulation of LPXN and limit its ability to enhance serum response factor (SRF)-dependent gene transcription.; [Isoform 6]: Isoform 6 (FRNK) does not contain a kinase domain and inhibits PTK2/FAK1 phosphorylation and signaling. Its enhanced expression can attenuate the nuclear accumulation of LPXN and limit its ability to enhance serum response factor (SRF)-dependent gene transcription.
TTD ID
T15068
Uniprot ID
Q05397
DrugMap ID
TTON5IT
Ensemble ID
ENST00000340930.7
HGNC ID
HGNC:9611
ChEMBL ID
CHEMBL2695

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 18 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		13.90  LDD0402  [1]
STPyne
 Probe Info  		K1000(10.00); K1017(5.10); K1044(5.26); K222(10.00)  LDD0277  [2]
Probe 1
 Probe Info  		Y925(13.22)  LDD3495  [3]
DBIA
 Probe Info  		C348(2.07); C647(1.98); C459(2.37)  LDD3310  [4]
BTD
 Probe Info  		C257(1.03)  LDD2093  [5]
Acrolein
 Probe Info  		N.A.  LDD0222  [6]
ATP probe
 Probe Info  		K581(0.00); K583(0.00); K467(0.00)  LDD0199  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		C348(0.00); C459(0.00)  LDD0038  [8]
IA-alkyne
 Probe Info  		C348(0.00); C459(0.00)  LDD0036  [8]
Lodoacetamide azide
 Probe Info  		C82(0.00); C348(0.00); C559(0.00)  LDD0037  [8]
ATP probe
 Probe Info  		K467(0.00); K578(0.00)  LDD0035  [9]
NAIA_4
 Probe Info  		C559(0.00); C348(0.00)  LDD2226  [10]
TFBX
 Probe Info  		N.A.  LDD0027  [11]
WYneN
 Probe Info  		N.A.  LDD0021  [12]
WYneO
 Probe Info  		N.A.  LDD0022  [12]
IPM
 Probe Info  		N.A.  LDD0147  [11]
AOyne
 Probe Info  		10.20  LDD0443  [13]
NAIA_5
 Probe Info  		C658(0.00); C611(0.00); C348(0.00); C502(0.00)  LDD2223  [10]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DFG-out-3
 Probe Info  		2.50  LDD0074  [14]
DFG-out-4
 Probe Info  		37.00  LDD0075  [14]
Staurosporine capture compound
 Probe Info  		N.A.  LDD0083  [15]

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 C257(0.93)  LDD2117  [5]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C559(2.66); C257(1.22)  LDD2152  [5]
 LDCM0214  AC1 HEK-293T C459(1.05); C427(1.10); C82(0.99); C559(0.97)  LDD1507  [16]
 LDCM0215  AC10 HEK-293T C459(1.06); C427(1.07); C82(1.00); C559(1.01)  LDD1508  [16]
 LDCM0226  AC11 HEK-293T C459(1.10); C427(1.06); C82(1.00); C559(1.05)  LDD1509  [16]
 LDCM0237  AC12 HEK-293T C459(1.07); C427(0.99); C82(0.98); C559(0.93)  LDD1510  [16]
 LDCM0259  AC14 HEK-293T C459(1.05); C427(1.05); C82(0.95); C559(0.91)  LDD1512  [16]
 LDCM0270  AC15 HEK-293T C459(1.18); C427(0.94); C82(1.05); C559(0.98)  LDD1513  [16]
 LDCM0276  AC17 HEK-293T C459(1.03); C427(0.98); C82(0.99); C559(0.99)  LDD1515  [16]
 LDCM0277  AC18 HEK-293T C459(1.00); C427(0.86); C82(0.97); C559(0.84)  LDD1516  [16]
 LDCM0278  AC19 HEK-293T C459(1.27); C427(1.17); C82(0.97); C559(0.94)  LDD1517  [16]
 LDCM0279  AC2 HEK-293T C459(0.98); C427(1.03); C82(0.88); C559(0.97)  LDD1518  [16]
 LDCM0280  AC20 HEK-293T C459(1.08); C427(0.82); C82(1.04); C559(0.92)  LDD1519  [16]
 LDCM0281  AC21 HEK-293T C459(1.04); C427(1.03); C82(1.02); C559(1.02)  LDD1520  [16]
 LDCM0282  AC22 HEK-293T C459(0.94); C427(1.10); C82(0.93); C559(1.04)  LDD1521  [16]
 LDCM0283  AC23 HEK-293T C459(1.08); C427(0.86); C82(1.03); C559(0.97)  LDD1522  [16]
 LDCM0284  AC24 HEK-293T C459(1.06); C427(1.00); C82(1.02); C559(1.00)  LDD1523  [16]
 LDCM0285  AC25 HEK-293T C459(1.05); C427(1.00); C82(1.03); C559(1.10)  LDD1524  [16]
 LDCM0286  AC26 HEK-293T C459(0.99); C427(0.99); C82(0.99); C559(1.00)  LDD1525  [16]
 LDCM0287  AC27 HEK-293T C459(1.05); C427(1.06); C82(1.03); C559(1.01)  LDD1526  [16]
 LDCM0288  AC28 HEK-293T C459(1.05); C427(1.03); C82(1.09); C559(0.89)  LDD1527  [16]
 LDCM0289  AC29 HEK-293T C459(1.05); C427(1.00); C82(1.08); C559(1.08)  LDD1528  [16]
 LDCM0290  AC3 HEK-293T C459(1.07); C427(1.14); C82(0.90); C559(0.97)  LDD1529  [16]
 LDCM0291  AC30 HEK-293T C459(0.98); C427(0.88); C82(1.00); C559(1.02)  LDD1530  [16]
 LDCM0292  AC31 HEK-293T C459(0.90); C427(0.90); C82(1.10); C559(1.04)  LDD1531  [16]
 LDCM0293  AC32 HEK-293T C459(1.07); C427(0.87); C82(0.91); C559(1.00)  LDD1532  [16]
 LDCM0294  AC33 HEK-293T C459(1.03); C427(1.02); C82(1.02); C559(0.89)  LDD1533  [16]
 LDCM0295  AC34 HEK-293T C459(1.02); C427(1.00); C82(1.06); C559(0.94)  LDD1534  [16]
 LDCM0296  AC35 HEK-293T C459(1.04); C427(1.01); C82(1.00); C559(0.90)  LDD1535  [16]
 LDCM0297  AC36 HEK-293T C459(1.06); C427(0.87); C82(0.99); C559(0.90)  LDD1536  [16]
 LDCM0298  AC37 HEK-293T C459(1.02); C427(1.12); C82(1.16); C559(1.06)  LDD1537  [16]
 LDCM0299  AC38 HEK-293T C459(0.96); C427(1.09); C82(0.95); C559(0.90)  LDD1538  [16]
 LDCM0300  AC39 HEK-293T C459(1.26); C427(0.96); C82(1.05); C559(0.98)  LDD1539  [16]
 LDCM0301  AC4 HEK-293T C459(0.99); C427(0.92); C82(0.91); C559(0.93)  LDD1540  [16]
 LDCM0302  AC40 HEK-293T C459(1.05); C427(0.96); C82(1.04); C559(0.96)  LDD1541  [16]
 LDCM0303  AC41 HEK-293T C459(1.10); C427(0.98); C82(1.06); C559(0.99)  LDD1542  [16]
 LDCM0304  AC42 HEK-293T C459(1.05); C427(0.95); C82(0.96); C559(1.04)  LDD1543  [16]
 LDCM0305  AC43 HEK-293T C459(1.07); C427(1.13); C82(1.07); C559(0.93)  LDD1544  [16]
 LDCM0306  AC44 HEK-293T C459(1.07); C427(0.95); C82(1.06); C559(0.98)  LDD1545  [16]
 LDCM0307  AC45 HEK-293T C459(1.05); C427(1.10); C82(1.14); C559(1.01)  LDD1546  [16]
 LDCM0308  AC46 HEK-293T C459(1.03); C427(1.03); C82(1.03); C559(0.92)  LDD1547  [16]
 LDCM0309  AC47 HEK-293T C459(1.14); C427(1.10); C82(1.07); C559(0.97)  LDD1548  [16]
 LDCM0310  AC48 HEK-293T C459(1.04); C427(1.08); C82(1.00); C559(1.11)  LDD1549  [16]
 LDCM0311  AC49 HEK-293T C459(1.15); C427(1.00); C82(1.00); C559(0.94)  LDD1550  [16]
 LDCM0312  AC5 HEK-293T C459(1.05); C427(1.18); C82(0.76); C559(1.05)  LDD1551  [16]
 LDCM0313  AC50 HEK-293T C459(1.04); C427(0.96); C82(0.93); C559(0.98)  LDD1552  [16]
 LDCM0314  AC51 HEK-293T C459(1.17); C427(1.06); C82(1.04); C559(0.96)  LDD1553  [16]
 LDCM0315  AC52 HEK-293T C459(1.09); C427(0.94); C82(1.00); C559(0.92)  LDD1554  [16]
 LDCM0316  AC53 HEK-293T C459(1.14); C427(1.13); C82(1.06); C559(1.13)  LDD1555  [16]
 LDCM0317  AC54 HEK-293T C459(0.99); C427(0.95); C82(0.97); C559(0.98)  LDD1556  [16]
 LDCM0318  AC55 HEK-293T C459(1.25); C427(0.94); C82(1.03); C559(1.04)  LDD1557  [16]
 LDCM0319  AC56 HEK-293T C459(1.07); C427(0.99); C82(0.94); C559(0.95)  LDD1558  [16]
 LDCM0320  AC57 HEK-293T C459(1.08); C427(0.99); C82(1.02); C559(0.84)  LDD1559  [16]
 LDCM0321  AC58 HEK-293T C459(1.01); C427(0.89); C82(1.02); C559(0.99)  LDD1560  [16]
 LDCM0322  AC59 HEK-293T C459(1.01); C427(0.96); C82(1.11); C559(1.00)  LDD1561  [16]
 LDCM0323  AC6 HEK-293T C459(0.97); C427(0.93); C82(0.87); C559(0.91)  LDD1562  [16]
 LDCM0324  AC60 HEK-293T C459(0.99); C427(0.89); C82(0.99); C559(0.86)  LDD1563  [16]
 LDCM0325  AC61 HEK-293T C459(1.02); C427(1.07); C82(1.03); C559(1.03)  LDD1564  [16]
 LDCM0326  AC62 HEK-293T C459(0.98); C427(1.01); C82(0.99); C559(0.92)  LDD1565  [16]
 LDCM0327  AC63 HEK-293T C459(1.34); C427(0.92); C82(0.97); C559(1.07)  LDD1566  [16]
 LDCM0328  AC64 HEK-293T C459(1.05); C427(1.05); C82(0.91); C559(1.00)  LDD1567  [16]
 LDCM0334  AC7 HEK-293T C459(1.08); C427(1.02); C82(0.89); C559(0.95)  LDD1568  [16]
 LDCM0345  AC8 HEK-293T C459(1.04); C427(1.01); C82(0.78); C559(0.98)  LDD1569  [16]
 LDCM0248  AKOS034007472 HEK-293T C459(1.09); C427(0.97); C82(1.09); C559(1.07)  LDD1511  [16]
 LDCM0356  AKOS034007680 HEK-293T C459(1.07); C427(1.04); C82(1.08); C559(1.02)  LDD1570  [16]
 LDCM0275  AKOS034007705 HEK-293T C459(1.13); C427(1.01); C82(0.99); C559(1.01)  LDD1514  [16]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [6]
 LDCM0632  CL-Sc Hep-G2 C559(0.29)  LDD2227  [10]
 LDCM0367  CL1 HEK-293T C459(0.81); C427(1.07); C82(1.10); C288(1.02)  LDD1571  [16]
 LDCM0368  CL10 HEK-293T C459(0.75); C427(1.05); C82(1.23); C559(1.33)  LDD1572  [16]
 LDCM0369  CL100 HEK-293T C459(0.98); C427(1.00); C82(0.75); C559(0.96)  LDD1573  [16]
 LDCM0370  CL101 HEK-293T C459(0.97); C427(1.07); C82(1.03); C288(1.04)  LDD1574  [16]
 LDCM0371  CL102 HEK-293T C459(1.00); C427(1.16); C82(1.21); C559(0.98)  LDD1575  [16]
 LDCM0372  CL103 HEK-293T C459(1.11); C427(0.93); C82(0.98); C559(0.96)  LDD1576  [16]
 LDCM0373  CL104 HEK-293T C459(0.99); C427(0.86); C82(1.00); C559(1.06)  LDD1577  [16]
 LDCM0374  CL105 HEK-293T C459(1.01); C427(0.95); C82(1.05); C288(0.91)  LDD1578  [16]
 LDCM0375  CL106 HEK-293T C459(1.08); C427(1.07); C82(1.00); C559(1.08)  LDD1579  [16]
 LDCM0376  CL107 HEK-293T C459(1.05); C427(0.99); C82(0.95); C559(1.01)  LDD1580  [16]
 LDCM0377  CL108 HEK-293T C459(1.04); C427(1.01); C82(0.97); C559(0.99)  LDD1581  [16]
 LDCM0378  CL109 HEK-293T C459(0.97); C427(1.03); C82(1.03); C288(1.04)  LDD1582  [16]
 LDCM0379  CL11 HEK-293T C459(0.94); C427(1.14); C82(1.19); C559(1.12)  LDD1583  [16]
 LDCM0380  CL110 HEK-293T C459(0.93); C427(1.05); C82(1.17); C559(0.96)  LDD1584  [16]
 LDCM0381  CL111 HEK-293T C459(0.98); C427(0.86); C82(1.06); C559(0.90)  LDD1585  [16]
 LDCM0382  CL112 HEK-293T C459(0.93); C427(0.90); C82(0.98); C559(1.04)  LDD1586  [16]
 LDCM0383  CL113 HEK-293T C459(0.96); C427(1.07); C82(1.15); C288(0.98)  LDD1587  [16]
 LDCM0384  CL114 HEK-293T C459(0.89); C427(1.07); C82(1.13); C559(0.99)  LDD1588  [16]
 LDCM0385  CL115 HEK-293T C459(1.02); C427(1.04); C82(1.08); C559(1.03)  LDD1589  [16]
 LDCM0386  CL116 HEK-293T C459(1.05); C427(1.02); C82(1.01); C559(1.04)  LDD1590  [16]
 LDCM0387  CL117 HEK-293T C459(1.05); C427(1.11); C82(1.04); C288(1.05)  LDD1591  [16]
 LDCM0388  CL118 HEK-293T C459(1.18); C427(0.97); C82(1.10); C559(1.05)  LDD1592  [16]
 LDCM0389  CL119 HEK-293T C459(1.08); C427(1.02); C82(1.08); C559(1.03)  LDD1593  [16]
 LDCM0390  CL12 HEK-293T C459(1.04); C427(0.95); C82(1.10); C559(1.33)  LDD1594  [16]
 LDCM0391  CL120 HEK-293T C459(0.98); C427(1.01); C82(1.03); C559(0.97)  LDD1595  [16]
 LDCM0392  CL121 HEK-293T C459(1.09); C427(1.00); C82(1.04); C288(0.97)  LDD1596  [16]
 LDCM0393  CL122 HEK-293T C459(1.10); C427(0.92); C82(1.06); C559(1.02)  LDD1597  [16]
 LDCM0394  CL123 HEK-293T C459(0.92); C427(1.03); C82(1.04); C559(0.93)  LDD1598  [16]
 LDCM0395  CL124 HEK-293T C459(1.22); C427(0.89); C82(1.06); C559(0.97)  LDD1599  [16]
 LDCM0396  CL125 HEK-293T C459(1.01); C427(1.01); C82(1.04); C288(1.07)  LDD1600  [16]
 LDCM0397  CL126 HEK-293T C459(0.98); C427(1.00); C82(1.12); C559(0.96)  LDD1601  [16]
 LDCM0398  CL127 HEK-293T C459(1.03); C427(0.91); C82(0.99); C559(0.94)  LDD1602  [16]
 LDCM0399  CL128 HEK-293T C459(1.02); C427(0.98); C82(0.94); C559(1.07)  LDD1603  [16]
 LDCM0400  CL13 HEK-293T C459(0.89); C427(1.04); C82(0.99); C288(0.99)  LDD1604  [16]
 LDCM0401  CL14 HEK-293T C459(0.97); C427(1.08); C82(1.23); C559(1.00)  LDD1605  [16]
 LDCM0402  CL15 HEK-293T C459(0.87); C427(1.05); C82(1.04); C559(1.09)  LDD1606  [16]
 LDCM0403  CL16 HEK-293T C459(0.97); C427(0.86); C82(1.07); C559(1.00)  LDD1607  [16]
 LDCM0404  CL17 HEK-293T C459(0.96); C427(0.93); C82(1.00); C559(0.95)  LDD1608  [16]
 LDCM0405  CL18 HEK-293T C459(1.04); C427(1.01); C82(1.21); C559(1.12)  LDD1609  [16]
 LDCM0406  CL19 HEK-293T C459(1.40); C427(1.07); C82(1.05); C559(0.99)  LDD1610  [16]
 LDCM0407  CL2 HEK-293T C459(0.87); C427(0.99); C82(1.16); C559(1.05)  LDD1611  [16]
 LDCM0408  CL20 HEK-293T C459(0.99); C427(0.85); C82(1.13); C559(1.05)  LDD1612  [16]
 LDCM0409  CL21 HEK-293T C459(0.91); C427(1.00); C82(1.32); C559(1.32)  LDD1613  [16]
 LDCM0410  CL22 HEK-293T C459(0.99); C427(1.13); C82(1.17); C559(1.26)  LDD1614  [16]
 LDCM0411  CL23 HEK-293T C459(1.03); C427(1.09); C82(1.18); C559(1.05)  LDD1615  [16]
 LDCM0412  CL24 HEK-293T C459(1.09); C427(0.98); C82(1.20); C559(1.28)  LDD1616  [16]
 LDCM0413  CL25 HEK-293T C459(0.87); C427(0.99); C82(1.17); C288(0.87)  LDD1617  [16]
 LDCM0414  CL26 HEK-293T C459(0.95); C427(0.97); C82(0.99); C559(0.94)  LDD1618  [16]
 LDCM0415  CL27 HEK-293T C459(1.03); C427(1.03); C82(1.00); C559(1.00)  LDD1619  [16]
 LDCM0416  CL28 HEK-293T C459(0.96); C427(1.05); C82(1.04); C559(1.06)  LDD1620  [16]
 LDCM0417  CL29 HEK-293T C459(1.09); C427(0.96); C82(0.99); C559(1.03)  LDD1621  [16]
 LDCM0418  CL3 HEK-293T C459(0.89); C427(1.00); C82(1.00); C559(1.12)  LDD1622  [16]
 LDCM0419  CL30 HEK-293T C459(1.02); C427(1.02); C82(1.12); C559(1.06)  LDD1623  [16]
 LDCM0420  CL31 HEK-293T C459(1.15); C427(1.04); C82(1.13); C559(1.07)  LDD1624  [16]
 LDCM0421  CL32 HEK-293T C459(1.02); C427(1.11); C82(1.09); C559(1.09)  LDD1625  [16]
 LDCM0422  CL33 HEK-293T C459(0.93); C427(1.07); C82(1.19); C559(1.28)  LDD1626  [16]
 LDCM0423  CL34 HEK-293T C459(1.03); C427(1.00); C82(1.10); C559(1.31)  LDD1627  [16]
 LDCM0424  CL35 HEK-293T C459(1.19); C427(0.92); C82(1.11); C559(1.20)  LDD1628  [16]
 LDCM0425  CL36 HEK-293T C459(1.12); C427(0.95); C82(1.16); C559(1.37)  LDD1629  [16]
 LDCM0426  CL37 HEK-293T C459(0.94); C427(1.06); C82(1.11); C288(0.95)  LDD1630  [16]
 LDCM0428  CL39 HEK-293T C459(1.00); C427(0.93); C82(1.11); C559(0.93)  LDD1632  [16]
 LDCM0429  CL4 HEK-293T C459(0.83); C427(0.89); C82(1.17); C559(1.00)  LDD1633  [16]
 LDCM0430  CL40 HEK-293T C459(0.90); C427(1.09); C82(1.05); C559(1.03)  LDD1634  [16]
 LDCM0431  CL41 HEK-293T C459(0.98); C427(0.90); C82(1.12); C559(0.91)  LDD1635  [16]
 LDCM0432  CL42 HEK-293T C459(0.98); C427(0.90); C82(1.10); C559(0.98)  LDD1636  [16]
 LDCM0433  CL43 HEK-293T C459(1.03); C427(1.26); C82(1.09); C559(0.88)  LDD1637  [16]
 LDCM0434  CL44 HEK-293T C459(1.07); C427(1.11); C82(1.22); C559(0.98)  LDD1638  [16]
 LDCM0435  CL45 HEK-293T C459(1.06); C427(0.94); C82(1.36); C559(1.32)  LDD1639  [16]
 LDCM0436  CL46 HEK-293T C459(0.96); C427(1.10); C82(1.07); C559(1.27)  LDD1640  [16]
 LDCM0437  CL47 HEK-293T C459(1.24); C427(0.93); C82(1.13); C559(1.14)  LDD1641  [16]
 LDCM0438  CL48 HEK-293T C459(1.09); C427(1.09); C82(1.14); C559(1.41)  LDD1642  [16]
 LDCM0439  CL49 HEK-293T C459(0.90); C427(1.07); C82(1.08); C288(1.03)  LDD1643  [16]
 LDCM0440  CL5 HEK-293T C459(0.97); C427(0.98); C82(1.19); C559(0.87)  LDD1644  [16]
 LDCM0441  CL50 HEK-293T C459(0.98); C427(1.01); C82(1.02); C559(0.95)  LDD1645  [16]
 LDCM0443  CL52 HEK-293T C459(0.99); C427(1.01); C82(1.17); C559(0.90)  LDD1646  [16]
 LDCM0444  CL53 HEK-293T C459(0.99); C427(1.05); C82(1.09); C559(0.93)  LDD1647  [16]
 LDCM0445  CL54 HEK-293T C459(1.03); C427(0.98); C82(1.06); C559(1.04)  LDD1648  [16]
 LDCM0446  CL55 HEK-293T C459(1.01); C427(1.13); C82(1.14); C559(1.00)  LDD1649  [16]
 LDCM0447  CL56 HEK-293T C459(1.05); C427(0.89); C82(1.12); C559(1.03)  LDD1650  [16]
 LDCM0448  CL57 HEK-293T C459(1.03); C427(1.27); C82(1.34); C559(1.46)  LDD1651  [16]
 LDCM0449  CL58 HEK-293T C459(1.04); C427(1.14); C82(1.10); C559(1.39)  LDD1652  [16]
 LDCM0450  CL59 HEK-293T C459(1.18); C427(1.10); C82(1.22); C559(1.08)  LDD1653  [16]
 LDCM0451  CL6 HEK-293T C459(0.86); C427(1.01); C82(1.09); C559(0.93)  LDD1654  [16]
 LDCM0452  CL60 HEK-293T C459(1.00); C427(1.10); C82(1.19); C559(1.26)  LDD1655  [16]
 LDCM0453  CL61 HEK-293T C459(0.96); C427(1.01); C82(1.01); C288(1.04)  LDD1656  [16]
 LDCM0454  CL62 HEK-293T C459(1.09); C427(0.99); C82(1.11); C559(0.92)  LDD1657  [16]
 LDCM0455  CL63 HEK-293T C459(1.11); C427(0.98); C82(1.02); C559(0.92)  LDD1658  [16]
 LDCM0456  CL64 HEK-293T C459(0.92); C427(1.01); C82(1.09); C559(1.05)  LDD1659  [16]
 LDCM0457  CL65 HEK-293T C459(1.07); C427(0.99); C82(1.07); C559(0.89)  LDD1660  [16]
 LDCM0458  CL66 HEK-293T C459(1.04); C427(1.04); C82(1.07); C559(0.99)  LDD1661  [16]
 LDCM0459  CL67 HEK-293T C459(1.11); C427(0.96); C82(1.09); C559(1.05)  LDD1662  [16]
 LDCM0460  CL68 HEK-293T C459(1.05); C427(1.08); C82(1.13); C559(0.94)  LDD1663  [16]
 LDCM0461  CL69 HEK-293T C459(1.05); C427(1.18); C82(1.24); C559(1.30)  LDD1664  [16]
 LDCM0462  CL7 HEK-293T C459(1.04); C427(1.17); C82(1.10); C559(0.88)  LDD1665  [16]
 LDCM0463  CL70 HEK-293T C459(0.95); C427(0.94); C82(1.15); C559(1.33)  LDD1666  [16]
 LDCM0464  CL71 HEK-293T C459(1.18); C427(1.07); C82(1.13); C559(1.18)  LDD1667  [16]
 LDCM0465  CL72 HEK-293T C459(1.22); C427(0.96); C82(1.12); C559(1.30)  LDD1668  [16]
 LDCM0466  CL73 HEK-293T C459(0.89); C427(0.98); C82(0.99); C288(1.08)  LDD1669  [16]
 LDCM0467  CL74 HEK-293T C459(1.12); C427(0.96); C82(1.25); C559(1.00)  LDD1670  [16]
 LDCM0469  CL76 HEK-293T C459(1.00); C427(0.86); C82(0.99); C559(0.98)  LDD1672  [16]
 LDCM0470  CL77 HEK-293T C459(1.01); C427(0.95); C82(1.16); C559(0.98)  LDD1673  [16]
 LDCM0471  CL78 HEK-293T C459(0.99); C427(1.03); C82(1.18); C559(0.82)  LDD1674  [16]
 LDCM0472  CL79 HEK-293T C459(1.10); C427(1.18); C82(1.07); C559(0.94)  LDD1675  [16]
 LDCM0473  CL8 HEK-293T C459(0.72); C427(0.84); C82(1.13); C559(1.13)  LDD1676  [16]
 LDCM0474  CL80 HEK-293T C459(1.05); C427(0.89); C82(1.17); C559(0.93)  LDD1677  [16]
 LDCM0475  CL81 HEK-293T C459(1.14); C427(1.20); C82(1.11); C559(1.43)  LDD1678  [16]
 LDCM0476  CL82 HEK-293T C459(0.93); C427(1.01); C82(1.05); C559(1.12)  LDD1679  [16]
 LDCM0477  CL83 HEK-293T C459(1.04); C427(1.02); C82(1.11); C559(1.18)  LDD1680  [16]
 LDCM0478  CL84 HEK-293T C459(1.04); C427(0.98); C82(1.08); C559(1.18)  LDD1681  [16]
 LDCM0479  CL85 HEK-293T C459(1.00); C427(1.07); C82(1.04); C288(0.94)  LDD1682  [16]
 LDCM0480  CL86 HEK-293T C459(0.92); C427(1.13); C82(0.95); C559(1.04)  LDD1683  [16]
 LDCM0481  CL87 HEK-293T C459(0.92); C427(1.03); C82(1.08); C559(0.90)  LDD1684  [16]
 LDCM0482  CL88 HEK-293T C459(0.94); C427(0.95); C82(0.98); C559(0.91)  LDD1685  [16]
 LDCM0483  CL89 HEK-293T C459(0.98); C427(0.97); C82(1.10); C559(0.82)  LDD1686  [16]
 LDCM0484  CL9 HEK-293T C459(0.99); C427(1.20); C82(1.30); C559(1.34)  LDD1687  [16]
 LDCM0485  CL90 HEK-293T C459(0.87); C427(1.03); C82(1.10); C559(1.01)  LDD1688  [16]
 LDCM0486  CL91 HEK-293T C459(1.00); C427(1.22); C82(1.09); C559(1.04)  LDD1689  [16]
 LDCM0487  CL92 HEK-293T C459(0.93); C427(0.88); C82(1.07); C559(0.96)  LDD1690  [16]
 LDCM0488  CL93 HEK-293T C459(0.99); C427(0.95); C82(1.14); C559(1.24)  LDD1691  [16]
 LDCM0489  CL94 HEK-293T C459(1.02); C427(1.02); C82(1.13); C559(1.11)  LDD1692  [16]
 LDCM0490  CL95 HEK-293T C459(1.00); C427(1.04); C82(1.12); C559(1.04)  LDD1693  [16]
 LDCM0491  CL96 HEK-293T C459(0.98); C427(1.02); C82(1.03); C559(1.19)  LDD1694  [16]
 LDCM0492  CL97 HEK-293T C459(0.91); C427(1.07); C82(1.02); C288(0.98)  LDD1695  [16]
 LDCM0493  CL98 HEK-293T C459(0.93); C427(1.02); C82(0.95); C559(0.99)  LDD1696  [16]
 LDCM0494  CL99 HEK-293T C459(0.95); C427(1.00); C82(0.84); C559(0.98)  LDD1697  [16]
 LDCM0017  DFG-out-2 A431 37.00  LDD0075  [14]
 LDCM0495  E2913 HEK-293T C459(1.05); C427(1.09); C82(1.05); C559(0.91)  LDD1698  [16]
 LDCM0468  Fragment33 HEK-293T C459(1.08); C427(0.95); C82(1.15); C559(1.04)  LDD1671  [16]
 LDCM0427  Fragment51 HEK-293T C459(0.97); C427(0.96); C82(1.09); C559(0.95)  LDD1631  [16]
 LDCM0022  KB02 HEK-293T C459(0.98); C82(0.87); C559(0.93); C288(1.06)  LDD1492  [16]
 LDCM0023  KB03 HEK-293T C459(0.94); C82(1.24); C559(1.02); C288(1.20)  LDD1497  [16]
 LDCM0024  KB05 COLO792 C348(2.07); C647(1.98); C459(2.37)  LDD3310  [4]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C257(1.03)  LDD2093  [5]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C559(1.59); C257(0.99); C173(1.04)  LDD2099  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C257(1.00)  LDD2107  [5]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C559(1.11); C173(0.70)  LDD2109  [5]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C559(2.58)  LDD2111  [5]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C257(0.83); C173(0.87)  LDD2123  [5]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C559(1.18); C257(0.82); C173(1.00)  LDD2125  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C257(0.90); C173(1.10)  LDD2127  [5]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C559(2.36)  LDD2129  [5]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C257(0.64)  LDD2134  [5]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C559(2.37)  LDD2135  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C559(1.48); C257(0.97); C173(1.25)  LDD2136  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C559(1.66); C257(0.87); C173(1.02)  LDD2137  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C257(0.94)  LDD2140  [5]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C257(2.36)  LDD2144  [5]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C257(1.15); C173(1.23)  LDD2146  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C257(0.51)  LDD2148  [5]
 LDCM0016  Ranjitkar_cp1 A431 2.50  LDD0074  [14]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [15]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
SRSF protein kinase 1 (SRPK1) CMGC Ser/Thr protein kinase family Q96SB4
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Ephrin type-A receptor 2 (EPHA2) Tyr protein kinase family P29317
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Tyrosine-protein kinase Yes (YES1) Tyr protein kinase family P07947
Tyrosine-protein phosphatase non-receptor type 23 (PTPN23) Protein-tyrosine phosphatase family Q9H3S7
Tensin-3 (TNS3) PTEN phosphatase protein family Q68CZ2
Peptidyl-tRNA hydrolase 2, mitochondrial (PTRH2) PTH2 family Q9Y3E5
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Signal transducer and activator of transcription 1-alpha/beta (STAT1) Transcription factor STAT family P42224
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Platelet-activating factor receptor (PTAFR) G-protein coupled receptor 1 family P25105
Other
Click To Hide/Show 9 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Breast cancer anti-estrogen resistance protein 1 (BCAR1) CAS family P56945
Adapter molecule crk (CRK) CRK family P46108
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Growth factor receptor-bound protein 7 (GRB7) GRB7/10/14 family Q14451
Integrin beta-4 (ITGB4) Integrin beta chain family P16144
Paxillin (PXN) Paxillin family P49023
Transforming growth factor beta-1-induced transcript 1 protein (TGFB1I1) Paxillin family O43294
Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) PI3K p85 subunit family Q92569
SH2 domain-containing protein 2A (SH2D2A) . Q9NP31

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
Vs-6063 Small molecular drug D0Y1UO
Phase 1
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cep-37440 Small molecular drug D0N6NM
Gsk-2256098 Small molecular drug D0B9MR
In10018 Small molecular drug D1EW3O
Pf-562271 Small molecular drug D01SJT
Bi-853520 . D00KNI
Vs-4718 . D0A6VD
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bms-536924 Small molecular drug D0M4SY
Pf-228 Small molecular drug D02QAZ
Pmid23414845c30 Small molecular drug D0AY0F
2-({5-chloro-2-[(2-methoxy-4-morpholin-4-ylphenyl)Amino]Pyrimidin-4-yl}Amino)-n-methylbenzamide . DB07460
7-pyridin-2-yl-n-(345-trimethoxyphenyl)-7h-pyrrolo[23-d]Pyrimidin-2-amine . DB07248
Endostatin . DB06423
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,2,4-triazolo[1,5a]Pyridine Derivative 1 Small molecular drug D07XYI

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 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
3 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
4 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
5 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
6 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
7 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
8 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
9 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
10 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
11 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
12 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
13 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.
14 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.
15 Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS). J Proteome Res. 2010 Feb 5;9(2):806-17. doi: 10.1021/pr9007333.
16 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