Details of the Target

General Information of Target

Target ID LDTP04555
Target Name Serine/threonine-protein kinase PLK1 (PLK1)
Gene Name PLK1
Gene ID 5347
Synonyms
PLK; Serine/threonine-protein kinase PLK1; EC 2.7.11.21; Polo-like kinase 1; PLK-1; Serine/threonine-protein kinase 13; STPK13
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLG
KGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFF
EDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLG
NLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCI
MYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELL
NDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEE
PVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDK
YGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLK
YFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTK
LILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRL
KAS
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Ser/Thr protein kinase family, CDC5/Polo subfamily
Subcellular location
Nucleus
Function
Serine/threonine-protein kinase that performs several important functions throughout M phase of the cell cycle, including the regulation of centrosome maturation and spindle assembly, the removal of cohesins from chromosome arms, the inactivation of anaphase-promoting complex/cyclosome (APC/C) inhibitors, and the regulation of mitotic exit and cytokinesis. Polo-like kinase proteins act by binding and phosphorylating proteins that are already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates BORA, BUB1B/BUBR1, CCNB1, CDC25C, CEP55, ECT2, ERCC6L, FBXO5/EMI1, FOXM1, KIF20A/MKLP2, CENPU, NEDD1, NINL, NPM1, NUDC, PKMYT1/MYT1, KIZ, PPP1R12A/MYPT1, POLQ, PRC1, RACGAP1/CYK4, RAD51, RHNO1, SGO1, STAG2/SA2, TEX14, TOPORS, p73/TP73, TPT1, WEE1 and HNRNPU. Plays a key role in centrosome functions and the assembly of bipolar spindles by phosphorylating KIZ, NEDD1 and NINL. NEDD1 phosphorylation promotes subsequent targeting of the gamma-tubulin ring complex (gTuRC) to the centrosome, an important step for spindle formation. Phosphorylation of NINL component of the centrosome leads to NINL dissociation from other centrosomal proteins. Involved in mitosis exit and cytokinesis by phosphorylating CEP55, ECT2, KIF20A/MKLP2, CENPU, PRC1 and RACGAP1. Recruited at the central spindle by phosphorylating and docking PRC1 and KIF20A/MKLP2; creates its own docking sites on PRC1 and KIF20A/MKLP2 by mediating phosphorylation of sites subsequently recognized by the POLO box domains. Phosphorylates RACGAP1, thereby creating a docking site for the Rho GTP exchange factor ECT2 that is essential for the cleavage furrow formation. Promotes the central spindle recruitment of ECT2. Plays a central role in G2/M transition of mitotic cell cycle by phosphorylating CCNB1, CDC25C, FOXM1, CENPU, PKMYT1/MYT1, PPP1R12A/MYPT1 and WEE1. Part of a regulatory circuit that promotes the activation of CDK1 by phosphorylating the positive regulator CDC25C and inhibiting the negative regulators WEE1 and PKMYT1/MYT1. Also acts by mediating phosphorylation of cyclin-B1 (CCNB1) on centrosomes in prophase. Phosphorylates FOXM1, a key mitotic transcription regulator, leading to enhance FOXM1 transcriptional activity. Involved in kinetochore functions and sister chromatid cohesion by phosphorylating BUB1B/BUBR1, FBXO5/EMI1 and STAG2/SA2. PLK1 is high on non-attached kinetochores suggesting a role of PLK1 in kinetochore attachment or in spindle assembly checkpoint (SAC) regulation. Required for kinetochore localization of BUB1B. Regulates the dissociation of cohesin from chromosomes by phosphorylating cohesin subunits such as STAG2/SA2. Phosphorylates SGO1: required for spindle pole localization of isoform 3 of SGO1 and plays a role in regulating its centriole cohesion function. Mediates phosphorylation of FBXO5/EMI1, a negative regulator of the APC/C complex during prophase, leading to FBXO5/EMI1 ubiquitination and degradation by the proteasome. Acts as a negative regulator of p53 family members: phosphorylates TOPORS, leading to inhibit the sumoylation of p53/TP53 and simultaneously enhance the ubiquitination and subsequent degradation of p53/TP53. Phosphorylates the transactivation domain of the transcription factor p73/TP73, leading to inhibit p73/TP73-mediated transcriptional activation and pro-apoptotic functions. Phosphorylates BORA, and thereby promotes the degradation of BORA. Contributes to the regulation of AURKA function. Also required for recovery after DNA damage checkpoint and entry into mitosis. Phosphorylates MISP, leading to stabilization of cortical and astral microtubule attachments required for proper spindle positioning. Together with MEIKIN, acts as a regulator of kinetochore function during meiosis I: required both for mono-orientation of kinetochores on sister chromosomes and protection of centromeric cohesin from separase-mediated cleavage. Phosphorylates CEP68 and is required for its degradation. Regulates nuclear envelope breakdown during prophase by phosphorylating DCTN1 resulting in its localization in the nuclear envelope. Phosphorylates the heat shock transcription factor HSF1, promoting HSF1 nuclear translocation upon heat shock. Phosphorylates HSF1 also in the early mitotic period; this phosphorylation regulates HSF1 localization to the spindle pole, the recruitment of the SCF(BTRC) ubiquitin ligase complex induicing HSF1 degradation, and hence mitotic progression. Regulates mitotic progression by phosphorylating RIOK2. Through the phosphorylation of DZIP1 regulates the localization during mitosis of the BBSome, a ciliary protein complex involved in cilium biogenesis. Regulates DNA repair during mitosis by mediating phosphorylation of POLQ and RHNO1, thereby promoting POLQ recruitment to DNA damage sites.
TTD ID
T40694
Uniprot ID
P53350
DrugMap ID
TTIYVQP
Ensemble ID
ENST00000300093.9
HGNC ID
HGNC:9077
ChEMBL ID
CHEMBL3024

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 21 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K143(6.90); K146(0.62); K589(8.94)  LDD0277  [2]
AHL-Pu-1
 Probe Info  		C372(2.25)  LDD0170  [3]
DBIA
 Probe Info  		C573(1.20); C212(1.07)  LDD0078  [4]
AMP probe
 Probe Info  		N.A.  LDD0200  [5]
ATP probe
 Probe Info  		K82(0.00); K272(0.00); K284(0.00)  LDD0199  [5]
4-Iodoacetamidophenylacetylene
 Probe Info  		C544(0.00); C212(0.00); C67(0.00); C164(0.00)  LDD0038  [6]
IA-alkyne
 Probe Info  		C164(0.00); C544(0.00)  LDD0036  [6]
Lodoacetamide azide
 Probe Info  		C212(0.00); C67(0.00); C544(0.00); C372(0.00)  LDD0037  [6]
NAIA_4
 Probe Info  		C67(0.00); C212(0.00); C372(0.00); C544(0.00)  LDD2226  [7]
TFBX
 Probe Info  		C67(0.00); C212(0.00)  LDD0027  [8]
IPM
 Probe Info  		N.A.  LDD0005  [9]
NPM
 Probe Info  		N.A.  LDD0016  [9]
PF-06672131
 Probe Info  		N.A.  LDD0017  [10]
VSF
 Probe Info  		N.A.  LDD0007  [9]
Phosphinate-6
 Probe Info  		C572(0.00); C67(0.00)  LDD0018  [11]
Acrolein
 Probe Info  		N.A.  LDD0217  [12]
Methacrolein
 Probe Info  		N.A.  LDD0218  [12]
W1
 Probe Info  		C405(0.00); C318(0.00)  LDD0236  [13]
AOyne
 Probe Info  		14.90  LDD0443  [14]
NAIA_5
 Probe Info  		C67(0.00); C544(0.00); C164(0.00)  LDD2223  [7]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C064
 Probe Info  		8.11  LDD1761  [15]
C280
 Probe Info  		9.45  LDD1950  [15]
FFF probe13
 Probe Info  		20.00  LDD0475  [16]
FFF probe3
 Probe Info  		9.71  LDD0465  [16]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C372(2.25)  LDD0170  [3]
 LDCM0214  AC1 HCT 116 C572(0.86); C573(1.06); C428(1.16); C164(0.83)  LDD0531  [4]
 LDCM0215  AC10 HCT 116 C573(1.19); C428(1.18); C164(1.04); C212(0.93)  LDD0532  [4]
 LDCM0216  AC100 HCT 116 C572(0.73); C573(0.77); C428(0.99); C164(1.51)  LDD0533  [4]
 LDCM0217  AC101 HCT 116 C572(0.74); C573(0.81); C428(1.02); C164(0.99)  LDD0534  [4]
 LDCM0218  AC102 HCT 116 C572(0.72); C573(0.78); C428(0.95); C164(0.82)  LDD0535  [4]
 LDCM0219  AC103 HCT 116 C572(0.70); C573(0.82); C428(0.95); C164(0.92)  LDD0536  [4]
 LDCM0220  AC104 HCT 116 C572(0.69); C573(0.81); C428(1.07); C164(1.10)  LDD0537  [4]
 LDCM0221  AC105 HCT 116 C572(0.71); C573(0.82); C428(1.02); C164(0.92)  LDD0538  [4]
 LDCM0222  AC106 HCT 116 C572(0.68); C573(0.80); C428(0.93); C164(1.12)  LDD0539  [4]
 LDCM0223  AC107 HCT 116 C572(0.63); C573(0.87); C428(0.99); C164(1.07)  LDD0540  [4]
 LDCM0224  AC108 HCT 116 C572(0.91); C573(0.79); C428(0.96); C164(1.55)  LDD0541  [4]
 LDCM0225  AC109 HCT 116 C572(0.93); C573(0.82); C428(1.04); C164(1.29)  LDD0542  [4]
 LDCM0226  AC11 HCT 116 C573(1.72); C428(1.20); C164(1.11); C212(0.90)  LDD0543  [4]
 LDCM0227  AC110 HCT 116 C572(0.91); C573(0.80); C428(1.03); C164(1.05)  LDD0544  [4]
 LDCM0228  AC111 HCT 116 C572(0.81); C573(0.76); C428(1.07); C164(1.10)  LDD0545  [4]
 LDCM0229  AC112 HCT 116 C572(0.69); C573(0.78); C428(0.85); C164(1.06)  LDD0546  [4]
 LDCM0230  AC113 HCT 116 C572(0.97); C573(0.95); C428(0.89); C164(0.81)  LDD0547  [4]
 LDCM0231  AC114 HCT 116 C572(0.86); C573(0.89); C428(1.06); C164(0.77)  LDD0548  [4]
 LDCM0232  AC115 HCT 116 C572(0.81); C573(0.91); C428(1.25); C164(1.08)  LDD0549  [4]
 LDCM0233  AC116 HCT 116 C572(0.95); C573(1.05); C428(1.42); C164(0.87)  LDD0550  [4]
 LDCM0234  AC117 HCT 116 C572(0.90); C573(1.07); C428(1.27); C164(0.84)  LDD0551  [4]
 LDCM0235  AC118 HCT 116 C572(0.93); C573(0.99); C428(1.05); C164(0.97)  LDD0552  [4]
 LDCM0236  AC119 HCT 116 C572(0.85); C573(0.96); C428(1.00); C164(0.71)  LDD0553  [4]
 LDCM0237  AC12 HCT 116 C573(1.28); C428(1.16); C164(1.04); C212(0.90)  LDD0554  [4]
 LDCM0238  AC120 HCT 116 C572(0.95); C573(1.02); C428(1.05); C164(0.78)  LDD0555  [4]
 LDCM0239  AC121 HCT 116 C572(0.96); C573(1.04); C428(1.05); C164(0.81)  LDD0556  [4]
 LDCM0240  AC122 HCT 116 C572(0.93); C573(0.96); C428(1.05); C164(0.86)  LDD0557  [4]
 LDCM0241  AC123 HCT 116 C572(0.92); C573(0.92); C428(1.28); C164(0.79)  LDD0558  [4]
 LDCM0242  AC124 HCT 116 C572(0.97); C573(1.08); C428(0.99); C164(0.87)  LDD0559  [4]
 LDCM0243  AC125 HCT 116 C572(0.98); C573(1.00); C428(1.09); C164(0.86)  LDD0560  [4]
 LDCM0244  AC126 HCT 116 C572(0.92); C573(0.98); C428(1.19); C164(0.93)  LDD0561  [4]
 LDCM0245  AC127 HCT 116 C572(0.93); C573(1.04); C428(1.16); C164(0.79)  LDD0562  [4]
 LDCM0246  AC128 HCT 116 C572(1.05); C573(1.22); C428(0.96); C164(1.01)  LDD0563  [4]
 LDCM0247  AC129 HCT 116 C572(1.02); C573(0.98); C428(0.82); C164(1.02)  LDD0564  [4]
 LDCM0249  AC130 HCT 116 C572(0.92); C573(1.01); C428(0.91); C164(1.00)  LDD0566  [4]
 LDCM0250  AC131 HCT 116 C572(0.96); C573(0.93); C428(0.68); C164(1.03)  LDD0567  [4]
 LDCM0251  AC132 HCT 116 C572(1.04); C573(1.02); C428(0.94); C164(1.09)  LDD0568  [4]
 LDCM0252  AC133 HCT 116 C572(0.97); C573(1.05); C428(0.91); C164(0.92)  LDD0569  [4]
 LDCM0253  AC134 HCT 116 C572(0.92); C573(1.02); C428(0.99); C164(0.99)  LDD0570  [4]
 LDCM0254  AC135 HCT 116 C572(0.97); C573(1.08); C428(0.95); C164(1.09)  LDD0571  [4]
 LDCM0255  AC136 HCT 116 C572(0.97); C573(1.01); C428(1.05); C164(1.02)  LDD0572  [4]
 LDCM0256  AC137 HCT 116 C572(1.02); C573(1.02); C428(1.04); C164(1.01)  LDD0573  [4]
 LDCM0257  AC138 HCT 116 C572(1.07); C573(1.06); C428(1.07); C164(1.06)  LDD0574  [4]
 LDCM0258  AC139 HCT 116 C572(1.05); C573(1.05); C428(1.15); C164(1.08)  LDD0575  [4]
 LDCM0259  AC14 HCT 116 C573(1.37); C428(1.11); C164(1.17); C212(1.09)  LDD0576  [4]
 LDCM0260  AC140 HCT 116 C572(1.00); C573(1.07); C428(1.24); C164(1.09)  LDD0577  [4]
 LDCM0261  AC141 HCT 116 C572(1.00); C573(1.05); C428(1.11); C164(1.00)  LDD0578  [4]
 LDCM0262  AC142 HCT 116 C572(0.96); C573(0.98); C428(0.97); C164(0.96)  LDD0579  [4]
 LDCM0263  AC143 HCT 116 C572(0.98); C573(0.89); C428(1.58); C318(0.82)  LDD0580  [4]
 LDCM0264  AC144 HCT 116 C572(0.87); C164(0.96); C67(1.02); C573(1.03)  LDD0581  [4]
 LDCM0265  AC145 HCT 116 C67(0.97); C572(1.06); C573(1.07); C164(1.09)  LDD0582  [4]
 LDCM0266  AC146 HCT 116 C164(0.78); C572(0.93); C67(1.00); C212(1.19)  LDD0583  [4]
 LDCM0267  AC147 HCT 116 C572(0.92); C318(0.95); C164(0.96); C67(0.96)  LDD0584  [4]
 LDCM0268  AC148 HCT 116 C572(0.94); C164(1.01); C67(1.07); C212(1.32)  LDD0585  [4]
 LDCM0269  AC149 HCT 116 C164(0.80); C572(0.82); C67(1.10); C573(1.10)  LDD0586  [4]
 LDCM0270  AC15 HCT 116 C318(0.93); C212(1.04); C67(1.14); C573(1.24)  LDD0587  [4]
 LDCM0271  AC150 HCT 116 C164(0.94); C67(0.99); C572(1.02); C573(1.04)  LDD0588  [4]
 LDCM0272  AC151 HCT 116 C572(0.93); C164(0.94); C573(1.00); C212(1.05)  LDD0589  [4]
 LDCM0273  AC152 HCT 116 C572(0.85); C164(0.89); C573(1.00); C67(1.06)  LDD0590  [4]
 LDCM0274  AC153 HCT 116 C572(0.90); C164(0.92); C67(1.08); C573(1.31)  LDD0591  [4]
 LDCM0621  AC154 HCT 116 C572(0.97); C573(1.00); C428(1.35); C164(0.89)  LDD2158  [4]
 LDCM0622  AC155 HCT 116 C572(0.99); C573(1.01); C428(1.20); C164(0.85)  LDD2159  [4]
 LDCM0623  AC156 HCT 116 C572(0.93); C573(0.98); C428(1.00); C164(0.93)  LDD2160  [4]
 LDCM0624  AC157 HCT 116 C572(1.02); C573(0.88); C428(0.91); C164(1.05)  LDD2161  [4]
 LDCM0276  AC17 HCT 116 C573(0.93); C428(0.95); C572(0.96); C212(0.99)  LDD0593  [4]
 LDCM0277  AC18 HCT 116 C573(0.90); C572(0.91); C67(0.94); C164(1.03)  LDD0594  [4]
 LDCM0278  AC19 HCT 116 C573(0.96); C212(0.97); C572(0.99); C67(1.04)  LDD0595  [4]
 LDCM0279  AC2 HCT 116 C212(0.82); C164(0.92); C572(1.00); C67(1.04)  LDD0596  [4]
 LDCM0280  AC20 HCT 116 C573(0.98); C572(1.01); C428(1.05); C212(1.06)  LDD0597  [4]
 LDCM0281  AC21 HCT 116 C573(0.93); C67(0.96); C164(1.00); C572(1.00)  LDD0598  [4]
 LDCM0282  AC22 HCT 116 C573(0.98); C212(1.01); C572(1.02); C67(1.03)  LDD0599  [4]
 LDCM0283  AC23 HCT 116 C67(0.96); C573(0.98); C212(1.00); C572(1.01)  LDD0600  [4]
 LDCM0284  AC24 HCT 116 C428(1.01); C573(1.05); C67(1.06); C572(1.07)  LDD0601  [4]
 LDCM0285  AC25 HCT 116 C572(0.87); C67(0.88); C573(0.97); C164(0.99)  LDD0602  [4]
 LDCM0286  AC26 HCT 116 C572(0.91); C164(0.94); C212(1.03); C67(1.04)  LDD0603  [4]
 LDCM0287  AC27 HCT 116 C572(0.88); C67(0.97); C428(0.98); C164(1.00)  LDD0604  [4]
 LDCM0288  AC28 HCT 116 C572(0.92); C164(0.93); C428(1.05); C67(1.05)  LDD0605  [4]
 LDCM0289  AC29 HCT 116 C572(0.85); C212(0.93); C164(1.01); C67(1.07)  LDD0606  [4]
 LDCM0290  AC3 HCT 116 C212(0.59); C428(0.93); C164(0.94); C572(0.98)  LDD0607  [4]
 LDCM0291  AC30 HCT 116 C572(0.97); C164(1.01); C67(1.07); C428(1.29)  LDD0608  [4]
 LDCM0292  AC31 HCT 116 C572(0.80); C164(0.91); C67(0.93); C428(1.08)  LDD0609  [4]
 LDCM0293  AC32 HCT 116 C572(0.85); C164(0.99); C67(1.22); C212(1.27)  LDD0610  [4]
 LDCM0294  AC33 HCT 116 C572(0.87); C164(0.96); C67(1.04); C428(1.16)  LDD0611  [4]
 LDCM0295  AC34 HCT 116 C572(0.81); C164(0.99); C212(1.00); C67(1.09)  LDD0612  [4]
 LDCM0296  AC35 HCT 116 C164(0.90); C67(0.96); C573(0.96); C428(0.98)  LDD0613  [4]
 LDCM0297  AC36 HCT 116 C428(0.87); C164(0.91); C573(0.95); C212(1.00)  LDD0614  [4]
 LDCM0298  AC37 HCT 116 C428(0.75); C212(0.89); C164(0.92); C573(0.95)  LDD0615  [4]
 LDCM0299  AC38 HCT 116 C428(0.77); C212(0.86); C164(0.93); C573(0.93)  LDD0616  [4]
 LDCM0300  AC39 HCT 116 C212(0.73); C164(0.87); C428(0.96); C572(1.02)  LDD0617  [4]
 LDCM0301  AC4 HCT 116 C212(0.70); C164(0.94); C572(0.98); C67(1.08)  LDD0618  [4]
 LDCM0302  AC40 HCT 116 C164(0.84); C572(0.96); C428(1.05); C573(1.05)  LDD0619  [4]
 LDCM0303  AC41 HCT 116 C572(1.01); C428(1.02); C573(1.06); C164(1.07)  LDD0620  [4]
 LDCM0304  AC42 HCT 116 C572(0.98); C428(1.00); C67(1.01); C573(1.03)  LDD0621  [4]
 LDCM0305  AC43 HCT 116 C572(0.91); C573(1.08); C428(1.15); C164(1.18)  LDD0622  [4]
 LDCM0306  AC44 HCT 116 C428(1.05); C572(1.06); C67(1.08); C164(1.08)  LDD0623  [4]
 LDCM0307  AC45 HCT 116 C164(0.94); C572(0.99); C428(1.02); C67(1.04)  LDD0624  [4]
 LDCM0308  AC46 HCT 116 C164(0.84); C318(0.88); C572(0.99); C212(1.01)  LDD0625  [4]
 LDCM0309  AC47 HCT 116 C212(0.83); C164(0.85); C572(0.92); C318(0.94)  LDD0626  [4]
 LDCM0310  AC48 HCT 116 C164(0.84); C212(0.93); C572(0.97); C318(1.02)  LDD0627  [4]
 LDCM0311  AC49 HCT 116 C164(0.93); C572(0.96); C212(0.97); C318(1.11)  LDD0628  [4]
 LDCM0312  AC5 HCT 116 C212(0.71); C164(0.92); C572(1.01); C428(1.11)  LDD0629  [4]
 LDCM0313  AC50 HCT 116 C318(0.87); C572(1.04); C164(1.05); C212(1.10)  LDD0630  [4]
 LDCM0314  AC51 HCT 116 C164(0.92); C318(0.94); C573(0.96); C572(0.96)  LDD0631  [4]
 LDCM0315  AC52 HCT 116 C318(0.88); C212(0.93); C164(0.96); C572(0.99)  LDD0632  [4]
 LDCM0316  AC53 HCT 116 C164(0.83); C572(0.95); C212(1.11); C573(1.17)  LDD0633  [4]
 LDCM0317  AC54 HCT 116 C164(0.85); C572(0.97); C212(1.02); C573(1.07)  LDD0634  [4]
 LDCM0318  AC55 HCT 116 C318(0.92); C212(0.93); C572(0.96); C164(0.97)  LDD0635  [4]
 LDCM0319  AC56 HCT 116 C164(1.00); C572(1.07); C212(1.18); C318(1.36)  LDD0636  [4]
 LDCM0320  AC57 HCT 116 C572(0.71); C164(0.76); C212(0.83); C67(1.03)  LDD0637  [4]
 LDCM0321  AC58 HCT 116 C572(0.66); C164(0.73); C67(0.92); C212(1.09)  LDD0638  [4]
 LDCM0322  AC59 HCT 116 C572(0.74); C164(0.87); C67(1.06); C212(1.10)  LDD0639  [4]
 LDCM0323  AC6 HCT 116 C212(0.99); C67(1.05); C164(1.11); C318(1.12)  LDD0640  [4]
 LDCM0324  AC60 HCT 116 C164(0.68); C572(0.70); C67(0.94); C212(1.00)  LDD0641  [4]
 LDCM0325  AC61 HCT 116 C164(0.57); C572(0.77); C212(0.81); C67(0.92)  LDD0642  [4]
 LDCM0326  AC62 HCT 116 C572(0.78); C212(0.79); C164(0.87); C67(1.16)  LDD0643  [4]
 LDCM0327  AC63 HCT 116 C164(0.64); C572(0.83); C212(0.87); C67(1.01)  LDD0644  [4]
 LDCM0328  AC64 HCT 116 C164(0.74); C212(0.78); C572(0.89); C67(1.09)  LDD0645  [4]
 LDCM0329  AC65 HCT 116 C572(0.79); C164(0.94); C212(0.98); C67(1.12)  LDD0646  [4]
 LDCM0330  AC66 HCT 116 C164(0.83); C572(0.85); C212(0.93); C67(1.01)  LDD0647  [4]
 LDCM0331  AC67 HCT 116 C164(0.74); C572(0.75); C212(0.95); C67(1.00)  LDD0648  [4]
 LDCM0332  AC68 HCT 116 C164(0.87); C67(0.93); C212(0.94); C572(0.95)  LDD0649  [4]
 LDCM0333  AC69 HCT 116 C572(0.75); C573(0.90); C67(0.99); C164(1.02)  LDD0650  [4]
 LDCM0334  AC7 HCT 116 C212(0.93); C318(0.94); C164(0.97); C573(1.14)  LDD0651  [4]
 LDCM0335  AC70 HCT 116 C572(0.80); C164(0.85); C212(0.90); C67(0.97)  LDD0652  [4]
 LDCM0336  AC71 HCT 116 C212(0.87); C67(0.89); C572(0.96); C573(1.01)  LDD0653  [4]
 LDCM0337  AC72 HCT 116 C572(0.91); C67(0.92); C212(0.97); C318(0.98)  LDD0654  [4]
 LDCM0338  AC73 HCT 116 C572(0.83); C164(1.09); C212(1.10); C67(1.12)  LDD0655  [4]
 LDCM0339  AC74 HCT 116 C572(0.83); C212(0.99); C67(1.01); C573(1.16)  LDD0656  [4]
 LDCM0340  AC75 HCT 116 C572(0.74); C212(0.84); C67(1.09); C318(1.10)  LDD0657  [4]
 LDCM0341  AC76 HCT 116 C572(0.87); C212(0.90); C573(0.99); C164(1.03)  LDD0658  [4]
 LDCM0342  AC77 HCT 116 C572(0.79); C164(1.02); C573(1.03); C67(1.09)  LDD0659  [4]
 LDCM0343  AC78 HCT 116 C164(0.77); C572(0.84); C573(0.96); C212(0.97)  LDD0660  [4]
 LDCM0344  AC79 HCT 116 C572(0.82); C573(0.94); C212(1.00); C164(1.07)  LDD0661  [4]
 LDCM0345  AC8 HCT 116 C318(1.05); C67(1.15); C212(1.16); C164(1.18)  LDD0662  [4]
 LDCM0346  AC80 HCT 116 C212(0.87); C67(0.92); C572(0.94); C164(1.04)  LDD0663  [4]
 LDCM0347  AC81 HCT 116 C67(0.83); C212(0.91); C164(0.92); C428(1.10)  LDD0664  [4]
 LDCM0348  AC82 HCT 116 C572(0.90); C212(0.91); C164(1.05); C67(1.10)  LDD0665  [4]
 LDCM0349  AC83 HCT 116 C428(0.72); C164(0.90); C318(0.93); C572(0.96)  LDD0666  [4]
 LDCM0350  AC84 HCT 116 C428(0.70); C164(0.92); C572(0.92); C318(0.95)  LDD0667  [4]
 LDCM0351  AC85 HCT 116 C428(0.76); C164(0.95); C572(0.95); C318(0.96)  LDD0668  [4]
 LDCM0352  AC86 HCT 116 C428(0.84); C318(0.97); C572(0.99); C164(1.02)  LDD0669  [4]
 LDCM0353  AC87 HCT 116 C428(0.67); C212(0.95); C67(0.97); C164(1.00)  LDD0670  [4]
 LDCM0354  AC88 HCT 116 C428(0.62); C572(1.01); C212(1.01); C164(1.05)  LDD0671  [4]
 LDCM0355  AC89 HCT 116 C428(0.68); C164(0.82); C572(0.89); C318(1.01)  LDD0672  [4]
 LDCM0357  AC90 HCT 116 C212(0.69); C428(0.78); C164(1.01); C318(1.02)  LDD0674  [4]
 LDCM0358  AC91 HCT 116 C428(0.82); C318(1.02); C164(1.05); C572(1.06)  LDD0675  [4]
 LDCM0359  AC92 HCT 116 C428(0.74); C164(0.89); C318(0.99); C572(1.01)  LDD0676  [4]
 LDCM0360  AC93 HCT 116 C428(0.62); C164(0.83); C318(0.91); C212(1.02)  LDD0677  [4]
 LDCM0361  AC94 HCT 116 C428(0.70); C318(1.00); C164(1.05); C67(1.08)  LDD0678  [4]
 LDCM0362  AC95 HCT 116 C428(0.72); C572(0.87); C212(0.92); C67(0.94)  LDD0679  [4]
 LDCM0363  AC96 HCT 116 C428(0.73); C164(0.90); C318(0.96); C573(1.03)  LDD0680  [4]
 LDCM0364  AC97 HCT 116 C428(0.74); C164(0.96); C318(1.00); C572(1.03)  LDD0681  [4]
 LDCM0365  AC98 HCT 116 C572(0.58); C67(0.77); C573(0.93); C428(0.93)  LDD0682  [4]
 LDCM0366  AC99 HCT 116 C67(0.74); C572(0.76); C573(0.79); C428(0.94)  LDD0683  [4]
 LDCM0248  AKOS034007472 HCT 116 C573(1.32); C428(1.12); C164(1.07); C212(0.77)  LDD0565  [4]
 LDCM0356  AKOS034007680 HCT 116 C212(0.89); C164(0.94); C318(0.99); C67(1.08)  LDD0673  [4]
 LDCM0275  AKOS034007705 HCT 116 C318(1.10); C164(1.16); C212(1.24); C67(1.48)  LDD0592  [4]
 LDCM0020  ARS-1620 HCC44 C573(1.20); C212(1.07)  LDD0078  [4]
 LDCM0632  CL-Sc Hep-G2 C405(1.21); C164(0.99); C67(0.57)  LDD2227  [7]
 LDCM0367  CL1 HCT 116 C318(0.80); C164(0.85); C67(0.95); C572(1.11)  LDD0684  [4]
 LDCM0368  CL10 HCT 116 C318(0.81); C164(0.85); C212(0.90); C67(0.97)  LDD0685  [4]
 LDCM0369  CL100 HCT 116 C212(0.64); C164(0.89); C572(0.92); C67(1.01)  LDD0686  [4]
 LDCM0370  CL101 HCT 116 C67(0.98); C318(0.99); C212(1.07); C428(1.31)  LDD0687  [4]
 LDCM0371  CL102 HCT 116 C318(0.83); C212(0.94); C428(0.99); C67(1.06)  LDD0688  [4]
 LDCM0372  CL103 HCT 116 C212(0.80); C318(0.98); C67(1.03); C573(1.25)  LDD0689  [4]
 LDCM0373  CL104 HCT 116 C318(1.01); C428(1.06); C212(1.06); C67(1.06)  LDD0690  [4]
 LDCM0374  CL105 HCT 116 C67(0.96); C573(0.99); C212(1.00); C164(1.01)  LDD0691  [4]
 LDCM0375  CL106 HCT 116 C573(0.87); C67(0.92); C572(0.97); C164(1.10)  LDD0692  [4]
 LDCM0376  CL107 HCT 116 C573(0.93); C572(0.97); C67(1.01); C212(1.11)  LDD0693  [4]
 LDCM0377  CL108 HCT 116 C573(0.94); C572(1.01); C67(1.04); C212(1.10)  LDD0694  [4]
 LDCM0378  CL109 HCT 116 C67(1.01); C212(1.16); C573(1.16); C164(1.16)  LDD0695  [4]
 LDCM0379  CL11 HCT 116 C318(0.77); C164(0.80); C212(0.89); C67(0.99)  LDD0696  [4]
 LDCM0380  CL110 HCT 116 C164(0.99); C67(1.02); C428(1.14); C212(1.17)  LDD0697  [4]
 LDCM0381  CL111 HCT 116 C164(0.96); C67(0.99); C572(1.02); C573(1.05)  LDD0698  [4]
 LDCM0382  CL112 HCT 116 C428(0.86); C67(0.91); C164(0.93); C572(0.98)  LDD0699  [4]
 LDCM0383  CL113 HCT 116 C572(0.88); C164(1.00); C67(1.10); C428(1.14)  LDD0700  [4]
 LDCM0384  CL114 HCT 116 C572(0.85); C164(0.87); C67(0.89); C573(1.26)  LDD0701  [4]
 LDCM0385  CL115 HCT 116 C572(0.87); C67(0.89); C164(0.94); C212(1.02)  LDD0702  [4]
 LDCM0386  CL116 HCT 116 C572(0.85); C164(0.95); C428(0.99); C67(0.99)  LDD0703  [4]
 LDCM0387  CL117 HCT 116 C164(0.99); C67(1.04); C572(1.04); C212(1.49)  LDD0704  [4]
 LDCM0388  CL118 HCT 116 C212(0.95); C572(0.96); C573(1.01); C164(1.03)  LDD0705  [4]
 LDCM0389  CL119 HCT 116 C212(0.95); C572(1.04); C428(1.06); C164(1.09)  LDD0706  [4]
 LDCM0390  CL12 HCT 116 C212(0.84); C318(0.91); C164(0.96); C428(1.08)  LDD0707  [4]
 LDCM0391  CL120 HCT 116 C428(0.84); C212(0.86); C572(1.01); C573(1.05)  LDD0708  [4]
 LDCM0392  CL121 HCT 116 C318(0.77); C164(0.77); C428(0.97); C573(1.05)  LDD0709  [4]
 LDCM0393  CL122 HCT 116 C164(0.86); C572(0.91); C318(0.91); C573(1.11)  LDD0710  [4]
 LDCM0394  CL123 HCT 116 C164(0.84); C212(1.00); C318(1.04); C67(1.49)  LDD0711  [4]
 LDCM0395  CL124 HCT 116 C164(0.76); C212(0.90); C318(0.97); C572(1.15)  LDD0712  [4]
 LDCM0396  CL125 HCT 116 C164(0.81); C212(0.89); C572(0.93); C67(1.00)  LDD0713  [4]
 LDCM0397  CL126 HCT 116 C572(0.85); C67(0.85); C164(0.95); C428(0.99)  LDD0714  [4]
 LDCM0398  CL127 HCT 116 C572(0.78); C164(0.86); C67(0.98); C212(0.99)  LDD0715  [4]
 LDCM0399  CL128 HCT 116 C164(0.84); C572(0.85); C67(0.99); C212(1.02)  LDD0716  [4]
 LDCM0400  CL13 HCT 116 C318(0.86); C164(0.90); C67(0.95); C572(1.05)  LDD0717  [4]
 LDCM0401  CL14 HCT 116 C318(0.82); C164(0.87); C572(0.90); C67(0.99)  LDD0718  [4]
 LDCM0402  CL15 HCT 116 C318(0.81); C164(0.88); C67(0.89); C428(1.01)  LDD0719  [4]
 LDCM0403  CL16 HCT 116 C67(0.93); C318(1.01); C164(1.04); C428(1.07)  LDD0720  [4]
 LDCM0404  CL17 HCT 116 C67(0.79); C212(0.92); C318(0.96); C572(1.06)  LDD0721  [4]
 LDCM0405  CL18 HCT 116 C572(0.81); C212(0.89); C67(0.90); C573(0.94)  LDD0722  [4]
 LDCM0406  CL19 HCT 116 C572(0.94); C67(0.97); C573(1.03); C212(1.03)  LDD0723  [4]
 LDCM0407  CL2 HCT 116 C164(0.79); C318(0.87); C572(0.87); C67(0.90)  LDD0724  [4]
 LDCM0408  CL20 HCT 116 C572(0.89); C318(1.02); C212(1.07); C573(1.09)  LDD0725  [4]
 LDCM0409  CL21 HCT 116 C318(0.92); C212(0.99); C67(1.04); C572(1.66)  LDD0726  [4]
 LDCM0410  CL22 HCT 116 C572(1.04); C318(1.12); C67(1.14); C573(1.49)  LDD0727  [4]
 LDCM0411  CL23 HCT 116 C572(0.89); C573(1.00); C67(1.02); C318(1.04)  LDD0728  [4]
 LDCM0412  CL24 HCT 116 C572(0.96); C212(1.00); C318(1.04); C67(1.09)  LDD0729  [4]
 LDCM0413  CL25 HCT 116 C572(0.96); C573(1.12); C428(1.41); C212(0.88)  LDD0730  [4]
 LDCM0414  CL26 HCT 116 C572(0.94); C573(1.09); C428(1.07); C212(1.12)  LDD0731  [4]
 LDCM0415  CL27 HCT 116 C572(1.00); C573(1.04); C428(1.21); C212(1.04)  LDD0732  [4]
 LDCM0416  CL28 HCT 116 C572(2.66); C573(3.17); C428(3.09); C212(0.82)  LDD0733  [4]
 LDCM0417  CL29 HCT 116 C572(1.02); C573(1.15); C428(1.27); C212(1.35)  LDD0734  [4]
 LDCM0418  CL3 HCT 116 C572(0.85); C573(1.04); C428(2.17); C164(1.01)  LDD0735  [4]
 LDCM0419  CL30 HCT 116 C572(0.96); C573(1.04); C428(1.48); C212(0.95)  LDD0736  [4]
 LDCM0420  CL31 HCT 116 C572(0.79); C573(1.08); C428(1.84); C164(0.83)  LDD0737  [4]
 LDCM0421  CL32 HCT 116 C572(0.86); C573(0.98); C428(1.63); C164(0.93)  LDD0738  [4]
 LDCM0422  CL33 HCT 116 C572(1.01); C573(1.30); C428(2.12); C164(1.01)  LDD0739  [4]
 LDCM0423  CL34 HCT 116 C572(2.00); C573(2.38); C428(1.69); C164(1.18)  LDD0740  [4]
 LDCM0424  CL35 HCT 116 C572(0.86); C573(0.96); C428(1.48); C164(1.30)  LDD0741  [4]
 LDCM0425  CL36 HCT 116 C572(0.95); C573(0.99); C428(1.53); C164(1.37)  LDD0742  [4]
 LDCM0426  CL37 HCT 116 C572(0.86); C573(0.94); C428(1.77); C164(1.56)  LDD0743  [4]
 LDCM0428  CL39 HCT 116 C572(1.98); C573(1.68); C428(2.14); C164(1.21)  LDD0745  [4]
 LDCM0429  CL4 HCT 116 C572(1.12); C573(1.26); C428(1.08); C164(0.92)  LDD0746  [4]
 LDCM0430  CL40 HCT 116 C572(1.00); C573(2.19); C428(1.73); C164(0.88)  LDD0747  [4]
 LDCM0431  CL41 HCT 116 C572(1.08); C573(1.11); C428(1.57); C164(1.22)  LDD0748  [4]
 LDCM0432  CL42 HCT 116 C572(1.36); C573(1.94); C428(2.14); C164(1.29)  LDD0749  [4]
 LDCM0433  CL43 HCT 116 C572(0.98); C573(1.07); C428(1.58); C164(1.06)  LDD0750  [4]
 LDCM0434  CL44 HCT 116 C572(1.30); C573(1.20); C428(1.72); C164(1.10)  LDD0751  [4]
 LDCM0435  CL45 HCT 116 C572(1.16); C573(1.21); C428(1.83); C164(1.25)  LDD0752  [4]
 LDCM0436  CL46 HCT 116 C572(1.43); C573(1.22); C428(1.14); C164(0.82)  LDD0753  [4]
 LDCM0437  CL47 HCT 116 C572(0.99); C573(0.91); C428(1.15); C164(0.86)  LDD0754  [4]
 LDCM0438  CL48 HCT 116 C572(0.91); C573(0.93); C428(0.96); C164(0.97)  LDD0755  [4]
 LDCM0439  CL49 HCT 116 C572(0.98); C573(0.87); C428(0.96); C164(1.06)  LDD0756  [4]
 LDCM0440  CL5 HCT 116 C572(1.06); C573(1.07); C428(0.81); C164(1.00)  LDD0757  [4]
 LDCM0441  CL50 HCT 116 C572(1.33); C573(1.11); C428(0.74); C164(0.94)  LDD0758  [4]
 LDCM0442  CL51 HCT 116 C572(1.26); C573(1.06); C428(0.84); C164(1.03)  LDD0759  [4]
 LDCM0443  CL52 HCT 116 C572(0.97); C573(0.90); C428(0.90); C164(0.95)  LDD0760  [4]
 LDCM0444  CL53 HCT 116 C572(0.96); C573(0.95); C428(0.85); C164(1.09)  LDD0761  [4]
 LDCM0445  CL54 HCT 116 C572(1.31); C573(2.46); C428(1.13); C164(0.93)  LDD0762  [4]
 LDCM0446  CL55 HCT 116 C572(2.61); C573(1.60); C428(0.74); C164(1.12)  LDD0763  [4]
 LDCM0447  CL56 HCT 116 C572(0.89); C573(0.86); C428(0.96); C164(1.10)  LDD0764  [4]
 LDCM0448  CL57 HCT 116 C572(1.45); C573(1.47); C428(0.88); C164(1.15)  LDD0765  [4]
 LDCM0449  CL58 HCT 116 C572(1.10); C573(1.03); C428(0.89); C164(1.07)  LDD0766  [4]
 LDCM0450  CL59 HCT 116 C572(1.04); C573(0.96); C428(0.89); C164(1.13)  LDD0767  [4]
 LDCM0451  CL6 HCT 116 C572(0.83); C573(1.04); C428(1.10); C164(0.83)  LDD0768  [4]
 LDCM0452  CL60 HCT 116 C572(0.79); C573(1.04); C428(0.97); C164(0.99)  LDD0769  [4]
 LDCM0453  CL61 HCT 116 C572(1.02); C573(1.11); C428(1.41); C164(1.15)  LDD0770  [4]
 LDCM0454  CL62 HCT 116 C572(0.99); C573(1.01); C428(0.97); C164(1.15)  LDD0771  [4]
 LDCM0455  CL63 HCT 116 C572(0.90); C573(1.26); C428(4.08); C164(1.08)  LDD0772  [4]
 LDCM0456  CL64 HCT 116 C572(1.22); C573(1.43); C428(1.62); C164(1.36)  LDD0773  [4]
 LDCM0457  CL65 HCT 116 C572(0.81); C573(0.99); C428(1.13); C164(1.10)  LDD0774  [4]
 LDCM0458  CL66 HCT 116 C572(0.93); C573(1.32); C428(2.57); C164(1.02)  LDD0775  [4]
 LDCM0459  CL67 HCT 116 C572(0.81); C573(1.10); C428(1.07); C164(1.50)  LDD0776  [4]
 LDCM0460  CL68 HCT 116 C572(0.86); C573(1.27); C428(1.40); C164(1.44)  LDD0777  [4]
 LDCM0461  CL69 HCT 116 C572(1.89); C573(3.29); C428(2.71); C164(1.20)  LDD0778  [4]
 LDCM0462  CL7 HCT 116 C572(1.13); C573(1.15); C428(1.08); C164(0.94)  LDD0779  [4]
 LDCM0463  CL70 HCT 116 C572(0.88); C573(1.09); C428(1.47); C164(1.22)  LDD0780  [4]
 LDCM0464  CL71 HCT 116 C572(1.03); C573(1.21); C428(0.96); C164(1.31)  LDD0781  [4]
 LDCM0465  CL72 HCT 116 C572(0.76); C573(0.95); C428(1.19); C164(1.37)  LDD0782  [4]
 LDCM0466  CL73 HCT 116 C572(0.76); C573(1.00); C428(1.30); C164(1.19)  LDD0783  [4]
 LDCM0467  CL74 HCT 116 C572(0.84); C573(1.09); C428(1.06); C164(1.33)  LDD0784  [4]
 LDCM0469  CL76 HCT 116 C572(0.68); C573(1.01); C428(0.93); C164(0.80)  LDD0786  [4]
 LDCM0470  CL77 HCT 116 C572(0.91); C573(1.27); C428(0.98); C164(0.95)  LDD0787  [4]
 LDCM0471  CL78 HCT 116 C572(0.88); C573(1.17); C428(0.91); C164(0.99)  LDD0788  [4]
 LDCM0472  CL79 HCT 116 C572(0.80); C573(1.25); C428(0.89); C164(0.89)  LDD0789  [4]
 LDCM0473  CL8 HCT 116 C572(9.58); C573(16.22); C428(3.12); C164(0.88)  LDD0790  [4]
 LDCM0474  CL80 HCT 116 C572(0.60); C573(1.03); C428(0.92); C164(0.72)  LDD0791  [4]
 LDCM0475  CL81 HCT 116 C572(0.77); C573(1.07); C428(0.91); C164(1.01)  LDD0792  [4]
 LDCM0476  CL82 HCT 116 C572(0.79); C573(1.45); C428(0.90); C164(0.99)  LDD0793  [4]
 LDCM0477  CL83 HCT 116 C572(0.73); C573(1.42); C428(0.86); C164(0.87)  LDD0794  [4]
 LDCM0478  CL84 HCT 116 C572(0.91); C573(1.93); C428(0.84); C164(0.88)  LDD0795  [4]
 LDCM0479  CL85 HCT 116 C572(0.78); C573(1.07); C428(1.00); C164(0.94)  LDD0796  [4]
 LDCM0480  CL86 HCT 116 C572(0.82); C573(1.03); C428(0.82); C164(0.92)  LDD0797  [4]
 LDCM0481  CL87 HCT 116 C572(0.75); C573(1.17); C428(0.97); C164(0.93)  LDD0798  [4]
 LDCM0482  CL88 HCT 116 C572(0.73); C573(1.24); C428(0.88); C164(0.99)  LDD0799  [4]
 LDCM0483  CL89 HCT 116 C572(0.89); C573(2.00); C428(0.78); C164(1.06)  LDD0800  [4]
 LDCM0484  CL9 HCT 116 C572(0.95); C573(1.02); C428(1.23); C164(0.91)  LDD0801  [4]
 LDCM0485  CL90 HCT 116 C572(0.95); C573(1.72); C428(1.08); C164(0.91)  LDD0802  [4]
 LDCM0486  CL91 HCT 116 C572(0.88); C573(0.99); C428(1.05); C164(0.95)  LDD0803  [4]
 LDCM0487  CL92 HCT 116 C572(2.39); C573(2.87); C428(1.45); C164(0.96)  LDD0804  [4]
 LDCM0488  CL93 HCT 116 C572(1.09); C573(1.19); C428(1.05); C164(0.91)  LDD0805  [4]
 LDCM0489  CL94 HCT 116 C572(0.91); C573(1.16); C428(1.05); C164(0.79)  LDD0806  [4]
 LDCM0490  CL95 HCT 116 C572(1.02); C573(1.21); C428(0.96); C164(0.85)  LDD0807  [4]
 LDCM0491  CL96 HCT 116 C572(1.03); C573(1.17); C428(0.96); C164(0.80)  LDD0808  [4]
 LDCM0492  CL97 HCT 116 C572(1.29); C573(1.58); C428(1.18); C164(0.92)  LDD0809  [4]
 LDCM0493  CL98 HCT 116 C572(0.97); C573(1.35); C428(1.23); C164(0.85)  LDD0810  [4]
 LDCM0494  CL99 HCT 116 C572(0.93); C573(1.13); C428(1.17); C164(0.82)  LDD0811  [4]
 LDCM0634  CY-0357 Hep-G2 C67(1.08)  LDD2228  [7]
 LDCM0495  E2913 HEK-293T C67(0.98); C428(1.71); C164(1.12); C212(0.93)  LDD1698  [17]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C573(1.06)  LDD1702  [18]
 LDCM0625  F8 Ramos C67(1.49); 0.99; C212(1.09); C372(1.14)  LDD2187  [19]
 LDCM0572  Fragment10 Ramos 2.19; C212(2.24)  LDD2189  [19]
 LDCM0573  Fragment11 Ramos C67(1.58); 4.77; C212(0.85); C372(0.18)  LDD2190  [19]
 LDCM0574  Fragment12 Ramos C67(0.92); 2.43; C212(1.01)  LDD2191  [19]
 LDCM0575  Fragment13 Ramos C67(0.97); C212(0.97)  LDD2192  [19]
 LDCM0576  Fragment14 Ramos C67(1.09); 1.04; C212(0.72); C372(0.54)  LDD2193  [19]
 LDCM0579  Fragment20 Ramos C67(0.75); 1.02; C212(1.00)  LDD2194  [19]
 LDCM0580  Fragment21 Ramos C67(1.02); 1.36; C212(0.97)  LDD2195  [19]
 LDCM0582  Fragment23 Ramos 1.56; C212(1.37)  LDD2196  [19]
 LDCM0578  Fragment27 Ramos C67(0.65); 0.79; C212(0.88)  LDD2197  [19]
 LDCM0586  Fragment28 Ramos C67(0.57); 0.41; C212(0.78); C372(0.90)  LDD2198  [19]
 LDCM0588  Fragment30 Ramos C67(0.91); 0.84; C212(1.12)  LDD2199  [19]
 LDCM0589  Fragment31 Ramos C67(0.69); 1.07; C212(0.88)  LDD2200  [19]
 LDCM0590  Fragment32 Ramos C67(0.68); C212(1.69)  LDD2201  [19]
 LDCM0468  Fragment33 HCT 116 C572(0.95); C573(1.26); C428(1.27); C164(1.14)  LDD0785  [4]
 LDCM0596  Fragment38 Ramos C67(0.57); 0.68; C212(0.72)  LDD2203  [19]
 LDCM0566  Fragment4 Ramos C67(0.83); 1.71; C212(0.85); C372(0.81)  LDD2184  [19]
 LDCM0427  Fragment51 HCT 116 C572(1.00); C573(1.11); C428(2.23); C164(1.06)  LDD0744  [4]
 LDCM0610  Fragment52 Ramos C67(0.54); 0.70; C212(1.00)  LDD2204  [19]
 LDCM0614  Fragment56 Ramos C67(0.74); 0.67; C212(0.98)  LDD2205  [19]
 LDCM0569  Fragment7 Ramos C67(1.01); 1.17; C212(1.07); C372(1.27)  LDD2186  [19]
 LDCM0571  Fragment9 Ramos C67(0.86); C212(1.22)  LDD2188  [19]
 LDCM0107  IAA HeLa N.A.  LDD0221  [12]
 LDCM0022  KB02 HCT 116 C572(7.47); C573(11.01); C67(5.58); C428(1.62)  LDD0080  [4]
 LDCM0023  KB03 HCT 116 C572(14.77); C573(20.00); C67(1.99); C428(3.83)  LDD0081  [4]
 LDCM0024  KB05 HCT 116 C572(2.19); C573(2.10); C67(1.82); C428(1.41)  LDD0082  [4]
 LDCM0627  NUDT7-COV-1 HEK-293T C67(0.99); C572(0.93); C428(0.60)  LDD2206  [20]
 LDCM0628  OTUB2-COV-1 HEK-293T C573(0.75); C212(0.72); C67(0.70); C372(0.30)  LDD2207  [20]
 LDCM0131  RA190 MM1.R C67(1.36); C212(1.28); C573(0.75)  LDD0304  [21]
 LDCM0021  THZ1 HCT 116 C573(1.16); C67(0.98)  LDD2173  [4]
 LDCM0112  W16 Hep-G2 C572(0.92); C573(0.92)  LDD0239  [13]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 14 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
RecQ-like DNA helicase BLM (BLM) Helicase family P54132
DNA replication licensing factor MCM2 (MCM2) MCM family P49736
DNA replication licensing factor MCM7 (MCM7) MCM family P33993
E3 ubiquitin-protein ligase Mdm2 (MDM2) MDM2/MDM4 family Q00987
M-phase inducer phosphatase 3 (CDC25C) MPI phosphatase family P30307
Histone acetyltransferase KAT7 (KAT7) MYST (SAS/MOZ) family O95251
Caspase-8 (CASP8) Peptidase C14A family Q14790
Serine/threonine-protein kinase Chk2 (CHEK2) CAMK Ser/Thr protein kinase family O96017
Serine/threonine-protein kinase Nek9 (NEK9) NEK Ser/Thr protein kinase family Q8TD19
Aurora kinase A (AURKA) Ser/Thr protein kinase family O14965
Serine/threonine-protein kinase PLK1 (PLK1) Ser/Thr protein kinase family P53350
Wee1-like protein kinase (WEE1) Ser/Thr protein kinase family P30291
DNA excision repair protein ERCC-6-like (ERCC6L) SNF2/RAD54 helicase family Q2NKX8
Baculoviral IAP repeat-containing protein 6 (BIRC6) Ubiquitin-conjugating enzyme family Q9NR09
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein TGIF1 (TGIF1) TALE/TGIF homeobox family Q15583
Other
Click To Hide/Show 16 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein aurora borealis (BORA) BORA family Q6PGQ7
Cell division control protein 6 homolog (CDC6) CDC6/cdc18 family Q99741
Segment polarity protein dishevelled homolog DVL-2 (DVL2) DSH family O14641
NHS-like protein 2 (NHSL2) NHS family Q5HYW2
Centriole and centriolar satellite protein OFD1 (OFD1) OFD1 family O75665
Structure-specific endonuclease subunit SLX4 (SLX4) SLX4 family Q8IY92
Axin-2 (AXIN2) . Q9Y2T1
Centrosomal protein of 68 kDa (CEP68) . Q76N32
Ecotropic viral integration site 5 protein homolog (EVI5) . O60447
Eukaryotic translation initiation factor 4B (EIF4B) . P23588
FAS-associated death domain protein (FADD) . Q13158
G2 and S phase-expressed protein 1 (GTSE1) . Q9NYZ3
Polyhomeotic-like protein 2 (PHC2) . Q8IXK0
Rac GTPase-activating protein 1 (RACGAP1) . Q9H0H5
TP53-binding protein 1 (TP53BP1) . Q12888
TRAF family member-associated NF-kappa-B activator (TANK) . Q92844

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 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rigosertib Small molecular drug D0KF9Q
Volasertib Small molecular drug D00BYM
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bi 2536 Small molecular drug D0O0LQ
Pcm-075 . D03HUX
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cyc140 Small molecular drug DK26FL
Gsk461364 Small molecular drug D08RMJ
Tak-960 Small molecular drug D09JGK
Mk-1496 . D05RGV
Preclinical
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cyc-800 Small molecular drug D0WZ4J
Zk-thiazolidinone Small molecular drug D07RMX
Dap-81 . D05ZCQ
Investigative
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gsk579289a Small molecular drug D0X1RH
Gw853606 Small molecular drug D09ZKY
Lc-445 Small molecular drug D0X5ZH
Mln-0905 Small molecular drug D05QMQ
Pmid19097784c2 Small molecular drug D0H8WY
Wortmannin Small molecular drug DB08059
1-[5-methyl-2-(Trifluoromethyl)Furan-3-yl]-3-[5-[2-[[6-(1h-124-triazol-5-ylamino)Pyrimidin-4-yl]Amino]Ethyl]-13-thiazol-2-yl]Urea . DB07789
3-[3-(3-methyl-6-{[(1s)-1-phenylethyl]Amino}-1h-pyrazolo[43-c]Pyridin-1-yl)Phenyl]Propanamide . DB06963
3-[3-chloro-5-(5-{[(1s)-1-phenylethyl]Amino}Isoxazolo[54-c]Pyridin-3-yl)Phenyl]Propan-1-ol . DB06897
4-(4-methylpiperazin-1-yl)-n-[5-(2-thienylacetyl)-15-dihydropyrrolo[34-c]Pyrazol-3-yl]Benzamide . DB07186
Chr-4125 . D01HHH
Nms-1 . D03BQD
Ro5203280 . D05WDM
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dihydropyrido Pyrazinone Compound 2 Small molecular drug D0S0HQ
Dihydropyrido Pyrazinone Compound 3 Small molecular drug D0F3GC
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hmn-214 Small molecular drug D0R7ID

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 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
3 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
4 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.
5 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.
6 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
7 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
8 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
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
10 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
11 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
12 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.
13 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
14 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
15 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
16 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
17 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
18 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
19 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
20 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.
21 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.