Details of the Target

General Information of Target

Target ID LDTP03445
Target Name Mitogen-activated protein kinase 1 (MAPK1)
Gene Name MAPK1
Gene ID 5594
Synonyms
ERK2; PRKM1; PRKM2; Mitogen-activated protein kinase 1; MAP kinase 1; MAPK 1; EC 2.7.11.24; ERT1; Extracellular signal-regulated kinase 2; ERK-2; MAP kinase isoform p42; p42-MAPK; Mitogen-activated protein kinase 2; MAP kinase 2; MAPK 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFE
HQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQH
LSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDH
TGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHI
LGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHK
RIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, MAP kinase subfamily
Subcellular location
Cytoplasm, cytoskeleton, spindle
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Many of these substrates are localized in the nucleus, and seem to participate in the regulation of transcription upon stimulation. However, other substrates are found in the cytosol as well as in other cellular organelles, and those are responsible for processes such as translation, mitosis and apoptosis. Moreover, the MAPK/ERK cascade is also involved in the regulation of the 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. The substrates include transcription factors (such as ATF2, BCL6, ELK1, ERF, FOS, HSF4 or SPZ1), cytoskeletal elements (such as CANX, CTTN, GJA1, MAP2, MAPT, PXN, SORBS3 or STMN1), regulators of apoptosis (such as BAD, BTG2, CASP9, DAPK1, IER3, MCL1 or PPARG), regulators of translation (such as EIF4EBP1 and FXR1) and a variety of other signaling-related molecules (like ARHGEF2, DCC, FRS2 or GRB10). Protein kinases (such as RAF1, RPS6KA1/RSK1, RPS6KA3/RSK2, RPS6KA2/RSK3, RPS6KA6/RSK4, SYK, MKNK1/MNK1, MKNK2/MNK2, RPS6KA5/MSK1, RPS6KA4/MSK2, MAPKAPK3 or MAPKAPK5) and phosphatases (such as DUSP1, DUSP4, DUSP6 or DUSP16) are other substrates which enable the propagation the MAPK/ERK signal to additional cytosolic and nuclear targets, thereby extending the specificity of the cascade. Mediates phosphorylation of TPR in response to EGF stimulation. May play a role in the spindle assembly checkpoint. Phosphorylates PML and promotes its interaction with PIN1, leading to PML degradation. Phosphorylates CDK2AP2.; Acts as a transcriptional repressor. Binds to a [GC]AAA[GC] consensus sequence. Repress the expression of interferon gamma-induced genes. Seems to bind to the promoter of CCL5, DMP1, IFIH1, IFITM1, IRF7, IRF9, LAMP3, OAS1, OAS2, OAS3 and STAT1. Transcriptional activity is independent of kinase activity.
TTD ID
T58970
Uniprot ID
P28482
DrugMap ID
TT4TQBX
Ensemble ID
ENST00000215832.11
HGNC ID
HGNC:6871
ChEMBL ID
CHEMBL4040

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
SUPT1 SNV: p.L76P DBIA    Probe Info 
SW403 SNV: p.G34C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 29 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		11.46  LDD0402  [1]
A-EBA
 Probe Info  		3.71  LDD0215  [2]
TH211
 Probe Info  		Y187(18.28)  LDD0257  [3]
STPyne
 Probe Info  		K270(6.86); K73(10.00)  LDD0277  [4]
BTD
 Probe Info  		C65(1.07)  LDD2117  [5]
Jackson_14
 Probe Info  		2.27  LDD0123  [6]
HHS-482
 Probe Info  		Y113(1.23); Y187(0.89)  LDD0285  [7]
HHS-475
 Probe Info  		Y64(0.82); Y113(6.21)  LDD0264  [8]
HHS-465
 Probe Info  		Y113(10.00); Y187(10.00); Y64(10.00)  LDD2237  [9]
DBIA
 Probe Info  		C166(0.98)  LDD0078  [10]
ATP probe
 Probe Info  		K203(0.00); K207(0.00)  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info  		C161(0.00); C254(0.00); C166(0.00); C65(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [13]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [14]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [14]
Lodoacetamide azide
 Probe Info  		C254(0.00); C127(0.00); C40(0.00)  LDD0037  [12]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [15]
NAIA_4
 Probe Info  		N.A.  LDD2226  [16]
TFBX
 Probe Info  		N.A.  LDD0027  [15]
WYneN
 Probe Info  		N.A.  LDD0021  [17]
IPM
 Probe Info  		C65(0.00); C166(0.00)  LDD0005  [17]
NHS
 Probe Info  		N.A.  LDD0010  [17]
SF
 Probe Info  		Y187(0.00); Y263(0.00); Y64(0.00)  LDD0028  [18]
VSF
 Probe Info  		N.A.  LDD0007  [17]
1c-yne
 Probe Info  		N.A.  LDD0228  [19]
Acrolein
 Probe Info  		N.A.  LDD0217  [20]
W1
 Probe Info  		N.A.  LDD0236  [21]
AOyne
 Probe Info  		15.00  LDD0443  [22]
NAIA_5
 Probe Info  		N.A.  LDD2223  [16]
PAL-AfBPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe13
 Probe Info  		12.61  LDD0475  [23]
FFF probe14
 Probe Info  		6.26  LDD0477  [23]
FFF probe3
 Probe Info  		5.15  LDD0465  [23]
JN0003
 Probe Info  		20.00  LDD0469  [23]
VE-P
 Probe Info  		N.A.  LDD0396  [24]
CR-1
 Probe Info  		3.49  LDD0429  [25]
DFG-out-3
 Probe Info  		19.00  LDD0074  [26]
Diazir
 Probe Info  		N.A.  LDD0011  [17]
Probe 12
 Probe Info  		N.A.  LDD0420  [27]

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 C65(1.07)  LDD2117  [5]
 LDCM0214  AC1 HCT 116 C161(0.90); C166(1.27); C40(0.38)  LDD0531  [10]
 LDCM0215  AC10 HCT 116 C161(1.53); C166(1.14); C40(1.03); C65(1.05)  LDD0532  [10]
 LDCM0216  AC100 HCT 116 C161(0.93); C166(1.19); C40(0.72); C65(1.20)  LDD0533  [10]
 LDCM0217  AC101 HCT 116 C161(1.02); C166(1.11); C40(0.96); C65(1.06)  LDD0534  [10]
 LDCM0218  AC102 HCT 116 C161(0.98); C166(1.02); C40(0.91); C65(1.12)  LDD0535  [10]
 LDCM0219  AC103 HCT 116 C161(1.18); C166(1.10); C40(0.82); C65(1.12)  LDD0536  [10]
 LDCM0220  AC104 HCT 116 C161(1.09); C166(1.14); C40(0.85); C65(1.41)  LDD0537  [10]
 LDCM0221  AC105 HCT 116 C161(1.08); C166(1.01); C40(0.85); C65(0.98)  LDD0538  [10]
 LDCM0222  AC106 HCT 116 C161(1.13); C166(1.04); C40(0.82); C65(1.04)  LDD0539  [10]
 LDCM0223  AC107 HCT 116 C161(1.45); C166(1.08); C40(0.93); C65(1.08)  LDD0540  [10]
 LDCM0224  AC108 HCT 116 C161(0.98); C166(1.13); C40(0.72); C65(1.07)  LDD0541  [10]
 LDCM0225  AC109 HCT 116 C161(0.91); C166(1.12); C40(0.85); C65(1.06)  LDD0542  [10]
 LDCM0226  AC11 HCT 116 C161(1.55); C166(1.23); C40(0.98); C65(0.81)  LDD0543  [10]
 LDCM0227  AC110 HCT 116 C161(0.92); C166(1.08); C40(0.92); C65(0.91)  LDD0544  [10]
 LDCM0228  AC111 HCT 116 C161(1.03); C166(1.03); C40(0.81); C65(0.89)  LDD0545  [10]
 LDCM0229  AC112 HCT 116 C161(1.14); C166(1.07); C40(1.00); C65(0.97)  LDD0546  [10]
 LDCM0230  AC113 HCT 116 C161(1.03); C166(1.09); C40(0.97); C65(0.88)  LDD0547  [10]
 LDCM0231  AC114 HCT 116 C161(1.13); C166(1.18); C40(1.00); C65(0.59)  LDD0548  [10]
 LDCM0232  AC115 HCT 116 C161(1.12); C166(1.03); C40(0.81); C65(0.67)  LDD0549  [10]
 LDCM0233  AC116 HCT 116 C161(1.05); C166(1.12); C40(0.98); C65(0.66)  LDD0550  [10]
 LDCM0234  AC117 HCT 116 C161(1.04); C166(1.28); C40(0.95); C65(0.63)  LDD0551  [10]
 LDCM0235  AC118 HCT 116 C161(1.01); C166(1.31); C40(0.99); C65(0.68)  LDD0552  [10]
 LDCM0236  AC119 HCT 116 C161(0.99); C166(1.02); C40(0.95); C65(0.65)  LDD0553  [10]
 LDCM0237  AC12 HCT 116 C161(1.09); C166(1.28); C40(1.26); C65(1.04)  LDD0554  [10]
 LDCM0238  AC120 HCT 116 C161(1.11); C166(1.08); C40(1.14); C65(1.04)  LDD0555  [10]
 LDCM0239  AC121 HCT 116 C161(0.98); C166(1.57); C40(0.98); C65(0.81)  LDD0556  [10]
 LDCM0240  AC122 HCT 116 C161(1.10); C166(1.16); C40(1.11); C65(0.57)  LDD0557  [10]
 LDCM0241  AC123 HCT 116 C161(0.90); C166(2.27); C40(1.06); C65(0.96)  LDD0558  [10]
 LDCM0242  AC124 HCT 116 C161(0.97); C166(1.24); C40(0.92); C65(0.80)  LDD0559  [10]
 LDCM0243  AC125 HCT 116 C161(1.03); C166(1.04); C40(1.10); C65(0.95)  LDD0560  [10]
 LDCM0244  AC126 HCT 116 C161(1.07); C166(1.12); C40(1.05); C65(0.80)  LDD0561  [10]
 LDCM0245  AC127 HCT 116 C161(0.95); C166(1.21); C40(1.10); C65(0.71)  LDD0562  [10]
 LDCM0246  AC128 HCT 116 C161(1.36); C166(1.02); C40(1.05)  LDD0563  [10]
 LDCM0247  AC129 HCT 116 C161(1.05); C166(1.11); C40(0.90)  LDD0564  [10]
 LDCM0249  AC130 HCT 116 C161(1.18); C166(1.17); C40(0.94)  LDD0566  [10]
 LDCM0250  AC131 HCT 116 C161(1.05); C166(0.99); C40(1.08)  LDD0567  [10]
 LDCM0251  AC132 HCT 116 C161(1.20); C166(1.21); C40(1.18)  LDD0568  [10]
 LDCM0252  AC133 HCT 116 C161(1.21); C166(1.29); C40(0.85)  LDD0569  [10]
 LDCM0253  AC134 HCT 116 C161(1.29); C166(1.06); C40(0.97)  LDD0570  [10]
 LDCM0254  AC135 HCT 116 C161(1.23); C166(1.05); C40(1.01)  LDD0571  [10]
 LDCM0255  AC136 HCT 116 C161(1.15); C166(1.22); C40(1.00)  LDD0572  [10]
 LDCM0256  AC137 HCT 116 C161(1.20); C166(1.14); C40(0.82)  LDD0573  [10]
 LDCM0257  AC138 HCT 116 C161(1.33); C166(1.19); C40(1.02)  LDD0574  [10]
 LDCM0258  AC139 HCT 116 C161(1.29); C166(1.16); C40(0.99)  LDD0575  [10]
 LDCM0259  AC14 HCT 116 C161(1.47); C166(1.12); C40(1.29); C65(0.93)  LDD0576  [10]
 LDCM0260  AC140 HCT 116 C161(1.43); C166(1.13); C40(1.11)  LDD0577  [10]
 LDCM0261  AC141 HCT 116 C161(1.44); C166(1.17); C40(0.98)  LDD0578  [10]
 LDCM0262  AC142 HCT 116 C161(1.01); C166(1.13); C40(1.00)  LDD0579  [10]
 LDCM0263  AC143 HCT 116 C40(0.71); C65(0.74); C161(0.99); C166(1.02)  LDD0580  [10]
 LDCM0264  AC144 HCT 116 C65(0.62); C161(0.93); C40(0.99); C166(1.05)  LDD0581  [10]
 LDCM0265  AC145 HCT 116 C40(0.80); C166(0.87); C161(0.89); C65(1.04)  LDD0582  [10]
 LDCM0266  AC146 HCT 116 C65(0.59); C40(0.72); C161(0.99); C166(1.23)  LDD0583  [10]
 LDCM0267  AC147 HCT 116 C65(0.79); C161(0.98); C166(1.04); C40(1.17)  LDD0584  [10]
 LDCM0268  AC148 HCT 116 C40(0.62); C65(0.73); C161(0.83); C166(0.92)  LDD0585  [10]
 LDCM0269  AC149 HCT 116 C65(0.53); C40(0.71); C161(0.89); C166(1.06)  LDD0586  [10]
 LDCM0270  AC15 HCT 116 C65(0.81); C40(1.10); C166(1.15); C161(1.46)  LDD0587  [10]
 LDCM0271  AC150 HCT 116 C161(0.87); C40(0.92); C65(0.95); C166(1.38)  LDD0588  [10]
 LDCM0272  AC151 HCT 116 C40(0.80); C161(0.82); C65(0.93); C166(1.22)  LDD0589  [10]
 LDCM0273  AC152 HCT 116 C161(0.73); C40(0.80); C65(0.95); C166(1.53)  LDD0590  [10]
 LDCM0274  AC153 HCT 116 C65(0.67); C40(0.68); C161(0.83); C166(0.94)  LDD0591  [10]
 LDCM0621  AC154 HCT 116 C161(0.88); C166(1.15); C40(0.72); C65(0.92)  LDD2158  [10]
 LDCM0622  AC155 HCT 116 C161(0.76); C166(1.30); C40(0.82); C65(0.84)  LDD2159  [10]
 LDCM0623  AC156 HCT 116 C161(0.87); C166(1.34); C40(0.84); C65(0.83)  LDD2160  [10]
 LDCM0624  AC157 HCT 116 C161(0.75); C166(1.21); C40(0.66); C65(0.91)  LDD2161  [10]
 LDCM0276  AC17 HCT 116 C65(0.73); C161(1.00); C166(1.10); C40(1.25)  LDD0593  [10]
 LDCM0277  AC18 HCT 116 C65(0.97); C161(1.01); C40(1.04); C166(1.09)  LDD0594  [10]
 LDCM0278  AC19 HCT 116 C65(0.94); C161(0.99); C166(1.13); C40(1.21)  LDD0595  [10]
 LDCM0279  AC2 HCT 116 C40(0.59); C161(1.00); C166(1.18)  LDD0596  [10]
 LDCM0280  AC20 HCT 116 C166(1.03); C65(1.05); C161(1.09); C40(1.18)  LDD0597  [10]
 LDCM0281  AC21 HCT 116 C65(1.02); C161(1.04); C40(1.06); C166(1.08)  LDD0598  [10]
 LDCM0282  AC22 HCT 116 C65(1.03); C40(1.15); C166(1.22); C161(1.26)  LDD0599  [10]
 LDCM0283  AC23 HCT 116 C161(1.06); C65(1.09); C166(1.18); C40(1.40)  LDD0600  [10]
 LDCM0284  AC24 HCT 116 C65(0.82); C161(1.04); C166(1.07); C40(1.21)  LDD0601  [10]
 LDCM0285  AC25 HCT 116 C40(0.81); C166(1.13); C161(1.23)  LDD0602  [10]
 LDCM0286  AC26 HCT 116 C40(0.75); C161(1.13); C166(1.16)  LDD0603  [10]
 LDCM0287  AC27 HCT 116 C40(0.75); C166(0.93); C161(1.23)  LDD0604  [10]
 LDCM0288  AC28 HCT 116 C40(0.76); C166(1.11); C161(1.14)  LDD0605  [10]
 LDCM0289  AC29 HCT 116 C40(0.70); C166(1.03); C161(1.17)  LDD0606  [10]
 LDCM0290  AC3 HCT 116 C40(0.62); C161(0.96); C166(1.15)  LDD0607  [10]
 LDCM0291  AC30 HCT 116 C40(0.68); C166(1.05); C161(1.21)  LDD0608  [10]
 LDCM0292  AC31 HCT 116 C40(0.64); C166(1.08); C161(1.19)  LDD0609  [10]
 LDCM0293  AC32 HCT 116 C40(0.61); C166(1.20); C161(1.35)  LDD0610  [10]
 LDCM0294  AC33 HCT 116 C40(0.70); C166(1.07); C161(1.39)  LDD0611  [10]
 LDCM0295  AC34 HCT 116 C40(0.71); C166(1.02); C161(1.37)  LDD0612  [10]
 LDCM0296  AC35 HCT 116 C166(0.85); C161(1.06); C40(3.50)  LDD0613  [10]
 LDCM0297  AC36 HCT 116 C166(0.88); C40(0.91); C161(1.12)  LDD0614  [10]
 LDCM0298  AC37 HCT 116 C161(0.86); C166(0.97); C40(1.09)  LDD0615  [10]
 LDCM0299  AC38 HCT 116 C161(1.07); C166(1.10); C40(1.35)  LDD0616  [10]
 LDCM0300  AC39 HCT 116 C161(0.90); C166(1.08); C40(1.18)  LDD0617  [10]
 LDCM0301  AC4 HCT 116 C40(0.54); C161(1.04); C166(1.21)  LDD0618  [10]
 LDCM0302  AC40 HCT 116 C166(1.00); C40(1.04); C161(1.24)  LDD0619  [10]
 LDCM0303  AC41 HCT 116 C166(1.03); C161(1.08); C40(1.66)  LDD0620  [10]
 LDCM0304  AC42 HCT 116 C166(0.92); C40(1.10); C161(1.19)  LDD0621  [10]
 LDCM0305  AC43 HCT 116 C166(1.02); C161(1.03); C40(1.05)  LDD0622  [10]
 LDCM0306  AC44 HCT 116 C166(0.93); C40(1.04); C161(1.44)  LDD0623  [10]
 LDCM0307  AC45 HCT 116 C166(0.83); C40(1.21); C161(1.45)  LDD0624  [10]
 LDCM0308  AC46 HCT 116 C40(0.65); C166(1.09); C161(1.10)  LDD0625  [10]
 LDCM0309  AC47 HCT 116 C40(0.63); C166(1.00); C161(1.03)  LDD0626  [10]
 LDCM0310  AC48 HCT 116 C40(0.44); C166(1.01); C161(1.05)  LDD0627  [10]
 LDCM0311  AC49 HCT 116 C40(0.54); C166(0.98); C161(1.16)  LDD0628  [10]
 LDCM0312  AC5 HCT 116 C40(0.56); C161(0.91); C166(1.26)  LDD0629  [10]
 LDCM0313  AC50 HCT 116 C40(0.51); C161(1.11); C166(1.20)  LDD0630  [10]
 LDCM0314  AC51 HCT 116 C40(0.77); C161(0.99); C166(1.10)  LDD0631  [10]
 LDCM0315  AC52 HCT 116 C40(0.80); C161(0.97); C166(1.04)  LDD0632  [10]
 LDCM0316  AC53 HCT 116 C40(0.71); C166(0.97); C161(0.99)  LDD0633  [10]
 LDCM0317  AC54 HCT 116 C40(0.67); C161(1.02); C166(1.03)  LDD0634  [10]
 LDCM0318  AC55 HCT 116 C40(0.80); C166(1.08); C161(1.29)  LDD0635  [10]
 LDCM0319  AC56 HCT 116 C40(0.47); C166(1.07); C161(1.31)  LDD0636  [10]
 LDCM0320  AC57 HCT 116 C40(0.67); C65(0.77); C161(1.11); C166(1.32)  LDD0637  [10]
 LDCM0321  AC58 HCT 116 C40(0.57); C166(1.07); C65(1.23); C161(1.31)  LDD0638  [10]
 LDCM0322  AC59 HCT 116 C40(0.81); C65(0.98); C166(1.21); C161(1.30)  LDD0639  [10]
 LDCM0323  AC6 HCT 116 C40(0.80); C166(0.94); C65(1.15); C161(1.43)  LDD0640  [10]
 LDCM0324  AC60 HCT 116 C40(0.69); C65(0.76); C166(1.25); C161(1.39)  LDD0641  [10]
 LDCM0325  AC61 HCT 116 C40(0.56); C65(0.93); C161(1.25); C166(1.29)  LDD0642  [10]
 LDCM0326  AC62 HCT 116 C40(0.68); C65(0.79); C161(1.35); C166(1.41)  LDD0643  [10]
 LDCM0327  AC63 HCT 116 C40(0.72); C65(0.84); C161(1.21); C166(1.38)  LDD0644  [10]
 LDCM0328  AC64 HCT 116 C40(0.79); C65(0.92); C161(1.19); C166(1.58)  LDD0645  [10]
 LDCM0329  AC65 HCT 116 C40(0.72); C65(0.83); C161(1.19); C166(1.28)  LDD0646  [10]
 LDCM0330  AC66 HCT 116 C40(0.74); C65(1.08); C166(1.31); C161(1.47)  LDD0647  [10]
 LDCM0331  AC67 HCT 116 C40(0.67); C65(0.82); C161(1.25); C166(1.37)  LDD0648  [10]
 LDCM0332  AC68 HCT 116 C40(0.53); C166(0.92); C65(1.08); C161(1.10)  LDD0649  [10]
 LDCM0333  AC69 HCT 116 C40(0.42); C65(0.77); C166(1.00); C161(1.10)  LDD0650  [10]
 LDCM0334  AC7 HCT 116 C40(0.90); C166(1.03); C65(1.19); C161(1.42)  LDD0651  [10]
 LDCM0335  AC70 HCT 116 C40(0.42); C166(0.89); C161(0.99); C65(1.02)  LDD0652  [10]
 LDCM0336  AC71 HCT 116 C40(0.49); C161(0.92); C65(1.09); C166(1.14)  LDD0653  [10]
 LDCM0337  AC72 HCT 116 C40(0.73); C161(0.98); C65(1.04); C166(1.12)  LDD0654  [10]
 LDCM0338  AC73 HCT 116 C40(0.35); C65(1.02); C166(1.17); C161(1.21)  LDD0655  [10]
 LDCM0339  AC74 HCT 116 C40(0.33); C161(1.14); C166(1.16); C65(1.33)  LDD0656  [10]
 LDCM0340  AC75 HCT 116 C40(0.33); C65(0.85); C166(1.14); C161(1.18)  LDD0657  [10]
 LDCM0341  AC76 HCT 116 C40(0.67); C166(1.00); C65(1.03); C161(1.03)  LDD0658  [10]
 LDCM0342  AC77 HCT 116 C40(0.56); C65(0.92); C166(1.05); C161(1.29)  LDD0659  [10]
 LDCM0343  AC78 HCT 116 C40(0.45); C161(0.96); C65(1.02); C166(1.33)  LDD0660  [10]
 LDCM0344  AC79 HCT 116 C40(0.84); C65(1.03); C161(1.04); C166(1.18)  LDD0661  [10]
 LDCM0345  AC8 HCT 116 C40(0.86); C65(1.02); C166(1.16); C161(1.56)  LDD0662  [10]
 LDCM0346  AC80 HCT 116 C40(0.60); C65(0.95); C161(1.01); C166(1.08)  LDD0663  [10]
 LDCM0347  AC81 HCT 116 C40(0.69); C161(0.93); C65(1.08); C166(1.15)  LDD0664  [10]
 LDCM0348  AC82 HCT 116 C40(0.25); C65(0.93); C161(0.99); C166(1.10)  LDD0665  [10]
 LDCM0349  AC83 HCT 116 C40(0.58); C166(1.16); C161(1.54)  LDD0666  [10]
 LDCM0350  AC84 HCT 116 C40(0.57); C166(1.28); C161(1.86)  LDD0667  [10]
 LDCM0351  AC85 HCT 116 C40(0.58); C161(1.37); C166(1.43)  LDD0668  [10]
 LDCM0352  AC86 HCT 116 C40(0.79); C161(1.25); C166(1.28)  LDD0669  [10]
 LDCM0353  AC87 HCT 116 C40(0.71); C161(0.98); C166(1.31)  LDD0670  [10]
 LDCM0354  AC88 HCT 116 C40(0.90); C166(1.31); C161(1.34)  LDD0671  [10]
 LDCM0355  AC89 HCT 116 C40(0.64); C166(1.25); C161(1.25)  LDD0672  [10]
 LDCM0357  AC90 HCT 116 C161(1.20); C166(1.25); C40(1.31)  LDD0674  [10]
 LDCM0358  AC91 HCT 116 C40(0.76); C161(1.39); C166(1.44)  LDD0675  [10]
 LDCM0359  AC92 HCT 116 C40(0.75); C166(1.51); C161(1.62)  LDD0676  [10]
 LDCM0360  AC93 HCT 116 C40(0.77); C161(1.05); C166(1.35)  LDD0677  [10]
 LDCM0361  AC94 HCT 116 C40(1.03); C161(1.17); C166(1.55)  LDD0678  [10]
 LDCM0362  AC95 HCT 116 C40(0.49); C161(1.19); C166(1.34)  LDD0679  [10]
 LDCM0363  AC96 HCT 116 C40(0.92); C166(1.33); C161(1.53)  LDD0680  [10]
 LDCM0364  AC97 HCT 116 C40(0.71); C161(1.23); C166(1.31)  LDD0681  [10]
 LDCM0365  AC98 HCT 116 C65(0.81); C166(0.96); C40(1.16); C161(1.41)  LDD0682  [10]
 LDCM0366  AC99 HCT 116 C40(0.79); C161(0.93); C65(0.96); C166(1.06)  LDD0683  [10]
 LDCM0248  AKOS034007472 HCT 116 C161(1.27); C166(1.13); C40(1.23); C65(1.10)  LDD0565  [10]
 LDCM0356  AKOS034007680 HCT 116 C40(0.88); C65(1.12); C166(1.12); C161(1.17)  LDD0673  [10]
 LDCM0275  AKOS034007705 HCT 116 C65(0.87); C40(0.88); C166(1.19); C161(2.10)  LDD0592  [10]
 LDCM0156  Aniline NCI-H1299 11.45  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C166(0.98)  LDD0078  [10]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [20]
 LDCM0632  CL-Sc Hep-G2 C161(1.80); C161(1.18)  LDD2227  [16]
 LDCM0367  CL1 HCT 116 C40(0.83); C166(0.90); C161(1.08); C65(1.24)  LDD0684  [10]
 LDCM0368  CL10 HCT 116 C40(0.79); C166(0.96); C65(1.11); C161(1.48)  LDD0685  [10]
 LDCM0369  CL100 HCT 116 C40(0.67); C161(1.10); C166(1.18)  LDD0686  [10]
 LDCM0370  CL101 HCT 116 C65(0.81); C166(1.11); C40(1.15); C161(1.64)  LDD0687  [10]
 LDCM0371  CL102 HCT 116 C166(1.01); C40(1.25); C161(1.28); C65(1.31)  LDD0688  [10]
 LDCM0372  CL103 HCT 116 C65(1.03); C161(1.06); C40(1.12); C166(1.22)  LDD0689  [10]
 LDCM0373  CL104 HCT 116 C40(1.08); C161(1.11); C65(1.11); C166(1.26)  LDD0690  [10]
 LDCM0374  CL105 HCT 116 C166(1.05); C40(1.06); C65(1.09); C161(1.15)  LDD0691  [10]
 LDCM0375  CL106 HCT 116 C161(1.15); C166(1.16); C40(1.18); C65(1.30)  LDD0692  [10]
 LDCM0376  CL107 HCT 116 C161(1.10); C40(1.12); C65(1.13); C166(1.20)  LDD0693  [10]
 LDCM0377  CL108 HCT 116 C65(0.83); C161(0.98); C166(1.06); C40(1.09)  LDD0694  [10]
 LDCM0378  CL109 HCT 116 C40(0.94); C166(1.07); C161(1.16); C65(1.28)  LDD0695  [10]
 LDCM0379  CL11 HCT 116 C40(0.85); C65(0.94); C166(1.10); C161(1.37)  LDD0696  [10]
 LDCM0380  CL110 HCT 116 C40(0.91); C65(1.07); C161(1.12); C166(1.22)  LDD0697  [10]
 LDCM0381  CL111 HCT 116 C65(0.91); C40(1.00); C166(1.17); C161(1.23)  LDD0698  [10]
 LDCM0382  CL112 HCT 116 C40(0.82); C161(0.97); C166(0.98)  LDD0699  [10]
 LDCM0383  CL113 HCT 116 C40(0.65); C166(1.18); C161(1.33)  LDD0700  [10]
 LDCM0384  CL114 HCT 116 C40(0.70); C166(1.01); C161(1.11)  LDD0701  [10]
 LDCM0385  CL115 HCT 116 C40(0.73); C166(0.98); C161(1.13)  LDD0702  [10]
 LDCM0386  CL116 HCT 116 C40(0.76); C166(0.99); C161(1.20)  LDD0703  [10]
 LDCM0387  CL117 HCT 116 C40(0.71); C166(1.09); C161(2.03)  LDD0704  [10]
 LDCM0388  CL118 HCT 116 C166(0.86); C161(1.21); C40(1.54)  LDD0705  [10]
 LDCM0389  CL119 HCT 116 C166(1.00); C40(1.09); C161(1.13)  LDD0706  [10]
 LDCM0390  CL12 HCT 116 C40(0.71); C166(0.84); C65(1.05); C161(1.39)  LDD0707  [10]
 LDCM0391  CL120 HCT 116 C40(0.86); C166(1.03); C161(1.55)  LDD0708  [10]
 LDCM0392  CL121 HCT 116 C40(0.60); C166(0.95); C161(1.04)  LDD0709  [10]
 LDCM0393  CL122 HCT 116 C40(0.44); C161(1.01); C166(1.01)  LDD0710  [10]
 LDCM0394  CL123 HCT 116 C40(0.57); C161(0.98); C166(1.14)  LDD0711  [10]
 LDCM0395  CL124 HCT 116 C40(0.51); C166(0.96); C161(1.10)  LDD0712  [10]
 LDCM0396  CL125 HCT 116 C65(0.73); C166(1.21); C40(1.28); C161(1.36)  LDD0713  [10]
 LDCM0397  CL126 HCT 116 C40(0.95); C166(1.06); C65(1.14); C161(1.27)  LDD0714  [10]
 LDCM0398  CL127 HCT 116 C40(0.79); C65(0.93); C161(1.08); C166(1.16)  LDD0715  [10]
 LDCM0399  CL128 HCT 116 C65(0.92); C40(0.99); C161(1.10); C166(1.30)  LDD0716  [10]
 LDCM0400  CL13 HCT 116 C40(0.67); C166(0.87); C65(1.01); C161(1.32)  LDD0717  [10]
 LDCM0401  CL14 HCT 116 C40(0.83); C65(0.88); C166(0.93); C161(1.21)  LDD0718  [10]
 LDCM0402  CL15 HCT 116 C40(0.62); C166(0.82); C65(1.05); C161(1.37)  LDD0719  [10]
 LDCM0403  CL16 HCT 116 C40(0.60); C161(1.42)  LDD0720  [10]
 LDCM0404  CL17 HCT 116 C65(0.62); C161(1.21); C40(1.31)  LDD0721  [10]
 LDCM0405  CL18 HCT 116 C65(0.73); C161(0.81); C40(0.90)  LDD0722  [10]
 LDCM0406  CL19 HCT 116 C65(0.86); C161(0.92); C40(1.06)  LDD0723  [10]
 LDCM0407  CL2 HCT 116 C166(0.89); C40(1.02); C161(1.03); C65(1.08)  LDD0724  [10]
 LDCM0408  CL20 HCT 116 C65(0.74); C40(0.98); C161(1.24)  LDD0725  [10]
 LDCM0409  CL21 HCT 116 C65(0.71); C161(0.91); C40(1.26)  LDD0726  [10]
 LDCM0410  CL22 HCT 116 C40(0.90); C161(0.98); C65(1.08)  LDD0727  [10]
 LDCM0411  CL23 HCT 116 C40(0.73); C65(0.85); C161(0.94)  LDD0728  [10]
 LDCM0412  CL24 HCT 116 C40(0.87); C65(0.89); C161(1.13)  LDD0729  [10]
 LDCM0413  CL25 HCT 116 C161(1.81); C40(0.79); C65(0.74)  LDD0730  [10]
 LDCM0414  CL26 HCT 116 C161(1.17); C40(0.71); C65(0.83)  LDD0731  [10]
 LDCM0415  CL27 HCT 116 C161(1.10); C40(0.95); C65(0.87)  LDD0732  [10]
 LDCM0416  CL28 HCT 116 C161(1.16); C40(0.88); C65(0.69)  LDD0733  [10]
 LDCM0417  CL29 HCT 116 C161(2.19); C40(0.99); C65(0.87)  LDD0734  [10]
 LDCM0418  CL3 HCT 116 C161(0.94); C166(0.98); C40(1.09); C65(1.27)  LDD0735  [10]
 LDCM0419  CL30 HCT 116 C161(1.24); C40(1.13); C65(1.01)  LDD0736  [10]
 LDCM0420  CL31 HCT 116 C161(1.08); C166(1.00); C40(0.83); C65(0.98)  LDD0737  [10]
 LDCM0421  CL32 HCT 116 C161(1.34); C166(1.25); C40(0.63)  LDD0738  [10]
 LDCM0422  CL33 HCT 116 C161(1.17); C166(0.99); C40(0.51)  LDD0739  [10]
 LDCM0423  CL34 HCT 116 C161(1.16); C166(1.02); C40(0.53)  LDD0740  [10]
 LDCM0424  CL35 HCT 116 C161(1.11); C166(1.11); C40(0.60)  LDD0741  [10]
 LDCM0425  CL36 HCT 116 C161(1.04); C166(1.01); C40(0.61)  LDD0742  [10]
 LDCM0426  CL37 HCT 116 C161(1.13); C166(1.04); C40(0.63)  LDD0743  [10]
 LDCM0428  CL39 HCT 116 C161(1.15); C166(1.14); C40(0.77)  LDD0745  [10]
 LDCM0429  CL4 HCT 116 C161(0.93); C166(0.79); C40(0.90); C65(0.98)  LDD0746  [10]
 LDCM0430  CL40 HCT 116 C161(1.07); C166(0.95); C40(0.83)  LDD0747  [10]
 LDCM0431  CL41 HCT 116 C161(0.97); C166(1.06); C40(0.76)  LDD0748  [10]
 LDCM0432  CL42 HCT 116 C161(1.08); C166(1.01); C40(0.66)  LDD0749  [10]
 LDCM0433  CL43 HCT 116 C161(1.03); C166(1.03); C40(0.73)  LDD0750  [10]
 LDCM0434  CL44 HCT 116 C161(1.10); C166(1.02); C40(0.58)  LDD0751  [10]
 LDCM0435  CL45 HCT 116 C161(1.08); C166(1.03); C40(0.61)  LDD0752  [10]
 LDCM0436  CL46 HCT 116 C161(0.94); C166(1.09); C40(1.70); C65(0.84)  LDD0753  [10]
 LDCM0437  CL47 HCT 116 C161(1.04); C166(1.14); C40(1.47); C65(1.06)  LDD0754  [10]
 LDCM0438  CL48 HCT 116 C161(0.92); C166(1.14); C40(1.90); C65(0.92)  LDD0755  [10]
 LDCM0439  CL49 HCT 116 C161(0.92); C166(1.15); C40(1.51); C65(0.78)  LDD0756  [10]
 LDCM0440  CL5 HCT 116 C161(0.97); C166(1.04); C40(0.97); C65(1.04)  LDD0757  [10]
 LDCM0441  CL50 HCT 116 C161(0.86); C166(1.03); C40(1.67); C65(1.24)  LDD0758  [10]
 LDCM0442  CL51 HCT 116 C161(0.88); C166(1.11); C40(1.47); C65(0.67)  LDD0759  [10]
 LDCM0443  CL52 HCT 116 C161(0.93); C166(1.06); C40(1.31); C65(1.16)  LDD0760  [10]
 LDCM0444  CL53 HCT 116 C161(0.82); C166(1.02); C40(1.82); C65(1.23)  LDD0761  [10]
 LDCM0445  CL54 HCT 116 C161(0.87); C166(1.13); C40(1.28); C65(0.98)  LDD0762  [10]
 LDCM0446  CL55 HCT 116 C161(0.86); C166(1.36); C40(1.72); C65(1.13)  LDD0763  [10]
 LDCM0447  CL56 HCT 116 C161(1.00); C166(1.30); C40(1.16); C65(1.14)  LDD0764  [10]
 LDCM0448  CL57 HCT 116 C161(0.95); C166(1.06); C40(1.60); C65(1.05)  LDD0765  [10]
 LDCM0449  CL58 HCT 116 C161(0.83); C166(1.10); C40(1.67); C65(0.83)  LDD0766  [10]
 LDCM0450  CL59 HCT 116 C161(0.92); C166(1.15); C40(1.36); C65(1.27)  LDD0767  [10]
 LDCM0451  CL6 HCT 116 C161(1.08); C166(1.00); C40(0.61); C65(0.85)  LDD0768  [10]
 LDCM0452  CL60 HCT 116 C161(1.00); C166(1.10); C40(1.18); C65(0.73)  LDD0769  [10]
 LDCM0453  CL61 HCT 116 C161(1.16); C166(0.98); C65(0.89)  LDD0770  [10]
 LDCM0454  CL62 HCT 116 C161(1.21); C166(1.09); C65(0.72)  LDD0771  [10]
 LDCM0455  CL63 HCT 116 C161(1.20); C166(0.93); C65(0.90)  LDD0772  [10]
 LDCM0456  CL64 HCT 116 C161(1.29); C166(0.98); C65(0.79)  LDD0773  [10]
 LDCM0457  CL65 HCT 116 C161(1.27); C166(0.96); C65(1.04)  LDD0774  [10]
 LDCM0458  CL66 HCT 116 C161(1.73); C166(0.99); C65(0.76)  LDD0775  [10]
 LDCM0459  CL67 HCT 116 C161(1.20); C166(0.99); C65(1.03)  LDD0776  [10]
 LDCM0460  CL68 HCT 116 C161(1.30); C166(0.94); C65(1.34)  LDD0777  [10]
 LDCM0461  CL69 HCT 116 C161(1.18); C166(0.88); C65(0.77)  LDD0778  [10]
 LDCM0462  CL7 HCT 116 C161(1.28); C166(0.97); C40(0.84); C65(0.84)  LDD0779  [10]
 LDCM0463  CL70 HCT 116 C161(1.40); C166(1.07); C65(0.94)  LDD0780  [10]
 LDCM0464  CL71 HCT 116 C161(1.08); C166(1.10); C65(1.03)  LDD0781  [10]
 LDCM0465  CL72 HCT 116 C161(1.05); C166(1.02); C65(0.92)  LDD0782  [10]
 LDCM0466  CL73 HCT 116 C161(1.12); C166(0.91); C65(1.31)  LDD0783  [10]
 LDCM0467  CL74 HCT 116 C161(1.20); C166(1.01); C65(1.04)  LDD0784  [10]
 LDCM0469  CL76 HCT 116 C161(0.97); C166(0.95)  LDD0786  [10]
 LDCM0470  CL77 HCT 116 C161(1.10); C166(0.90)  LDD0787  [10]
 LDCM0471  CL78 HCT 116 C161(1.01); C166(1.00)  LDD0788  [10]
 LDCM0472  CL79 HCT 116 C161(1.06); C166(0.86)  LDD0789  [10]
 LDCM0473  CL8 HCT 116 C161(1.63); C166(0.88); C40(0.91); C65(1.07)  LDD0790  [10]
 LDCM0474  CL80 HCT 116 C161(0.97); C166(0.93)  LDD0791  [10]
 LDCM0475  CL81 HCT 116 C161(0.90); C166(0.96)  LDD0792  [10]
 LDCM0476  CL82 HCT 116 C161(0.93); C166(0.93)  LDD0793  [10]
 LDCM0477  CL83 HCT 116 C161(0.92); C166(0.89)  LDD0794  [10]
 LDCM0478  CL84 HCT 116 C161(0.94); C166(0.97)  LDD0795  [10]
 LDCM0479  CL85 HCT 116 C161(0.99); C166(1.05)  LDD0796  [10]
 LDCM0480  CL86 HCT 116 C161(0.95); C166(1.02)  LDD0797  [10]
 LDCM0481  CL87 HCT 116 C161(0.90); C166(0.95)  LDD0798  [10]
 LDCM0482  CL88 HCT 116 C161(0.87); C166(0.95)  LDD0799  [10]
 LDCM0483  CL89 HCT 116 C161(0.93); C166(0.96)  LDD0800  [10]
 LDCM0484  CL9 HCT 116 C161(1.09); C166(0.94); C40(0.74); C65(1.11)  LDD0801  [10]
 LDCM0485  CL90 HCT 116 C161(0.96); C166(0.90)  LDD0802  [10]
 LDCM0486  CL91 HCT 116 C161(1.10); C166(1.08); C40(0.86)  LDD0803  [10]
 LDCM0487  CL92 HCT 116 C161(1.04); C166(1.06); C40(0.86)  LDD0804  [10]
 LDCM0488  CL93 HCT 116 C161(0.86); C166(1.09); C40(1.06)  LDD0805  [10]
 LDCM0489  CL94 HCT 116 C161(0.85); C166(1.03); C40(0.34)  LDD0806  [10]
 LDCM0490  CL95 HCT 116 C161(0.88); C166(1.13); C40(0.56)  LDD0807  [10]
 LDCM0491  CL96 HCT 116 C161(1.03); C166(1.22); C40(0.72)  LDD0808  [10]
 LDCM0492  CL97 HCT 116 C161(0.95); C166(1.15); C40(0.50)  LDD0809  [10]
 LDCM0493  CL98 HCT 116 C161(1.02); C166(1.19); C40(0.63)  LDD0810  [10]
 LDCM0494  CL99 HCT 116 C161(0.94); C166(1.26); C40(0.52)  LDD0811  [10]
 LDCM0165  Compound 9 HL-60 N.A.  LDD0420  [27]
 LDCM0168  Crenolanib NCI-H1703 3.49  LDD0429  [25]
 LDCM0495  E2913 HEK-293T C254(0.94); C40(0.86)  LDD1698  [28]
 LDCM0468  Fragment33 HCT 116 C161(1.22); C166(1.03); C65(0.93)  LDD0785  [10]
 LDCM0427  Fragment51 HCT 116 C161(1.10); C166(1.06); C40(0.58)  LDD0744  [10]
 LDCM0116  HHS-0101 DM93 Y64(0.82); Y113(6.21)  LDD0264  [8]
 LDCM0117  HHS-0201 DM93 Y113(0.07); Y64(0.82)  LDD0265  [8]
 LDCM0118  HHS-0301 DM93 Y64(0.81); Y113(2.72)  LDD0266  [8]
 LDCM0119  HHS-0401 DM93 Y113(0.21); Y64(0.91)  LDD0267  [8]
 LDCM0120  HHS-0701 DM93 Y64(0.93); Y113(1.51)  LDD0268  [8]
 LDCM0123  JWB131 DM93 Y113(1.23); Y187(0.89)  LDD0285  [7]
 LDCM0124  JWB142 DM93 Y113(1.91); Y187(1.00)  LDD0286  [7]
 LDCM0125  JWB146 DM93 Y113(0.85); Y187(1.19)  LDD0287  [7]
 LDCM0126  JWB150 DM93 Y113(4.05); Y187(3.61)  LDD0288  [7]
 LDCM0127  JWB152 DM93 Y187(2.26)  LDD0289  [7]
 LDCM0128  JWB198 DM93 Y113(0.32); Y187(1.31)  LDD0290  [7]
 LDCM0129  JWB202 DM93 Y113(1.14); Y187(0.40)  LDD0291  [7]
 LDCM0130  JWB211 DM93 Y113(1.32); Y187(1.85)  LDD0292  [7]
 LDCM0022  KB02 HEK-293T C127(1.16); C254(1.05)  LDD1492  [28]
 LDCM0023  KB03 Jurkat C166(42.38)  LDD0209  [29]
 LDCM0024  KB05 MKN-1 C254(1.34)  LDD3331  [30]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C65(1.23)  LDD2123  [5]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C65(0.98)  LDD2136  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C65(0.92)  LDD2137  [5]
 LDCM0016  Ranjitkar_cp1 A431 19.00  LDD0074  [26]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 21 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA-directed RNA polymerase II subunit RPB7 (POLR2G) Eukaryotic RPB7/RPC8 RNA polymerase subunit family P62487
Biliverdin reductase A (BLVRA) Gfo/Idh/MocA family P53004
COP9 signalosome complex subunit 6 (COPS6) Peptidase M67A family Q7L5N1
Proteasome subunit alpha type-1 (PSMA1) Peptidase T1A family P25786
Protein phosphatase 1A (PPM1A) PP2C family P35813
Ribosomal protein S6 kinase alpha-1 (RPS6KA1) AGC Ser/Thr protein kinase family Q15418
Ribosomal protein S6 kinase alpha-2 (RPS6KA2) AGC Ser/Thr protein kinase family Q15349
Ribosomal protein S6 kinase alpha-3 (RPS6KA3) AGC Ser/Thr protein kinase family P51812
MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1) CAMK Ser/Thr protein kinase family Q9BUB5
Mitogen-activated protein kinase 1 (MAPK1) CMGC Ser/Thr protein kinase family P28482
Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) STE Ser/Thr protein kinase family Q02750
Dual specificity protein phosphatase 1 (DUSP1) Protein-tyrosine phosphatase family P28562
Dual specificity protein phosphatase 4 (DUSP4) Protein-tyrosine phosphatase family Q13115
Dual specificity protein phosphatase 5 (DUSP5) Protein-tyrosine phosphatase family Q16690
Dual specificity protein phosphatase 6 (DUSP6) Protein-tyrosine phosphatase family Q16828
Dual specificity protein phosphatase 9 (DUSP9) Protein-tyrosine phosphatase family Q99956
Protein tyrosine phosphatase domain-containing protein 1 (PTPDC1) Protein-tyrosine phosphatase family A2A3K4
Tyrosine-protein phosphatase non-receptor type 7 (PTPN7) Protein-tyrosine phosphatase family P35236
Receptor-type tyrosine-protein phosphatase eta (PTPRJ) Protein-tyrosine phosphatase family Q12913
Receptor-type tyrosine-protein phosphatase R (PTPRR) Protein-tyrosine phosphatase family Q15256
E3 ubiquitin-protein ligase RNF8 (RNF8) RNF8 family O76064
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
MyoD family inhibitor (MDFI) MDFI family Q99750
Syntaxin-binding protein 1 (STXBP1) STXBP/unc-18/SEC1 family P61764
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein PLAGL2 (PLAGL2) Krueppel C2H2-type zinc-finger protein family Q9UPG8
Zinc finger and BTB domain-containing protein 42 (ZBTB42) Krueppel C2H2-type zinc-finger protein family B2RXF5
Homeobox protein MSX-2 (MSX2) Msh homeobox family P35548
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Leucine zipper putative tumor suppressor 2 (LZTS2) LZTS2 family Q9BRK4
Trafficking protein particle complex subunit 4 (TRAPPC4) TRAPP small subunits family Q9Y296
Astrocytic phosphoprotein PEA-15 (PEA15) . Q15121
N-chimaerin (CHN1) . P15882
Phostensin (PPP1R18) . Q6NYC8

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetylsalicylic Acid Small molecular drug DB00945
Arsenic Trioxide Small molecular drug DB01169
Minocycline Small molecular drug DB01017
Turpentine . DB11120
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Astx029 Small molecular drug DM1FD5
Bvd-523 . D01IED
Hh2710 . D1KIY9
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jsi-1187 Small molecular drug DBU16T
Gdc-0994 . D0Q4IX
Ly3214996 . D0TN3Q
Van-10-4-eluting Stent . D08KNG
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cor-d Small molecular drug DOJ6D9
Investigative
Click To Hide/Show 31 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(4-fluoro-phenyl)-(9-methyl-9h-purin-6-yl)-amine Small molecular drug D0Q1AC
4,5,6,7-tetrabromo-1h-benzo[D][1,2,3]Triazole Small molecular drug D0O1YH
4-[(3,5-diamino-1h-pyrazol-4-yl)Diazenyl]Phenol Small molecular drug D0A5RM
5-(2-phenylpyrazolo[15-a]Pyridin-3-yl)-1h-pyrazolo[34-c]Pyridazin-3-amine Small molecular drug DB07794
Bisindolylmaleimide-i Small molecular drug D0TO6S
Bms-536924 Small molecular drug D0M4SY
Ci-1040 Small molecular drug D0B9BU
Colforsin Small molecular drug DB02587
Debromohymenialdisine Small molecular drug D01WAI
Erk Inhibitor Iii Small molecular drug D0C5AD
Fr-180204 Small molecular drug D0ZG4G
Kn-62 Small molecular drug D0N6ES
Kt-5720 Small molecular drug D0G2VC
Olomoucine Small molecular drug DB02116
Perifosine Small molecular drug DB06641
Phosphonothreonine Small molecular drug D05BHG
Purvalanol Small molecular drug DB02733
Ro-316233 Small molecular drug D0L8HO
Ro-4396686 Small molecular drug D09XIL
Ro31-8220 Small molecular drug D0M5FF
Sch772984 Small molecular drug D08XVZ
Seliciclib Small molecular drug DB06195
(3r5z8s9s11e)-8916-trihydroxy-14-methoxy-3-methyl-34910-tetrahydro-1h-2-benzoxacyclotetradecine-17(8h)-dione . DB07788
(S)-n-(1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl)-4-(4-(3-chlorophenyl)-1h-pyrazol-3-yl)-1h-pyrrole-2-carboxamide . DB07264
4-[4-(4-fluorophenyl)-2-[4-[(R)-methylsulfinyl]Phenyl]-1h-imidazol-5-yl]Pyridine . DB08521
Aezs-131 . D07NEE
Hypothemycin . DB07905
N-benzyl-4-[4-(3-chlorophenyl)-1h-pyrazol-3-yl]-1h-pyrrole-2-carboxamide . DB07010
Nn-dimethyl-4-(4-phenyl-1h-pyrazol-3-yl)-1h-pyrrole-2-carboxamide . DB06877
Ulixertinib . DB13930
[4-({5-(Aminocarbonyl)-4-[(3-methylphenyl)Amino]Pyrimidin-2-yl}Amino)Phenyl]Acetic Acid . DB08513
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Chir-99021 Small molecular drug D0YK9D
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sb220025 Small molecular drug D09ICC

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 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
3 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.
4 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
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 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
7 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.
8 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
9 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
10 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.
11 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.
12 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
13 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
14 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
15 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
16 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
17 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
18 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
19 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.
20 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.
21 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
22 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.
23 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.
24 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
25 Crenolanib-Derived Probes Suitable for Cell- and Tissue-Based Protein Profiling and Single-Cell Imaging. Chembiochem. 2019 Jul 15;20(14):1783-1788. doi: 10.1002/cbic.201900067. Epub 2019 Jul 3.
26 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.
27 A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family. Angew Chem Int Ed Engl. 2019 Nov 25;58(48):17322-17327. doi: 10.1002/anie.201906321. Epub 2019 Oct 31.
28 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
29 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
30 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