Details of the Target

General Information of Target

Target ID LDTP00422
Target Name Serine/threonine-protein kinase Chk1 (CHEK1)
Gene Name CHEK1
Gene ID 1111
Synonyms
CHK1; Serine/threonine-protein kinase Chk1; EC 2.7.11.1; CHK1 checkpoint homolog; Cell cycle checkpoint kinase; Checkpoint kinase-1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINK
MLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVY
LHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLK
RREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLA
LLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDF
SPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLL
GTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRR
NNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, NIM1 subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest and activation of DNA repair in response to the presence of DNA damage or unreplicated DNA. May also negatively regulate cell cycle progression during unperturbed cell cycles. This regulation is achieved by a number of mechanisms that together help to preserve the integrity of the genome. Recognizes the substrate consensus sequence [R-X-X-S/T]. Binds to and phosphorylates CDC25A, CDC25B and CDC25C. Phosphorylation of CDC25A at 'Ser-178' and 'Thr-507' and phosphorylation of CDC25C at 'Ser-216' creates binding sites for 14-3-3 proteins which inhibit CDC25A and CDC25C. Phosphorylation of CDC25A at 'Ser-76', 'Ser-124', 'Ser-178', 'Ser-279' and 'Ser-293' promotes proteolysis of CDC25A . Phosphorylation of CDC25A at 'Ser-76' primes the protein for subsequent phosphorylation at 'Ser-79', 'Ser-82' and 'Ser-88' by NEK11, which is required for polyubiquitination and degradation of CDCD25A. Inhibition of CDC25 leads to increased inhibitory tyrosine phosphorylation of CDK-cyclin complexes and blocks cell cycle progression. Also phosphorylates NEK6. Binds to and phosphorylates RAD51 at 'Thr-309', which promotes the release of RAD51 from BRCA2 and enhances the association of RAD51 with chromatin, thereby promoting DNA repair by homologous recombination. Phosphorylates multiple sites within the C-terminus of TP53, which promotes activation of TP53 by acetylation and promotes cell cycle arrest and suppression of cellular proliferation. Also promotes repair of DNA cross-links through phosphorylation of FANCE. Binds to and phosphorylates TLK1 at 'Ser-743', which prevents the TLK1-dependent phosphorylation of the chromatin assembly factor ASF1A. This may enhance chromatin assembly both in the presence or absence of DNA damage. May also play a role in replication fork maintenance through regulation of PCNA. May regulate the transcription of genes that regulate cell-cycle progression through the phosphorylation of histones. Phosphorylates histone H3.1 (to form H3T11ph), which leads to epigenetic inhibition of a subset of genes. May also phosphorylate RB1 to promote its interaction with the E2F family of transcription factors and subsequent cell cycle arrest. Phosphorylates SPRTN, promoting SPRTN recruitment to chromatin. Reduces replication stress and activates the G2/M checkpoint, by phosphorylating and inactivating PABIR1/FAM122A and promoting the serine/threonine-protein phosphatase 2A-mediated dephosphorylation and stabilization of WEE1 levels and activity.; [Isoform 2]: Endogenous repressor of isoform 1, interacts with, and antagonizes CHK1 to promote the S to G2/M phase transition.
TTD ID
T62449
Uniprot ID
O14757
DrugMap ID
TTTU902
Ensemble ID
ENST00000278916.8
HGNC ID
HGNC:1925
ChEMBL ID
CHEMBL4630

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL51 Deletion: p.L355Ter .
IGROV1 Deletion: p.T226HfsTer14 .
NCIH358 Insertion: p.G117_V118insGG .
REH SNV: p.D209N DBIA    Probe Info 
SKMEL24 SNV: p.R453Ter .
TE4 SNV: p.D434Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 14 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
CY-1
 Probe Info  		100.00  LDD0243  [2]
STPyne
 Probe Info  		K452(1.23); K53(8.33)  LDD0277  [3]
BTD
 Probe Info  		C48(0.49)  LDD2089  [4]
AHL-Pu-1
 Probe Info  		C57(2.57); C349(2.55)  LDD0169  [5]
DBIA
 Probe Info  		C408(1.08)  LDD0078  [6]
ATP probe
 Probe Info  		N.A.  LDD0199  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		C48(0.00); C349(0.00); C168(0.00); C408(0.00)  LDD0038  [8]
IA-alkyne
 Probe Info  		C349(0.00); C168(0.00); C48(0.00)  LDD0036  [8]
Lodoacetamide azide
 Probe Info  		C349(0.00); C168(0.00); C48(0.00); C408(0.00)  LDD0037  [8]
IPM
 Probe Info  		N.A.  LDD0005  [9]
TFBX
 Probe Info  		C392(0.00); C168(0.00)  LDD0148  [10]
AOyne
 Probe Info  		15.00  LDD0443  [11]
NAIA_5
 Probe Info  		N.A.  LDD2223  [12]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C305
 Probe Info  		12.21  LDD1974  [13]
FFF probe11
 Probe Info  		20.00  LDD0471  [14]
FFF probe2
 Probe Info  		20.00  LDD0463  [14]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C48(0.80)  LDD2142  [4]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C48(1.02)  LDD2112  [4]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C48(1.06)  LDD2117  [4]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C392(1.06)  LDD2152  [4]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C48(0.95)  LDD2103  [4]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C48(0.55)  LDD2132  [4]
 LDCM0025  4SU-RNA DM93 C57(3.24)  LDD0170  [5]
 LDCM0026  4SU-RNA+native RNA HEK-293T C57(2.57); C349(2.55)  LDD0169  [5]
 LDCM0214  AC1 HCT 116 C408(1.01); C48(0.97)  LDD0531  [6]
 LDCM0215  AC10 HCT 116 C408(1.20); C48(1.04); C87(0.46)  LDD0532  [6]
 LDCM0216  AC100 HCT 116 C408(1.12); C48(0.78)  LDD0533  [6]
 LDCM0217  AC101 HCT 116 C408(1.23); C48(1.11)  LDD0534  [6]
 LDCM0218  AC102 HCT 116 C408(1.04); C48(0.86)  LDD0535  [6]
 LDCM0219  AC103 HCT 116 C408(1.17); C48(0.99)  LDD0536  [6]
 LDCM0220  AC104 HCT 116 C408(2.12); C48(0.91)  LDD0537  [6]
 LDCM0221  AC105 HCT 116 C408(1.52); C48(0.93)  LDD0538  [6]
 LDCM0222  AC106 HCT 116 C408(1.09); C48(1.01)  LDD0539  [6]
 LDCM0223  AC107 HCT 116 C408(1.22); C48(1.03)  LDD0540  [6]
 LDCM0224  AC108 HCT 116 C408(0.84); C48(0.87)  LDD0541  [6]
 LDCM0225  AC109 HCT 116 C408(0.92); C48(0.79)  LDD0542  [6]
 LDCM0226  AC11 HCT 116 C408(1.15); C48(1.07); C87(0.53)  LDD0543  [6]
 LDCM0227  AC110 HCT 116 C408(0.92); C48(0.91)  LDD0544  [6]
 LDCM0228  AC111 HCT 116 C408(1.11); C48(0.82)  LDD0545  [6]
 LDCM0229  AC112 HCT 116 C408(1.50); C48(0.97)  LDD0546  [6]
 LDCM0230  AC113 HCT 116 C408(1.16); C48(1.01)  LDD0547  [6]
 LDCM0231  AC114 HCT 116 C408(0.90); C48(1.02)  LDD0548  [6]
 LDCM0232  AC115 HCT 116 C408(1.30); C48(0.94)  LDD0549  [6]
 LDCM0233  AC116 HCT 116 C408(1.47); C48(1.01)  LDD0550  [6]
 LDCM0234  AC117 HCT 116 C408(1.28); C48(1.07)  LDD0551  [6]
 LDCM0235  AC118 HCT 116 C408(0.94); C48(1.09)  LDD0552  [6]
 LDCM0236  AC119 HCT 116 C408(1.22); C48(1.22)  LDD0553  [6]
 LDCM0237  AC12 HCT 116 C408(1.14); C48(1.04); C87(0.43)  LDD0554  [6]
 LDCM0238  AC120 HCT 116 C408(1.03); C48(1.04)  LDD0555  [6]
 LDCM0239  AC121 HCT 116 C408(0.95); C48(0.91)  LDD0556  [6]
 LDCM0240  AC122 HCT 116 C408(1.12); C48(1.33)  LDD0557  [6]
 LDCM0241  AC123 HCT 116 C408(1.16); C48(0.88)  LDD0558  [6]
 LDCM0242  AC124 HCT 116 C408(1.01); C48(1.02)  LDD0559  [6]
 LDCM0243  AC125 HCT 116 C408(1.04); C48(1.23)  LDD0560  [6]
 LDCM0244  AC126 HCT 116 C408(1.22); C48(1.03)  LDD0561  [6]
 LDCM0245  AC127 HCT 116 C408(1.05); C48(1.09)  LDD0562  [6]
 LDCM0246  AC128 HCT 116 C408(0.97)  LDD0563  [6]
 LDCM0247  AC129 HCT 116 C408(0.91)  LDD0564  [6]
 LDCM0249  AC130 HCT 116 C408(1.15)  LDD0566  [6]
 LDCM0250  AC131 HCT 116 C408(0.85)  LDD0567  [6]
 LDCM0251  AC132 HCT 116 C408(1.13)  LDD0568  [6]
 LDCM0252  AC133 HCT 116 C408(0.81)  LDD0569  [6]
 LDCM0253  AC134 HCT 116 C408(1.13)  LDD0570  [6]
 LDCM0254  AC135 HCT 116 C408(0.96)  LDD0571  [6]
 LDCM0255  AC136 HCT 116 C408(1.09)  LDD0572  [6]
 LDCM0256  AC137 HCT 116 C408(1.19)  LDD0573  [6]
 LDCM0257  AC138 HCT 116 C408(1.63)  LDD0574  [6]
 LDCM0258  AC139 HCT 116 C408(1.18)  LDD0575  [6]
 LDCM0259  AC14 HCT 116 C408(1.23); C48(1.25); C87(0.48)  LDD0576  [6]
 LDCM0260  AC140 HCT 116 C408(1.32)  LDD0577  [6]
 LDCM0261  AC141 HCT 116 C408(1.58)  LDD0578  [6]
 LDCM0262  AC142 HCT 116 C408(1.25)  LDD0579  [6]
 LDCM0263  AC143 HCT 116 C168(0.87); C408(0.99)  LDD0580  [6]
 LDCM0264  AC144 HCT 116 C168(0.47); C408(1.01)  LDD0581  [6]
 LDCM0265  AC145 HCT 116 C168(0.58); C408(1.16)  LDD0582  [6]
 LDCM0266  AC146 HCT 116 C168(0.49); C408(1.17)  LDD0583  [6]
 LDCM0267  AC147 HCT 116 C168(0.50); C408(1.06)  LDD0584  [6]
 LDCM0268  AC148 HCT 116 C168(0.45); C408(1.39)  LDD0585  [6]
 LDCM0269  AC149 HCT 116 C168(0.42); C408(1.32)  LDD0586  [6]
 LDCM0270  AC15 HCT 116 C87(0.37); C408(1.27); C48(1.36)  LDD0587  [6]
 LDCM0271  AC150 HCT 116 C168(0.78); C408(0.99)  LDD0588  [6]
 LDCM0272  AC151 HCT 116 C168(0.82); C408(0.90)  LDD0589  [6]
 LDCM0273  AC152 HCT 116 C168(0.46); C408(1.35)  LDD0590  [6]
 LDCM0274  AC153 HCT 116 C168(0.45); C408(2.07)  LDD0591  [6]
 LDCM0621  AC154 HCT 116 C168(0.53); C408(1.00)  LDD2158  [6]
 LDCM0622  AC155 HCT 116 C168(0.49); C408(0.90)  LDD2159  [6]
 LDCM0623  AC156 HCT 116 C168(0.78); C408(1.15)  LDD2160  [6]
 LDCM0624  AC157 HCT 116 C168(0.83); C408(0.86)  LDD2161  [6]
 LDCM0276  AC17 HCT 116 C48(1.11); C408(1.21)  LDD0593  [6]
 LDCM0277  AC18 HCT 116 C48(1.65); C408(2.00)  LDD0594  [6]
 LDCM0278  AC19 HCT 116 C408(1.28); C48(1.55)  LDD0595  [6]
 LDCM0279  AC2 HCT 116 C408(1.11); C48(1.19)  LDD0596  [6]
 LDCM0280  AC20 HCT 116 C408(1.09); C48(1.27)  LDD0597  [6]
 LDCM0281  AC21 HCT 116 C48(0.98); C408(1.13)  LDD0598  [6]
 LDCM0282  AC22 HCT 116 C48(1.05); C408(1.10)  LDD0599  [6]
 LDCM0283  AC23 HCT 116 C408(1.16); C48(1.19)  LDD0600  [6]
 LDCM0284  AC24 HCT 116 C408(0.92); C48(1.18)  LDD0601  [6]
 LDCM0285  AC25 HCT 116 C408(1.19)  LDD0602  [6]
 LDCM0286  AC26 HCT 116 C408(1.28)  LDD0603  [6]
 LDCM0287  AC27 HCT 116 C408(1.30)  LDD0604  [6]
 LDCM0288  AC28 HCT 116 C408(1.33)  LDD0605  [6]
 LDCM0289  AC29 HCT 116 C408(1.25)  LDD0606  [6]
 LDCM0290  AC3 HCT 116 C408(1.15); C48(1.29)  LDD0607  [6]
 LDCM0291  AC30 HCT 116 C408(1.25)  LDD0608  [6]
 LDCM0292  AC31 HCT 116 C408(1.42)  LDD0609  [6]
 LDCM0293  AC32 HCT 116 C408(1.65)  LDD0610  [6]
 LDCM0294  AC33 HCT 116 C408(1.40)  LDD0611  [6]
 LDCM0295  AC34 HCT 116 C408(1.42)  LDD0612  [6]
 LDCM0296  AC35 HCT 116 C408(1.12); C48(1.29)  LDD0613  [6]
 LDCM0297  AC36 HCT 116 C48(1.22); C408(1.29)  LDD0614  [6]
 LDCM0298  AC37 HCT 116 C408(1.13); C48(1.26)  LDD0615  [6]
 LDCM0299  AC38 HCT 116 C408(1.02); C48(1.28)  LDD0616  [6]
 LDCM0300  AC39 HCT 116 C408(1.16); C48(1.23)  LDD0617  [6]
 LDCM0301  AC4 HCT 116 C48(1.15); C408(1.24)  LDD0618  [6]
 LDCM0302  AC40 HCT 116 C48(1.01); C408(1.71)  LDD0619  [6]
 LDCM0303  AC41 HCT 116 C48(1.05); C408(1.13)  LDD0620  [6]
 LDCM0304  AC42 HCT 116 C48(1.05); C408(1.26)  LDD0621  [6]
 LDCM0305  AC43 HCT 116 C408(1.26); C48(1.54)  LDD0622  [6]
 LDCM0306  AC44 HCT 116 C48(1.02); C408(1.34)  LDD0623  [6]
 LDCM0307  AC45 HCT 116 C48(1.14); C408(1.17)  LDD0624  [6]
 LDCM0308  AC46 HCT 116 C408(1.31)  LDD0625  [6]
 LDCM0309  AC47 HCT 116 C408(1.05)  LDD0626  [6]
 LDCM0310  AC48 HCT 116 C408(1.07)  LDD0627  [6]
 LDCM0311  AC49 HCT 116 C408(1.54)  LDD0628  [6]
 LDCM0312  AC5 HCT 116 C408(1.12); C48(1.28)  LDD0629  [6]
 LDCM0313  AC50 HCT 116 C408(1.29)  LDD0630  [6]
 LDCM0314  AC51 HCT 116 C408(0.96)  LDD0631  [6]
 LDCM0315  AC52 HCT 116 C408(0.98)  LDD0632  [6]
 LDCM0316  AC53 HCT 116 C408(1.41)  LDD0633  [6]
 LDCM0317  AC54 HCT 116 C408(1.42)  LDD0634  [6]
 LDCM0318  AC55 HCT 116 C408(1.20)  LDD0635  [6]
 LDCM0319  AC56 HCT 116 C408(1.31)  LDD0636  [6]
 LDCM0320  AC57 HCT 116 C87(0.88); C48(1.24); C408(1.34)  LDD0637  [6]
 LDCM0321  AC58 HCT 116 C87(0.48); C48(0.94); C408(1.14)  LDD0638  [6]
 LDCM0322  AC59 HCT 116 C87(0.71); C48(1.09); C408(1.20)  LDD0639  [6]
 LDCM0323  AC6 HCT 116 C87(0.49); C48(1.08); C408(1.23)  LDD0640  [6]
 LDCM0324  AC60 HCT 116 C87(0.80); C48(1.09); C408(1.24)  LDD0641  [6]
 LDCM0325  AC61 HCT 116 C87(0.73); C48(1.08); C408(1.40)  LDD0642  [6]
 LDCM0326  AC62 HCT 116 C87(1.00); C48(1.31); C408(1.56)  LDD0643  [6]
 LDCM0327  AC63 HCT 116 C87(0.73); C48(1.21); C408(1.24)  LDD0644  [6]
 LDCM0328  AC64 HCT 116 C87(0.73); C408(1.20); C48(1.24)  LDD0645  [6]
 LDCM0329  AC65 HCT 116 C87(0.76); C48(1.16); C408(1.19)  LDD0646  [6]
 LDCM0330  AC66 HCT 116 C48(0.96); C87(0.98); C408(1.11)  LDD0647  [6]
 LDCM0331  AC67 HCT 116 C87(0.65); C48(1.25); C408(1.88)  LDD0648  [6]
 LDCM0332  AC68 HCT 116 C168(0.84); C408(0.96)  LDD0649  [6]
 LDCM0333  AC69 HCT 116 C168(0.80); C408(1.01)  LDD0650  [6]
 LDCM0334  AC7 HCT 116 C87(0.50); C48(1.18); C408(1.18)  LDD0651  [6]
 LDCM0335  AC70 HCT 116 C168(0.66); C408(1.25)  LDD0652  [6]
 LDCM0336  AC71 HCT 116 C408(0.85); C168(0.87)  LDD0653  [6]
 LDCM0337  AC72 HCT 116 C168(0.75); C408(0.95)  LDD0654  [6]
 LDCM0338  AC73 HCT 116 C168(0.55); C408(1.53)  LDD0655  [6]
 LDCM0339  AC74 HCT 116 C168(0.68); C408(1.99)  LDD0656  [6]
 LDCM0340  AC75 HCT 116 C168(0.44); C408(1.80)  LDD0657  [6]
 LDCM0341  AC76 HCT 116 C168(0.75); C408(1.21)  LDD0658  [6]
 LDCM0342  AC77 HCT 116 C168(0.77); C408(1.07)  LDD0659  [6]
 LDCM0343  AC78 HCT 116 C168(0.78); C408(0.88)  LDD0660  [6]
 LDCM0344  AC79 HCT 116 C168(0.89); C408(1.10)  LDD0661  [6]
 LDCM0345  AC8 HCT 116 C87(0.31); C48(1.14); C408(1.18)  LDD0662  [6]
 LDCM0346  AC80 HCT 116 C168(0.73); C408(1.17)  LDD0663  [6]
 LDCM0347  AC81 HCT 116 C168(0.54); C408(1.45)  LDD0664  [6]
 LDCM0348  AC82 HCT 116 C168(0.43); C408(1.66)  LDD0665  [6]
 LDCM0349  AC83 HCT 116 C168(0.81); C48(1.29); C408(1.56)  LDD0666  [6]
 LDCM0350  AC84 HCT 116 C168(0.87); C48(1.34); C408(1.66)  LDD0667  [6]
 LDCM0351  AC85 HCT 116 C168(0.79); C48(1.03); C408(1.28)  LDD0668  [6]
 LDCM0352  AC86 HCT 116 C48(1.14); C408(1.27); C168(1.28)  LDD0669  [6]
 LDCM0353  AC87 HCT 116 C168(0.99); C408(1.05); C48(1.05)  LDD0670  [6]
 LDCM0354  AC88 HCT 116 C168(1.04); C48(1.16); C408(1.30)  LDD0671  [6]
 LDCM0355  AC89 HCT 116 C168(1.09); C48(1.25); C408(1.31)  LDD0672  [6]
 LDCM0357  AC90 HCT 116 C168(0.92); C408(1.13); C48(1.39)  LDD0674  [6]
 LDCM0358  AC91 HCT 116 C168(0.91); C48(1.54); C408(1.61)  LDD0675  [6]
 LDCM0359  AC92 HCT 116 C168(0.99); C48(1.30); C408(1.39)  LDD0676  [6]
 LDCM0360  AC93 HCT 116 C168(0.81); C48(1.04); C408(1.20)  LDD0677  [6]
 LDCM0361  AC94 HCT 116 C168(0.83); C48(1.22); C408(1.27)  LDD0678  [6]
 LDCM0362  AC95 HCT 116 C168(1.06); C408(1.13); C48(1.21)  LDD0679  [6]
 LDCM0363  AC96 HCT 116 C168(0.84); C48(1.17); C408(1.50)  LDD0680  [6]
 LDCM0364  AC97 HCT 116 C168(0.82); C48(1.30); C408(1.69)  LDD0681  [6]
 LDCM0365  AC98 HCT 116 C48(1.32); C408(1.52)  LDD0682  [6]
 LDCM0366  AC99 HCT 116 C48(0.90); C408(0.98)  LDD0683  [6]
 LDCM0545  Acetamide MDA-MB-231 C48(0.38)  LDD2138  [4]
 LDCM0248  AKOS034007472 HCT 116 C408(1.05); C48(1.14); C87(0.64)  LDD0565  [6]
 LDCM0356  AKOS034007680 HCT 116 C87(0.40); C48(1.07); C408(1.26)  LDD0673  [6]
 LDCM0275  AKOS034007705 HCT 116 C87(0.30); C48(1.59); C408(1.74)  LDD0592  [6]
 LDCM0156  Aniline NCI-H1299 11.55  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C408(1.08)  LDD0078  [6]
 LDCM0367  CL1 HCT 116 C408(0.94); C48(0.97); C168(1.24)  LDD0684  [6]
 LDCM0368  CL10 HCT 116 C168(0.74); C48(0.84); C408(1.23)  LDD0685  [6]
 LDCM0369  CL100 HCT 116 C48(1.04); C408(1.20)  LDD0686  [6]
 LDCM0370  CL101 HCT 116 C87(0.51); C48(1.23); C408(1.43)  LDD0687  [6]
 LDCM0371  CL102 HCT 116 C87(0.73); C48(1.05); C408(1.25)  LDD0688  [6]
 LDCM0372  CL103 HCT 116 C87(0.75); C48(1.00); C408(1.27)  LDD0689  [6]
 LDCM0373  CL104 HCT 116 C87(0.37); C48(1.08); C408(1.29)  LDD0690  [6]
 LDCM0374  CL105 HCT 116 C408(1.17); C48(1.24)  LDD0691  [6]
 LDCM0375  CL106 HCT 116 C48(1.39); C408(1.41)  LDD0692  [6]
 LDCM0376  CL107 HCT 116 C408(1.43); C48(1.60)  LDD0693  [6]
 LDCM0377  CL108 HCT 116 C408(1.60); C48(1.75)  LDD0694  [6]
 LDCM0378  CL109 HCT 116 C48(1.30); C408(1.51)  LDD0695  [6]
 LDCM0379  CL11 HCT 116 C168(0.63); C48(0.86); C408(1.25)  LDD0696  [6]
 LDCM0380  CL110 HCT 116 C48(1.39); C408(1.48)  LDD0697  [6]
 LDCM0381  CL111 HCT 116 C48(1.31); C408(1.48)  LDD0698  [6]
 LDCM0382  CL112 HCT 116 C408(1.11)  LDD0699  [6]
 LDCM0383  CL113 HCT 116 C408(1.38)  LDD0700  [6]
 LDCM0384  CL114 HCT 116 C408(1.25)  LDD0701  [6]
 LDCM0385  CL115 HCT 116 C408(1.27)  LDD0702  [6]
 LDCM0386  CL116 HCT 116 C408(1.32)  LDD0703  [6]
 LDCM0387  CL117 HCT 116 C48(1.15); C408(1.67)  LDD0704  [6]
 LDCM0388  CL118 HCT 116 C408(1.25); C48(1.75)  LDD0705  [6]
 LDCM0389  CL119 HCT 116 C408(1.18); C48(1.18)  LDD0706  [6]
 LDCM0390  CL12 HCT 116 C168(0.73); C48(1.02); C408(1.19)  LDD0707  [6]
 LDCM0391  CL120 HCT 116 C408(1.14); C48(1.26)  LDD0708  [6]
 LDCM0392  CL121 HCT 116 C408(1.48)  LDD0709  [6]
 LDCM0393  CL122 HCT 116 C408(1.25)  LDD0710  [6]
 LDCM0394  CL123 HCT 116 C408(1.09)  LDD0711  [6]
 LDCM0395  CL124 HCT 116 C408(1.33)  LDD0712  [6]
 LDCM0396  CL125 HCT 116 C408(1.04); C87(1.08); C48(1.25)  LDD0713  [6]
 LDCM0397  CL126 HCT 116 C48(0.89); C87(1.03); C408(1.08)  LDD0714  [6]
 LDCM0398  CL127 HCT 116 C408(1.01); C48(1.05); C87(1.15)  LDD0715  [6]
 LDCM0399  CL128 HCT 116 C87(0.63); C48(1.21); C408(1.31)  LDD0716  [6]
 LDCM0400  CL13 HCT 116 C168(0.73); C48(1.01); C408(1.20)  LDD0717  [6]
 LDCM0401  CL14 HCT 116 C168(0.99); C408(1.03); C48(1.05)  LDD0718  [6]
 LDCM0402  CL15 HCT 116 C168(0.79); C48(1.00); C408(1.36)  LDD0719  [6]
 LDCM0403  CL16 HCT 116 C87(0.68); C48(1.08); C408(1.11)  LDD0720  [6]
 LDCM0404  CL17 HCT 116 C87(0.58); C48(1.07); C408(1.24)  LDD0721  [6]
 LDCM0405  CL18 HCT 116 C87(0.56); C48(1.12); C408(1.13)  LDD0722  [6]
 LDCM0406  CL19 HCT 116 C87(0.56); C48(0.97); C408(1.11)  LDD0723  [6]
 LDCM0407  CL2 HCT 116 C48(0.88); C408(1.01); C168(1.12)  LDD0724  [6]
 LDCM0408  CL20 HCT 116 C87(0.50); C48(1.09); C408(1.28)  LDD0725  [6]
 LDCM0409  CL21 HCT 116 C87(0.64); C48(1.03); C408(1.49)  LDD0726  [6]
 LDCM0410  CL22 HCT 116 C87(0.61); C48(0.83); C408(1.40)  LDD0727  [6]
 LDCM0411  CL23 HCT 116 C87(0.59); C48(1.02); C408(1.28)  LDD0728  [6]
 LDCM0412  CL24 HCT 116 C87(0.62); C48(1.14); C408(1.27)  LDD0729  [6]
 LDCM0413  CL25 HCT 116 C408(1.39); C48(1.01); C87(0.41)  LDD0730  [6]
 LDCM0414  CL26 HCT 116 C408(1.12); C48(1.04); C87(0.65)  LDD0731  [6]
 LDCM0415  CL27 HCT 116 C408(1.27); C48(1.04); C87(0.59)  LDD0732  [6]
 LDCM0416  CL28 HCT 116 C408(1.36); C48(1.17); C87(0.52)  LDD0733  [6]
 LDCM0417  CL29 HCT 116 C408(1.13); C48(1.20); C87(0.64)  LDD0734  [6]
 LDCM0418  CL3 HCT 116 C168(0.95); C408(0.99); C48(0.76)  LDD0735  [6]
 LDCM0419  CL30 HCT 116 C408(1.16); C48(1.18); C87(0.70)  LDD0736  [6]
 LDCM0420  CL31 HCT 116 C168(0.86); C408(1.05); C48(1.12); C87(0.87)  LDD0737  [6]
 LDCM0421  CL32 HCT 116 C168(0.70); C408(1.08); C48(1.00); C87(0.71)  LDD0738  [6]
 LDCM0422  CL33 HCT 116 C168(0.79); C408(1.09); C48(0.96); C87(0.76)  LDD0739  [6]
 LDCM0423  CL34 HCT 116 C168(0.74); C408(0.95); C48(1.12); C87(0.58)  LDD0740  [6]
 LDCM0424  CL35 HCT 116 C168(0.80); C408(1.18); C48(1.06); C87(0.61)  LDD0741  [6]
 LDCM0425  CL36 HCT 116 C168(0.77); C408(1.01); C48(0.91); C87(0.64)  LDD0742  [6]
 LDCM0426  CL37 HCT 116 C168(0.71); C408(1.02); C48(1.09); C87(0.62)  LDD0743  [6]
 LDCM0428  CL39 HCT 116 C168(0.76); C408(1.04); C48(1.14); C87(0.63)  LDD0745  [6]
 LDCM0429  CL4 HCT 116 C168(0.97); C408(1.06); C48(0.95)  LDD0746  [6]
 LDCM0430  CL40 HCT 116 C168(0.71); C408(1.04); C48(0.97); C87(0.56)  LDD0747  [6]
 LDCM0431  CL41 HCT 116 C168(0.67); C408(1.01); C48(0.87); C87(0.88)  LDD0748  [6]
 LDCM0432  CL42 HCT 116 C168(0.90); C408(0.87); C48(1.44); C87(0.73)  LDD0749  [6]
 LDCM0433  CL43 HCT 116 C168(0.76); C408(1.04); C48(1.16); C87(0.67)  LDD0750  [6]
 LDCM0434  CL44 HCT 116 C168(0.73); C408(1.08); C48(0.96); C87(0.67)  LDD0751  [6]
 LDCM0435  CL45 HCT 116 C168(0.64); C408(1.00); C48(1.08); C87(0.52)  LDD0752  [6]
 LDCM0436  CL46 HCT 116 C408(1.00); C48(0.81)  LDD0753  [6]
 LDCM0437  CL47 HCT 116 C408(0.90); C48(0.84)  LDD0754  [6]
 LDCM0438  CL48 HCT 116 C408(0.93); C48(0.84)  LDD0755  [6]
 LDCM0439  CL49 HCT 116 C408(1.19); C48(0.95)  LDD0756  [6]
 LDCM0440  CL5 HCT 116 C168(0.90); C408(1.08); C48(1.03)  LDD0757  [6]
 LDCM0441  CL50 HCT 116 C408(1.20); C48(0.87)  LDD0758  [6]
 LDCM0442  CL51 HCT 116 C408(1.06); C48(1.01)  LDD0759  [6]
 LDCM0443  CL52 HCT 116 C408(0.98); C48(0.86)  LDD0760  [6]
 LDCM0444  CL53 HCT 116 C408(0.77); C48(0.79)  LDD0761  [6]
 LDCM0445  CL54 HCT 116 C408(0.94); C48(0.80)  LDD0762  [6]
 LDCM0446  CL55 HCT 116 C408(0.92); C48(0.82)  LDD0763  [6]
 LDCM0447  CL56 HCT 116 C408(0.86); C48(1.09)  LDD0764  [6]
 LDCM0448  CL57 HCT 116 C408(0.91); C48(0.84)  LDD0765  [6]
 LDCM0449  CL58 HCT 116 C408(1.01); C48(0.86)  LDD0766  [6]
 LDCM0450  CL59 HCT 116 C408(0.93); C48(0.94)  LDD0767  [6]
 LDCM0451  CL6 HCT 116 C168(0.77); C408(1.26); C48(1.34)  LDD0768  [6]
 LDCM0452  CL60 HCT 116 C408(1.07); C48(0.93)  LDD0769  [6]
 LDCM0453  CL61 HCT 116 C168(0.94); C408(1.15); C48(1.04); C87(0.58)  LDD0770  [6]
 LDCM0454  CL62 HCT 116 C168(1.04); C408(1.24); C48(0.98); C87(0.80)  LDD0771  [6]
 LDCM0455  CL63 HCT 116 C168(0.86); C408(1.64); C48(0.96); C87(0.58)  LDD0772  [6]
 LDCM0456  CL64 HCT 116 C168(0.77); C408(1.30); C48(1.10); C87(0.64)  LDD0773  [6]
 LDCM0457  CL65 HCT 116 C168(1.01); C408(1.11); C48(0.94); C87(0.67)  LDD0774  [6]
 LDCM0458  CL66 HCT 116 C168(0.76); C408(1.64); C48(1.16); C87(0.55)  LDD0775  [6]
 LDCM0459  CL67 HCT 116 C168(0.71); C408(1.29); C48(1.05); C87(0.63)  LDD0776  [6]
 LDCM0460  CL68 HCT 116 C168(0.76); C408(1.47); C48(1.00); C87(0.69)  LDD0777  [6]
 LDCM0461  CL69 HCT 116 C168(0.83); C408(1.31); C48(0.90); C87(0.69)  LDD0778  [6]
 LDCM0462  CL7 HCT 116 C168(0.73); C408(1.33); C48(1.22)  LDD0779  [6]
 LDCM0463  CL70 HCT 116 C168(0.73); C408(1.39); C48(1.04); C87(0.93)  LDD0780  [6]
 LDCM0464  CL71 HCT 116 C168(1.08); C408(1.61); C48(1.18); C87(0.77)  LDD0781  [6]
 LDCM0465  CL72 HCT 116 C168(1.05); C408(1.49); C48(1.21); C87(0.86)  LDD0782  [6]
 LDCM0466  CL73 HCT 116 C168(0.74); C408(1.54); C48(0.96); C87(0.74)  LDD0783  [6]
 LDCM0467  CL74 HCT 116 C168(0.85); C408(1.46); C48(1.15); C87(0.65)  LDD0784  [6]
 LDCM0469  CL76 HCT 116 C408(0.87); C48(0.75)  LDD0786  [6]
 LDCM0470  CL77 HCT 116 C408(0.91); C48(0.64)  LDD0787  [6]
 LDCM0471  CL78 HCT 116 C408(1.08); C48(0.76)  LDD0788  [6]
 LDCM0472  CL79 HCT 116 C408(1.17); C48(0.88)  LDD0789  [6]
 LDCM0473  CL8 HCT 116 C168(0.80); C408(1.63); C48(0.91)  LDD0790  [6]
 LDCM0474  CL80 HCT 116 C408(1.25); C48(0.83)  LDD0791  [6]
 LDCM0475  CL81 HCT 116 C408(1.17); C48(0.93)  LDD0792  [6]
 LDCM0476  CL82 HCT 116 C408(1.26); C48(0.89)  LDD0793  [6]
 LDCM0477  CL83 HCT 116 C408(1.25); C48(0.71)  LDD0794  [6]
 LDCM0478  CL84 HCT 116 C408(1.80); C48(0.78)  LDD0795  [6]
 LDCM0479  CL85 HCT 116 C408(1.19); C48(0.71)  LDD0796  [6]
 LDCM0480  CL86 HCT 116 C408(1.01); C48(0.66)  LDD0797  [6]
 LDCM0481  CL87 HCT 116 C408(1.04); C48(0.64)  LDD0798  [6]
 LDCM0482  CL88 HCT 116 C408(1.20); C48(0.71)  LDD0799  [6]
 LDCM0483  CL89 HCT 116 C408(1.54); C48(0.73)  LDD0800  [6]
 LDCM0484  CL9 HCT 116 C168(0.80); C408(1.19); C48(1.08)  LDD0801  [6]
 LDCM0485  CL90 HCT 116 C408(0.87); C48(0.57)  LDD0802  [6]
 LDCM0486  CL91 HCT 116 C408(1.07); C48(0.98)  LDD0803  [6]
 LDCM0487  CL92 HCT 116 C408(0.90); C48(0.96)  LDD0804  [6]
 LDCM0488  CL93 HCT 116 C408(0.95); C48(1.01)  LDD0805  [6]
 LDCM0489  CL94 HCT 116 C408(1.27); C48(1.36)  LDD0806  [6]
 LDCM0490  CL95 HCT 116 C408(1.22); C48(1.05)  LDD0807  [6]
 LDCM0491  CL96 HCT 116 C408(1.19); C48(1.13)  LDD0808  [6]
 LDCM0492  CL97 HCT 116 C408(1.18); C48(1.16)  LDD0809  [6]
 LDCM0493  CL98 HCT 116 C408(1.19); C48(0.90)  LDD0810  [6]
 LDCM0494  CL99 HCT 116 C408(1.30); C48(1.01)  LDD0811  [6]
 LDCM0495  E2913 HEK-293T C48(0.98); C349(0.90); C408(1.07)  LDD1698  [15]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C392(1.73); C48(0.85)  LDD1702  [4]
 LDCM0625  F8 Ramos C48(1.53)  LDD2187  [16]
 LDCM0572  Fragment10 Ramos C48(1.37)  LDD2189  [16]
 LDCM0573  Fragment11 Ramos C48(0.60)  LDD2190  [16]
 LDCM0574  Fragment12 Ramos C48(0.82)  LDD2191  [16]
 LDCM0575  Fragment13 Ramos C48(1.06)  LDD2192  [16]
 LDCM0576  Fragment14 Ramos C48(1.02)  LDD2193  [16]
 LDCM0579  Fragment20 Ramos C48(1.15)  LDD2194  [16]
 LDCM0580  Fragment21 Ramos C48(0.91)  LDD2195  [16]
 LDCM0582  Fragment23 Ramos C48(0.88)  LDD2196  [16]
 LDCM0578  Fragment27 Ramos C48(0.94)  LDD2197  [16]
 LDCM0586  Fragment28 Ramos C48(0.97)  LDD2198  [16]
 LDCM0588  Fragment30 Ramos C48(0.87)  LDD2199  [16]
 LDCM0589  Fragment31 Ramos C48(0.72)  LDD2200  [16]
 LDCM0590  Fragment32 Ramos C48(1.64)  LDD2201  [16]
 LDCM0468  Fragment33 HCT 116 C168(0.81); C408(1.45); C48(0.94); C87(0.63)  LDD0785  [6]
 LDCM0596  Fragment38 Ramos C48(0.83)  LDD2203  [16]
 LDCM0566  Fragment4 Ramos C48(1.38)  LDD2184  [16]
 LDCM0427  Fragment51 HCT 116 C168(0.75); C408(1.10); C48(1.06); C87(0.53)  LDD0744  [6]
 LDCM0610  Fragment52 Ramos C48(1.26)  LDD2204  [16]
 LDCM0614  Fragment56 Ramos C48(1.27)  LDD2205  [16]
 LDCM0569  Fragment7 Ramos C48(1.00)  LDD2186  [16]
 LDCM0571  Fragment9 Ramos C48(1.02)  LDD2188  [16]
 LDCM0022  KB02 HCT 116 C408(5.00); C48(1.53)  LDD0080  [6]
 LDCM0023  KB03 HCT 116 C408(2.67); C48(1.61)  LDD0081  [6]
 LDCM0024  KB05 HCT 116 C408(2.77); C48(1.37)  LDD0082  [6]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C48(1.17)  LDD2102  [4]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C48(0.66)  LDD2121  [4]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C48(0.49)  LDD2089  [4]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C48(1.20)  LDD2090  [4]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C48(0.83)  LDD2092  [4]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C48(1.26)  LDD2094  [4]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C48(0.52)  LDD2096  [4]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C48(0.86)  LDD2098  [4]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C392(0.55); C48(0.81)  LDD2099  [4]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C48(1.65)  LDD2105  [4]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C48(0.75)  LDD2106  [4]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C48(1.05)  LDD2107  [4]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C48(0.77)  LDD2108  [4]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C48(0.65)  LDD2114  [4]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C48(0.89)  LDD2116  [4]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C48(0.91)  LDD2118  [4]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C48(0.83)  LDD2122  [4]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C48(0.87)  LDD2124  [4]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C392(0.96)  LDD2127  [4]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C392(1.17)  LDD2129  [4]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C392(0.98)  LDD2136  [4]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C48(0.60)  LDD2140  [4]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C48(1.06)  LDD2149  [4]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C48(0.38)  LDD2150  [4]
 LDCM0021  THZ1 HCT 116 C408(1.00)  LDD2173  [6]

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
M-phase inducer phosphatase 3 (CDC25C) MPI phosphatase family P30307
Breast cancer type 1 susceptibility protein (BRCA1) . P38398
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein gamma (YWHAG) 14-3-3 family P61981
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Claspin (CLSPN) Claspin family Q9HAW4
ERBB receptor feedback inhibitor 1 (ERRFI1) MIG6 family Q9UJM3
DNA repair protein RAD51 homolog 1 (RAD51) RecA family Q06609
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
Protein timeless homolog (TIMELESS) Timeless family Q9UNS1
Menin (MEN1) . O00255

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 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ly2603618 Small molecular drug D00NZL
Ly2880070 Small molecular drug DXJ4B7
Sch-900776 Small molecular drug D05FWH
Ucn-01 Small molecular drug D0Z9VY
Ly2606368 . D08UUL
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd7762 Small molecular drug D0PM7Q
Mk-8776 Small molecular drug D4MW3O
Gdc-0425 . D01ZUV
Rg7741 . D00UQW
Investigative
Click To Hide/Show 66 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(3z)-6-(4-hydroxy-3-methoxyphenyl)-3-(1h-pyrrol-2-ylmethylene)-13-dihydro-2h-indol-2-one Small molecular drug DB07078
2-(1h-indazol-3-yl)-1h-benzo[D]Imidazole Small molecular drug D0XC6G
2-(Cyclohexylamino)Benzoic Acid Small molecular drug D08XCD
3-(1h-indol-2-yl)-1h-quinolin-2-one Small molecular drug D0M9OF
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
6-(3-aminopropyl)Benzo[H]Isoquinolin-1(2h)-one Small molecular drug D09YVU
6-morpholin-4-yl-9h-purine Small molecular drug D0S3TJ
9-chlorobenzo[H]Isoquinolin-1(2h)-one Small molecular drug D09YHQ
9-hydroxypyrrolo[3,4-c]Carbazole-1,3(2h,6h)-dione Small molecular drug D0Y3PH
A-432411 Small molecular drug D0D6DH
Bis-imide A Small molecular drug D01HUO
Bisindolylmaleimide-i Small molecular drug D0TO6S
Bx-795 Small molecular drug D0RG0Z
Bx-912 Small molecular drug D0IX7Y
Cct244747 Small molecular drug D0Z8PT
Ci-1040 Small molecular drug D0B9BU
Debromohymenialdisine Small molecular drug D01WAI
Enzastaurin Small molecular drug DB06486
Granulatimide Small molecular drug D06EZQ
Isogranulatimide Small molecular drug D0Z2CN
Kn-62 Small molecular drug D0N6ES
Ly-2608204 Small molecular drug DB12284
N-(5,6-diphenylfuro[2,3-d]Pyrimidin-4-yl)Glycine Small molecular drug D0FO2K
N-(56-diphenylfuro[23-d]Pyrimidin-4-yl)Glycine Small molecular drug DB07653
Nu-6102 Small molecular drug D0Y5RO
Pmid17935989c25 Small molecular drug D00ERW
Pmid19364658c33 Small molecular drug D01YWE
Pmid20855207c25 Small molecular drug D0ME9B
Rel-(9r12s)-9101112-tetrahydro-912-epoxy-1h-diindolo[123-fg:3'2'1'-kl]Pyrrolo[34-i][16]Benzodiazocine-13(2h)-dione Small molecular drug DB08683
Ro-316233 Small molecular drug D0L8HO
Sb 218078 Small molecular drug D00KDF
Sb218078 Small molecular drug DYS56C
V158411 Small molecular drug D3U1LH
(2r)-1-[(56-diphenyl-7h-pyrrolo[23-d]Pyrimidin-4-yl)Amino]Propan-2-ol . DB07647
(2r)-3-{[(4z)-56-diphenyl-67-dihydro-4h-pyrrolo[23-d]Pyrimidin-4-ylidene]Amino}Propane-12-diol . DB07648
(2s)-1-amino-3-[(5-nitroquinolin-8-yl)Amino]Propan-2-ol . DB07037
(3-endo)-8-methyl-8-azabicyclo[3.2.1]Oct-3-yl 1h-pyrrolo[23-b]Pyridine-3-carboxylate . DB07243
(5-{3-[5-(Piperidin-1-ylmethyl)-1h-indol-2-yl]-1h-indazol-6-yl}-2h-123-triazol-4-yl)Methanol . DB07213
(56-diphenyl-furo[23-d]Pyrimidin-4-ylamino)-acetic . DB07654
1-(5-chloro-2-methoxyphenyl)-3-{6-[2-(Dimethylamino)-1-methylethoxy]Pyrazin-2-yl}Urea . DB07228
1-(5-chloro-24-dimethoxyphenyl)-3-(5-cyanopyrazin-2-yl)Urea . DB07314
1-[(2s)-4-(5-bromo-1h-pyrazolo[34-b]Pyridin-4-yl)Morpholin-2-yl]Methanamine . DB08781
1-[(2s)-4-(5-phenyl-1h-pyrazolo[34-b]Pyridin-4-yl)Morpholin-2-yl]Methanamine . DB08774
18-chloro-11121314-tetrahydro-1h10h-84-(Azeno)-915136-benzodioxatriazacycloheptadecin-2-one . DB07311
2-(Methylsulfanyl)-5-(Thiophen-2-ylmethyl)-1h-imidazol-4-ol . DB08779
2-[(56-diphenylfuro[23-d]Pyrimidin-4-yl)Amino]Ethanol . DB08393
2-[56-bis-(4-methoxy-phenyl)-furo[23-d]Pyrimidin-4-ylamino]-ethanol . DB08392
22'-{[9-(Hydroxyimino)-9h-fluorene-27-diyl]Bis(Oxy)}Diacetic Acid . DB07034
3-(1h-benzimidazol-2-yl)-1h-indazole . DB07959
3-(5-{[4-(Aminomethyl)Piperidin-1-yl]Methyl}-1h-indol-2-yl)-1h-indazole-6-carbonitrile . DB07075
3-(5-{[4-(Aminomethyl)Piperidin-1-yl]Methyl}-1h-indol-2-yl)Quinolin-2(1h)-one . DB07025
3-amino-3-benzyl-[4.3.0]Bicyclo-16-diazanonan-2-one . DB07655
4-(6-{[(4-methylcyclohexyl)Amino]Methyl}-14-dihydroindeno[12-c]Pyrazol-3-yl)Benzoic Acid . DB07320
4-[3-(1h-benzimidazol-2-yl)-1h-indazol-6-yl]-2-methoxyphenol . DB07336
5-ethyl-3-methyl-15-dihydro-4h-pyrazolo[43-c]Quinolin-4-one . DB07158
5678-tetrahydro[1]Benzothieno[23-d]Pyrimidin-4(3h)-one . DB08777
Arry-575 . D08OPW
Chir-124 . DB06852
Chk1-a . D03CQN
N-(4-oxo-5678-tetrahydro-4h-[13]Thiazolo[54-c]Azepin-2-yl)Acetamide . DB08776
N-{5-[4-(4-methylpiperazin-1-yl)Phenyl]-1h-pyrrolo[23-b]Pyridin-3-yl}Nicotinamide . DB06876
Prexasertib . DB12008
S-024 . D0OC6H
S-070 . D0P4DG
[4-amino-2-(Tert-butylamino)-13-thiazol-5-yl](Phenyl)Methanone . DB08778
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Diamidothiazole Derivative 1 Small molecular drug D0LR2Y
Discontinued
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pf-477736 Small molecular drug D0U9IQ
Xl844 Small molecular drug D05UGJ
Rg7602 . D0O3KA

References

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2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
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Mass spectrometry data entry: PXD028270
4 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
5 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
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Mass spectrometry data entry: PXD028853
9 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
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Mass spectrometry data entry: PXD029255
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Mass spectrometry data entry: PXD041264
13 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
14 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.
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Mass spectrometry data entry: PXD044402
16 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