Details of the Target

General Information of Target

Target ID LDTP02149
Target Name Cyclin-dependent kinase 1 (CDK1)
Gene Name CDK1
Gene ID 983
Synonyms
CDC2; CDC28A; CDKN1; P34CDC2; Cyclin-dependent kinase 1; CDK1; EC 2.7.11.22; EC 2.7.11.23; Cell division control protein 2 homolog; Cell division protein kinase 1; p34 protein kinase
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MEDYTKIEKIGEGTYGVVYKGRHKTTGQVVAMKKIRLESEEEGVPSTAIREISLLKELRH
PNIVSLQDVLMQDSRLYLIFEFLSMDLKKYLDSIPPGQYMDSSLVKSYLYQILQGIVFCH
SRRVLHRDLKPQNLLIDDKGTIKLADFGLARAFGIPIRVYTHEVVTLWYRSPEVLLGSAR
YSTPVDIWSIGTIFAELATKKPLFHGDSEIDQLFRIFRALGTPNNEVWPEVESLQDYKNT
FPKWKPGSLASHVKNLDENGLDLLSKMLIYDPAKRISGKMALNHPYFNDLDNQIKKM
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, CDC2/CDKX subfamily
Subcellular location
Nucleus
Function
Plays a key role in the control of the eukaryotic cell cycle by modulating the centrosome cycle as well as mitotic onset; promotes G2-M transition via association with multiple interphase cyclins. Phosphorylates PARVA/actopaxin, APC, AMPH, APC, BARD1, Bcl-xL/BCL2L1, BRCA2, CALD1, CASP8, CDC7, CDC20, CDC25A, CDC25C, CC2D1A, CENPA, CSNK2 proteins/CKII, FZR1/CDH1, CDK7, CEBPB, CHAMP1, DMD/dystrophin, EEF1 proteins/EF-1, EZH2, KIF11/EG5, EGFR, FANCG, FOS, GFAP, GOLGA2/GM130, GRASP1, UBE2A/hHR6A, HIST1H1 proteins/histone H1, HMGA1, HIVEP3/KRC, KAT5, LMNA, LMNB, LBR, LATS1, MAP1B, MAP4, MARCKS, MCM2, MCM4, MKLP1, MLST8, MYB, NEFH, NFIC, NPC/nuclear pore complex, PITPNM1/NIR2, NPM1, NCL, NUCKS1, NPM1/numatrin, ORC1, PRKAR2A, EEF1E1/p18, EIF3F/p47, p53/TP53, NONO/p54NRB, PAPOLA, PLEC/plectin, RB1, TPPP, UL40/R2, RAB4A, RAP1GAP, RCC1, RPS6KB1/S6K1, KHDRBS1/SAM68, ESPL1, SKI, BIRC5/survivin, STIP1, TEX14, beta-tubulins, MAPT/TAU, NEDD1, VIM/vimentin, TK1, FOXO1, RUNX1/AML1, SAMHD1, SIRT2, CGAS and RUNX2. CDK1/CDC2-cyclin-B controls pronuclear union in interphase fertilized eggs. Essential for early stages of embryonic development. During G2 and early mitosis, CDC25A/B/C-mediated dephosphorylation activates CDK1/cyclin complexes which phosphorylate several substrates that trigger at least centrosome separation, Golgi dynamics, nuclear envelope breakdown and chromosome condensation. Once chromosomes are condensed and aligned at the metaphase plate, CDK1 activity is switched off by WEE1- and PKMYT1-mediated phosphorylation to allow sister chromatid separation, chromosome decondensation, reformation of the nuclear envelope and cytokinesis. Phosphorylates KRT5 during prometaphase and metaphase. Inactivated by PKR/EIF2AK2- and WEE1-mediated phosphorylation upon DNA damage to stop cell cycle and genome replication at the G2 checkpoint thus facilitating DNA repair. Reactivated after successful DNA repair through WIP1-dependent signaling leading to CDC25A/B/C-mediated dephosphorylation and restoring cell cycle progression. Catalyzes lamin (LMNA, LMNB1 and LMNB2) phosphorylation at the onset of mitosis, promoting nuclear envelope breakdown. In proliferating cells, CDK1-mediated FOXO1 phosphorylation at the G2-M phase represses FOXO1 interaction with 14-3-3 proteins and thereby promotes FOXO1 nuclear accumulation and transcription factor activity, leading to cell death of postmitotic neurons. The phosphorylation of beta-tubulins regulates microtubule dynamics during mitosis. NEDD1 phosphorylation promotes PLK1-mediated NEDD1 phosphorylation and subsequent targeting of the gamma-tubulin ring complex (gTuRC) to the centrosome, an important step for spindle formation. In addition, CC2D1A phosphorylation regulates CC2D1A spindle pole localization and association with SCC1/RAD21 and centriole cohesion during mitosis. The phosphorylation of Bcl-xL/BCL2L1 after prolongated G2 arrest upon DNA damage triggers apoptosis. In contrast, CASP8 phosphorylation during mitosis prevents its activation by proteolysis and subsequent apoptosis. This phosphorylation occurs in cancer cell lines, as well as in primary breast tissues and lymphocytes. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. CALD1 phosphorylation promotes Schwann cell migration during peripheral nerve regeneration. CDK1-cyclin-B complex phosphorylates NCKAP5L and mediates its dissociation from centrosomes during mitosis. Regulates the amplitude of the cyclic expression of the core clock gene BMAL1 by phosphorylating its transcriptional repressor NR1D1, and this phosphorylation is necessary for SCF(FBXW7)-mediated ubiquitination and proteasomal degradation of NR1D1. Phosphorylates EML3 at 'Thr-881' which is essential for its interaction with HAUS augmin-like complex and TUBG1. Phosphorylates CGAS during mitosis, leading to its inhibition, thereby preventing CGAS activation by self DNA during mitosis.; (Microbial infection) Acts as a receptor for hepatitis C virus (HCV) in hepatocytes and facilitates its cell entry.
TTD ID
T49898
Uniprot ID
P06493
DrugMap ID
TTH6V3D
Ensemble ID
ENST00000316629.8
HGNC ID
HGNC:1722
ChEMBL ID
CHEMBL308

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.A250V .
Ishikawa (Heraklio) 02 ER SNV: p.H284R .
KMCH1 Deletion: p.Y108SfsTer13 DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 33 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info  		10.26  LDD0215  [1]
CHEMBL5175495
 Probe Info  		6.65  LDD0196  [2]
TH211
 Probe Info  		Y286(20.00); Y270(16.74); Y181(14.46); Y237(11.69)  LDD0257  [3]
TH214
 Probe Info  		Y270(8.31)  LDD0258  [3]
TH216
 Probe Info  		Y286(18.26); Y237(14.52); Y270(10.67); Y181(9.57)  LDD0259  [3]
YN-1
 Probe Info  		100.00  LDD0444  [4]
ONAyne
 Probe Info  		N.A.  LDD0273  [5]
Probe 1
 Probe Info  		Y15(66.67); Y19(83.68); Y90(6.99); Y237(8.81)  LDD3495  [6]
DBIA
 Probe Info  		C119(1.67)  LDD3331  [7]
HPAP
 Probe Info  		3.23  LDD0063  [8]
HHS-482
 Probe Info  		Y15(0.67); Y160(1.01); Y19(0.81); Y286(1.05)  LDD0285  [9]
HHS-475
 Probe Info  		Y99(0.59); Y19(1.04); Y181(1.11); Y160(2.06)  LDD0264  [10]
HHS-465
 Probe Info  		Y160(2.30); Y181(4.63); Y19(10.00); Y270(2.37)  LDD2237  [11]
5E-2FA
 Probe Info  		H205(0.00); H284(0.00)  LDD2235  [12]
ATP probe
 Probe Info  		K130(0.00); K201(0.00); K9(0.00); K245(0.00)  LDD0199  [13]
m-APA
 Probe Info  		H205(0.00); H284(0.00)  LDD2231  [12]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [14]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [14]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [14]
ATP probe
 Probe Info  		K130(0.00); K201(0.00)  LDD0035  [15]
KY-26
 Probe Info  		N.A.  LDD0301  [16]
IPM
 Probe Info  		N.A.  LDD2156  [17]
NHS
 Probe Info  		K279(0.00); K6(0.00); K20(0.00); K9(0.00)  LDD0010  [18]
SF
 Probe Info  		K33(0.00); K20(0.00); Y19(0.00)  LDD0028  [19]
STPyne
 Probe Info  		K20(0.00); K9(0.00)  LDD0009  [18]
Ox-W18
 Probe Info  		W244(0.00); W168(0.00); W188(0.00)  LDD2175  [20]
1c-yne
 Probe Info  		K9(0.00); K279(0.00); K238(0.00); K266(0.00)  LDD0228  [21]
1d-yne
 Probe Info  		N.A.  LDD0357  [21]
Acrolein
 Probe Info  		N.A.  LDD0217  [22]
AOyne
 Probe Info  		7.60  LDD0443  [23]
MPP-AC
 Probe Info  		N.A.  LDD0428  [24]
NAIA_5
 Probe Info  		N.A.  LDD2223  [25]
TER-AC
 Probe Info  		N.A.  LDD0426  [24]
PAL-AfBPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C289
 Probe Info  		31.56  LDD1959  [26]
C391
 Probe Info  		16.68  LDD2050  [26]
C432
 Probe Info  		5.54  LDD2087  [26]
FFF probe11
 Probe Info  		9.56  LDD0472  [27]
FFF probe13
 Probe Info  		11.73  LDD0475  [27]
FFF probe14
 Probe Info  		20.00  LDD0477  [27]
FFF probe2
 Probe Info  		8.79  LDD0463  [27]
FFF probe3
 Probe Info  		20.00  LDD0464  [27]
FFF probe6
 Probe Info  		13.63  LDD0482  [27]
DFG-out-3
 Probe Info  		2.10  LDD0074  [28]
DA-2
 Probe Info  		N.A.  LDD0070  [29]
STS-1
 Probe Info  		N.A.  LDD0068  [30]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 PaTu 8988t C119(0.50)  LDD1093  [31]
 LDCM0215  AC10 PaTu 8988t C119(0.34)  LDD1094  [31]
 LDCM0216  AC100 PaTu 8988t C119(0.98)  LDD1095  [31]
 LDCM0217  AC101 PaTu 8988t C119(1.27)  LDD1096  [31]
 LDCM0218  AC102 PaTu 8988t C119(1.14)  LDD1097  [31]
 LDCM0219  AC103 PaTu 8988t C119(0.77)  LDD1098  [31]
 LDCM0220  AC104 PaTu 8988t C119(1.14)  LDD1099  [31]
 LDCM0221  AC105 PaTu 8988t C119(1.83)  LDD1100  [31]
 LDCM0222  AC106 PaTu 8988t C119(0.78)  LDD1101  [31]
 LDCM0223  AC107 PaTu 8988t C119(1.07)  LDD1102  [31]
 LDCM0224  AC108 PaTu 8988t C119(0.94)  LDD1103  [31]
 LDCM0225  AC109 PaTu 8988t C119(0.88)  LDD1104  [31]
 LDCM0226  AC11 PaTu 8988t C119(0.37)  LDD1105  [31]
 LDCM0227  AC110 PaTu 8988t C119(0.76)  LDD1106  [31]
 LDCM0228  AC111 PaTu 8988t C119(1.02)  LDD1107  [31]
 LDCM0229  AC112 PaTu 8988t C119(1.19)  LDD1108  [31]
 LDCM0237  AC12 PaTu 8988t C119(0.50)  LDD1116  [31]
 LDCM0259  AC14 PaTu 8988t C119(0.51)  LDD1138  [31]
 LDCM0270  AC15 PaTu 8988t C119(0.43)  LDD1149  [31]
 LDCM0276  AC17 PaTu 8988t C119(0.62)  LDD1155  [31]
 LDCM0277  AC18 PaTu 8988t C119(0.46)  LDD1156  [31]
 LDCM0278  AC19 PaTu 8988t C119(0.57)  LDD1157  [31]
 LDCM0279  AC2 PaTu 8988t C119(1.20)  LDD1158  [31]
 LDCM0280  AC20 PaTu 8988t C119(0.51)  LDD1159  [31]
 LDCM0281  AC21 PaTu 8988t C119(0.46)  LDD1160  [31]
 LDCM0282  AC22 PaTu 8988t C119(0.36)  LDD1161  [31]
 LDCM0283  AC23 PaTu 8988t C119(0.35)  LDD1162  [31]
 LDCM0284  AC24 PaTu 8988t C119(0.49)  LDD1163  [31]
 LDCM0285  AC25 HEK-293T C119(0.91)  LDD1524  [32]
 LDCM0286  AC26 HEK-293T C119(0.93)  LDD1525  [32]
 LDCM0287  AC27 HEK-293T C119(0.80)  LDD1526  [32]
 LDCM0288  AC28 HEK-293T C119(0.87)  LDD1527  [32]
 LDCM0289  AC29 HEK-293T C119(0.83)  LDD1528  [32]
 LDCM0290  AC3 PaTu 8988t C119(0.66)  LDD1169  [31]
 LDCM0291  AC30 HEK-293T C119(0.88)  LDD1530  [32]
 LDCM0292  AC31 HEK-293T C119(0.95)  LDD1531  [32]
 LDCM0293  AC32 HEK-293T C119(0.96)  LDD1532  [32]
 LDCM0294  AC33 HEK-293T C119(0.90)  LDD1533  [32]
 LDCM0295  AC34 HEK-293T C119(0.88)  LDD1534  [32]
 LDCM0296  AC35 HEK-293T C119(0.71)  LDD1535  [32]
 LDCM0297  AC36 HEK-293T C119(0.89)  LDD1536  [32]
 LDCM0298  AC37 HEK-293T C119(0.92)  LDD1537  [32]
 LDCM0299  AC38 HEK-293T C119(0.90)  LDD1538  [32]
 LDCM0300  AC39 HEK-293T C119(0.86)  LDD1539  [32]
 LDCM0301  AC4 PaTu 8988t C119(0.89)  LDD1180  [31]
 LDCM0302  AC40 HEK-293T C119(1.03)  LDD1541  [32]
 LDCM0303  AC41 HEK-293T C119(0.99)  LDD1542  [32]
 LDCM0304  AC42 HEK-293T C119(0.90)  LDD1543  [32]
 LDCM0305  AC43 HEK-293T C119(0.80)  LDD1544  [32]
 LDCM0306  AC44 HEK-293T C119(0.83)  LDD1545  [32]
 LDCM0307  AC45 HEK-293T C119(0.95)  LDD1546  [32]
 LDCM0308  AC46 HEK-293T C119(0.96)  LDD1547  [32]
 LDCM0309  AC47 HEK-293T C119(0.92)  LDD1548  [32]
 LDCM0310  AC48 HEK-293T C119(0.89)  LDD1549  [32]
 LDCM0311  AC49 HEK-293T C119(1.08)  LDD1550  [32]
 LDCM0312  AC5 PaTu 8988t C119(0.90)  LDD1191  [31]
 LDCM0313  AC50 HEK-293T C119(0.97)  LDD1552  [32]
 LDCM0314  AC51 HEK-293T C119(0.82)  LDD1553  [32]
 LDCM0315  AC52 HEK-293T C119(0.86)  LDD1554  [32]
 LDCM0316  AC53 HEK-293T C119(0.89)  LDD1555  [32]
 LDCM0317  AC54 HEK-293T C119(0.91)  LDD1556  [32]
 LDCM0318  AC55 HEK-293T C119(0.88)  LDD1557  [32]
 LDCM0319  AC56 HEK-293T C119(1.03)  LDD1558  [32]
 LDCM0320  AC57 PaTu 8988t C119(1.28)  LDD1199  [31]
 LDCM0321  AC58 PaTu 8988t C119(0.85)  LDD1200  [31]
 LDCM0322  AC59 PaTu 8988t C119(0.90)  LDD1201  [31]
 LDCM0323  AC6 PaTu 8988t C119(0.73)  LDD1202  [31]
 LDCM0324  AC60 PaTu 8988t C119(0.96)  LDD1203  [31]
 LDCM0325  AC61 PaTu 8988t C119(0.86)  LDD1204  [31]
 LDCM0326  AC62 PaTu 8988t C119(1.50)  LDD1205  [31]
 LDCM0327  AC63 PaTu 8988t C119(1.21)  LDD1206  [31]
 LDCM0328  AC64 PaTu 8988t C119(1.02)  LDD1207  [31]
 LDCM0329  AC65 PaTu 8988t C119(0.87)  LDD1208  [31]
 LDCM0330  AC66 PaTu 8988t C119(0.71)  LDD1209  [31]
 LDCM0331  AC67 PaTu 8988t C119(1.03)  LDD1210  [31]
 LDCM0332  AC68 PaTu 8988t C119(1.41)  LDD1211  [31]
 LDCM0333  AC69 PaTu 8988t C119(0.89)  LDD1212  [31]
 LDCM0334  AC7 PaTu 8988t C119(1.00)  LDD1213  [31]
 LDCM0335  AC70 PaTu 8988t C119(1.14)  LDD1214  [31]
 LDCM0336  AC71 PaTu 8988t C119(1.05)  LDD1215  [31]
 LDCM0337  AC72 PaTu 8988t C119(1.45)  LDD1216  [31]
 LDCM0338  AC73 PaTu 8988t C119(1.97)  LDD1217  [31]
 LDCM0339  AC74 PaTu 8988t C119(2.08)  LDD1218  [31]
 LDCM0340  AC75 PaTu 8988t C119(0.77)  LDD1219  [31]
 LDCM0341  AC76 PaTu 8988t C119(1.29)  LDD1220  [31]
 LDCM0342  AC77 PaTu 8988t C119(0.97)  LDD1221  [31]
 LDCM0343  AC78 PaTu 8988t C119(1.77)  LDD1222  [31]
 LDCM0344  AC79 PaTu 8988t C119(0.92)  LDD1223  [31]
 LDCM0345  AC8 PaTu 8988t C119(0.60)  LDD1224  [31]
 LDCM0346  AC80 PaTu 8988t C119(1.30)  LDD1225  [31]
 LDCM0347  AC81 PaTu 8988t C119(1.46)  LDD1226  [31]
 LDCM0348  AC82 PaTu 8988t C119(1.70)  LDD1227  [31]
 LDCM0349  AC83 PaTu 8988t C119(1.16)  LDD1228  [31]
 LDCM0350  AC84 PaTu 8988t C119(1.12)  LDD1229  [31]
 LDCM0351  AC85 PaTu 8988t C119(1.27)  LDD1230  [31]
 LDCM0352  AC86 PaTu 8988t C119(1.19)  LDD1231  [31]
 LDCM0353  AC87 PaTu 8988t C119(1.54)  LDD1232  [31]
 LDCM0354  AC88 PaTu 8988t C119(1.36)  LDD1233  [31]
 LDCM0355  AC89 PaTu 8988t C119(1.09)  LDD1234  [31]
 LDCM0357  AC90 PaTu 8988t C119(1.93)  LDD1236  [31]
 LDCM0358  AC91 PaTu 8988t C119(1.58)  LDD1237  [31]
 LDCM0359  AC92 PaTu 8988t C119(1.11)  LDD1238  [31]
 LDCM0360  AC93 PaTu 8988t C119(2.65)  LDD1239  [31]
 LDCM0361  AC94 PaTu 8988t C119(1.50)  LDD1240  [31]
 LDCM0362  AC95 PaTu 8988t C119(1.21)  LDD1241  [31]
 LDCM0363  AC96 PaTu 8988t C119(2.40)  LDD1242  [31]
 LDCM0364  AC97 PaTu 8988t C119(1.63)  LDD1243  [31]
 LDCM0365  AC98 PaTu 8988t C119(0.96)  LDD1244  [31]
 LDCM0366  AC99 PaTu 8988t C119(1.07)  LDD1245  [31]
 LDCM0248  AKOS034007472 PaTu 8988t C119(0.37)  LDD1127  [31]
 LDCM0356  AKOS034007680 PaTu 8988t C119(0.59)  LDD1235  [31]
 LDCM0275  AKOS034007705 PaTu 8988t C119(0.49)  LDD1154  [31]
 LDCM0108  Chloroacetamide HeLa H205(0.00); H252(0.00)  LDD0222  [22]
 LDCM0367  CL1 HEK-293T C119(1.06)  LDD1571  [32]
 LDCM0368  CL10 HEK-293T C119(1.01)  LDD1572  [32]
 LDCM0369  CL100 PaTu 8988t C119(0.66)  LDD1248  [31]
 LDCM0370  CL101 PaTu 8988t C119(0.73)  LDD1249  [31]
 LDCM0371  CL102 PaTu 8988t C119(0.58)  LDD1250  [31]
 LDCM0372  CL103 PaTu 8988t C119(0.38)  LDD1251  [31]
 LDCM0373  CL104 PaTu 8988t C119(0.51)  LDD1252  [31]
 LDCM0374  CL105 PaTu 8988t C119(0.70)  LDD1253  [31]
 LDCM0375  CL106 PaTu 8988t C119(0.78)  LDD1254  [31]
 LDCM0376  CL107 PaTu 8988t C119(1.10)  LDD1255  [31]
 LDCM0377  CL108 PaTu 8988t C119(0.84)  LDD1256  [31]
 LDCM0378  CL109 PaTu 8988t C119(0.62)  LDD1257  [31]
 LDCM0379  CL11 HEK-293T C119(0.88)  LDD1583  [32]
 LDCM0380  CL110 PaTu 8988t C119(0.56)  LDD1259  [31]
 LDCM0381  CL111 PaTu 8988t C119(0.35)  LDD1260  [31]
 LDCM0382  CL112 HEK-293T C119(1.15)  LDD1586  [32]
 LDCM0383  CL113 HEK-293T C119(0.96)  LDD1587  [32]
 LDCM0384  CL114 HEK-293T C119(1.69)  LDD1588  [32]
 LDCM0385  CL115 HEK-293T C119(0.86)  LDD1589  [32]
 LDCM0386  CL116 HEK-293T C119(0.99)  LDD1590  [32]
 LDCM0387  CL117 HEK-293T C119(1.01)  LDD1591  [32]
 LDCM0388  CL118 HEK-293T C119(1.02)  LDD1592  [32]
 LDCM0389  CL119 HEK-293T C119(0.81)  LDD1593  [32]
 LDCM0390  CL12 HEK-293T C119(1.04)  LDD1594  [32]
 LDCM0391  CL120 HEK-293T C119(1.00)  LDD1595  [32]
 LDCM0392  CL121 HEK-293T C119(0.95)  LDD1596  [32]
 LDCM0393  CL122 HEK-293T C119(0.97)  LDD1597  [32]
 LDCM0394  CL123 HEK-293T C119(1.14)  LDD1598  [32]
 LDCM0395  CL124 HEK-293T C119(1.01)  LDD1599  [32]
 LDCM0396  CL125 PaTu 8988t C119(1.10)  LDD1275  [31]
 LDCM0397  CL126 PaTu 8988t C119(0.92)  LDD1276  [31]
 LDCM0398  CL127 PaTu 8988t C119(1.21)  LDD1277  [31]
 LDCM0399  CL128 PaTu 8988t C119(0.93)  LDD1278  [31]
 LDCM0400  CL13 HEK-293T C119(0.89)  LDD1604  [32]
 LDCM0401  CL14 HEK-293T C119(0.88)  LDD1605  [32]
 LDCM0402  CL15 HEK-293T C119(1.11)  LDD1606  [32]
 LDCM0403  CL16 HEK-293T C119(1.05)  LDD1607  [32]
 LDCM0404  CL17 HEK-293T C119(1.26)  LDD1608  [32]
 LDCM0405  CL18 HEK-293T C119(0.87)  LDD1609  [32]
 LDCM0406  CL19 HEK-293T C119(0.70)  LDD1610  [32]
 LDCM0407  CL2 HEK-293T C119(0.77)  LDD1611  [32]
 LDCM0408  CL20 HEK-293T C119(0.82)  LDD1612  [32]
 LDCM0409  CL21 HEK-293T C119(0.73)  LDD1613  [32]
 LDCM0410  CL22 HEK-293T C119(0.75)  LDD1614  [32]
 LDCM0411  CL23 HEK-293T C119(0.79)  LDD1615  [32]
 LDCM0412  CL24 HEK-293T C119(1.03)  LDD1616  [32]
 LDCM0413  CL25 HEK-293T C119(1.44)  LDD1617  [32]
 LDCM0414  CL26 HEK-293T C119(1.03)  LDD1618  [32]
 LDCM0415  CL27 HEK-293T C119(0.88)  LDD1619  [32]
 LDCM0416  CL28 HEK-293T C119(1.19)  LDD1620  [32]
 LDCM0417  CL29 HEK-293T C119(0.91)  LDD1621  [32]
 LDCM0418  CL3 HEK-293T C119(1.01)  LDD1622  [32]
 LDCM0419  CL30 HEK-293T C119(0.86)  LDD1623  [32]
 LDCM0420  CL31 HEK-293T C119(0.70)  LDD1624  [32]
 LDCM0421  CL32 HEK-293T C119(0.83)  LDD1625  [32]
 LDCM0422  CL33 HEK-293T C119(1.19)  LDD1626  [32]
 LDCM0423  CL34 HEK-293T C119(0.93)  LDD1627  [32]
 LDCM0424  CL35 HEK-293T C119(0.83)  LDD1628  [32]
 LDCM0425  CL36 HEK-293T C119(1.18)  LDD1629  [32]
 LDCM0426  CL37 HEK-293T C119(0.95)  LDD1630  [32]
 LDCM0428  CL39 HEK-293T C119(0.95)  LDD1632  [32]
 LDCM0429  CL4 HEK-293T C119(0.97)  LDD1633  [32]
 LDCM0430  CL40 HEK-293T C119(0.88)  LDD1634  [32]
 LDCM0431  CL41 HEK-293T C119(1.01)  LDD1635  [32]
 LDCM0432  CL42 HEK-293T C119(0.80)  LDD1636  [32]
 LDCM0433  CL43 HEK-293T C119(0.85)  LDD1637  [32]
 LDCM0434  CL44 HEK-293T C119(0.84)  LDD1638  [32]
 LDCM0435  CL45 HEK-293T C119(1.00)  LDD1639  [32]
 LDCM0436  CL46 PaTu 8988t C119(0.93)  LDD1315  [31]
 LDCM0437  CL47 PaTu 8988t C119(0.69)  LDD1316  [31]
 LDCM0438  CL48 PaTu 8988t C119(0.94)  LDD1317  [31]
 LDCM0439  CL49 PaTu 8988t C119(0.90)  LDD1318  [31]
 LDCM0440  CL5 HEK-293T C119(0.81)  LDD1644  [32]
 LDCM0441  CL50 PaTu 8988t C119(0.60)  LDD1320  [31]
 LDCM0442  CL51 PaTu 8988t C119(0.76)  LDD1321  [31]
 LDCM0443  CL52 PaTu 8988t C119(0.89)  LDD1322  [31]
 LDCM0444  CL53 PaTu 8988t C119(0.70)  LDD1323  [31]
 LDCM0445  CL54 PaTu 8988t C119(0.68)  LDD1324  [31]
 LDCM0446  CL55 PaTu 8988t C119(0.63)  LDD1325  [31]
 LDCM0447  CL56 PaTu 8988t C119(0.15)  LDD1326  [31]
 LDCM0448  CL57 PaTu 8988t C119(0.34)  LDD1327  [31]
 LDCM0449  CL58 PaTu 8988t C119(0.49)  LDD1328  [31]
 LDCM0450  CL59 PaTu 8988t C119(0.37)  LDD1329  [31]
 LDCM0451  CL6 HEK-293T C119(1.30)  LDD1654  [32]
 LDCM0452  CL60 PaTu 8988t C119(0.34)  LDD1331  [31]
 LDCM0453  CL61 HEK-293T C119(0.95)  LDD1656  [32]
 LDCM0454  CL62 HEK-293T C119(0.89)  LDD1657  [32]
 LDCM0455  CL63 HEK-293T C119(0.79)  LDD1658  [32]
 LDCM0456  CL64 HEK-293T C119(1.13)  LDD1659  [32]
 LDCM0457  CL65 HEK-293T C119(0.76)  LDD1660  [32]
 LDCM0458  CL66 HEK-293T C119(0.88)  LDD1661  [32]
 LDCM0459  CL67 HEK-293T C119(0.67)  LDD1662  [32]
 LDCM0460  CL68 HEK-293T C119(0.81)  LDD1663  [32]
 LDCM0461  CL69 HEK-293T C119(0.95)  LDD1664  [32]
 LDCM0462  CL7 HEK-293T C119(0.81)  LDD1665  [32]
 LDCM0463  CL70 HEK-293T C119(0.81)  LDD1666  [32]
 LDCM0464  CL71 HEK-293T C119(0.82)  LDD1667  [32]
 LDCM0465  CL72 HEK-293T C119(1.04)  LDD1668  [32]
 LDCM0466  CL73 HEK-293T C119(1.06)  LDD1669  [32]
 LDCM0467  CL74 HEK-293T C119(0.88)  LDD1670  [32]
 LDCM0469  CL76 HEK-293T C119(1.10)  LDD1672  [32]
 LDCM0470  CL77 HEK-293T C119(1.14)  LDD1673  [32]
 LDCM0471  CL78 HEK-293T C119(0.99)  LDD1674  [32]
 LDCM0472  CL79 HEK-293T C119(0.78)  LDD1675  [32]
 LDCM0473  CL8 HEK-293T C119(2.01)  LDD1676  [32]
 LDCM0474  CL80 HEK-293T C119(0.85)  LDD1677  [32]
 LDCM0475  CL81 HEK-293T C119(0.91)  LDD1678  [32]
 LDCM0476  CL82 HEK-293T C119(0.94)  LDD1679  [32]
 LDCM0477  CL83 HEK-293T C119(0.88)  LDD1680  [32]
 LDCM0478  CL84 HEK-293T C119(1.16)  LDD1681  [32]
 LDCM0479  CL85 HEK-293T C119(0.94)  LDD1682  [32]
 LDCM0480  CL86 HEK-293T C119(0.93)  LDD1683  [32]
 LDCM0481  CL87 HEK-293T C119(0.86)  LDD1684  [32]
 LDCM0482  CL88 HEK-293T C119(0.96)  LDD1685  [32]
 LDCM0483  CL89 HEK-293T C119(0.84)  LDD1686  [32]
 LDCM0484  CL9 HEK-293T C119(0.93)  LDD1687  [32]
 LDCM0485  CL90 HEK-293T C119(1.79)  LDD1688  [32]
 LDCM0486  CL91 PaTu 8988t C119(0.80)  LDD1365  [31]
 LDCM0487  CL92 PaTu 8988t C119(0.76)  LDD1366  [31]
 LDCM0488  CL93 PaTu 8988t C119(0.83)  LDD1367  [31]
 LDCM0489  CL94 PaTu 8988t C119(1.04)  LDD1368  [31]
 LDCM0490  CL95 PaTu 8988t C119(0.86)  LDD1369  [31]
 LDCM0491  CL96 PaTu 8988t C119(0.74)  LDD1370  [31]
 LDCM0492  CL97 PaTu 8988t C119(0.92)  LDD1371  [31]
 LDCM0493  CL98 PaTu 8988t C119(0.82)  LDD1372  [31]
 LDCM0494  CL99 PaTu 8988t C119(1.16)  LDD1373  [31]
 LDCM0495  E2913 HEK-293T C119(0.86)  LDD1698  [32]
 LDCM0468  Fragment33 HEK-293T C119(0.99)  LDD1671  [32]
 LDCM0427  Fragment51 HEK-293T C119(0.82)  LDD1631  [32]
 LDCM0116  HHS-0101 DM93 Y99(0.59); Y19(1.04); Y181(1.11); Y160(2.06)  LDD0264  [10]
 LDCM0117  HHS-0201 DM93 Y19(0.57); Y160(0.80); Y99(1.21); Y181(1.36)  LDD0265  [10]
 LDCM0118  HHS-0301 DM93 Y160(0.54); Y19(0.64); Y181(1.40); Y99(2.46)  LDD0266  [10]
 LDCM0119  HHS-0401 DM93 Y160(0.51); Y19(0.78); Y99(1.32); Y181(1.88)  LDD0267  [10]
 LDCM0120  HHS-0701 DM93 Y99(0.71); Y160(0.80); Y19(1.07); Y181(1.26)  LDD0268  [10]
 LDCM0107  IAA HeLa N.A.  LDD0221  [22]
 LDCM0123  JWB131 DM93 Y15(0.67); Y160(1.01); Y19(0.81); Y286(1.05)  LDD0285  [9]
 LDCM0124  JWB142 DM93 Y15(0.60); Y160(1.06); Y19(0.63); Y286(0.71)  LDD0286  [9]
 LDCM0125  JWB146 DM93 Y15(0.96); Y160(1.32); Y19(1.09); Y286(1.41)  LDD0287  [9]
 LDCM0126  JWB150 DM93 Y15(3.00); Y160(4.10); Y19(2.91); Y286(2.47)  LDD0288  [9]
 LDCM0127  JWB152 DM93 Y15(1.55); Y160(5.11); Y19(1.74); Y286(1.88)  LDD0289  [9]
 LDCM0128  JWB198 DM93 Y15(0.58); Y160(2.57); Y19(1.06); Y286(1.05)  LDD0290  [9]
 LDCM0129  JWB202 DM93 Y15(0.44); Y160(0.49); Y19(0.55); Y286(0.57)  LDD0291  [9]
 LDCM0130  JWB211 DM93 Y15(0.83); Y160(1.87); Y19(0.89); Y286(1.06)  LDD0292  [9]
 LDCM0022  KB02 HEK-293T C119(1.08)  LDD1492  [32]
 LDCM0023  KB03 HEK-293T C119(1.20)  LDD1497  [32]
 LDCM0024  KB05 MKN-1 C119(1.67)  LDD3331  [7]
 LDCM0109  NEM HeLa H60(0.00); H205(0.00)  LDD0223  [22]
 LDCM0627  NUDT7-COV-1 HEK-293T C119(0.28)  LDD2206  [33]
 LDCM0628  OTUB2-COV-1 HEK-293T C119(0.40); C119(0.19)  LDD2207  [33]
 LDCM0014  Panhematin K562 3.23  LDD0063  [8]
 LDCM0016  Ranjitkar_cp1 A431 2.10  LDD0074  [28]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Dihydrolipoyllysine-residue succinyltransferase component of 2-oxoglutarate dehydrogenase complex, mitochondrial (DLST) 2-oxoacid dehydrogenase family P36957
M-phase inducer phosphatase 3 (CDC25C) MPI phosphatase family P30307
Serine/threonine-protein kinase LATS1 (LATS1) AGC Ser/Thr protein kinase family O95835
Interferon-induced, double-stranded RNA-activated protein kinase (EIF2AK2) Ser/Thr protein kinase family P19525
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (PKMYT1) Ser/Thr protein kinase family Q99640
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
THO complex subunit 4 (ALYREF) ALYREF family Q86V81
Amyloid-beta precursor protein (APP) APP family P05067
G2/mitotic-specific cyclin-B1 (CCNB1) Cyclin family P14635
Voltage-dependent anion-selective channel protein 1 (VDAC1) Eukaryotic mitochondrial porin family P21796
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Forkhead box protein O1 (FOXO1) . Q12778
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tumor necrosis factor ligand superfamily member 12 (TNFSF12) Tumor necrosis factor family O43508
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cell division control protein 6 homolog (CDC6) CDC6/cdc18 family Q99741
Cyclin-dependent kinase inhibitor 1 (CDKN1A) CDI family P38936
Cyclin-dependent kinase inhibitor 1B (CDKN1B) CDI family P46527
Cyclin-dependent kinases regulatory subunit 1 (CKS1B) CKS family P61024
Baculoviral IAP repeat-containing protein 5 (BIRC5) IAP family O15392
Polyubiquitin-C (UBC) Ubiquitin family P0CG48

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Phase 2
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
P-276 Small molecular drug D0W8IY
P276-00 Small molecular drug D05IRT
R-roscovitine Small molecular drug D05ADP
Ro 31-7453 Small molecular drug D01UMT
Phase 1
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ag-024322 Small molecular drug D0IX4B
Pha-793887 Small molecular drug D0P1CV
Rgb-286638 Small molecular drug D03DKV
Preclinical
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
L-751250 Small molecular drug D0WS1V
On-01135 . D02MNY
Investigative
Click To Hide/Show 43 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2,6-diamino-pyridin-3-yl)-phenyl-methanone Small molecular drug D03XGJ
10z-hymenialdisine Small molecular drug D0F0AX
2-(P-toluidino)-4-phenylpyrimidine-5-carbonitrile Small molecular drug D0E9DI
3,4-bis(Indol-3-yl)Maleimide Derivative Small molecular drug D07HRP
3,4-di-(4-methoxyphenyl)-1h-pyrrole-2,5-dione Small molecular drug D00NYT
3,4-diphenyl-1h-pyrrole-2,5-dione Small molecular drug D0C3WY
3-(4-methoxyphenyl)-4-phenyl-1h-pyrrole-2,5-dione Small molecular drug D0EK0G
3-(Indole-3-yl)-4-phenyl-1h-pyrrole-2,5-dione Small molecular drug D06AOY
4-(Quinolin-3-yl)-n-p-tolylpyrimidin-2-amine Small molecular drug D0Y7QZ
4-(Quinolin-4-yl)-n-p-tolylpyrimidin-2-amine Small molecular drug D0L5GS
4-phenyl-2-(Phenylamino)Pyrimidine-5-carbonitrile Small molecular drug D06BVH
9-nitropaullone Small molecular drug D0H3EV
Aloisine A Small molecular drug D02XHC
Alsterpaullone Small molecular drug DB04014
Alsterpaullone 2-cyanoethyl Small molecular drug D05NKG
Alvocidib Small molecular drug DB03496
Aminopurvalanol A Small molecular drug D0G2GA
At-7519 Small molecular drug DB08142
Azakenpaullone Small molecular drug D0DR8N
Bisindolylmaleimide-i Small molecular drug D0TO6S
Bms-265246 Small molecular drug D05SZH
Cdk1 Inhibitor Small molecular drug D03YVL
Cdk1/2 Inhibitor Iii Small molecular drug D07OCA
Cgp74514a Small molecular drug D0D2FC
Cvt-313 Small molecular drug D0P2WA
In1535 Small molecular drug D0DM5S
Indirubin-3'-monoxime Small molecular drug D0Y0ES
Indirubin-5-sulfonate Small molecular drug D0G2CT
Jnj-7706621 Small molecular drug D04NGS
K00024 Small molecular drug D0D5HQ
Microxine Small molecular drug D08JML
Nu6140 Small molecular drug D04WFN
Pf-228 Small molecular drug D02QAZ
Pmid18986805c9b Small molecular drug D0P6JS
Pmid19115845c89s Small molecular drug D0T8NU
Purvalanol A Small molecular drug D07OAT
Quinoxaline1 Small molecular drug D0R5FH
Ro-316233 Small molecular drug D0L8HO
Seliciclib Small molecular drug DB06195
Su9516 Small molecular drug D0L3FK
Thieno Analogue Of Kenpaullone Small molecular drug D0TF9P
Avotaciclib . DB16652
Hymenialdisine . DB02950
Patented
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4-(Thiazol-5-yl)-pyrimidine Derivative 2 Small molecular drug D01CJE
Chir-99021 Small molecular drug D0YK9D
Indole-based Analog 13 Small molecular drug D0LX6X
Kenpaullone Small molecular drug D00PWQ
Naphthyridine And Isoquinoline Derivative 1 Small molecular drug D08WJG
Oxazolyl Methylthiothiazole Derivative 1 Small molecular drug D0M5DX
Pmid25991433-compound-a1 Small molecular drug D0H4HD
Pyrazolo[1,5-a]-1,3,5-triazine Derivative 1 Small molecular drug D0NB7Y
Pyrrolo[2,3-d]Pyrimidine Derivative 10 Small molecular drug D04AKA
Pyrrolo[2,3-d]Pyrimidine Derivative 9 Small molecular drug D08KKC
Roscovitine Derivative 1 Small molecular drug D07DUX
Tricyclic Benzimidazole Derivative 1 Small molecular drug D0NY7M
Isoquinoline 1,3-dione Derivative 1 . D0W4MN
Discontinued
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bay 10-00394 Small molecular drug D0NV9O
Cgp-60474 Small molecular drug D0U2TQ
Olomoucine Small molecular drug D00BPA
R547 Small molecular drug D04FHB
Sch 727965 Small molecular drug D0D3PX
Zk 304709 Small molecular drug D00VBT

References

1 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
2 Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20. ACS Med Chem Lett. 2022 Sep 26;13(10):1648-1654. doi: 10.1021/acsmedchemlett.2c00336. eCollection 2022 Oct 13.
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 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
5 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
6 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.
7 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
8 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
9 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.
10 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.
11 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.
12 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
13 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.
14 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
15 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
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 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
18 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
19 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
20 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
21 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.
22 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.
23 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.
24 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
25 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
26 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
27 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.
28 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.
29 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
30 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
31 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.
32 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
33 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.