General Information of Target

Target ID LDTP05245
Target Name Cyclin-dependent kinase 5 (CDK5)
Gene Name CDK5
Gene ID 1020
Synonyms
CDKN5; PSSALRE; Cyclin-dependent kinase 5; EC 2.7.11.1; Cell division protein kinase 5; Cyclin-dependent-like kinase 5; Serine/threonine-protein kinase PSSALRE; Tau protein kinase II catalytic subunit; TPKII catalytic subunit
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKH
KNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSR
NVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYS
TSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYP
MYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, CDC2/CDKX subfamily
Subcellular location
Cytoplasm; Nucleus
Function
Proline-directed serine/threonine-protein kinase essential for neuronal cell cycle arrest and differentiation and may be involved in apoptotic cell death in neuronal diseases by triggering abortive cell cycle re-entry. Interacts with D1 and D3-type G1 cyclins. Phosphorylates SRC, NOS3, VIM/vimentin, p35/CDK5R1, MEF2A, SIPA1L1, SH3GLB1, PXN, PAK1, MCAM/MUC18, SEPT5, SYN1, DNM1, AMPH, SYNJ1, CDK16, RAC1, RHOA, CDC42, TONEBP/NFAT5, MAPT/TAU, MAP1B, histone H1, p53/TP53, HDAC1, APEX1, PTK2/FAK1, huntingtin/HTT, ATM, MAP2, NEFH and NEFM. Regulates several neuronal development and physiological processes including neuronal survival, migration and differentiation, axonal and neurite growth, synaptogenesis, oligodendrocyte differentiation, synaptic plasticity and neurotransmission, by phosphorylating key proteins. Negatively regulates the CACNA1B/CAV2.2 -mediated Ca(2+) release probability at hippocampal neuronal soma and synaptic terminals. Activated by interaction with CDK5R1 (p35) and CDK5R2 (p39), especially in postmitotic neurons, and promotes CDK5R1 (p35) expression in an autostimulation loop. Phosphorylates many downstream substrates such as Rho and Ras family small GTPases (e.g. PAK1, RAC1, RHOA, CDC42) or microtubule-binding proteins (e.g. MAPT/TAU, MAP2, MAP1B), and modulates actin dynamics to regulate neurite growth and/or spine morphogenesis. Phosphorylates also exocytosis associated proteins such as MCAM/MUC18, SEPT5, SYN1, and CDK16/PCTAIRE1 as well as endocytosis associated proteins such as DNM1, AMPH and SYNJ1 at synaptic terminals. In the mature central nervous system (CNS), regulates neurotransmitter movements by phosphorylating substrates associated with neurotransmitter release and synapse plasticity; synaptic vesicle exocytosis, vesicles fusion with the presynaptic membrane, and endocytosis. Promotes cell survival by activating anti-apoptotic proteins BCL2 and STAT3, and negatively regulating of JNK3/MAPK10 activity. Phosphorylation of p53/TP53 in response to genotoxic and oxidative stresses enhances its stabilization by preventing ubiquitin ligase-mediated proteasomal degradation, and induces transactivation of p53/TP53 target genes, thus regulating apoptosis. Phosphorylation of p35/CDK5R1 enhances its stabilization by preventing calpain-mediated proteolysis producing p25/CDK5R1 and avoiding ubiquitin ligase-mediated proteasomal degradation. During aberrant cell-cycle activity and DNA damage, p25/CDK5 activity elicits cell-cycle activity and double-strand DNA breaks that precedes neuronal death by deregulating HDAC1. DNA damage triggered phosphorylation of huntingtin/HTT in nuclei of neurons protects neurons against polyglutamine expansion as well as DNA damage mediated toxicity. Phosphorylation of PXN reduces its interaction with PTK2/FAK1 in matrix-cell focal adhesions (MCFA) during oligodendrocytes (OLs) differentiation. Negative regulator of Wnt/beta-catenin signaling pathway. Activator of the GAIT (IFN-gamma-activated inhibitor of translation) pathway, which suppresses expression of a post-transcriptional regulon of proinflammatory genes in myeloid cells; phosphorylates the linker domain of glutamyl-prolyl tRNA synthetase (EPRS) in a IFN-gamma-dependent manner, the initial event in assembly of the GAIT complex. Phosphorylation of SH3GLB1 is required for autophagy induction in starved neurons. Phosphorylation of TONEBP/NFAT5 in response to osmotic stress mediates its rapid nuclear localization. MEF2 is inactivated by phosphorylation in nucleus in response to neurotoxin, thus leading to neuronal apoptosis. APEX1 AP-endodeoxyribonuclease is repressed by phosphorylation, resulting in accumulation of DNA damage and contributing to neuronal death. NOS3 phosphorylation down regulates NOS3-derived nitrite (NO) levels. SRC phosphorylation mediates its ubiquitin-dependent degradation and thus leads to cytoskeletal reorganization. May regulate endothelial cell migration and angiogenesis via the modulation of lamellipodia formation. Involved in dendritic spine morphogenesis by mediating the EFNA1-EPHA4 signaling. The complex p35/CDK5 participates in the regulation of the circadian clock by modulating the function of CLOCK protein: phosphorylates CLOCK at 'Thr-451' and 'Thr-461' and regulates the transcriptional activity of the CLOCK-BMAL1 heterodimer in association with altered stability and subcellular distribution.
TTD ID
T20973
Uniprot ID
Q00535
DrugMap ID
TTL4Q97
Ensemble ID
ENST00000297518.4
HGNC ID
HGNC:1774
ChEMBL ID
CHEMBL4036

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.K56N; p.G138E DBIA    Probe Info 
JURKAT SNV: p.A198T .
SNGM SNV: p.R149Ter DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 26 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
15.00  LDD0402  [1]
TH211
 Probe Info 
Y236(20.00)  LDD0257  [2]
TH216
 Probe Info 
Y242(20.00)  LDD0259  [2]
STPyne
 Probe Info 
K20(3.00); K33(6.65); K56(8.39)  LDD0277  [3]
ONAyne
 Probe Info 
K33(9.51)  LDD0275  [3]
OPA-S-S-alkyne
 Probe Info 
K33(6.80)  LDD3494  [4]
Probe 1
 Probe Info 
Y15(49.82)  LDD3495  [5]
BTD
 Probe Info 
C117(1.28)  LDD2111  [6]
DA-P3
 Probe Info 
4.25  LDD0183  [7]
AHL-Pu-1
 Probe Info 
C157(2.56)  LDD0169  [8]
HHS-475
 Probe Info 
Y242(0.82)  LDD0264  [9]
DBIA
 Probe Info 
C157(2.61); C117(1.51); C94(1.22)  LDD0080  [10]
AMP probe
 Probe Info 
N.A.  LDD0200  [11]
ATP probe
 Probe Info 
K33(0.00); K128(0.00); K89(0.00); K9(0.00)  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info 
C157(0.00); C117(0.00); C290(0.00); C94(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info 
C157(0.00); C117(0.00); C290(0.00); C94(0.00)  LDD0036  [12]
Lodoacetamide azide
 Probe Info 
C157(0.00); C117(0.00); C290(0.00); C94(0.00)  LDD0037  [12]
ATP probe
 Probe Info 
N.A.  LDD0035  [13]
NAIA_4
 Probe Info 
N.A.  LDD2226  [14]
TFBX
 Probe Info 
N.A.  LDD0027  [15]
KY-26
 Probe Info 
N.A.  LDD0301  [16]
IPM
 Probe Info 
N.A.  LDD0005  [17]
SF
 Probe Info 
K33(0.00); K20(0.00)  LDD0028  [18]
1c-yne
 Probe Info 
N.A.  LDD0228  [19]
AOyne
 Probe Info 
15.00  LDD0443  [20]
NAIA_5
 Probe Info 
C157(0.00); C269(0.00); C290(0.00)  LDD2223  [14]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C391
 Probe Info 
15.24  LDD2050  [21]
VE-P
 Probe Info 
N.A.  LDD0396  [22]
Staurosporine capture compound
 Probe Info 
N.A.  LDD0083  [23]
Probe 12
 Probe Info 
N.A.  LDD0420  [24]

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 C117(1.03)  LDD2117  [6]
 LDCM0026  4SU-RNA+native RNA HEK-293T C157(2.56)  LDD0169  [8]
 LDCM0214  AC1 HCT 116 C117(1.10); C94(0.99)  LDD0531  [10]
 LDCM0215  AC10 HCT 116 C157(0.92); C117(1.07); C94(0.94)  LDD0532  [10]
 LDCM0216  AC100 HCT 116 C117(0.98); C94(0.75)  LDD0533  [10]
 LDCM0217  AC101 HCT 116 C117(1.03); C94(0.74)  LDD0534  [10]
 LDCM0218  AC102 HCT 116 C117(1.10); C94(0.82)  LDD0535  [10]
 LDCM0219  AC103 HCT 116 C117(1.03); C94(0.50)  LDD0536  [10]
 LDCM0220  AC104 HCT 116 C117(1.14); C94(0.65)  LDD0537  [10]
 LDCM0221  AC105 HCT 116 C117(1.03); C94(0.68)  LDD0538  [10]
 LDCM0222  AC106 HCT 116 C117(0.97); C94(0.48)  LDD0539  [10]
 LDCM0223  AC107 HCT 116 C117(1.09); C94(0.74)  LDD0540  [10]
 LDCM0224  AC108 HCT 116 C117(0.89); C94(0.55)  LDD0541  [10]
 LDCM0225  AC109 HCT 116 C117(1.16); C94(0.51)  LDD0542  [10]
 LDCM0226  AC11 HCT 116 C157(0.93); C117(0.90); C94(1.12)  LDD0543  [10]
 LDCM0227  AC110 HCT 116 C117(0.90); C94(0.49)  LDD0544  [10]
 LDCM0228  AC111 HCT 116 C117(0.94); C94(0.57)  LDD0545  [10]
 LDCM0229  AC112 HCT 116 C117(0.84); C94(0.67)  LDD0546  [10]
 LDCM0230  AC113 HCT 116 C117(1.01)  LDD0547  [10]
 LDCM0231  AC114 HCT 116 C117(0.89)  LDD0548  [10]
 LDCM0232  AC115 HCT 116 C117(0.91)  LDD0549  [10]
 LDCM0233  AC116 HCT 116 C117(0.82)  LDD0550  [10]
 LDCM0234  AC117 HCT 116 C117(1.26)  LDD0551  [10]
 LDCM0235  AC118 HCT 116 C117(1.05)  LDD0552  [10]
 LDCM0236  AC119 HCT 116 C117(0.88)  LDD0553  [10]
 LDCM0237  AC12 HCT 116 C157(1.05); C117(0.96); C94(0.99)  LDD0554  [10]
 LDCM0238  AC120 HCT 116 C117(0.87)  LDD0555  [10]
 LDCM0239  AC121 HCT 116 C117(1.33)  LDD0556  [10]
 LDCM0240  AC122 HCT 116 C117(0.86)  LDD0557  [10]
 LDCM0241  AC123 HCT 116 C117(1.31)  LDD0558  [10]
 LDCM0242  AC124 HCT 116 C117(1.10)  LDD0559  [10]
 LDCM0243  AC125 HCT 116 C117(0.94)  LDD0560  [10]
 LDCM0244  AC126 HCT 116 C117(1.01)  LDD0561  [10]
 LDCM0245  AC127 HCT 116 C117(0.97)  LDD0562  [10]
 LDCM0246  AC128 HCT 116 C117(1.44); C94(0.58)  LDD0563  [10]
 LDCM0247  AC129 HCT 116 C117(1.12); C94(1.10)  LDD0564  [10]
 LDCM0249  AC130 HCT 116 C117(1.10); C94(0.82)  LDD0566  [10]
 LDCM0250  AC131 HCT 116 C117(1.31); C94(1.28)  LDD0567  [10]
 LDCM0251  AC132 HCT 116 C117(0.93); C94(1.35)  LDD0568  [10]
 LDCM0252  AC133 HCT 116 C117(1.03); C94(0.98)  LDD0569  [10]
 LDCM0253  AC134 HCT 116 C117(1.14); C94(0.94)  LDD0570  [10]
 LDCM0254  AC135 HCT 116 C117(1.17); C94(0.96)  LDD0571  [10]
 LDCM0255  AC136 HCT 116 C117(1.01); C94(1.00)  LDD0572  [10]
 LDCM0256  AC137 HCT 116 C117(1.06); C94(1.23)  LDD0573  [10]
 LDCM0257  AC138 HCT 116 C117(0.96); C94(1.24)  LDD0574  [10]
 LDCM0258  AC139 HCT 116 C117(0.93); C94(1.18)  LDD0575  [10]
 LDCM0259  AC14 HCT 116 C157(0.70); C117(1.06); C94(0.96)  LDD0576  [10]
 LDCM0260  AC140 HCT 116 C117(0.90); C94(1.01)  LDD0577  [10]
 LDCM0261  AC141 HCT 116 C117(0.92); C94(1.14)  LDD0578  [10]
 LDCM0262  AC142 HCT 116 C117(0.95); C94(1.22)  LDD0579  [10]
 LDCM0263  AC143 HCT 116 C117(1.03); C94(1.00)  LDD0580  [10]
 LDCM0264  AC144 HCT 116 C117(0.51); C94(0.68)  LDD0581  [10]
 LDCM0265  AC145 HCT 116 C117(0.90); C94(1.07)  LDD0582  [10]
 LDCM0266  AC146 HCT 116 C117(0.60); C94(1.60)  LDD0583  [10]
 LDCM0267  AC147 HCT 116 C117(0.38); C94(0.85)  LDD0584  [10]
 LDCM0268  AC148 HCT 116 C117(0.16); C94(0.83)  LDD0585  [10]
 LDCM0269  AC149 HCT 116 C117(0.35); C94(1.60)  LDD0586  [10]
 LDCM0270  AC15 HCT 116 C94(0.91); C117(1.02); C157(1.03)  LDD0587  [10]
 LDCM0271  AC150 HCT 116 C117(1.24); C94(1.51)  LDD0588  [10]
 LDCM0272  AC151 HCT 116 C117(0.85); C94(1.15)  LDD0589  [10]
 LDCM0273  AC152 HCT 116 C117(0.37); C94(0.73)  LDD0590  [10]
 LDCM0274  AC153 HCT 116 C117(0.14); C94(1.10)  LDD0591  [10]
 LDCM0621  AC154 HCT 116 C117(0.55); C94(1.23)  LDD2158  [10]
 LDCM0622  AC155 HCT 116 C117(0.64); C94(1.55)  LDD2159  [10]
 LDCM0623  AC156 HCT 116 C117(0.84); C94(1.96)  LDD2160  [10]
 LDCM0624  AC157 HCT 116 C117(0.83); C94(1.10)  LDD2161  [10]
 LDCM0276  AC17 HCT 116 C117(1.14); C157(1.78)  LDD0593  [10]
 LDCM0277  AC18 HCT 116 C157(0.95); C117(1.09)  LDD0594  [10]
 LDCM0278  AC19 HCT 116 C117(0.97); C157(1.94)  LDD0595  [10]
 LDCM0279  AC2 HCT 116 C117(0.90); C94(1.09)  LDD0596  [10]
 LDCM0280  AC20 HCT 116 C117(1.02); C157(1.73)  LDD0597  [10]
 LDCM0281  AC21 HCT 116 C117(0.98); C157(1.66)  LDD0598  [10]
 LDCM0282  AC22 HCT 116 C117(1.09); C157(1.35)  LDD0599  [10]
 LDCM0283  AC23 HCT 116 C117(0.96); C157(1.67)  LDD0600  [10]
 LDCM0284  AC24 HCT 116 C117(1.22); C157(2.42)  LDD0601  [10]
 LDCM0285  AC25 HCT 116 C117(1.00); C157(1.12)  LDD0602  [10]
 LDCM0286  AC26 HCT 116 C117(0.73); C157(0.98)  LDD0603  [10]
 LDCM0287  AC27 HCT 116 C117(0.82); C157(1.38)  LDD0604  [10]
 LDCM0288  AC28 HCT 116 C117(0.75); C157(1.48)  LDD0605  [10]
 LDCM0289  AC29 HCT 116 C117(0.68); C157(1.43)  LDD0606  [10]
 LDCM0290  AC3 HCT 116 C117(0.97); C94(1.18)  LDD0607  [10]
 LDCM0291  AC30 HCT 116 C117(0.70); C157(1.12)  LDD0608  [10]
 LDCM0292  AC31 HCT 116 C117(0.66); C157(1.08)  LDD0609  [10]
 LDCM0293  AC32 HCT 116 C117(0.55); C157(1.26)  LDD0610  [10]
 LDCM0294  AC33 HCT 116 C117(0.80); C157(1.40)  LDD0611  [10]
 LDCM0295  AC34 HCT 116 C117(0.70); C157(1.90)  LDD0612  [10]
 LDCM0296  AC35 HCT 116 C94(1.19); C117(1.69)  LDD0613  [10]
 LDCM0297  AC36 HCT 116 C94(0.95); C117(1.59)  LDD0614  [10]
 LDCM0298  AC37 HCT 116 C94(1.01); C117(1.20)  LDD0615  [10]
 LDCM0299  AC38 HCT 116 C94(1.17); C117(1.19)  LDD0616  [10]
 LDCM0300  AC39 HCT 116 C117(1.02); C94(1.10)  LDD0617  [10]
 LDCM0301  AC4 HCT 116 C117(1.08); C94(1.15)  LDD0618  [10]
 LDCM0302  AC40 HCT 116 C117(0.76); C94(0.85)  LDD0619  [10]
 LDCM0303  AC41 HCT 116 C94(0.97); C117(1.01)  LDD0620  [10]
 LDCM0304  AC42 HCT 116 C94(0.96); C117(0.98)  LDD0621  [10]
 LDCM0305  AC43 HCT 116 C94(0.94); C117(0.98)  LDD0622  [10]
 LDCM0306  AC44 HCT 116 C94(0.88); C117(0.93)  LDD0623  [10]
 LDCM0307  AC45 HCT 116 C94(0.68); C117(0.69)  LDD0624  [10]
 LDCM0308  AC46 HCT 116 C117(0.68); C94(1.07); C157(1.31)  LDD0625  [10]
 LDCM0309  AC47 HCT 116 C117(0.86); C94(0.93); C157(0.93)  LDD0626  [10]
 LDCM0310  AC48 HCT 116 C157(0.70); C117(0.82); C94(1.05)  LDD0627  [10]
 LDCM0311  AC49 HCT 116 C94(0.35); C117(0.78); C157(1.70)  LDD0628  [10]
 LDCM0312  AC5 HCT 116 C94(1.02); C117(1.04)  LDD0629  [10]
 LDCM0313  AC50 HCT 116 C94(0.39); C117(0.78); C157(2.03)  LDD0630  [10]
 LDCM0314  AC51 HCT 116 C157(0.81); C117(0.90); C94(1.08)  LDD0631  [10]
 LDCM0315  AC52 HCT 116 C117(0.77); C94(0.93); C157(0.99)  LDD0632  [10]
 LDCM0316  AC53 HCT 116 C94(0.52); C117(0.88); C157(1.49)  LDD0633  [10]
 LDCM0317  AC54 HCT 116 C94(0.59); C117(0.94); C157(1.50)  LDD0634  [10]
 LDCM0318  AC55 HCT 116 C94(0.35); C117(0.84); C157(1.82)  LDD0635  [10]
 LDCM0319  AC56 HCT 116 C94(0.32); C117(0.86); C157(2.14)  LDD0636  [10]
 LDCM0320  AC57 HCT 116 C117(0.79); C94(0.92)  LDD0637  [10]
 LDCM0321  AC58 HCT 116 C117(0.84); C94(0.88)  LDD0638  [10]
 LDCM0322  AC59 HCT 116 C117(0.72); C94(0.86)  LDD0639  [10]
 LDCM0323  AC6 HCT 116 C157(0.79); C94(0.82); C117(0.91)  LDD0640  [10]
 LDCM0324  AC60 HCT 116 C117(0.73); C94(0.85)  LDD0641  [10]
 LDCM0325  AC61 HCT 116 C117(0.72); C94(0.95)  LDD0642  [10]
 LDCM0326  AC62 HCT 116 C117(0.65); C94(0.83)  LDD0643  [10]
 LDCM0327  AC63 HCT 116 C117(0.71); C94(0.79)  LDD0644  [10]
 LDCM0328  AC64 HCT 116 C117(0.66); C94(0.88)  LDD0645  [10]
 LDCM0329  AC65 HCT 116 C117(0.67); C94(0.96)  LDD0646  [10]
 LDCM0330  AC66 HCT 116 C117(0.70); C94(1.00)  LDD0647  [10]
 LDCM0331  AC67 HCT 116 C117(0.58); C94(0.69)  LDD0648  [10]
 LDCM0332  AC68 HCT 116 C94(0.74); C117(0.88)  LDD0649  [10]
 LDCM0333  AC69 HCT 116 C94(0.62); C117(0.83)  LDD0650  [10]
 LDCM0334  AC7 HCT 116 C157(0.85); C117(0.86); C94(0.87)  LDD0651  [10]
 LDCM0335  AC70 HCT 116 C94(0.34); C117(0.60)  LDD0652  [10]
 LDCM0336  AC71 HCT 116 C94(1.02); C117(1.20)  LDD0653  [10]
 LDCM0337  AC72 HCT 116 C94(0.65); C117(0.74)  LDD0654  [10]
 LDCM0338  AC73 HCT 116 C94(0.30); C117(0.57)  LDD0655  [10]
 LDCM0339  AC74 HCT 116 C94(0.33); C117(0.80)  LDD0656  [10]
 LDCM0340  AC75 HCT 116 C94(0.31); C117(0.49)  LDD0657  [10]
 LDCM0341  AC76 HCT 116 C94(0.48); C117(0.74)  LDD0658  [10]
 LDCM0342  AC77 HCT 116 C94(0.47); C117(0.65)  LDD0659  [10]
 LDCM0343  AC78 HCT 116 C117(0.85); C94(0.89)  LDD0660  [10]
 LDCM0344  AC79 HCT 116 C94(0.86); C117(0.88)  LDD0661  [10]
 LDCM0345  AC8 HCT 116 C94(0.88); C117(0.95); C157(1.18)  LDD0662  [10]
 LDCM0346  AC80 HCT 116 C94(0.60); C117(0.72)  LDD0663  [10]
 LDCM0347  AC81 HCT 116 C94(0.83); C117(1.18)  LDD0664  [10]
 LDCM0348  AC82 HCT 116 C94(0.34); C117(0.71)  LDD0665  [10]
 LDCM0349  AC83 HCT 116 C117(0.85)  LDD0666  [10]
 LDCM0350  AC84 HCT 116 C117(0.87)  LDD0667  [10]
 LDCM0351  AC85 HCT 116 C117(0.87)  LDD0668  [10]
 LDCM0352  AC86 HCT 116 C117(0.79)  LDD0669  [10]
 LDCM0353  AC87 HCT 116 C117(0.95)  LDD0670  [10]
 LDCM0354  AC88 HCT 116 C117(0.97)  LDD0671  [10]
 LDCM0355  AC89 HCT 116 C117(0.77)  LDD0672  [10]
 LDCM0357  AC90 HCT 116 C117(0.76)  LDD0674  [10]
 LDCM0358  AC91 HCT 116 C117(0.87)  LDD0675  [10]
 LDCM0359  AC92 HCT 116 C117(0.82)  LDD0676  [10]
 LDCM0360  AC93 HCT 116 C117(0.87)  LDD0677  [10]
 LDCM0361  AC94 HCT 116 C117(0.99)  LDD0678  [10]
 LDCM0362  AC95 HCT 116 C117(0.81)  LDD0679  [10]
 LDCM0363  AC96 HCT 116 C117(1.12)  LDD0680  [10]
 LDCM0364  AC97 HCT 116 C117(0.65)  LDD0681  [10]
 LDCM0365  AC98 HCT 116 C94(0.22); C117(0.86)  LDD0682  [10]
 LDCM0366  AC99 HCT 116 C94(0.80); C117(0.97)  LDD0683  [10]
 LDCM0248  AKOS034007472 HCT 116 C157(0.60); C117(0.94); C94(0.97)  LDD0565  [10]
 LDCM0356  AKOS034007680 HCT 116 C117(0.82); C157(0.83); C94(0.96)  LDD0673  [10]
 LDCM0275  AKOS034007705 HCT 116 C94(0.82); C157(0.89); C117(0.94)  LDD0592  [10]
 LDCM0156  Aniline NCI-H1299 13.42  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C157(2.05)  LDD2214  [25]
 LDCM0367  CL1 HCT 116 C117(0.90); C94(1.00)  LDD0684  [10]
 LDCM0368  CL10 HCT 116 C117(0.75); C94(0.96)  LDD0685  [10]
 LDCM0369  CL100 HCT 116 C117(0.95); C94(1.06)  LDD0686  [10]
 LDCM0370  CL101 HCT 116 C157(0.71); C94(0.80); C117(0.97)  LDD0687  [10]
 LDCM0371  CL102 HCT 116 C117(0.79); C94(0.82); C157(0.98)  LDD0688  [10]
 LDCM0372  CL103 HCT 116 C157(0.82); C94(0.92); C117(0.99)  LDD0689  [10]
 LDCM0373  CL104 HCT 116 C94(0.88); C117(0.99); C157(1.23)  LDD0690  [10]
 LDCM0374  CL105 HCT 116 C117(0.77); C157(1.16)  LDD0691  [10]
 LDCM0375  CL106 HCT 116 C117(0.61); C157(1.33)  LDD0692  [10]
 LDCM0376  CL107 HCT 116 C117(0.67); C157(1.21)  LDD0693  [10]
 LDCM0377  CL108 HCT 116 C117(0.62); C157(1.80)  LDD0694  [10]
 LDCM0378  CL109 HCT 116 C117(0.68); C157(2.22)  LDD0695  [10]
 LDCM0379  CL11 HCT 116 C117(0.77); C94(0.85)  LDD0696  [10]
 LDCM0380  CL110 HCT 116 C117(0.69); C157(1.47)  LDD0697  [10]
 LDCM0381  CL111 HCT 116 C117(0.79); C157(1.98)  LDD0698  [10]
 LDCM0382  CL112 HCT 116 C157(0.72); C117(0.95)  LDD0699  [10]
 LDCM0383  CL113 HCT 116 C117(0.75); C157(1.26)  LDD0700  [10]
 LDCM0384  CL114 HCT 116 C117(0.73); C157(1.08)  LDD0701  [10]
 LDCM0385  CL115 HCT 116 C117(0.83); C157(1.23)  LDD0702  [10]
 LDCM0386  CL116 HCT 116 C157(0.65); C117(0.91)  LDD0703  [10]
 LDCM0387  CL117 HCT 116 C94(0.59); C117(0.63)  LDD0704  [10]
 LDCM0388  CL118 HCT 116 C117(0.89); C94(1.00)  LDD0705  [10]
 LDCM0389  CL119 HCT 116 C94(0.81); C117(0.84)  LDD0706  [10]
 LDCM0390  CL12 HCT 116 C117(0.73); C94(0.87)  LDD0707  [10]
 LDCM0391  CL120 HCT 116 C117(0.96); C94(1.10)  LDD0708  [10]
 LDCM0392  CL121 HCT 116 C117(0.79); C94(0.79); C157(0.86)  LDD0709  [10]
 LDCM0393  CL122 HCT 116 C117(0.83); C94(0.85); C157(0.88)  LDD0710  [10]
 LDCM0394  CL123 HCT 116 C94(0.55); C117(0.72); C157(1.62)  LDD0711  [10]
 LDCM0395  CL124 HCT 116 C94(0.44); C117(0.64); C157(2.01)  LDD0712  [10]
 LDCM0396  CL125 HCT 116 C117(0.99); C94(1.02)  LDD0713  [10]
 LDCM0397  CL126 HCT 116 C94(0.90); C117(1.01)  LDD0714  [10]
 LDCM0398  CL127 HCT 116 C117(0.86); C94(0.92)  LDD0715  [10]
 LDCM0399  CL128 HCT 116 C117(0.69); C94(0.94)  LDD0716  [10]
 LDCM0400  CL13 HCT 116 C117(0.94); C94(0.97)  LDD0717  [10]
 LDCM0401  CL14 HCT 116 C117(0.88); C94(1.05)  LDD0718  [10]
 LDCM0402  CL15 HCT 116 C117(0.89); C94(0.94)  LDD0719  [10]
 LDCM0403  CL16 HCT 116 C117(0.73); C94(0.85); C157(0.99)  LDD0720  [10]
 LDCM0404  CL17 HCT 116 C117(0.80); C94(0.96); C157(1.30)  LDD0721  [10]
 LDCM0405  CL18 HCT 116 C94(0.81); C117(0.88); C157(1.80)  LDD0722  [10]
 LDCM0406  CL19 HCT 116 C117(0.97); C94(1.02); C157(1.46)  LDD0723  [10]
 LDCM0407  CL2 HCT 116 C117(0.91); C94(0.97)  LDD0724  [10]
 LDCM0408  CL20 HCT 116 C117(0.74); C94(0.82); C157(1.27)  LDD0725  [10]
 LDCM0409  CL21 HCT 116 C117(0.79); C94(0.81); C157(2.28)  LDD0726  [10]
 LDCM0410  CL22 HCT 116 C94(0.68); C117(0.99); C157(1.53)  LDD0727  [10]
 LDCM0411  CL23 HCT 116 C94(0.89); C117(0.90); C157(1.56)  LDD0728  [10]
 LDCM0412  CL24 HCT 116 C94(0.72); C117(0.75); C157(1.85)  LDD0729  [10]
 LDCM0413  CL25 HCT 116 C157(2.08); C117(0.58); C94(0.59)  LDD0730  [10]
 LDCM0414  CL26 HCT 116 C157(0.96); C117(0.80); C94(0.72)  LDD0731  [10]
 LDCM0415  CL27 HCT 116 C157(0.99); C117(0.79); C94(1.00)  LDD0732  [10]
 LDCM0416  CL28 HCT 116 C157(1.26); C117(0.68); C94(0.89)  LDD0733  [10]
 LDCM0417  CL29 HCT 116 C157(1.05); C117(0.76); C94(0.99)  LDD0734  [10]
 LDCM0418  CL3 HCT 116 C117(0.81); C94(1.01)  LDD0735  [10]
 LDCM0419  CL30 HCT 116 C157(1.63); C117(0.91); C94(0.98)  LDD0736  [10]
 LDCM0420  CL31 HCT 116 C157(1.76); C117(0.90); C94(0.86)  LDD0737  [10]
 LDCM0421  CL32 HCT 116 C157(1.65); C117(0.91); C94(0.59)  LDD0738  [10]
 LDCM0422  CL33 HCT 116 C157(2.76); C117(0.88); C94(0.60)  LDD0739  [10]
 LDCM0423  CL34 HCT 116 C157(2.70); C117(0.88); C94(0.49)  LDD0740  [10]
 LDCM0424  CL35 HCT 116 C157(4.36); C117(0.94); C94(0.43)  LDD0741  [10]
 LDCM0425  CL36 HCT 116 C157(3.08); C117(0.96); C94(0.60)  LDD0742  [10]
 LDCM0426  CL37 HCT 116 C157(4.52); C117(0.95); C94(0.43)  LDD0743  [10]
 LDCM0428  CL39 HCT 116 C157(2.58); C117(0.83); C94(0.47)  LDD0745  [10]
 LDCM0429  CL4 HCT 116 C117(0.97); C94(0.95)  LDD0746  [10]
 LDCM0430  CL40 HCT 116 C157(2.73); C117(0.80); C94(0.56)  LDD0747  [10]
 LDCM0431  CL41 HCT 116 C157(2.11); C117(0.83); C94(0.67)  LDD0748  [10]
 LDCM0432  CL42 HCT 116 C157(3.87); C117(0.87); C94(0.28)  LDD0749  [10]
 LDCM0433  CL43 HCT 116 C157(5.17); C117(1.01); C94(0.34)  LDD0750  [10]
 LDCM0434  CL44 HCT 116 C157(3.09); C117(0.88); C94(0.56)  LDD0751  [10]
 LDCM0435  CL45 HCT 116 C157(2.63); C117(0.94); C94(0.50)  LDD0752  [10]
 LDCM0436  CL46 HCT 116 C117(0.93)  LDD0753  [10]
 LDCM0437  CL47 HCT 116 C117(1.08)  LDD0754  [10]
 LDCM0438  CL48 HCT 116 C117(1.02)  LDD0755  [10]
 LDCM0439  CL49 HCT 116 C117(0.86)  LDD0756  [10]
 LDCM0440  CL5 HCT 116 C117(1.00); C94(1.01)  LDD0757  [10]
 LDCM0441  CL50 HCT 116 C117(0.99)  LDD0758  [10]
 LDCM0442  CL51 HCT 116 C117(1.01)  LDD0759  [10]
 LDCM0443  CL52 HCT 116 C117(1.01)  LDD0760  [10]
 LDCM0444  CL53 HCT 116 C117(1.04)  LDD0761  [10]
 LDCM0445  CL54 HCT 116 C117(0.83)  LDD0762  [10]
 LDCM0446  CL55 HCT 116 C117(1.02)  LDD0763  [10]
 LDCM0447  CL56 HCT 116 C117(0.98)  LDD0764  [10]
 LDCM0448  CL57 HCT 116 C117(1.03)  LDD0765  [10]
 LDCM0449  CL58 HCT 116 C117(1.08)  LDD0766  [10]
 LDCM0450  CL59 HCT 116 C117(1.01)  LDD0767  [10]
 LDCM0451  CL6 HCT 116 C117(0.80); C94(0.88)  LDD0768  [10]
 LDCM0452  CL60 HCT 116 C117(0.94)  LDD0769  [10]
 LDCM0453  CL61 HCT 116 C117(0.78); C94(1.18)  LDD0770  [10]
 LDCM0454  CL62 HCT 116 C117(0.76); C94(1.00)  LDD0771  [10]
 LDCM0455  CL63 HCT 116 C117(0.71); C94(1.04)  LDD0772  [10]
 LDCM0456  CL64 HCT 116 C117(0.76); C94(0.91)  LDD0773  [10]
 LDCM0457  CL65 HCT 116 C117(1.09); C94(1.03)  LDD0774  [10]
 LDCM0458  CL66 HCT 116 C117(0.81); C94(0.62)  LDD0775  [10]
 LDCM0459  CL67 HCT 116 C117(1.04); C94(0.89)  LDD0776  [10]
 LDCM0460  CL68 HCT 116 C117(1.18); C94(0.87)  LDD0777  [10]
 LDCM0461  CL69 HCT 116 C117(0.66); C94(0.81)  LDD0778  [10]
 LDCM0462  CL7 HCT 116 C117(0.93); C94(0.98)  LDD0779  [10]
 LDCM0463  CL70 HCT 116 C117(0.92); C94(0.99)  LDD0780  [10]
 LDCM0464  CL71 HCT 116 C117(0.76); C94(0.94)  LDD0781  [10]
 LDCM0465  CL72 HCT 116 C117(0.77); C94(0.98)  LDD0782  [10]
 LDCM0466  CL73 HCT 116 C117(0.83); C94(0.91)  LDD0783  [10]
 LDCM0467  CL74 HCT 116 C117(1.14); C94(0.96)  LDD0784  [10]
 LDCM0469  CL76 HCT 116 C117(1.37); C94(1.07)  LDD0786  [10]
 LDCM0470  CL77 HCT 116 C117(1.33); C94(1.14)  LDD0787  [10]
 LDCM0471  CL78 HCT 116 C117(1.19); C94(0.88)  LDD0788  [10]
 LDCM0472  CL79 HCT 116 C117(1.30); C94(0.69)  LDD0789  [10]
 LDCM0473  CL8 HCT 116 C117(0.68); C94(0.61)  LDD0790  [10]
 LDCM0474  CL80 HCT 116 C117(1.22); C94(0.91)  LDD0791  [10]
 LDCM0475  CL81 HCT 116 C117(1.17); C94(0.96)  LDD0792  [10]
 LDCM0476  CL82 HCT 116 C117(1.21); C94(0.43)  LDD0793  [10]
 LDCM0477  CL83 HCT 116 C117(1.09); C94(0.55)  LDD0794  [10]
 LDCM0478  CL84 HCT 116 C117(1.05); C94(0.38)  LDD0795  [10]
 LDCM0479  CL85 HCT 116 C117(1.18); C94(1.04)  LDD0796  [10]
 LDCM0480  CL86 HCT 116 C117(1.20); C94(1.31)  LDD0797  [10]
 LDCM0481  CL87 HCT 116 C117(1.23); C94(1.06)  LDD0798  [10]
 LDCM0482  CL88 HCT 116 C117(1.31); C94(0.62)  LDD0799  [10]
 LDCM0483  CL89 HCT 116 C117(1.20); C94(0.42)  LDD0800  [10]
 LDCM0484  CL9 HCT 116 C117(0.90); C94(1.01)  LDD0801  [10]
 LDCM0485  CL90 HCT 116 C117(1.12); C94(1.04)  LDD0802  [10]
 LDCM0486  CL91 HCT 116 C117(0.77); C94(1.16)  LDD0803  [10]
 LDCM0487  CL92 HCT 116 C117(0.90); C94(1.03)  LDD0804  [10]
 LDCM0488  CL93 HCT 116 C117(1.12); C94(1.11)  LDD0805  [10]
 LDCM0489  CL94 HCT 116 C117(1.38); C94(0.93)  LDD0806  [10]
 LDCM0490  CL95 HCT 116 C117(0.99); C94(0.99)  LDD0807  [10]
 LDCM0491  CL96 HCT 116 C117(0.89); C94(1.10)  LDD0808  [10]
 LDCM0492  CL97 HCT 116 C117(0.86); C94(1.03)  LDD0809  [10]
 LDCM0493  CL98 HCT 116 C117(0.77); C94(1.01)  LDD0810  [10]
 LDCM0494  CL99 HCT 116 C117(0.85); C94(1.08)  LDD0811  [10]
 LDCM0165  Compound 9 HL-60 N.A.  LDD0420  [24]
 LDCM0495  E2913 HEK-293T C94(0.97); C83(1.22); C157(1.07); C190(1.57)  LDD1698  [26]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C269(3.36)  LDD1702  [6]
 LDCM0031  Epigallocatechin gallate HEK-293T 4.25  LDD0183  [7]
 LDCM0625  F8 Ramos C117(1.09); C290(1.16)  LDD2187  [27]
 LDCM0572  Fragment10 Ramos C290(0.56)  LDD2189  [27]
 LDCM0573  Fragment11 Ramos C290(0.31)  LDD2190  [27]
 LDCM0574  Fragment12 Ramos C290(1.69)  LDD2191  [27]
 LDCM0575  Fragment13 Ramos C290(2.02)  LDD2192  [27]
 LDCM0576  Fragment14 Ramos C117(0.80); C290(0.85)  LDD2193  [27]
 LDCM0579  Fragment20 Ramos C290(0.15)  LDD2194  [27]
 LDCM0580  Fragment21 Ramos C290(1.14)  LDD2195  [27]
 LDCM0582  Fragment23 Ramos C290(0.27)  LDD2196  [27]
 LDCM0578  Fragment27 Ramos C290(0.94)  LDD2197  [27]
 LDCM0586  Fragment28 Ramos C117(0.72); C290(1.26)  LDD2198  [27]
 LDCM0588  Fragment30 Ramos C290(0.72)  LDD2199  [27]
 LDCM0589  Fragment31 Ramos C290(0.94)  LDD2200  [27]
 LDCM0590  Fragment32 Ramos C290(0.74)  LDD2201  [27]
 LDCM0468  Fragment33 HCT 116 C117(0.74); C94(0.88)  LDD0785  [10]
 LDCM0596  Fragment38 Ramos C290(1.91)  LDD2203  [27]
 LDCM0566  Fragment4 Ramos C117(0.73); C290(0.28)  LDD2184  [27]
 LDCM0427  Fragment51 HCT 116 C157(4.37); C117(0.68); C94(0.30)  LDD0744  [10]
 LDCM0610  Fragment52 Ramos C290(0.78)  LDD2204  [27]
 LDCM0614  Fragment56 Ramos C290(0.41)  LDD2205  [27]
 LDCM0569  Fragment7 Ramos C117(0.33); C290(1.91)  LDD2186  [27]
 LDCM0571  Fragment9 Ramos C290(1.13)  LDD2188  [27]
 LDCM0116  HHS-0101 DM93 Y242(0.82)  LDD0264  [9]
 LDCM0117  HHS-0201 DM93 Y242(6.87)  LDD0265  [9]
 LDCM0120  HHS-0701 DM93 Y242(0.61)  LDD0268  [9]
 LDCM0022  KB02 HCT 116 C157(2.61); C117(1.51); C94(1.22)  LDD0080  [10]
 LDCM0023  KB03 HCT 116 C157(7.52); C117(0.49); C94(0.41)  LDD0081  [10]
 LDCM0024  KB05 HCT 116 C157(1.36); C117(0.45); C94(0.40)  LDD0082  [10]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C117(1.28)  LDD2111  [6]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C117(1.46)  LDD2119  [6]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C117(0.92)  LDD2123  [6]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C117(0.79)  LDD2137  [6]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C117(0.93)  LDD2140  [6]
 LDCM0627  NUDT7-COV-1 HEK-293T C157(0.61)  LDD2206  [28]
 LDCM0628  OTUB2-COV-1 HEK-293T C269(1.76); C157(0.70)  LDD2207  [28]
 LDCM0131  RA190 MM1.R C290(1.31); C157(1.11)  LDD0304  [29]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [23]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Peptidyl-prolyl cis-trans isomerase A (PPIA) Cyclophilin-type PPIase family P62937
Ubiquitin carboxyl-terminal hydrolase isozyme L1 (UCHL1) Peptidase C12 family P09936
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
TATA-box-binding protein (TBP) TBP family P20226
Other
Click To Hide/Show 13 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Actin-related protein 3 (ACTR3) Actin family P61158
Cyclin-dependent kinase inhibitor 1 (CDKN1A) CDI family P38936
Cyclin-dependent kinase inhibitor 1B (CDKN1B) CDI family P46527
CDK5 and ABL1 enzyme substrate 1 (CABLES1) Cyclin family Q8TDN4
Cyclin-I (CCNI) Cyclin family Q14094
Cyclin-C (CCNC) Cyclin family P24863
G1/S-specific cyclin-D2 (CCND2) Cyclin family P30279
G1/S-specific cyclin-D3 (CCND3) Cyclin family P30281
Cyclin-dependent kinase 5 activator 1 (CDK5R1) Cyclin-dependent kinase 5 activator family Q15078
Protein Hook homolog 1 (HOOK1) Hook family Q9UJC3
Speedy protein A (SPDYA) Speedy/Ringo family Q5MJ70
Speedy protein E4 (SPDYE4) Speedy/Ringo family A6NLX3
Numb-like protein (NUMBL) . Q9Y6R0

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Trilaciclib . DB15442
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
L-751250 Small molecular drug D0WS1V
Investigative
Click To Hide/Show 20 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-phenyl-3-(2-(Pyridin-4-yl)Thiazol-4-yl)Urea Small molecular drug D0YE4B
10z-hymenialdisine Small molecular drug D0F0AX
3-(2-phenylthiazol-4-yl)Quinolin-2(1h)-one Small molecular drug D04AEG
9-nitropaullone Small molecular drug D0H3EV
Aloisine A Small molecular drug D02XHC
Alsterpaullone Small molecular drug DB04014
Alvocidib Small molecular drug DB03496
Aminopurvalanol A Small molecular drug D0G2GA
Azakenpaullone Small molecular drug D0DR8N
Indirubin-3'-monoxime Small molecular drug D0Y0ES
Indirubin-5-sulfonate Small molecular drug D0G2CT
Manzamine A Small molecular drug D0Q4QF
Nu6140 Small molecular drug D04WFN
Oxindole 16 (Compound 3) Small molecular drug D03ALC
Quinoxaline1 Small molecular drug D0R5FH
Su9516 Small molecular drug D0L3FK
Thieno Analogue Of Kenpaullone Small molecular drug D0TF9P
6-phenyl[5h]Pyrrolo[23-b]Pyrazine . DB07364
Hymenialdisine . DB02950
Oxindole 95 . D0MS4R
Patented
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-(Thiazol-5-yl)-pyrimidine Derivative 2 Small molecular drug D01CJE
Flavonoid Derivative 7 Small molecular drug D0KP8N
Kenpaullone Small molecular drug D00PWQ
Naphthyridine And Isoquinoline Derivative 1 Small molecular drug D08WJG
Pmid26161698-compound-18 Small molecular drug D0F7DS
Pyrazolo[1,5-a]-1,3,5-triazine Derivative 1 Small molecular drug D0NB7Y
Roscovitine Derivative 1 Small molecular drug D07DUX
Tricyclic Benzimidazole Derivative 1 Small molecular drug D0NY7M
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Olomoucine Small molecular drug D00BPA

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 chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
5 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
6 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
7 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
8 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
9 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.
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 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
14 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
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 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
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 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.
21 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
22 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.
23 Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS). J Proteome Res. 2010 Feb 5;9(2):806-17. doi: 10.1021/pr9007333.
24 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.
25 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.
26 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
27 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
28 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.
29 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.