Details of the Target

General Information of Target

Target ID LDTP10940
Target Name Mitogen-activated protein kinase kinase kinase 5 (MAP3K5)
Gene Name MAP3K5
Gene ID 4217
Synonyms
ASK1; MAPKKK5; MEKK5; Mitogen-activated protein kinase kinase kinase 5; EC 2.7.11.25; Apoptosis signal-regulating kinase 1; ASK-1; MAPK/ERK kinase kinase 5; MEK kinase 5; MEKK 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGDRRFIDFQFQDSNSSLRPRLGNATANNTCIVDDSFKYNLNGAVYSVVFILGLITNSVS
LFVFCFRMKMRSETAIFITNLAVSDLLFVCTLPFKIFYNFNRHWPFGDTLCKISGTAFLT
NIYGSMLFLTCISVDRFLAIVYPFRSRTIRTRRNSAIVCAGVWILVLSGGISASLFSTTN
VNNATTTCFEGFSKRVWKTYLSKITIFIEVVGFIIPLILNVSCSSVVLRTLRKPATLSQI
GTNKKKVLKMITVHMAVFVVCFVPYNSVLFLYALVRSQAITNCFLERFAKIMYPITLCLA
TLNCCFDPFIYYFTLESFQKSFYINAHIRMESLFKTETPLTTKPSLPAIQEEVSDQTTNN
GGELMLESTF
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase kinase subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. Plays an important role in the cascades of cellular responses evoked by changes in the environment. Mediates signaling for determination of cell fate such as differentiation and survival. Plays a crucial role in the apoptosis signal transduction pathway through mitochondria-dependent caspase activation. MAP3K5/ASK1 is required for the innate immune response, which is essential for host defense against a wide range of pathogens. Mediates signal transduction of various stressors like oxidative stress as well as by receptor-mediated inflammatory signals, such as the tumor necrosis factor (TNF) or lipopolysaccharide (LPS). Once activated, acts as an upstream activator of the MKK/JNK signal transduction cascade and the p38 MAPK signal transduction cascade through the phosphorylation and activation of several MAP kinase kinases like MAP2K4/SEK1, MAP2K3/MKK3, MAP2K6/MKK6 and MAP2K7/MKK7. These MAP2Ks in turn activate p38 MAPKs and c-jun N-terminal kinases (JNKs). Both p38 MAPK and JNKs control the transcription factors activator protein-1 (AP-1).
TTD ID
T97589
Uniprot ID
Q99683
DrugMap ID
TTOQCD8
Ensemble ID
ENST00000359015.5
HGNC ID
HGNC:6857
ChEMBL ID
CHEMBL5285

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2780 SNV: p.M375V .
A3KAW SNV: p.I599M .
CCK81 SNV: p.V800A; p.I832T .
COLO679 SNV: p.R256C .
HEL SNV: p.T1308I DBIA    Probe Info 
HEL9217 SNV: p.T1308I DBIA    Probe Info 
HT SNV: p.K878N .
KMS11 SNV: p.I653V .
LN18 SNV: p.E710G .
MCC13 SNV: p.P1290L .
MDAMB468 SNV: p.S83C .
MELJUSO SNV: p.R256C .
MEWO SNV: p.L1270F .
NCIH2172 SNV: p.R1254S .
NCIH358 SNV: p.G681V .
OVK18 Deletion: p.S980del
SNV: p.K584N		 .
PF382 SNV: p.L260P; p.R302Ter .
RKO Insertion: p.V1127SfsTer14 .
SHP77 SNV: p.D674V .
SKMEL24 SNV: p.G170E .
SNGM SNV: p.T1186I .
SUPT1 Deletion: p.L1018WfsTer27 .
TE11 SNV: p.T585A .
WM793 SNV: p.H900Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C1360(1.01)  LDD2198  [1]
DBIA
 Probe Info  		C225(1.36); C226(1.36)  LDD0563  [2]
AMP probe
 Probe Info  		N.A.  LDD0200  [3]
ATP probe
 Probe Info  		K709(0.00); K805(0.00)  LDD0199  [3]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [4]
IPM
 Probe Info  		N.A.  LDD0005  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C928(1.00); C1360(1.20)  LDD1507  [6]
 LDCM0215  AC10 HEK-293T C928(0.76); C1360(1.24)  LDD1508  [6]
 LDCM0226  AC11 HEK-293T C928(1.32)  LDD1509  [6]
 LDCM0237  AC12 HEK-293T C928(1.06)  LDD1510  [6]
 LDCM0246  AC128 HCT 116 C225(1.36); C226(1.36)  LDD0563  [2]
 LDCM0247  AC129 HCT 116 C225(1.50); C226(1.50)  LDD0564  [2]
 LDCM0249  AC130 HCT 116 C225(1.25); C226(1.25)  LDD0566  [2]
 LDCM0250  AC131 HCT 116 C225(1.30); C226(1.30)  LDD0567  [2]
 LDCM0251  AC132 HCT 116 C225(1.37); C226(1.37)  LDD0568  [2]
 LDCM0252  AC133 HCT 116 C225(1.34); C226(1.34)  LDD0569  [2]
 LDCM0253  AC134 HCT 116 C225(1.35); C226(1.35)  LDD0570  [2]
 LDCM0254  AC135 HCT 116 C225(1.07); C226(1.07)  LDD0571  [2]
 LDCM0255  AC136 HCT 116 C225(1.25); C226(1.25)  LDD0572  [2]
 LDCM0256  AC137 HCT 116 C225(1.25); C226(1.25)  LDD0573  [2]
 LDCM0257  AC138 HCT 116 C225(1.23); C226(1.23)  LDD0574  [2]
 LDCM0258  AC139 HCT 116 C225(1.42); C226(1.42)  LDD0575  [2]
 LDCM0259  AC14 HEK-293T C928(1.10)  LDD1512  [6]
 LDCM0260  AC140 HCT 116 C225(1.29); C226(1.29)  LDD0577  [2]
 LDCM0261  AC141 HCT 116 C225(1.41); C226(1.41)  LDD0578  [2]
 LDCM0262  AC142 HCT 116 C225(1.38); C226(1.38)  LDD0579  [2]
 LDCM0270  AC15 HEK-293T C928(0.80)  LDD1513  [6]
 LDCM0276  AC17 HEK-293T C928(1.27); C1360(1.01)  LDD1515  [6]
 LDCM0277  AC18 HEK-293T C928(0.98); C1360(1.22)  LDD1516  [6]
 LDCM0278  AC19 HEK-293T C928(1.04)  LDD1517  [6]
 LDCM0279  AC2 HEK-293T C928(0.93); C1360(0.93)  LDD1518  [6]
 LDCM0280  AC20 HEK-293T C928(0.99)  LDD1519  [6]
 LDCM0281  AC21 HEK-293T C928(1.01); C1360(0.90)  LDD1520  [6]
 LDCM0282  AC22 HEK-293T C928(0.98)  LDD1521  [6]
 LDCM0283  AC23 HEK-293T C928(0.98)  LDD1522  [6]
 LDCM0284  AC24 HEK-293T C928(0.83); C1360(0.92)  LDD1523  [6]
 LDCM0285  AC25 HEK-293T C928(1.25); C1360(0.97)  LDD1524  [6]
 LDCM0286  AC26 HEK-293T C928(1.17); C1360(0.92)  LDD1525  [6]
 LDCM0287  AC27 HEK-293T C928(0.91)  LDD1526  [6]
 LDCM0288  AC28 HEK-293T C928(1.26)  LDD1527  [6]
 LDCM0289  AC29 HEK-293T C928(0.90); C1360(0.90)  LDD1528  [6]
 LDCM0290  AC3 HEK-293T C928(1.28)  LDD1529  [6]
 LDCM0291  AC30 HEK-293T C928(1.05)  LDD1530  [6]
 LDCM0292  AC31 HEK-293T C928(0.96)  LDD1531  [6]
 LDCM0293  AC32 HEK-293T C928(1.05); C1360(1.08)  LDD1532  [6]
 LDCM0294  AC33 HEK-293T C928(1.09); C1360(1.12)  LDD1533  [6]
 LDCM0295  AC34 HEK-293T C928(1.00); C1360(1.33)  LDD1534  [6]
 LDCM0296  AC35 HEK-293T C928(1.42)  LDD1535  [6]
 LDCM0297  AC36 HEK-293T C928(1.01)  LDD1536  [6]
 LDCM0298  AC37 HEK-293T C928(0.97); C1360(0.99)  LDD1537  [6]
 LDCM0299  AC38 HEK-293T C928(1.03)  LDD1538  [6]
 LDCM0300  AC39 HEK-293T C928(0.90)  LDD1539  [6]
 LDCM0301  AC4 HEK-293T C928(1.28)  LDD1540  [6]
 LDCM0302  AC40 HEK-293T C928(0.91); C1360(1.22)  LDD1541  [6]
 LDCM0303  AC41 HEK-293T C928(1.00); C1360(1.20)  LDD1542  [6]
 LDCM0304  AC42 HEK-293T C928(1.04); C1360(0.94)  LDD1543  [6]
 LDCM0305  AC43 HEK-293T C928(1.23)  LDD1544  [6]
 LDCM0306  AC44 HEK-293T C928(0.97)  LDD1545  [6]
 LDCM0307  AC45 HEK-293T C928(0.99); C1360(0.90)  LDD1546  [6]
 LDCM0308  AC46 HEK-293T C928(0.89)  LDD1547  [6]
 LDCM0309  AC47 HEK-293T C928(0.93)  LDD1548  [6]
 LDCM0310  AC48 HEK-293T C928(0.61); C1360(1.29)  LDD1549  [6]
 LDCM0311  AC49 HEK-293T C928(0.89); C1360(1.10)  LDD1550  [6]
 LDCM0312  AC5 HEK-293T C928(1.05); C1360(1.10)  LDD1551  [6]
 LDCM0313  AC50 HEK-293T C928(1.36); C1360(1.24)  LDD1552  [6]
 LDCM0314  AC51 HEK-293T C928(1.05)  LDD1553  [6]
 LDCM0315  AC52 HEK-293T C928(0.98)  LDD1554  [6]
 LDCM0316  AC53 HEK-293T C928(1.67); C1360(0.97)  LDD1555  [6]
 LDCM0317  AC54 HEK-293T C928(0.93)  LDD1556  [6]
 LDCM0318  AC55 HEK-293T C928(1.03)  LDD1557  [6]
 LDCM0319  AC56 HEK-293T C928(1.12); C1360(1.03)  LDD1558  [6]
 LDCM0320  AC57 HCT 116 C225(0.78); C226(0.78)  LDD0637  [2]
 LDCM0321  AC58 HCT 116 C225(0.71); C226(0.71)  LDD0638  [2]
 LDCM0322  AC59 HCT 116 C225(0.77); C226(0.77)  LDD0639  [2]
 LDCM0323  AC6 HEK-293T C928(1.12)  LDD1562  [6]
 LDCM0324  AC60 HCT 116 C225(0.76); C226(0.76)  LDD0641  [2]
 LDCM0325  AC61 HCT 116 C225(0.70); C226(0.70)  LDD0642  [2]
 LDCM0326  AC62 HCT 116 C225(0.77); C226(0.77)  LDD0643  [2]
 LDCM0327  AC63 HCT 116 C225(0.69); C226(0.69)  LDD0644  [2]
 LDCM0328  AC64 HCT 116 C225(0.80); C226(0.80)  LDD0645  [2]
 LDCM0329  AC65 HCT 116 C225(0.82); C226(0.82)  LDD0646  [2]
 LDCM0330  AC66 HCT 116 C225(0.80); C226(0.80)  LDD0647  [2]
 LDCM0331  AC67 HCT 116 C225(0.82); C226(0.82)  LDD0648  [2]
 LDCM0332  AC68 HCT 116 C225(0.92); C226(0.92)  LDD0649  [2]
 LDCM0333  AC69 HCT 116 C225(0.98); C226(0.98)  LDD0650  [2]
 LDCM0334  AC7 HEK-293T C928(1.12)  LDD1568  [6]
 LDCM0335  AC70 HCT 116 C225(1.04); C226(1.04)  LDD0652  [2]
 LDCM0336  AC71 HCT 116 C225(0.97); C226(0.97)  LDD0653  [2]
 LDCM0337  AC72 HCT 116 C225(0.94); C226(0.94)  LDD0654  [2]
 LDCM0338  AC73 HCT 116 C225(1.15); C226(1.15)  LDD0655  [2]
 LDCM0339  AC74 HCT 116 C225(1.12); C226(1.12)  LDD0656  [2]
 LDCM0340  AC75 HCT 116 C225(1.33); C226(1.33)  LDD0657  [2]
 LDCM0341  AC76 HCT 116 C225(1.02); C226(1.02)  LDD0658  [2]
 LDCM0342  AC77 HCT 116 C225(0.91); C226(0.91)  LDD0659  [2]
 LDCM0343  AC78 HCT 116 C225(0.79); C226(0.79)  LDD0660  [2]
 LDCM0344  AC79 HCT 116 C225(1.05); C226(1.05)  LDD0661  [2]
 LDCM0345  AC8 HEK-293T C928(1.06); C1360(1.00)  LDD1569  [6]
 LDCM0346  AC80 HCT 116 C225(0.99); C226(0.99)  LDD0663  [2]
 LDCM0347  AC81 HCT 116 C225(0.90); C226(0.90)  LDD0664  [2]
 LDCM0348  AC82 HCT 116 C225(1.40); C226(1.40)  LDD0665  [2]
 LDCM0349  AC83 HCT 116 C225(0.95); C226(0.95)  LDD0666  [2]
 LDCM0350  AC84 HCT 116 C225(1.03); C226(1.03)  LDD0667  [2]
 LDCM0351  AC85 HCT 116 C225(1.05); C226(1.05)  LDD0668  [2]
 LDCM0352  AC86 HCT 116 C225(1.11); C226(1.11)  LDD0669  [2]
 LDCM0353  AC87 HCT 116 C225(1.12); C226(1.12)  LDD0670  [2]
 LDCM0354  AC88 HCT 116 C225(1.22); C226(1.22)  LDD0671  [2]
 LDCM0355  AC89 HCT 116 C225(1.03); C226(1.03)  LDD0672  [2]
 LDCM0357  AC90 HCT 116 C225(1.05); C226(1.05)  LDD0674  [2]
 LDCM0358  AC91 HCT 116 C225(1.24); C226(1.24)  LDD0675  [2]
 LDCM0359  AC92 HCT 116 C225(1.08); C226(1.08)  LDD0676  [2]
 LDCM0360  AC93 HCT 116 C225(1.02); C226(1.02)  LDD0677  [2]
 LDCM0361  AC94 HCT 116 C225(1.42); C226(1.42)  LDD0678  [2]
 LDCM0362  AC95 HCT 116 C225(1.02); C226(1.02)  LDD0679  [2]
 LDCM0363  AC96 HCT 116 C225(1.42); C226(1.42)  LDD0680  [2]
 LDCM0364  AC97 HCT 116 C225(1.04); C226(1.04)  LDD0681  [2]
 LDCM0248  AKOS034007472 HEK-293T C928(1.31); C1360(1.01)  LDD1511  [6]
 LDCM0356  AKOS034007680 HEK-293T C928(1.11); C1360(1.19)  LDD1570  [6]
 LDCM0275  AKOS034007705 HEK-293T C928(0.91); C1360(1.26)  LDD1514  [6]
 LDCM0367  CL1 HEK-293T C928(1.01)  LDD1571  [6]
 LDCM0368  CL10 HEK-293T C928(1.13)  LDD1572  [6]
 LDCM0369  CL100 HEK-293T C928(0.93); C1360(0.98)  LDD1573  [6]
 LDCM0370  CL101 HEK-293T C928(1.07)  LDD1574  [6]
 LDCM0371  CL102 HEK-293T C928(1.08); C1360(1.23)  LDD1575  [6]
 LDCM0372  CL103 HEK-293T C928(0.93); C1360(1.46)  LDD1576  [6]
 LDCM0373  CL104 HEK-293T C928(1.36); C1360(1.06)  LDD1577  [6]
 LDCM0374  CL105 HEK-293T C928(1.06)  LDD1578  [6]
 LDCM0375  CL106 HEK-293T C928(0.94); C1360(1.13)  LDD1579  [6]
 LDCM0376  CL107 HEK-293T C928(1.21); C1360(1.04)  LDD1580  [6]
 LDCM0377  CL108 HEK-293T C928(1.60); C1360(1.02)  LDD1581  [6]
 LDCM0378  CL109 HEK-293T C928(1.30)  LDD1582  [6]
 LDCM0379  CL11 HEK-293T C928(0.90)  LDD1583  [6]
 LDCM0380  CL110 HEK-293T C928(0.82); C1360(1.14)  LDD1584  [6]
 LDCM0381  CL111 HEK-293T C928(1.40); C1360(0.86)  LDD1585  [6]
 LDCM0382  CL112 HEK-293T C928(1.18); C1360(1.15)  LDD1586  [6]
 LDCM0383  CL113 HEK-293T C928(0.98)  LDD1587  [6]
 LDCM0384  CL114 HEK-293T C928(1.11); C1360(1.65)  LDD1588  [6]
 LDCM0385  CL115 HEK-293T C928(1.06); C1360(1.64)  LDD1589  [6]
 LDCM0386  CL116 HEK-293T C928(1.34); C1360(0.89)  LDD1590  [6]
 LDCM0387  CL117 HEK-293T C928(1.14)  LDD1591  [6]
 LDCM0388  CL118 HEK-293T C928(1.02); C1360(1.23)  LDD1592  [6]
 LDCM0389  CL119 HEK-293T C928(1.27); C1360(1.20)  LDD1593  [6]
 LDCM0390  CL12 HEK-293T C928(0.96); C1360(1.20)  LDD1594  [6]
 LDCM0391  CL120 HEK-293T C928(1.31); C1360(1.01)  LDD1595  [6]
 LDCM0392  CL121 HEK-293T C928(1.16)  LDD1596  [6]
 LDCM0393  CL122 HEK-293T C928(0.96); C1360(1.13)  LDD1597  [6]
 LDCM0394  CL123 HEK-293T C928(0.86); C1360(1.70)  LDD1598  [6]
 LDCM0395  CL124 HEK-293T C928(1.11); C1360(1.11)  LDD1599  [6]
 LDCM0396  CL125 HCT 116 C225(1.27); C226(1.27)  LDD0713  [2]
 LDCM0397  CL126 HCT 116 C225(1.10); C226(1.10)  LDD0714  [2]
 LDCM0398  CL127 HCT 116 C225(0.99); C226(0.99)  LDD0715  [2]
 LDCM0399  CL128 HCT 116 C225(0.67); C226(0.67)  LDD0716  [2]
 LDCM0400  CL13 HEK-293T C928(0.84)  LDD1604  [6]
 LDCM0401  CL14 HEK-293T C928(0.97); C1360(1.14)  LDD1605  [6]
 LDCM0402  CL15 HEK-293T C928(0.87); C1360(0.77)  LDD1606  [6]
 LDCM0403  CL16 HCT 116 C225(1.36); C226(1.36)  LDD0720  [2]
 LDCM0404  CL17 HCT 116 C225(0.90); C226(0.90)  LDD0721  [2]
 LDCM0405  CL18 HCT 116 C225(0.66); C226(0.66)  LDD0722  [2]
 LDCM0406  CL19 HCT 116 C225(1.01); C226(1.01)  LDD0723  [2]
 LDCM0407  CL2 HEK-293T C928(1.14); C1360(1.23)  LDD1611  [6]
 LDCM0408  CL20 HCT 116 C225(0.86); C226(0.86)  LDD0725  [2]
 LDCM0409  CL21 HCT 116 C225(0.88); C226(0.88)  LDD0726  [2]
 LDCM0410  CL22 HCT 116 C225(0.98); C226(0.98)  LDD0727  [2]
 LDCM0411  CL23 HCT 116 C225(0.71); C226(0.71)  LDD0728  [2]
 LDCM0412  CL24 HCT 116 C225(0.73); C226(0.73)  LDD0729  [2]
 LDCM0413  CL25 HCT 116 C225(1.25); C226(1.25)  LDD0730  [2]
 LDCM0414  CL26 HCT 116 C225(0.85); C226(0.85)  LDD0731  [2]
 LDCM0415  CL27 HCT 116 C225(1.26); C226(1.26)  LDD0732  [2]
 LDCM0416  CL28 HCT 116 C225(0.92); C226(0.92)  LDD0733  [2]
 LDCM0417  CL29 HCT 116 C225(0.89); C226(0.89)  LDD0734  [2]
 LDCM0418  CL3 HEK-293T C928(1.09); C1360(1.24)  LDD1622  [6]
 LDCM0419  CL30 HCT 116 C225(0.84); C226(0.84)  LDD0736  [2]
 LDCM0420  CL31 HEK-293T C928(0.95)  LDD1624  [6]
 LDCM0421  CL32 HEK-293T C928(1.11)  LDD1625  [6]
 LDCM0422  CL33 HEK-293T C928(0.98); C1360(1.99)  LDD1626  [6]
 LDCM0423  CL34 HEK-293T C928(1.04)  LDD1627  [6]
 LDCM0424  CL35 HEK-293T C928(0.88)  LDD1628  [6]
 LDCM0425  CL36 HEK-293T C928(0.60); C1360(1.17)  LDD1629  [6]
 LDCM0426  CL37 HEK-293T C928(1.05)  LDD1630  [6]
 LDCM0428  CL39 HEK-293T C928(1.35); C1360(1.28)  LDD1632  [6]
 LDCM0429  CL4 HEK-293T C928(1.16); C1360(1.08)  LDD1633  [6]
 LDCM0430  CL40 HEK-293T C928(1.08); C1360(0.83)  LDD1634  [6]
 LDCM0431  CL41 HEK-293T C928(0.86); C1360(1.11)  LDD1635  [6]
 LDCM0432  CL42 HEK-293T C928(0.93); C1360(1.12)  LDD1636  [6]
 LDCM0433  CL43 HEK-293T C928(1.12)  LDD1637  [6]
 LDCM0434  CL44 HEK-293T C928(1.14)  LDD1638  [6]
 LDCM0435  CL45 HEK-293T C928(1.70); C1360(1.81)  LDD1639  [6]
 LDCM0436  CL46 HCT 116 C225(1.13); C226(1.13)  LDD0753  [2]
 LDCM0437  CL47 HCT 116 C225(1.30); C226(1.30)  LDD0754  [2]
 LDCM0438  CL48 HCT 116 C225(1.08); C226(1.08)  LDD0755  [2]
 LDCM0439  CL49 HCT 116 C225(1.07); C226(1.07)  LDD0756  [2]
 LDCM0440  CL5 HEK-293T C928(1.28); C1360(0.88)  LDD1644  [6]
 LDCM0441  CL50 HCT 116 C225(1.08); C226(1.08)  LDD0758  [2]
 LDCM0442  CL51 HCT 116 C225(0.94); C226(0.94)  LDD0759  [2]
 LDCM0443  CL52 HCT 116 C225(0.95); C226(0.95)  LDD0760  [2]
 LDCM0444  CL53 HCT 116 C225(1.33); C226(1.33)  LDD0761  [2]
 LDCM0445  CL54 HCT 116 C225(1.37); C226(1.37)  LDD0762  [2]
 LDCM0446  CL55 HCT 116 C225(0.81); C226(0.81)  LDD0763  [2]
 LDCM0447  CL56 HCT 116 C225(1.00); C226(1.00)  LDD0764  [2]
 LDCM0448  CL57 HCT 116 C225(1.31); C226(1.31)  LDD0765  [2]
 LDCM0449  CL58 HCT 116 C225(0.84); C226(0.84)  LDD0766  [2]
 LDCM0450  CL59 HCT 116 C225(1.13); C226(1.13)  LDD0767  [2]
 LDCM0451  CL6 HEK-293T C928(1.06); C1360(1.49)  LDD1654  [6]
 LDCM0452  CL60 HCT 116 C225(1.08); C226(1.08)  LDD0769  [2]
 LDCM0453  CL61 HCT 116 C225(1.02); C226(1.02)  LDD0770  [2]
 LDCM0454  CL62 HCT 116 C225(1.06); C226(1.06)  LDD0771  [2]
 LDCM0455  CL63 HCT 116 C225(0.98); C226(0.98)  LDD0772  [2]
 LDCM0456  CL64 HCT 116 C225(1.22); C226(1.22)  LDD0773  [2]
 LDCM0457  CL65 HCT 116 C225(0.96); C226(0.96)  LDD0774  [2]
 LDCM0458  CL66 HCT 116 C225(1.10); C226(1.10)  LDD0775  [2]
 LDCM0459  CL67 HCT 116 C225(0.86); C226(0.86)  LDD0776  [2]
 LDCM0460  CL68 HCT 116 C225(1.23); C226(1.23)  LDD0777  [2]
 LDCM0461  CL69 HCT 116 C225(1.33); C226(1.33)  LDD0778  [2]
 LDCM0462  CL7 HEK-293T C928(1.08)  LDD1665  [6]
 LDCM0463  CL70 HCT 116 C225(0.87); C226(0.87)  LDD0780  [2]
 LDCM0464  CL71 HCT 116 C225(1.13); C226(1.13)  LDD0781  [2]
 LDCM0465  CL72 HCT 116 C225(1.02); C226(1.02)  LDD0782  [2]
 LDCM0466  CL73 HCT 116 C225(1.05); C226(1.05)  LDD0783  [2]
 LDCM0467  CL74 HCT 116 C225(0.99); C226(0.99)  LDD0784  [2]
 LDCM0469  CL76 HEK-293T C928(1.57); C1360(0.85)  LDD1672  [6]
 LDCM0470  CL77 HEK-293T C928(1.23); C1360(1.00)  LDD1673  [6]
 LDCM0471  CL78 HEK-293T C928(0.92); C1360(1.08)  LDD1674  [6]
 LDCM0472  CL79 HEK-293T C928(1.40)  LDD1675  [6]
 LDCM0473  CL8 HEK-293T C928(0.85)  LDD1676  [6]
 LDCM0474  CL80 HEK-293T C928(0.85)  LDD1677  [6]
 LDCM0475  CL81 HEK-293T C928(1.28); C1360(1.33)  LDD1678  [6]
 LDCM0476  CL82 HEK-293T C928(1.03)  LDD1679  [6]
 LDCM0477  CL83 HEK-293T C928(1.11)  LDD1680  [6]
 LDCM0478  CL84 HEK-293T C928(0.82); C1360(1.46)  LDD1681  [6]
 LDCM0479  CL85 HEK-293T C928(1.25)  LDD1682  [6]
 LDCM0480  CL86 HEK-293T C928(1.07); C1360(1.12)  LDD1683  [6]
 LDCM0481  CL87 HEK-293T C928(1.62); C1360(1.29)  LDD1684  [6]
 LDCM0482  CL88 HEK-293T C928(1.01); C1360(1.20)  LDD1685  [6]
 LDCM0483  CL89 HEK-293T C928(1.13); C1360(0.95)  LDD1686  [6]
 LDCM0484  CL9 HEK-293T C928(1.03); C1360(1.18)  LDD1687  [6]
 LDCM0485  CL90 HEK-293T C928(1.03); C1360(1.20)  LDD1688  [6]
 LDCM0486  CL91 HEK-293T C928(1.17)  LDD1689  [6]
 LDCM0487  CL92 HEK-293T C928(0.95)  LDD1690  [6]
 LDCM0488  CL93 HEK-293T C928(1.45); C1360(1.44)  LDD1691  [6]
 LDCM0489  CL94 HEK-293T C928(1.11)  LDD1692  [6]
 LDCM0490  CL95 HEK-293T C928(1.01)  LDD1693  [6]
 LDCM0491  CL96 HEK-293T C928(1.13); C1360(1.18)  LDD1694  [6]
 LDCM0492  CL97 HEK-293T C928(1.12)  LDD1695  [6]
 LDCM0493  CL98 HEK-293T C928(1.17); C1360(0.98)  LDD1696  [6]
 LDCM0494  CL99 HEK-293T C928(1.18); C1360(1.22)  LDD1697  [6]
 LDCM0495  E2913 HEK-293T C928(1.29); C1360(1.62)  LDD1698  [6]
 LDCM0586  Fragment28 Ramos C1360(1.01)  LDD2198  [1]
 LDCM0468  Fragment33 HCT 116 C225(1.17); C226(1.17)  LDD0785  [2]
 LDCM0596  Fragment38 Ramos C1360(0.84)  LDD2203  [1]
 LDCM0427  Fragment51 HEK-293T C928(0.96); C1360(0.94)  LDD1631  [6]
 LDCM0610  Fragment52 Ramos C1360(2.22)  LDD2204  [1]
 LDCM0022  KB02 EoL-1 C607(3.63)  LDD2324  [7]
 LDCM0023  KB03 EoL-1 C607(4.49)  LDD2741  [7]
 LDCM0024  KB05 EoL-1 C607(4.26)  LDD3158  [7]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Kallikrein-6 (KLK6) Peptidase S1 family Q92876
Serine protease HTRA2, mitochondrial (HTRA2) Peptidase S1C family O43464
Serine/threonine-protein phosphatase PGAM5, mitochondrial (PGAM5) Phosphoglycerate mutase family Q96HS1
RAC-alpha serine/threonine-protein kinase (AKT1) AGC Ser/Thr protein kinase family P31749
Mitogen-activated protein kinase kinase kinase 5 (MAP3K5) STE Ser/Thr protein kinase family Q99683
Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3) STE Ser/Thr protein kinase family P46734
Ribose-phosphate pyrophosphokinase 1 (PRPS1) Ribose-phosphate pyrophosphokinase family P60891
Thioredoxin (TXN) Thioredoxin family P10599
TNF receptor-associated factor 2 (TRAF2) TNF receptor-associated factor family Q12933
Eukaryotic translation initiation factor 2 subunit 3 (EIF2S3) Classic translation factor GTPase family P41091
Transporter and channel
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Beta-arrestin-1 (ARRB1) Arrestin family P49407
Beta-arrestin-2 (ARRB2) Arrestin family P32121
Huntingtin (HTT) Huntingtin family P42858
Alpha-crystallin A chain (CRYAA) Small heat shock protein (HSP20) family P02489
Calcium and integrin-binding protein 1 (CIB1) . Q99828
Other
Click To Hide/Show 14 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein beta/alpha (YWHAB) 14-3-3 family P31946
14-3-3 protein eta (YWHAH) 14-3-3 family Q04917
Calcineurin subunit B type 1 (PPP3R1) Calcineurin regulatory subunit family P63098
Death domain-associated protein 6 (DAXX) DAXX family Q9UER7
Cytoplasmic dynein 1 heavy chain 1 (DYNC1H1) Dynein heavy chain family Q14204
Eukaryotic translation initiation factor 2 subunit 2 (EIF2S2) EIF-2-beta/eIF-5 family P20042
Progranulin (GRN) Granulin family P28799
Ganglioside-induced differentiation-associated protein 1 (GDAP1) GST superfamily Q8TB36
Heat shock-related 70 kDa protein 2 (HSPA2) Heat shock protein 70 family P54652
Cytoplasmic 60S subunit biogenesis factor ZNF622 (ZNF622) REI1 family Q969S3
Heat shock protein beta-1 (HSPB1) Small heat shock protein (HSP20) family P04792
Survival motor neuron protein (SMN1; SMN2) SMN family Q16637
Disabled homolog 2-interacting protein (DAB2IP) . Q5VWQ8
Microspherule protein 1 (MCRS1) . Q96EZ8

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gs-4977 . D0D0OT
Gs-4997 . D0RN3S
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Msc2032964a Small molecular drug D0F0XZ
Pmid23147077c10 Small molecular drug D0Q0YV

References

1 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
2 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.
3 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.
4 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
5 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
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
7 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