Details of the Target

General Information of Target

Target ID LDTP05369
Target Name Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1)
Gene Name MAP2K1
Gene ID 5604
Synonyms
MEK1; PRKMK1; Dual specificity mitogen-activated protein kinase kinase 1; MAP kinase kinase 1; MAPKK 1; MKK1; EC 2.7.12.2; ERK activator kinase 1; MAPK/ERK kinase 1; MEK 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase subfamily
Subcellular location
Cytoplasm, cytoskeleton, microtubule organizing center, centrosome
Function
Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones to their cell-surface receptors activates RAS and this initiates RAF1 activation. RAF1 then further activates the dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2. Both MAP2K1/MEK1 and MAP2K2/MEK2 function specifically in the MAPK/ERK cascade, and catalyze the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2, leading to their activation and further transduction of the signal within the MAPK/ERK cascade. Activates BRAF in a KSR1 or KSR2-dependent manner; by binding to KSR1 or KSR2 releases the inhibitory intramolecular interaction between KSR1 or KSR2 protein kinase and N-terminal domains which promotes KSR1 or KSR2-BRAF dimerization and BRAF activation. Depending on the cellular context, this pathway mediates diverse biological functions such as cell growth, adhesion, survival and differentiation, predominantly through the regulation of transcription, metabolism and cytoskeletal rearrangements. One target of the MAPK/ERK cascade is peroxisome proliferator-activated receptor gamma (PPARG), a nuclear receptor that promotes differentiation and apoptosis. MAP2K1/MEK1 has been shown to export PPARG from the nucleus. The MAPK/ERK cascade is also involved in the regulation of endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC), as well as in the fragmentation of the Golgi apparatus during mitosis.
TTD ID
T35940
Uniprot ID
Q02750
DrugMap ID
TTAW3TO
Ensemble ID
ENST00000307102.10
HGNC ID
HGNC:6840
ChEMBL ID
CHEMBL3587

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.P124S .
CAL148 SNV: p.E203K DBIA    Probe Info 
ECC2 SNV: p.K57N DBIA    Probe Info 
HS936T SNV: p.P124L DBIA    Probe Info 
HUPT3 SNV: p.Q10K DBIA    Probe Info 
MOLT4 SNV: p.D67N IA-alkyne    Probe Info 
OCUM1 SNV: p.Q56P DBIA    Probe Info 
PF382 SNV: p.V211A DBIA    Probe Info 
SNGM SNV: p.G80S DBIA    Probe Info 

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  		14.15  LDD0402  [1]
TH211
 Probe Info  		Y240(8.11)  LDD0257  [2]
ONAyne
 Probe Info  		K59(0.76)  LDD0274  [3]
STPyne
 Probe Info  		K36(7.88)  LDD0277  [3]
THZ1-DTB
 Probe Info  		C376(1.05)  LDD0460  [4]
DBIA
 Probe Info  		C277(0.99)  LDD0078  [5]
AMP probe
 Probe Info  		N.A.  LDD0200  [6]
ATP probe
 Probe Info  		K192(0.00); K104(0.00)  LDD0199  [6]
4-Iodoacetamidophenylacetylene
 Probe Info  		C277(0.00); C207(0.00); C376(0.00); C341(0.00)  LDD0038  [7]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [8]
Lodoacetamide azide
 Probe Info  		C341(0.00); C277(0.00); C207(0.00); C376(0.00)  LDD0037  [7]
ATP probe
 Probe Info  		K5(0.00); K4(0.00)  LDD0035  [9]
NAIA_4
 Probe Info  		C207(0.00); C277(0.00)  LDD2226  [10]
IPM
 Probe Info  		N.A.  LDD0005  [11]
Phosphinate-6
 Probe Info  		C277(0.00); C207(0.00)  LDD0018  [12]
1c-yne
 Probe Info  		K353(0.00); K205(0.00)  LDD0228  [13]
AOyne
 Probe Info  		9.80  LDD0443  [14]
NAIA_5
 Probe Info  		N.A.  LDD2223  [10]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C290
 Probe Info  		5.03  LDD1960  [15]
FFF probe14
 Probe Info  		12.02  LDD0477  [16]
FFF probe4
 Probe Info  		15.62  LDD0466  [16]
STS-1
 Probe Info  		N.A.  LDD0137  [17]
STS-2
 Probe Info  		N.A.  LDD0138  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C277(0.99)  LDD0531  [5]
 LDCM0215  AC10 HCT 116 C277(1.05)  LDD0532  [5]
 LDCM0216  AC100 HCT 116 C277(0.82)  LDD0533  [5]
 LDCM0217  AC101 HCT 116 C277(1.32)  LDD0534  [5]
 LDCM0218  AC102 HCT 116 C277(1.13)  LDD0535  [5]
 LDCM0219  AC103 HCT 116 C277(1.27)  LDD0536  [5]
 LDCM0220  AC104 HCT 116 C277(1.08)  LDD0537  [5]
 LDCM0221  AC105 HCT 116 C277(1.66)  LDD0538  [5]
 LDCM0222  AC106 HCT 116 C277(1.70)  LDD0539  [5]
 LDCM0223  AC107 HCT 116 C277(2.01)  LDD0540  [5]
 LDCM0224  AC108 HCT 116 C277(0.91)  LDD0541  [5]
 LDCM0225  AC109 HCT 116 C277(1.01)  LDD0542  [5]
 LDCM0226  AC11 HCT 116 C277(1.02)  LDD0543  [5]
 LDCM0227  AC110 HCT 116 C277(0.96)  LDD0544  [5]
 LDCM0228  AC111 HCT 116 C277(1.07)  LDD0545  [5]
 LDCM0229  AC112 HCT 116 C277(1.46)  LDD0546  [5]
 LDCM0230  AC113 HCT 116 C277(1.14)  LDD0547  [5]
 LDCM0231  AC114 HCT 116 C277(1.15)  LDD0548  [5]
 LDCM0232  AC115 HCT 116 C277(1.28)  LDD0549  [5]
 LDCM0233  AC116 HCT 116 C277(1.33)  LDD0550  [5]
 LDCM0234  AC117 HCT 116 C277(1.33)  LDD0551  [5]
 LDCM0235  AC118 HCT 116 C277(1.41)  LDD0552  [5]
 LDCM0236  AC119 HCT 116 C277(1.06)  LDD0553  [5]
 LDCM0237  AC12 HCT 116 C277(0.94)  LDD0554  [5]
 LDCM0238  AC120 HCT 116 C277(1.04)  LDD0555  [5]
 LDCM0239  AC121 HCT 116 C277(1.66)  LDD0556  [5]
 LDCM0240  AC122 HCT 116 C277(0.90)  LDD0557  [5]
 LDCM0241  AC123 HCT 116 C277(1.75)  LDD0558  [5]
 LDCM0242  AC124 HCT 116 C277(1.15)  LDD0559  [5]
 LDCM0243  AC125 HCT 116 C277(1.00)  LDD0560  [5]
 LDCM0244  AC126 HCT 116 C277(1.14)  LDD0561  [5]
 LDCM0245  AC127 HCT 116 C277(1.25)  LDD0562  [5]
 LDCM0246  AC128 HCT 116 C277(1.66)  LDD0563  [5]
 LDCM0247  AC129 HCT 116 C277(1.07)  LDD0564  [5]
 LDCM0249  AC130 HCT 116 C277(1.05)  LDD0566  [5]
 LDCM0250  AC131 HCT 116 C277(1.28)  LDD0567  [5]
 LDCM0251  AC132 HCT 116 C277(1.39)  LDD0568  [5]
 LDCM0252  AC133 HCT 116 C277(1.38)  LDD0569  [5]
 LDCM0253  AC134 HCT 116 C277(1.46)  LDD0570  [5]
 LDCM0254  AC135 HCT 116 C277(1.78)  LDD0571  [5]
 LDCM0255  AC136 HCT 116 C277(1.40)  LDD0572  [5]
 LDCM0256  AC137 HCT 116 C277(1.20)  LDD0573  [5]
 LDCM0257  AC138 HCT 116 C277(1.27)  LDD0574  [5]
 LDCM0258  AC139 HCT 116 C277(1.76)  LDD0575  [5]
 LDCM0259  AC14 HCT 116 C277(1.06)  LDD0576  [5]
 LDCM0260  AC140 HCT 116 C277(1.91)  LDD0577  [5]
 LDCM0261  AC141 HCT 116 C277(1.69)  LDD0578  [5]
 LDCM0262  AC142 HCT 116 C277(1.12)  LDD0579  [5]
 LDCM0263  AC143 HCT 116 C277(1.02)  LDD0580  [5]
 LDCM0264  AC144 HCT 116 C277(1.19)  LDD0581  [5]
 LDCM0265  AC145 HCT 116 C277(1.07)  LDD0582  [5]
 LDCM0266  AC146 HCT 116 C277(1.33)  LDD0583  [5]
 LDCM0267  AC147 HCT 116 C277(1.17)  LDD0584  [5]
 LDCM0268  AC148 HCT 116 C277(1.60)  LDD0585  [5]
 LDCM0269  AC149 HCT 116 C277(1.24)  LDD0586  [5]
 LDCM0270  AC15 HCT 116 C277(1.09)  LDD0587  [5]
 LDCM0271  AC150 HCT 116 C277(1.22)  LDD0588  [5]
 LDCM0272  AC151 HCT 116 C277(1.01)  LDD0589  [5]
 LDCM0273  AC152 HCT 116 C277(1.25)  LDD0590  [5]
 LDCM0274  AC153 HCT 116 C277(1.69)  LDD0591  [5]
 LDCM0621  AC154 HCT 116 C277(1.15)  LDD2158  [5]
 LDCM0622  AC155 HCT 116 C277(1.13)  LDD2159  [5]
 LDCM0623  AC156 HCT 116 C277(1.08)  LDD2160  [5]
 LDCM0624  AC157 HCT 116 C277(0.95)  LDD2161  [5]
 LDCM0276  AC17 HCT 116 C277(1.09)  LDD0593  [5]
 LDCM0277  AC18 HCT 116 C277(1.06)  LDD0594  [5]
 LDCM0278  AC19 HCT 116 C277(0.98)  LDD0595  [5]
 LDCM0279  AC2 HCT 116 C277(1.13)  LDD0596  [5]
 LDCM0280  AC20 HCT 116 C277(0.97)  LDD0597  [5]
 LDCM0281  AC21 HCT 116 C277(1.06)  LDD0598  [5]
 LDCM0282  AC22 HCT 116 C277(0.94)  LDD0599  [5]
 LDCM0283  AC23 HCT 116 C277(0.93)  LDD0600  [5]
 LDCM0284  AC24 HCT 116 C277(0.96)  LDD0601  [5]
 LDCM0285  AC25 HCT 116 C277(1.11)  LDD0602  [5]
 LDCM0286  AC26 HCT 116 C277(1.15)  LDD0603  [5]
 LDCM0287  AC27 HCT 116 C277(1.54)  LDD0604  [5]
 LDCM0288  AC28 HCT 116 C277(1.52)  LDD0605  [5]
 LDCM0289  AC29 HCT 116 C277(1.30)  LDD0606  [5]
 LDCM0290  AC3 HCT 116 C277(0.97)  LDD0607  [5]
 LDCM0291  AC30 HCT 116 C277(1.18)  LDD0608  [5]
 LDCM0292  AC31 HCT 116 C277(1.46)  LDD0609  [5]
 LDCM0293  AC32 HCT 116 C277(2.01)  LDD0610  [5]
 LDCM0294  AC33 HCT 116 C277(1.32)  LDD0611  [5]
 LDCM0295  AC34 HCT 116 C277(1.59)  LDD0612  [5]
 LDCM0296  AC35 HCT 116 C277(0.88)  LDD0613  [5]
 LDCM0297  AC36 HCT 116 C277(0.82)  LDD0614  [5]
 LDCM0298  AC37 HCT 116 C277(1.04)  LDD0615  [5]
 LDCM0299  AC38 HCT 116 C277(0.96)  LDD0616  [5]
 LDCM0300  AC39 HCT 116 C277(1.02)  LDD0617  [5]
 LDCM0301  AC4 HCT 116 C277(0.96)  LDD0618  [5]
 LDCM0302  AC40 HCT 116 C277(1.19)  LDD0619  [5]
 LDCM0303  AC41 HCT 116 C277(0.90)  LDD0620  [5]
 LDCM0304  AC42 HCT 116 C277(1.06)  LDD0621  [5]
 LDCM0305  AC43 HCT 116 C277(1.14)  LDD0622  [5]
 LDCM0306  AC44 HCT 116 C277(1.04)  LDD0623  [5]
 LDCM0307  AC45 HCT 116 C277(1.12)  LDD0624  [5]
 LDCM0308  AC46 HCT 116 C277(1.10)  LDD0625  [5]
 LDCM0309  AC47 HCT 116 C277(0.87)  LDD0626  [5]
 LDCM0310  AC48 HCT 116 C277(1.17)  LDD0627  [5]
 LDCM0311  AC49 HCT 116 C277(1.37)  LDD0628  [5]
 LDCM0312  AC5 HCT 116 C277(1.07)  LDD0629  [5]
 LDCM0313  AC50 HCT 116 C277(1.22)  LDD0630  [5]
 LDCM0314  AC51 HCT 116 C277(1.00)  LDD0631  [5]
 LDCM0315  AC52 HCT 116 C277(1.10)  LDD0632  [5]
 LDCM0316  AC53 HCT 116 C277(1.25)  LDD0633  [5]
 LDCM0317  AC54 HCT 116 C277(1.24)  LDD0634  [5]
 LDCM0318  AC55 HCT 116 C277(1.25)  LDD0635  [5]
 LDCM0319  AC56 HCT 116 C277(1.52)  LDD0636  [5]
 LDCM0320  AC57 HCT 116 C277(1.91)  LDD0637  [5]
 LDCM0321  AC58 HCT 116 C277(1.97)  LDD0638  [5]
 LDCM0322  AC59 HCT 116 C277(1.69)  LDD0639  [5]
 LDCM0323  AC6 HCT 116 C277(1.05)  LDD0640  [5]
 LDCM0324  AC60 HCT 116 C277(1.64)  LDD0641  [5]
 LDCM0325  AC61 HCT 116 C277(1.30)  LDD0642  [5]
 LDCM0326  AC62 HCT 116 C277(1.97)  LDD0643  [5]
 LDCM0327  AC63 HCT 116 C277(1.26)  LDD0644  [5]
 LDCM0328  AC64 HCT 116 C277(1.75)  LDD0645  [5]
 LDCM0329  AC65 HCT 116 C277(2.26)  LDD0646  [5]
 LDCM0330  AC66 HCT 116 C277(2.04)  LDD0647  [5]
 LDCM0331  AC67 HCT 116 C277(2.52)  LDD0648  [5]
 LDCM0332  AC68 HCT 116 C277(1.16)  LDD0649  [5]
 LDCM0333  AC69 HCT 116 C277(1.06)  LDD0650  [5]
 LDCM0334  AC7 HCT 116 C277(0.94)  LDD0651  [5]
 LDCM0335  AC70 HCT 116 C277(1.02)  LDD0652  [5]
 LDCM0336  AC71 HCT 116 C277(0.90)  LDD0653  [5]
 LDCM0337  AC72 HCT 116 C277(1.05)  LDD0654  [5]
 LDCM0338  AC73 HCT 116 C277(1.19)  LDD0655  [5]
 LDCM0339  AC74 HCT 116 C277(1.32)  LDD0656  [5]
 LDCM0340  AC75 HCT 116 C277(1.31)  LDD0657  [5]
 LDCM0341  AC76 HCT 116 C277(1.10)  LDD0658  [5]
 LDCM0342  AC77 HCT 116 C277(1.02)  LDD0659  [5]
 LDCM0343  AC78 HCT 116 C277(0.99)  LDD0660  [5]
 LDCM0344  AC79 HCT 116 C277(1.27)  LDD0661  [5]
 LDCM0345  AC8 HCT 116 C277(1.02)  LDD0662  [5]
 LDCM0346  AC80 HCT 116 C277(1.27)  LDD0663  [5]
 LDCM0347  AC81 HCT 116 C277(1.03)  LDD0664  [5]
 LDCM0348  AC82 HCT 116 C277(1.26)  LDD0665  [5]
 LDCM0349  AC83 HCT 116 C277(1.70)  LDD0666  [5]
 LDCM0350  AC84 HCT 116 C277(1.52)  LDD0667  [5]
 LDCM0351  AC85 HCT 116 C277(1.38)  LDD0668  [5]
 LDCM0352  AC86 HCT 116 C277(1.41)  LDD0669  [5]
 LDCM0353  AC87 HCT 116 C277(1.24)  LDD0670  [5]
 LDCM0354  AC88 HCT 116 C277(1.21)  LDD0671  [5]
 LDCM0355  AC89 HCT 116 C277(1.48)  LDD0672  [5]
 LDCM0357  AC90 HCT 116 C277(1.15)  LDD0674  [5]
 LDCM0358  AC91 HCT 116 C277(1.56)  LDD0675  [5]
 LDCM0359  AC92 HCT 116 C277(1.57)  LDD0676  [5]
 LDCM0360  AC93 HCT 116 C277(1.22)  LDD0677  [5]
 LDCM0361  AC94 HCT 116 C277(1.26)  LDD0678  [5]
 LDCM0362  AC95 HCT 116 C277(1.39)  LDD0679  [5]
 LDCM0363  AC96 HCT 116 C277(1.30)  LDD0680  [5]
 LDCM0364  AC97 HCT 116 C277(1.61)  LDD0681  [5]
 LDCM0365  AC98 HCT 116 C277(1.78)  LDD0682  [5]
 LDCM0366  AC99 HCT 116 C277(1.32)  LDD0683  [5]
 LDCM0248  AKOS034007472 HCT 116 C277(1.04)  LDD0565  [5]
 LDCM0356  AKOS034007680 HCT 116 C277(1.03)  LDD0673  [5]
 LDCM0275  AKOS034007705 HCT 116 C277(1.35)  LDD0592  [5]
 LDCM0156  Aniline NCI-H1299 11.79  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C277(0.99)  LDD0078  [5]
 LDCM0630  CCW28-3 231MFP C277(1.23)  LDD2214  [18]
 LDCM0632  CL-Sc Hep-G2 C341(1.85)  LDD2227  [10]
 LDCM0367  CL1 HCT 116 C277(1.08)  LDD0684  [5]
 LDCM0368  CL10 HCT 116 C277(1.17)  LDD0685  [5]
 LDCM0369  CL100 HCT 116 C277(1.02)  LDD0686  [5]
 LDCM0370  CL101 HCT 116 C277(1.15)  LDD0687  [5]
 LDCM0371  CL102 HCT 116 C277(0.84)  LDD0688  [5]
 LDCM0372  CL103 HCT 116 C277(0.94)  LDD0689  [5]
 LDCM0373  CL104 HCT 116 C277(1.06)  LDD0690  [5]
 LDCM0374  CL105 HCT 116 C277(1.22)  LDD0691  [5]
 LDCM0375  CL106 HCT 116 C277(1.24)  LDD0692  [5]
 LDCM0376  CL107 HCT 116 C277(1.19)  LDD0693  [5]
 LDCM0377  CL108 HCT 116 C277(1.30)  LDD0694  [5]
 LDCM0378  CL109 HCT 116 C277(1.06)  LDD0695  [5]
 LDCM0379  CL11 HCT 116 C277(1.07)  LDD0696  [5]
 LDCM0380  CL110 HCT 116 C277(1.20)  LDD0697  [5]
 LDCM0381  CL111 HCT 116 C277(1.22)  LDD0698  [5]
 LDCM0382  CL112 HCT 116 C277(1.02)  LDD0699  [5]
 LDCM0383  CL113 HCT 116 C277(1.46)  LDD0700  [5]
 LDCM0384  CL114 HCT 116 C277(1.22)  LDD0701  [5]
 LDCM0385  CL115 HCT 116 C277(1.25)  LDD0702  [5]
 LDCM0386  CL116 HCT 116 C277(1.57)  LDD0703  [5]
 LDCM0387  CL117 HCT 116 C277(1.10)  LDD0704  [5]
 LDCM0388  CL118 HCT 116 C277(0.95)  LDD0705  [5]
 LDCM0389  CL119 HCT 116 C277(1.22)  LDD0706  [5]
 LDCM0390  CL12 HCT 116 C277(1.23)  LDD0707  [5]
 LDCM0391  CL120 HCT 116 C277(1.15)  LDD0708  [5]
 LDCM0392  CL121 HCT 116 C277(1.12)  LDD0709  [5]
 LDCM0393  CL122 HCT 116 C277(1.19)  LDD0710  [5]
 LDCM0394  CL123 HCT 116 C277(1.07)  LDD0711  [5]
 LDCM0395  CL124 HCT 116 C277(1.29)  LDD0712  [5]
 LDCM0396  CL125 HCT 116 C277(1.10)  LDD0713  [5]
 LDCM0397  CL126 HCT 116 C277(1.47)  LDD0714  [5]
 LDCM0398  CL127 HCT 116 C277(1.25)  LDD0715  [5]
 LDCM0399  CL128 HCT 116 C277(1.80)  LDD0716  [5]
 LDCM0400  CL13 HCT 116 C277(0.96)  LDD0717  [5]
 LDCM0401  CL14 HCT 116 C277(1.05)  LDD0718  [5]
 LDCM0402  CL15 HCT 116 C277(0.94)  LDD0719  [5]
 LDCM0403  CL16 HCT 116 C277(1.33)  LDD0720  [5]
 LDCM0404  CL17 HCT 116 C277(0.99)  LDD0721  [5]
 LDCM0405  CL18 HCT 116 C277(1.17)  LDD0722  [5]
 LDCM0406  CL19 HCT 116 C277(1.06)  LDD0723  [5]
 LDCM0407  CL2 HCT 116 C277(1.06)  LDD0724  [5]
 LDCM0408  CL20 HCT 116 C277(1.28)  LDD0725  [5]
 LDCM0409  CL21 HCT 116 C277(1.13)  LDD0726  [5]
 LDCM0410  CL22 HCT 116 C277(1.31)  LDD0727  [5]
 LDCM0411  CL23 HCT 116 C277(1.05)  LDD0728  [5]
 LDCM0412  CL24 HCT 116 C277(1.28)  LDD0729  [5]
 LDCM0413  CL25 HCT 116 C277(1.38)  LDD0730  [5]
 LDCM0414  CL26 HCT 116 C277(1.11)  LDD0731  [5]
 LDCM0415  CL27 HCT 116 C277(1.40)  LDD0732  [5]
 LDCM0416  CL28 HCT 116 C277(1.30)  LDD0733  [5]
 LDCM0417  CL29 HCT 116 C277(1.24)  LDD0734  [5]
 LDCM0418  CL3 HCT 116 C277(0.93)  LDD0735  [5]
 LDCM0419  CL30 HCT 116 C277(1.08)  LDD0736  [5]
 LDCM0420  CL31 HCT 116 C277(1.08)  LDD0737  [5]
 LDCM0421  CL32 HCT 116 C277(1.36)  LDD0738  [5]
 LDCM0422  CL33 HCT 116 C277(1.11)  LDD0739  [5]
 LDCM0423  CL34 HCT 116 C277(1.37)  LDD0740  [5]
 LDCM0424  CL35 HCT 116 C277(1.50)  LDD0741  [5]
 LDCM0425  CL36 HCT 116 C277(1.35)  LDD0742  [5]
 LDCM0426  CL37 HCT 116 C277(1.11)  LDD0743  [5]
 LDCM0428  CL39 HCT 116 C277(1.66)  LDD0745  [5]
 LDCM0429  CL4 HCT 116 C277(0.94)  LDD0746  [5]
 LDCM0430  CL40 HCT 116 C277(1.01)  LDD0747  [5]
 LDCM0431  CL41 HCT 116 C277(1.13)  LDD0748  [5]
 LDCM0432  CL42 HCT 116 C277(1.24)  LDD0749  [5]
 LDCM0433  CL43 HCT 116 C277(1.63)  LDD0750  [5]
 LDCM0434  CL44 HCT 116 C277(1.17)  LDD0751  [5]
 LDCM0435  CL45 HCT 116 C277(1.44)  LDD0752  [5]
 LDCM0436  CL46 HCT 116 C277(1.25)  LDD0753  [5]
 LDCM0437  CL47 HCT 116 C277(0.96)  LDD0754  [5]
 LDCM0438  CL48 HCT 116 C277(0.88)  LDD0755  [5]
 LDCM0439  CL49 HCT 116 C277(0.99)  LDD0756  [5]
 LDCM0440  CL5 HCT 116 C277(0.93)  LDD0757  [5]
 LDCM0441  CL50 HCT 116 C277(0.96)  LDD0758  [5]
 LDCM0442  CL51 HCT 116 C277(0.89)  LDD0759  [5]
 LDCM0443  CL52 HCT 116 C277(0.94)  LDD0760  [5]
 LDCM0444  CL53 HCT 116 C277(0.81)  LDD0761  [5]
 LDCM0445  CL54 HCT 116 C277(0.88)  LDD0762  [5]
 LDCM0446  CL55 HCT 116 C277(0.84)  LDD0763  [5]
 LDCM0447  CL56 HCT 116 C277(1.04)  LDD0764  [5]
 LDCM0448  CL57 HCT 116 C277(0.89)  LDD0765  [5]
 LDCM0449  CL58 HCT 116 C277(0.92)  LDD0766  [5]
 LDCM0450  CL59 HCT 116 C277(0.94)  LDD0767  [5]
 LDCM0451  CL6 HCT 116 C277(1.04)  LDD0768  [5]
 LDCM0452  CL60 HCT 116 C277(0.91)  LDD0769  [5]
 LDCM0453  CL61 HCT 116 C277(1.20)  LDD0770  [5]
 LDCM0454  CL62 HCT 116 C277(1.08)  LDD0771  [5]
 LDCM0455  CL63 HCT 116 C277(1.10)  LDD0772  [5]
 LDCM0456  CL64 HCT 116 C277(1.22)  LDD0773  [5]
 LDCM0457  CL65 HCT 116 C277(1.15)  LDD0774  [5]
 LDCM0458  CL66 HCT 116 C277(1.32)  LDD0775  [5]
 LDCM0459  CL67 HCT 116 C277(1.10)  LDD0776  [5]
 LDCM0460  CL68 HCT 116 C277(1.21)  LDD0777  [5]
 LDCM0461  CL69 HCT 116 C277(1.14)  LDD0778  [5]
 LDCM0462  CL7 HCT 116 C277(1.11)  LDD0779  [5]
 LDCM0463  CL70 HCT 116 C277(1.14)  LDD0780  [5]
 LDCM0464  CL71 HCT 116 C277(1.22)  LDD0781  [5]
 LDCM0465  CL72 HCT 116 C277(1.20)  LDD0782  [5]
 LDCM0466  CL73 HCT 116 C277(1.26)  LDD0783  [5]
 LDCM0467  CL74 HCT 116 C277(1.18)  LDD0784  [5]
 LDCM0469  CL76 HCT 116 C277(0.89)  LDD0786  [5]
 LDCM0470  CL77 HCT 116 C277(0.83)  LDD0787  [5]
 LDCM0471  CL78 HCT 116 C277(1.04)  LDD0788  [5]
 LDCM0472  CL79 HCT 116 C277(0.94)  LDD0789  [5]
 LDCM0473  CL8 HCT 116 C277(1.08)  LDD0790  [5]
 LDCM0474  CL80 HCT 116 C277(0.86)  LDD0791  [5]
 LDCM0475  CL81 HCT 116 C277(0.95)  LDD0792  [5]
 LDCM0476  CL82 HCT 116 C277(0.96)  LDD0793  [5]
 LDCM0477  CL83 HCT 116 C277(0.88)  LDD0794  [5]
 LDCM0478  CL84 HCT 116 C277(0.96)  LDD0795  [5]
 LDCM0479  CL85 HCT 116 C277(0.94)  LDD0796  [5]
 LDCM0480  CL86 HCT 116 C277(0.86)  LDD0797  [5]
 LDCM0481  CL87 HCT 116 C277(0.84)  LDD0798  [5]
 LDCM0482  CL88 HCT 116 C277(0.87)  LDD0799  [5]
 LDCM0483  CL89 HCT 116 C277(0.84)  LDD0800  [5]
 LDCM0484  CL9 HCT 116 C277(1.10)  LDD0801  [5]
 LDCM0485  CL90 HCT 116 C277(0.89)  LDD0802  [5]
 LDCM0486  CL91 HCT 116 C277(1.37)  LDD0803  [5]
 LDCM0487  CL92 HCT 116 C277(1.20)  LDD0804  [5]
 LDCM0488  CL93 HCT 116 C277(1.19)  LDD0805  [5]
 LDCM0489  CL94 HCT 116 C277(1.17)  LDD0806  [5]
 LDCM0490  CL95 HCT 116 C277(1.09)  LDD0807  [5]
 LDCM0491  CL96 HCT 116 C277(1.37)  LDD0808  [5]
 LDCM0492  CL97 HCT 116 C277(1.30)  LDD0809  [5]
 LDCM0493  CL98 HCT 116 C277(1.24)  LDD0810  [5]
 LDCM0494  CL99 HCT 116 C277(1.19)  LDD0811  [5]
 LDCM0495  E2913 HEK-293T C277(0.92); C376(1.03)  LDD1698  [19]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C207(5.75)  LDD1702  [20]
 LDCM0625  F8 Ramos C341(1.22); C207(0.93); C277(1.02)  LDD2187  [21]
 LDCM0572  Fragment10 Ramos C341(0.72); C207(1.30)  LDD2189  [21]
 LDCM0573  Fragment11 Ramos C341(0.02); C207(0.40); C277(0.58)  LDD2190  [21]
 LDCM0574  Fragment12 Ramos C341(0.90); C207(1.64)  LDD2191  [21]
 LDCM0575  Fragment13 Ramos C341(1.12); C207(1.31)  LDD2192  [21]
 LDCM0576  Fragment14 Ramos C341(0.83); C207(1.88); C277(0.67)  LDD2193  [21]
 LDCM0579  Fragment20 Ramos C341(1.04); C207(1.20)  LDD2194  [21]
 LDCM0580  Fragment21 Ramos C341(0.86); C207(0.99)  LDD2195  [21]
 LDCM0582  Fragment23 Ramos C341(1.07); C207(1.96)  LDD2196  [21]
 LDCM0578  Fragment27 Ramos C341(0.89); C207(1.21)  LDD2197  [21]
 LDCM0586  Fragment28 Ramos C341(0.74); C207(0.51); C277(0.97)  LDD2198  [21]
 LDCM0588  Fragment30 Ramos C341(1.19); C207(2.02)  LDD2199  [21]
 LDCM0589  Fragment31 Ramos C341(1.00); C207(0.89)  LDD2200  [21]
 LDCM0590  Fragment32 Ramos C341(0.70); C207(1.67)  LDD2201  [21]
 LDCM0468  Fragment33 HCT 116 C277(1.14)  LDD0785  [5]
 LDCM0596  Fragment38 Ramos C341(1.05); C207(1.43)  LDD2203  [21]
 LDCM0566  Fragment4 Ramos C341(0.95); C207(0.68); C277(0.42)  LDD2184  [21]
 LDCM0427  Fragment51 HCT 116 C277(1.55)  LDD0744  [5]
 LDCM0610  Fragment52 Ramos C341(1.34); C207(1.43)  LDD2204  [21]
 LDCM0614  Fragment56 Ramos C341(1.32); C207(1.18)  LDD2205  [21]
 LDCM0569  Fragment7 Ramos C341(0.63); C207(1.05); C277(0.56)  LDD2186  [21]
 LDCM0571  Fragment9 Ramos C341(0.86); C207(1.37)  LDD2188  [21]
 LDCM0022  KB02 HEK-293T C277(0.98); C376(1.06)  LDD1492  [19]
 LDCM0023  KB03 HEK-293T C277(0.91); C376(1.31)  LDD1497  [19]
 LDCM0024  KB05 HMCB C277(1.96)  LDD3312  [22]
 LDCM0627  NUDT7-COV-1 HEK-293T C207(1.19); C207(0.90)  LDD2206  [23]
 LDCM0628  OTUB2-COV-1 HEK-293T C207(0.54); C207(0.41)  LDD2207  [23]
 LDCM0131  RA190 MM1.R C277(1.16)  LDD0304  [24]
 LDCM0021  THZ1 HeLa S3 C376(1.05)  LDD0460  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serine/threonine-protein kinase VRK2 (VRK2) CK1 Ser/Thr protein kinase family Q86Y07
Mitogen-activated protein kinase 1 (MAPK1) CMGC Ser/Thr protein kinase family P28482
Mitogen-activated protein kinase 3 (MAPK3) CMGC Ser/Thr protein kinase family P27361
RAF proto-oncogene serine/threonine-protein kinase (RAF1) TKL Ser/Thr protein kinase family P04049
Serine/threonine-protein kinase B-raf (BRAF) TKL Ser/Thr protein kinase family P15056
Baculoviral IAP repeat-containing protein 6 (BIRC6) Ubiquitin-conjugating enzyme family Q9NR09
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (PIN1) . Q13526
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein BANP (BANP) BANP/SMAR1 family Q8N9N5
Transcriptional coactivator YAP1 (YAP1) YAP1 family P46937
F-box/WD repeat-containing protein 1A (BTRC) . Q9Y297
Pleckstrin homology domain-containing family F member 2 (PLEKHF2) . Q9H8W4

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bosutinib Small molecular drug DB06616
Cobimetinib Small molecular drug DB05239
Trametinib Small molecular drug DB08911
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Selumetinib Small molecular drug D0T5DP
Investigative
Click To Hide/Show 15 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4,5,6,7-tetrabromo-1h-benzo[D][1,2,3]Triazole Small molecular drug D0O1YH
4,5-dibromo-1h-pyrrole-2-carboxylic Acid Amide Small molecular drug D0I4NN
5-phenylamino-4-cyano-3-hydroxy-isothiazole Small molecular drug D0T0VC
Aldisin Small molecular drug D0TF0V
Debromohymenialdisine Small molecular drug D01WAI
K-252a Small molecular drug DB02152
Mirdametinib Small molecular drug DB07101
Oroidin Small molecular drug D08BMM
Pd98059 Small molecular drug D9ILC1
Reversine Small molecular drug D00JMT
(5s)-45-difluoro-6-[(2-fluoro-4-iodophenyl)Imino]-n-(2-hydroxyethoxy)Cyclohexa-13-diene-1-carboxamide . DB06892
2-[(2-chloro-4-iodophenyl)Amino]-n-{[(2r)-23-dihydroxypropyl]Oxy}-34-difluorobenzamide . DB07046
2-[(4-ethynyl-2-fluorophenyl)Amino]-34-difluoro-n-(2-hydroxyethoxy)Benzamide . DB08208
5-bromo-n-[(2s)-23-dihydroxypropoxy]-34-difluoro-2-[(2-fluoro-4-iodophenyl)Amino]Benzamide . DB03115
N-(5-{34-difluoro-2-[(2-fluoro-4-iodophenyl)Amino]Phenyl}-134-oxadiazol-2-yl)Ethane-12-diamine . DB08130
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Diamidothiazole Derivative 1 Small molecular drug D0LR2Y
Pyridic Ketone Derivative 1 Small molecular drug D0XW4G
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rdea-436 . D02UQG

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 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
3 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
4 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
5 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.
6 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.
7 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
8 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
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 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
12 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
13 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
14 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.
15 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
16 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
17 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
18 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
19 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
20 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
21 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
22 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
23 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
24 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.