General Information of Target

Target ID LDTP01766
Target Name L-lactate dehydrogenase A chain (LDHA)
Gene Name LDHA
Gene ID 3939
Synonyms
L-lactate dehydrogenase A chain; LDH-A; EC 1.1.1.27; Cell proliferation-inducing gene 19 protein; LDH muscle subunit; LDH-M; Renal carcinoma antigen NY-REN-59
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATLKDQLIYNLLKEEQTPQNKITVVGVGAVGMACAISILMKDLADELALVDVIEDKLKG
EMMDLQHGSLFLRTPKIVSGKDYNVTANSKLVIITAGARQQEGESRLNLVQRNVNIFKFI
IPNVVKYSPNCKLLIVSNPVDILTYVAWKISGFPKNRVIGSGCNLDSARFRYLMGERLGV
HPLSCHGWVLGEHGDSSVPVWSGMNVAGVSLKTLHPDLGTDKDKEQWKEVHKQVVESAYE
VIKLKGYTSWAIGLSVADLAESIMKNLRRVHPVSTMIKGLYGIKDDVFLSVPCILGQNGI
SDLVKVTLTSEEEARLKKSADTLWGIQKELQF
Target Type
Successful
Target Bioclass
Enzyme
Family
LDH/MDH superfamily, LDH family
Subcellular location
Cytoplasm
Function Interconverts simultaneously and stereospecifically pyruvate and lactate with concomitant interconversion of NADH and NAD(+).
TTD ID
T32790
Uniprot ID
P00338
DrugMap ID
TTNFMAL
Ensemble ID
ENST00000227157.8
HGNC ID
HGNC:6535
ChEMBL ID
CHEMBL4835

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.A168T DBIA    Probe Info 
JURKAT SNV: p.V291F .
NALM6 SNV: p.R169Ter DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 62 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Hsieh_2
 Probe Info 
N.A.  LDD0425  [1]
P1
 Probe Info 
2.12  LDD0452  [2]
P2
 Probe Info 
1.77  LDD0453  [2]
P3
 Probe Info 
1.99  LDD0454  [2]
P8
 Probe Info 
2.40  LDD0455  [2]
A-EBA
 Probe Info 
4.01  LDD0215  [3]
8RK64
 Probe Info 
N.A.  LDD0039  [4]
CHEMBL5175495
 Probe Info 
7.45  LDD0196  [5]
CY4
 Probe Info 
2.49  LDD0244  [6]
N1
 Probe Info 
2.39  LDD0242  [6]
C-Sul
 Probe Info 
3.53  LDD0066  [7]
TH211
 Probe Info 
Y127(14.26); Y239(13.39); Y10(12.92); Y172(6.34)  LDD0257  [8]
TH214
 Probe Info 
Y127(20.00); Y239(19.61)  LDD0258  [8]
TH216
 Probe Info 
Y172(20.00); Y239(20.00); Y83(20.00); Y281(17.09)  LDD0259  [8]
YN-4
 Probe Info 
100.00  LDD0445  [9]
BTD
 Probe Info 
C131(4.77)  LDD1699  [10]
AZ-9
 Probe Info 
E236(0.83); E311(0.99); E313(0.99); D82(1.03)  LDD2208  [11]
ONAyne
 Probe Info 
K76(0.00); K318(0.00); K81(0.00)  LDD0273  [12]
OPA-S-S-alkyne
 Probe Info 
K59(0.14); K155(2.54)  LDD3494  [13]
Probe 1
 Probe Info 
Y10(74.90); Y239(126.30); Y281(35.19)  LDD3495  [14]
DBIA
 Probe Info 
C322(0.50); C64(0.99)  LDD3310  [15]
JZ128-DTB
 Probe Info 
C293(0.00); C163(0.00); C131(0.00)  LDD0462  [16]
THZ1-DTB
 Probe Info 
C163(1.11); C293(1.05); C185(0.94)  LDD0460  [16]
AHL-Pu-1
 Probe Info 
C131(3.95)  LDD0168  [17]
EA-probe
 Probe Info 
C185(2.70); C163(1.27)  LDD2210  [18]
HHS-482
 Probe Info 
Y10(0.84); Y127(0.96); Y145(1.12); Y172(0.79)  LDD0285  [19]
HHS-475
 Probe Info 
Y127(0.74); Y83(0.78); Y10(0.78); Y239(0.83)  LDD0264  [20]
HHS-465
 Probe Info 
Y10(4.90); Y127(6.03); Y172(3.38); Y239(9.60)  LDD2237  [21]
5E-2FA
 Probe Info 
H231(0.00); H67(0.00); H215(0.00)  LDD2235  [22]
AMP probe
 Probe Info 
K81(0.00); K222(0.00); K224(0.00); K228(0.00)  LDD0200  [23]
ATP probe
 Probe Info 
K81(0.00); K222(0.00); K224(0.00); K228(0.00)  LDD0199  [23]
4-Iodoacetamidophenylacetylene
 Probe Info 
C293(0.00); C35(0.00); C185(0.00); C163(0.00)  LDD0038  [24]
IA-alkyne
 Probe Info 
C185(0.00); C293(0.00); C163(0.00)  LDD0032  [25]
IPIAA_H
 Probe Info 
C185(0.00); C163(0.00); C293(0.00); C131(0.00)  LDD0030  [26]
IPIAA_L
 Probe Info 
C163(0.00); C185(0.00); C131(0.00); C293(0.00)  LDD0031  [26]
Lodoacetamide azide
 Probe Info 
C293(0.00); C131(0.00); C35(0.00); C185(0.00)  LDD0037  [24]
ATP probe
 Probe Info 
K132(0.00); K155(0.00); K278(0.00); K245(0.00)  LDD0035  [27]
NAIA_4
 Probe Info 
N.A.  LDD2226  [28]
TFBX
 Probe Info 
N.A.  LDD0027  [29]
WYneC
 Probe Info 
N.A.  LDD0014  [30]
WYneN
 Probe Info 
N.A.  LDD0021  [30]
WYneO
 Probe Info 
N.A.  LDD0022  [30]
1d-yne
 Probe Info 
K132(0.00); K126(0.00)  LDD0356  [31]
Compound 11
 Probe Info 
N.A.  LDD2213  [32]
ENE
 Probe Info 
N.A.  LDD0006  [30]
IPM
 Probe Info 
C131(0.00); C163(0.00)  LDD0005  [30]
NHS
 Probe Info 
K59(0.00); K318(0.00); K222(0.00); K81(0.00)  LDD0010  [30]
PF-06672131
 Probe Info 
N.A.  LDD0017  [33]
SF
 Probe Info 
K318(0.00); K155(0.00); Y10(0.00); K76(0.00)  LDD0028  [34]
STPyne
 Probe Info 
K243(0.00); K224(0.00); K14(0.00); K222(0.00)  LDD0009  [30]
VSF
 Probe Info 
N.A.  LDD0007  [30]
YN-1
 Probe Info 
N.A.  LDD0447  [9]
Phosphinate-6
 Probe Info 
C163(0.00); C185(0.00)  LDD0018  [35]
Ox-W18
 Probe Info 
W201(0.00); W227(0.00); W250(0.00); W324(0.00)  LDD2175  [36]
1c-yne
 Probe Info 
K59(0.00); K90(0.00); K14(0.00); K5(0.00)  LDD0228  [31]
Acrolein
 Probe Info 
H215(0.00); H271(0.00); C131(0.00)  LDD0217  [37]
Cinnamaldehyde
 Probe Info 
N.A.  LDD0220  [37]
Crotonaldehyde
 Probe Info 
H271(0.00); C131(0.00); H215(0.00)  LDD0219  [37]
Methacrolein
 Probe Info 
H215(0.00); H271(0.00); C131(0.00); C35(0.00)  LDD0218  [37]
W1
 Probe Info 
N.A.  LDD0236  [38]
m-APA
 Probe Info 
N.A.  LDD0404  [39]
NAIA_5
 Probe Info 
C293(0.00); C35(0.00); C131(0.00); C163(0.00)  LDD2223  [28]
PAL-AfBPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info 
6.00  LDD0471  [40]
JN0003
 Probe Info 
5.04  LDD0469  [40]
STS-2
 Probe Info 
1.25  LDD0138  [41]
VE-P
 Probe Info 
N.A.  LDD0396  [42]
Kambe_26
 Probe Info 
3.29  LDD0127  [43]
Diazir
 Probe Info 
E313(0.00); C163(0.00); E240(0.00); Y239(0.00)  LDD0011  [30]
BD-F
 Probe Info 
I9(0.00); Y10(0.00); L12(0.00); N11(0.00)  LDD0024  [44]
Photonaproxen
 Probe Info 
E236(0.00); V234(0.00)  LDD0157  [45]
STS-1
 Probe Info 
N.A.  LDD0069  [46]

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 C131(0.77)  LDD2142  [10]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C131(0.91)  LDD2112  [10]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C131(0.49)  LDD2095  [10]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C131(0.97)  LDD2130  [10]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C131(0.98)  LDD2117  [10]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C131(1.25)  LDD2152  [10]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C131(1.41)  LDD2103  [10]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C131(0.41)  LDD2132  [10]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C131(0.72)  LDD2131  [10]
 LDCM0025  4SU-RNA HEK-293T C131(3.95)  LDD0168  [17]
 LDCM0026  4SU-RNA+native RNA HEK-293T C163(4.33); C131(3.00)  LDD0169  [17]
 LDCM0214  AC1 HEK-293T C185(1.12); C293(0.94); C35(0.98)  LDD1507  [47]
 LDCM0215  AC10 HEK-293T C185(1.14); C293(1.19); C35(0.92)  LDD1508  [47]
 LDCM0226  AC11 HEK-293T C185(1.02); C293(1.04)  LDD1509  [47]
 LDCM0237  AC12 HEK-293T C185(1.11); C293(1.09); C35(1.01)  LDD1510  [47]
 LDCM0259  AC14 HEK-293T C185(1.20); C293(1.15); C35(0.97)  LDD1512  [47]
 LDCM0270  AC15 HEK-293T C185(1.07); C293(1.10); C35(0.80)  LDD1513  [47]
 LDCM0276  AC17 HEK-293T C185(1.09); C293(0.98); C35(0.97)  LDD1515  [47]
 LDCM0277  AC18 HEK-293T C185(1.05); C293(1.13); C35(0.87)  LDD1516  [47]
 LDCM0278  AC19 HEK-293T C185(0.83); C293(0.96)  LDD1517  [47]
 LDCM0279  AC2 HEK-293T C185(1.35); C293(1.11); C35(0.97)  LDD1518  [47]
 LDCM0280  AC20 HEK-293T C185(1.15); C293(1.15); C35(1.06)  LDD1519  [47]
 LDCM0281  AC21 HEK-293T C185(0.98); C293(1.04); C35(0.91)  LDD1520  [47]
 LDCM0282  AC22 HEK-293T C185(1.25); C293(1.17); C35(1.03)  LDD1521  [47]
 LDCM0283  AC23 HEK-293T C185(1.13); C293(1.12); C35(0.92)  LDD1522  [47]
 LDCM0284  AC24 HEK-293T C185(1.27); C293(1.22); C35(1.04)  LDD1523  [47]
 LDCM0285  AC25 HEK-293T C185(1.02); C293(0.98); C35(0.79)  LDD1524  [47]
 LDCM0286  AC26 HEK-293T C185(1.07); C293(1.11); C35(0.80)  LDD1525  [47]
 LDCM0287  AC27 HEK-293T C185(1.11); C293(1.11)  LDD1526  [47]
 LDCM0288  AC28 HEK-293T C185(1.07); C293(1.14); C35(1.03)  LDD1527  [47]
 LDCM0289  AC29 HEK-293T C185(1.06); C293(1.00); C35(0.87)  LDD1528  [47]
 LDCM0290  AC3 HEK-293T C185(1.03); C293(1.04)  LDD1529  [47]
 LDCM0291  AC30 HEK-293T C185(1.17); C293(1.20); C35(1.09)  LDD1530  [47]
 LDCM0292  AC31 HEK-293T C185(1.18); C293(1.15); C35(0.86)  LDD1531  [47]
 LDCM0293  AC32 HEK-293T C185(1.22); C293(1.04); C35(0.89)  LDD1532  [47]
 LDCM0294  AC33 HEK-293T C185(1.18); C293(1.02); C35(0.88)  LDD1533  [47]
 LDCM0295  AC34 HEK-293T C185(1.13); C293(1.19); C35(0.87)  LDD1534  [47]
 LDCM0296  AC35 HEK-293T C185(1.16); C293(1.09)  LDD1535  [47]
 LDCM0297  AC36 HEK-293T C185(1.31); C293(1.18); C35(1.05)  LDD1536  [47]
 LDCM0298  AC37 HEK-293T C185(1.03); C293(1.11); C35(1.06)  LDD1537  [47]
 LDCM0299  AC38 HEK-293T C185(1.17); C293(1.14); C35(1.02)  LDD1538  [47]
 LDCM0300  AC39 HEK-293T C185(1.21); C293(1.12); C35(0.97)  LDD1539  [47]
 LDCM0301  AC4 HEK-293T C185(1.21); C293(1.17); C35(1.04)  LDD1540  [47]
 LDCM0302  AC40 HEK-293T C185(1.17); C293(1.06); C35(0.97)  LDD1541  [47]
 LDCM0303  AC41 HEK-293T C185(1.02); C293(1.00); C35(0.94)  LDD1542  [47]
 LDCM0304  AC42 HEK-293T C185(1.24); C293(1.16); C35(0.90)  LDD1543  [47]
 LDCM0305  AC43 HEK-293T C185(1.00); C293(1.10)  LDD1544  [47]
 LDCM0306  AC44 HEK-293T C185(1.09); C293(1.13); C35(0.95)  LDD1545  [47]
 LDCM0307  AC45 HEK-293T C185(1.02); C293(1.10); C35(0.98)  LDD1546  [47]
 LDCM0308  AC46 HEK-293T C185(1.29); C293(1.10); C35(1.19)  LDD1547  [47]
 LDCM0309  AC47 HEK-293T C185(1.09); C293(1.17); C35(0.93)  LDD1548  [47]
 LDCM0310  AC48 HEK-293T C185(1.05); C293(1.13); C35(1.08)  LDD1549  [47]
 LDCM0311  AC49 HEK-293T C185(1.04); C293(1.04); C35(0.87)  LDD1550  [47]
 LDCM0312  AC5 HEK-293T C185(1.01); C293(1.07); C35(0.93)  LDD1551  [47]
 LDCM0313  AC50 HEK-293T C185(1.24); C293(1.24); C35(0.87)  LDD1552  [47]
 LDCM0314  AC51 HEK-293T C185(1.02); C293(1.17)  LDD1553  [47]
 LDCM0315  AC52 HEK-293T C185(1.08); C293(1.12); C35(0.96)  LDD1554  [47]
 LDCM0316  AC53 HEK-293T C185(1.02); C293(1.05); C35(0.89)  LDD1555  [47]
 LDCM0317  AC54 HEK-293T C185(1.12); C293(1.04); C35(1.00)  LDD1556  [47]
 LDCM0318  AC55 HEK-293T C185(1.06); C293(1.09); C35(0.94)  LDD1557  [47]
 LDCM0319  AC56 HEK-293T C185(1.02); C293(1.11); C35(1.06)  LDD1558  [47]
 LDCM0320  AC57 HEK-293T C185(0.91); C293(1.12); C35(1.10)  LDD1559  [47]
 LDCM0321  AC58 HEK-293T C185(1.07); C293(1.32); C35(1.10)  LDD1560  [47]
 LDCM0322  AC59 HEK-293T C185(0.97); C293(1.19)  LDD1561  [47]
 LDCM0323  AC6 HEK-293T C185(1.05); C293(1.06); C35(0.98)  LDD1562  [47]
 LDCM0324  AC60 HEK-293T C185(1.15); C293(1.19); C35(1.03)  LDD1563  [47]
 LDCM0325  AC61 HEK-293T C185(0.92); C293(1.10); C35(1.20)  LDD1564  [47]
 LDCM0326  AC62 HEK-293T C185(1.01); C293(1.21); C35(1.09)  LDD1565  [47]
 LDCM0327  AC63 HEK-293T C185(1.06); C293(1.19); C35(1.04)  LDD1566  [47]
 LDCM0328  AC64 HEK-293T C185(1.14); C293(1.31); C35(1.04)  LDD1567  [47]
 LDCM0334  AC7 HEK-293T C185(1.06); C293(1.14); C35(0.91)  LDD1568  [47]
 LDCM0345  AC8 HEK-293T C185(1.14); C293(1.13); C35(1.03)  LDD1569  [47]
 LDCM0545  Acetamide MDA-MB-231 C131(0.52)  LDD2138  [10]
 LDCM0520  AKOS000195272 MDA-MB-231 C131(0.68)  LDD2113  [10]
 LDCM0248  AKOS034007472 HEK-293T C185(0.88); C293(1.04); C35(1.07)  LDD1511  [47]
 LDCM0356  AKOS034007680 HEK-293T C185(0.96); C293(0.96); C35(0.89)  LDD1570  [47]
 LDCM0275  AKOS034007705 HEK-293T C185(1.02); C293(1.09); C35(1.07)  LDD1514  [47]
 LDCM0156  Aniline NCI-H1299 N.A.  LDD0404  [39]
 LDCM0498  BS-3668 MDA-MB-231 C131(0.60)  LDD2091  [10]
 LDCM0630  CCW28-3 231MFP C293(1.21); C163(1.16)  LDD2214  [48]
 LDCM0108  Chloroacetamide HeLa H215(0.00); C163(0.00); H271(0.00); C131(0.00)  LDD0222  [37]
 LDCM0632  CL-Sc Hep-G2 C163(1.18); C163(1.08)  LDD2227  [28]
 LDCM0367  CL1 HEK-293T C185(1.07); C293(1.18)  LDD1571  [47]
 LDCM0368  CL10 HEK-293T C185(1.15); C293(0.72); C35(0.81)  LDD1572  [47]
 LDCM0369  CL100 HEK-293T C185(1.06); C293(1.11)  LDD1573  [47]
 LDCM0370  CL101 HEK-293T C185(0.98); C293(1.08)  LDD1574  [47]
 LDCM0371  CL102 HEK-293T C185(1.08); C293(1.07); C35(0.98)  LDD1575  [47]
 LDCM0372  CL103 HEK-293T C185(1.12); C293(1.13); C35(0.90)  LDD1576  [47]
 LDCM0373  CL104 HEK-293T C185(1.05); C293(1.17)  LDD1577  [47]
 LDCM0374  CL105 HEK-293T C185(1.06); C293(1.13)  LDD1578  [47]
 LDCM0375  CL106 HEK-293T C185(1.07); C293(1.07); C35(0.92)  LDD1579  [47]
 LDCM0376  CL107 HEK-293T C185(1.09); C293(1.20); C35(0.85)  LDD1580  [47]
 LDCM0377  CL108 HEK-293T C185(1.15); C293(1.16)  LDD1581  [47]
 LDCM0378  CL109 HEK-293T C185(1.06); C293(1.14)  LDD1582  [47]
 LDCM0379  CL11 HEK-293T C185(0.89); C293(0.99); C35(1.03)  LDD1583  [47]
 LDCM0380  CL110 HEK-293T C185(0.99); C293(1.03); C35(0.90)  LDD1584  [47]
 LDCM0381  CL111 HEK-293T C185(1.07); C293(1.08); C35(0.87)  LDD1585  [47]
 LDCM0382  CL112 HEK-293T C185(1.16); C293(1.07)  LDD1586  [47]
 LDCM0383  CL113 HEK-293T C185(1.09); C293(1.11)  LDD1587  [47]
 LDCM0384  CL114 HEK-293T C185(1.14); C293(1.16); C35(0.98)  LDD1588  [47]
 LDCM0385  CL115 HEK-293T C185(1.32); C293(1.15); C35(0.99)  LDD1589  [47]
 LDCM0386  CL116 HEK-293T C185(1.14); C293(1.11)  LDD1590  [47]
 LDCM0387  CL117 HEK-293T C185(1.03); C293(1.16)  LDD1591  [47]
 LDCM0388  CL118 HEK-293T C185(1.06); C293(1.11); C35(1.09)  LDD1592  [47]
 LDCM0389  CL119 HEK-293T C185(1.28); C293(1.18); C35(0.84)  LDD1593  [47]
 LDCM0390  CL12 HEK-293T C185(1.04); C293(0.98); C35(1.24)  LDD1594  [47]
 LDCM0391  CL120 HEK-293T C185(1.10); C293(1.22)  LDD1595  [47]
 LDCM0392  CL121 HEK-293T C185(1.00); C293(1.17)  LDD1596  [47]
 LDCM0393  CL122 HEK-293T C185(0.94); C293(1.09); C35(1.05)  LDD1597  [47]
 LDCM0394  CL123 HEK-293T C185(1.02); C293(1.09); C35(0.95)  LDD1598  [47]
 LDCM0395  CL124 HEK-293T C185(0.90); C293(1.05)  LDD1599  [47]
 LDCM0396  CL125 HEK-293T C185(0.75); C293(1.45)  LDD1600  [47]
 LDCM0397  CL126 HEK-293T C185(0.91); C293(1.24); C35(1.25)  LDD1601  [47]
 LDCM0398  CL127 HEK-293T C185(0.88); C293(1.31); C35(1.13)  LDD1602  [47]
 LDCM0399  CL128 HEK-293T C185(0.91); C293(1.23)  LDD1603  [47]
 LDCM0400  CL13 HEK-293T C185(0.73); C293(0.89)  LDD1604  [47]
 LDCM0401  CL14 HEK-293T C185(1.10); C293(1.10); C35(0.94)  LDD1605  [47]
 LDCM0402  CL15 HEK-293T C185(0.77); C293(0.87); C35(1.10)  LDD1606  [47]
 LDCM0403  CL16 HEK-293T C185(0.94); C293(1.22)  LDD1607  [47]
 LDCM0404  CL17 HEK-293T C185(0.67); C293(0.72); C35(0.86)  LDD1608  [47]
 LDCM0405  CL18 HEK-293T C185(1.00); C293(1.05); C35(1.00)  LDD1609  [47]
 LDCM0406  CL19 HEK-293T C185(0.65); C293(0.87)  LDD1610  [47]
 LDCM0407  CL2 HEK-293T C185(0.91); C293(0.91); C35(0.95)  LDD1611  [47]
 LDCM0408  CL20 HEK-293T C185(0.77); C293(0.86); C35(1.11)  LDD1612  [47]
 LDCM0409  CL21 HEK-293T C185(0.86); C293(0.86); C35(0.86)  LDD1613  [47]
 LDCM0410  CL22 HEK-293T C185(0.81); C293(0.74); C35(1.06)  LDD1614  [47]
 LDCM0411  CL23 HEK-293T C185(0.86); C293(0.98); C35(1.07)  LDD1615  [47]
 LDCM0412  CL24 HEK-293T C185(0.85); C293(0.82); C35(1.10)  LDD1616  [47]
 LDCM0413  CL25 HEK-293T C185(0.79); C293(1.03)  LDD1617  [47]
 LDCM0414  CL26 HEK-293T C185(0.91); C293(0.99); C35(1.01)  LDD1618  [47]
 LDCM0415  CL27 HEK-293T C185(1.00); C293(1.08); C35(0.90)  LDD1619  [47]
 LDCM0416  CL28 HEK-293T C185(0.92); C293(0.98)  LDD1620  [47]
 LDCM0417  CL29 HEK-293T C185(0.92); C293(0.93); C35(0.84)  LDD1621  [47]
 LDCM0418  CL3 HEK-293T C185(0.90); C293(1.06); C35(0.95)  LDD1622  [47]
 LDCM0419  CL30 HEK-293T C185(0.95); C293(0.95); C35(1.03)  LDD1623  [47]
 LDCM0420  CL31 HEK-293T C185(0.69); C293(0.85)  LDD1624  [47]
 LDCM0421  CL32 HEK-293T C185(0.74); C293(0.90); C35(1.05)  LDD1625  [47]
 LDCM0422  CL33 HEK-293T C185(0.66); C293(0.76); C35(0.99)  LDD1626  [47]
 LDCM0423  CL34 HEK-293T C185(0.82); C293(0.75); C35(0.96)  LDD1627  [47]
 LDCM0424  CL35 HEK-293T C185(0.88); C293(1.08); C35(0.96)  LDD1628  [47]
 LDCM0425  CL36 HEK-293T C185(0.93); C293(0.91); C35(1.11)  LDD1629  [47]
 LDCM0426  CL37 HEK-293T C185(0.81); C293(1.14)  LDD1630  [47]
 LDCM0428  CL39 HEK-293T C185(1.07); C293(1.09); C35(0.79)  LDD1632  [47]
 LDCM0429  CL4 HEK-293T C185(0.82); C293(0.97)  LDD1633  [47]
 LDCM0430  CL40 HEK-293T C185(1.07); C293(1.03)  LDD1634  [47]
 LDCM0431  CL41 HEK-293T C185(1.01); C293(0.98); C35(0.85)  LDD1635  [47]
 LDCM0432  CL42 HEK-293T C185(0.83); C293(0.98); C35(0.94)  LDD1636  [47]
 LDCM0433  CL43 HEK-293T C185(0.92); C293(1.01)  LDD1637  [47]
 LDCM0434  CL44 HEK-293T C185(0.91); C293(0.91); C35(1.06)  LDD1638  [47]
 LDCM0435  CL45 HEK-293T C185(0.77); C293(0.83); C35(0.98)  LDD1639  [47]
 LDCM0436  CL46 HEK-293T C185(1.01); C293(0.91); C35(0.97)  LDD1640  [47]
 LDCM0437  CL47 HEK-293T C185(0.97); C293(1.08); C35(1.12)  LDD1641  [47]
 LDCM0438  CL48 HEK-293T C185(0.92); C293(0.91); C35(1.39)  LDD1642  [47]
 LDCM0439  CL49 HEK-293T C185(0.78); C293(1.20)  LDD1643  [47]
 LDCM0440  CL5 HEK-293T C185(0.61); C293(0.77); C35(0.98)  LDD1644  [47]
 LDCM0441  CL50 HEK-293T C185(1.00); C293(1.03); C35(0.87)  LDD1645  [47]
 LDCM0443  CL52 HEK-293T C185(0.96); C293(0.94)  LDD1646  [47]
 LDCM0444  CL53 HEK-293T C185(0.94); C293(0.86); C35(0.92)  LDD1647  [47]
 LDCM0445  CL54 HEK-293T C185(0.94); C293(0.90); C35(0.84)  LDD1648  [47]
 LDCM0446  CL55 HEK-293T C185(1.01); C293(0.95)  LDD1649  [47]
 LDCM0447  CL56 HEK-293T C185(0.88); C293(0.97); C35(1.24)  LDD1650  [47]
 LDCM0448  CL57 HEK-293T C185(0.81); C293(0.80); C35(0.89)  LDD1651  [47]
 LDCM0449  CL58 HEK-293T C185(0.89); C293(0.77); C35(0.96)  LDD1652  [47]
 LDCM0450  CL59 HEK-293T C185(0.84); C293(1.08); C35(1.01)  LDD1653  [47]
 LDCM0451  CL6 HEK-293T C185(0.72); C293(0.95); C35(0.83)  LDD1654  [47]
 LDCM0452  CL60 HEK-293T C185(1.00); C293(0.90); C35(1.33)  LDD1655  [47]
 LDCM0453  CL61 HEK-293T C185(0.83); C293(1.31)  LDD1656  [47]
 LDCM0454  CL62 HEK-293T C185(1.07); C293(1.09); C35(1.11)  LDD1657  [47]
 LDCM0455  CL63 HEK-293T C185(1.04); C293(1.12); C35(0.89)  LDD1658  [47]
 LDCM0456  CL64 HEK-293T C185(0.96); C293(0.99)  LDD1659  [47]
 LDCM0457  CL65 HEK-293T C185(0.96); C293(0.97); C35(0.94)  LDD1660  [47]
 LDCM0458  CL66 HEK-293T C185(0.93); C293(0.93); C35(0.94)  LDD1661  [47]
 LDCM0459  CL67 HEK-293T C185(0.99); C293(1.00)  LDD1662  [47]
 LDCM0460  CL68 HEK-293T C185(0.90); C293(1.00); C35(1.01)  LDD1663  [47]
 LDCM0461  CL69 HEK-293T C185(0.70); C293(0.85); C35(1.26)  LDD1664  [47]
 LDCM0462  CL7 HEK-293T C185(0.66); C293(0.86)  LDD1665  [47]
 LDCM0463  CL70 HEK-293T C185(0.99); C293(0.90); C35(1.06)  LDD1666  [47]
 LDCM0464  CL71 HEK-293T C185(0.87); C293(1.08); C35(1.06)  LDD1667  [47]
 LDCM0465  CL72 HEK-293T C185(0.94); C293(0.87); C35(1.05)  LDD1668  [47]
 LDCM0466  CL73 HEK-293T C185(0.95); C293(1.21)  LDD1669  [47]
 LDCM0467  CL74 HEK-293T C185(1.00); C293(1.23); C35(1.05)  LDD1670  [47]
 LDCM0469  CL76 HEK-293T C185(0.89); C293(0.99)  LDD1672  [47]
 LDCM0470  CL77 HEK-293T C185(0.83); C293(0.87); C35(0.82)  LDD1673  [47]
 LDCM0471  CL78 HEK-293T C185(0.94); C293(1.04); C35(0.81)  LDD1674  [47]
 LDCM0472  CL79 HEK-293T C185(0.83); C293(1.08)  LDD1675  [47]
 LDCM0473  CL8 HEK-293T C185(0.68); C293(0.85); C35(1.01)  LDD1676  [47]
 LDCM0474  CL80 HEK-293T C185(0.88); C293(1.02); C35(1.19)  LDD1677  [47]
 LDCM0475  CL81 HEK-293T C185(0.72); C293(0.88); C35(0.98)  LDD1678  [47]
 LDCM0476  CL82 HEK-293T C185(1.00); C293(1.00); C35(1.17)  LDD1679  [47]
 LDCM0477  CL83 HEK-293T C185(0.92); C293(1.16); C35(0.94)  LDD1680  [47]
 LDCM0478  CL84 HEK-293T C185(0.89); C293(1.05); C35(1.21)  LDD1681  [47]
 LDCM0479  CL85 HEK-293T C185(0.84); C293(1.37)  LDD1682  [47]
 LDCM0480  CL86 HEK-293T C185(0.78); C293(1.27); C35(1.24)  LDD1683  [47]
 LDCM0481  CL87 HEK-293T C185(0.76); C293(1.17); C35(1.16)  LDD1684  [47]
 LDCM0482  CL88 HEK-293T C185(0.74); C293(1.09)  LDD1685  [47]
 LDCM0483  CL89 HEK-293T C185(0.64); C293(1.01); C35(1.00)  LDD1686  [47]
 LDCM0484  CL9 HEK-293T C185(0.78); C293(0.83); C35(1.10)  LDD1687  [47]
 LDCM0485  CL90 HEK-293T C185(0.69); C293(0.88); C35(0.83)  LDD1688  [47]
 LDCM0486  CL91 HEK-293T C185(0.59); C293(1.05)  LDD1689  [47]
 LDCM0487  CL92 HEK-293T C185(0.79); C293(0.98); C35(1.17)  LDD1690  [47]
 LDCM0488  CL93 HEK-293T C185(0.74); C293(0.94); C35(1.13)  LDD1691  [47]
 LDCM0489  CL94 HEK-293T C185(0.90); C293(1.00); C35(1.25)  LDD1692  [47]
 LDCM0490  CL95 HEK-293T C185(0.78); C293(0.90); C35(0.97)  LDD1693  [47]
 LDCM0491  CL96 HEK-293T C185(0.65); C293(1.06); C35(1.36)  LDD1694  [47]
 LDCM0492  CL97 HEK-293T C185(0.88); C293(1.07)  LDD1695  [47]
 LDCM0493  CL98 HEK-293T C185(1.14); C293(1.04); C35(0.82)  LDD1696  [47]
 LDCM0494  CL99 HEK-293T C185(1.14); C293(1.16); C35(0.84)  LDD1697  [47]
 LDCM0634  CY-0357 Hep-G2 C163(1.13)  LDD2228  [28]
 LDCM0495  E2913 HEK-293T C185(1.08); C293(1.09); C35(0.80)  LDD1698  [47]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C131(2.07)  LDD1702  [10]
 LDCM0175  Ethacrynic acid HeLa C185(2.70); C163(1.27)  LDD2210  [18]
 LDCM0625  F8 Ramos C163(0.91); C293(0.34); C185(0.08)  LDD2187  [49]
 LDCM0572  Fragment10 Ramos C163(0.49); C293(0.52)  LDD2189  [49]
 LDCM0573  Fragment11 Ramos C163(0.01); C293(0.18); C185(0.08)  LDD2190  [49]
 LDCM0574  Fragment12 Ramos C163(0.39); C293(0.31)  LDD2191  [49]
 LDCM0575  Fragment13 Ramos C163(0.82); C293(0.47)  LDD2192  [49]
 LDCM0576  Fragment14 Ramos C163(0.74); C293(1.01); C185(1.32)  LDD2193  [49]
 LDCM0579  Fragment20 Ramos C163(0.33); C293(0.33)  LDD2194  [49]
 LDCM0580  Fragment21 Ramos C163(0.98); C293(0.74)  LDD2195  [49]
 LDCM0582  Fragment23 Ramos C163(0.92); C293(0.73)  LDD2196  [49]
 LDCM0578  Fragment27 Ramos C163(0.95); C293(0.67)  LDD2197  [49]
 LDCM0586  Fragment28 Ramos C163(0.63); C293(0.48); C185(0.22)  LDD2198  [49]
 LDCM0588  Fragment30 Ramos C163(1.10); C293(0.65)  LDD2199  [49]
 LDCM0589  Fragment31 Ramos C163(1.15); C293(0.76)  LDD2200  [49]
 LDCM0590  Fragment32 Ramos C163(0.40); C293(0.30)  LDD2201  [49]
 LDCM0468  Fragment33 HEK-293T C185(0.99); C293(1.12); C35(0.94)  LDD1671  [47]
 LDCM0596  Fragment38 Ramos C163(1.01); C293(0.45)  LDD2203  [49]
 LDCM0566  Fragment4 Ramos C163(0.68); C293(0.38); C185(0.32)  LDD2184  [49]
 LDCM0427  Fragment51 HEK-293T C185(1.12); C293(1.07); C35(0.80)  LDD1631  [47]
 LDCM0610  Fragment52 Ramos C163(0.91); C293(0.65)  LDD2204  [49]
 LDCM0614  Fragment56 Ramos C163(1.23); C293(0.86)  LDD2205  [49]
 LDCM0569  Fragment7 Ramos C163(0.48); C293(0.59); C185(0.65)  LDD2186  [49]
 LDCM0571  Fragment9 Ramos C163(0.45); C293(0.40)  LDD2188  [49]
 LDCM0116  HHS-0101 DM93 Y127(0.74); Y83(0.78); Y10(0.78); Y239(0.83)  LDD0264  [20]
 LDCM0117  HHS-0201 DM93 Y127(0.57); Y10(0.72); Y145(0.78); Y247(0.82)  LDD0265  [20]
 LDCM0118  HHS-0301 DM93 Y127(0.63); Y247(0.66); Y10(0.76); Y145(0.80)  LDD0266  [20]
 LDCM0119  HHS-0401 DM93 Y127(0.71); Y145(0.84); Y83(0.84); Y10(0.85)  LDD0267  [20]
 LDCM0120  HHS-0701 DM93 Y127(0.50); Y145(0.73); Y10(0.82); Y83(0.92)  LDD0268  [20]
 LDCM0107  IAA HeLa H215(0.00); H271(0.00); C131(0.00); C35(0.00)  LDD0221  [37]
 LDCM0123  JWB131 DM93 Y10(0.84); Y127(0.96); Y145(1.12); Y172(0.79)  LDD0285  [19]
 LDCM0124  JWB142 DM93 Y10(0.69); Y127(1.01); Y145(1.31); Y172(0.40)  LDD0286  [19]
 LDCM0125  JWB146 DM93 Y10(0.88); Y127(0.96); Y145(1.04); Y172(0.91)  LDD0287  [19]
 LDCM0126  JWB150 DM93 Y10(3.08); Y127(3.49); Y145(4.26); Y172(2.33)  LDD0288  [19]
 LDCM0127  JWB152 DM93 Y10(1.98); Y127(2.16); Y145(3.27); Y172(1.75)  LDD0289  [19]
 LDCM0128  JWB198 DM93 Y10(1.23); Y127(1.56); Y145(0.24); Y172(1.00)  LDD0290  [19]
 LDCM0129  JWB202 DM93 Y10(0.59); Y127(1.04); Y145(0.78); Y172(0.55)  LDD0291  [19]
 LDCM0130  JWB211 DM93 Y10(0.92); Y127(1.09); Y145(0.94); Y172(0.82)  LDD0292  [19]
 LDCM0179  JZ128 PC-3 C293(0.00); C163(0.00); C131(0.00)  LDD0462  [16]
 LDCM0073  Kambe_cp3 PC-3 3.29  LDD0127  [43]
 LDCM0022  KB02 HEK-293T C185(1.10); C293(1.11)  LDD1492  [47]
 LDCM0023  KB03 HEK-293T C185(0.94); C293(0.97)  LDD1497  [47]
 LDCM0024  KB05 COLO792 C322(0.50); C64(0.99)  LDD3310  [15]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C131(1.07)  LDD2102  [10]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C131(0.74)  LDD2121  [10]
 LDCM0109  NEM HeLa H215(0.00); H271(0.00); H67(0.00); C131(0.00)  LDD0223  [37]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C131(0.75)  LDD2089  [10]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C131(1.26)  LDD2090  [10]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C131(1.28)  LDD2092  [10]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C131(1.15)  LDD2093  [10]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C131(2.59)  LDD2094  [10]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C131(0.18)  LDD2096  [10]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C131(0.69)  LDD2097  [10]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C131(0.97)  LDD2098  [10]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C131(1.05)  LDD2099  [10]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C131(0.55)  LDD2100  [10]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C131(0.69)  LDD2101  [10]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C131(0.68)  LDD2104  [10]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C131(1.63)  LDD2105  [10]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C131(0.56)  LDD2106  [10]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C131(0.88)  LDD2107  [10]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C131(0.92)  LDD2108  [10]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C131(0.60)  LDD2109  [10]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C131(0.74)  LDD2110  [10]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C131(1.05)  LDD2111  [10]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C131(0.74)  LDD2114  [10]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C131(0.54)  LDD2115  [10]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C131(0.36)  LDD2116  [10]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C131(0.38)  LDD2118  [10]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C131(2.36)  LDD2119  [10]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C131(0.81)  LDD2120  [10]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C131(0.29)  LDD2122  [10]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C131(0.96)  LDD2123  [10]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C131(0.25)  LDD2124  [10]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C131(0.88)  LDD2125  [10]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C131(0.23)  LDD2126  [10]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C131(1.04)  LDD2127  [10]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C131(0.91)  LDD2128  [10]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C131(1.15)  LDD2129  [10]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C131(0.55)  LDD2133  [10]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C131(0.48)  LDD2134  [10]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C131(1.49)  LDD2135  [10]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C131(1.12)  LDD2136  [10]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C131(1.02)  LDD2137  [10]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C131(1.89)  LDD1700  [10]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C131(0.81)  LDD2140  [10]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C131(0.53)  LDD2141  [10]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C131(0.94)  LDD2143  [10]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C131(2.63)  LDD2144  [10]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C131(0.25)  LDD2145  [10]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C131(0.88)  LDD2146  [10]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C131(2.99)  LDD2147  [10]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C131(0.51)  LDD2148  [10]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C131(0.26)  LDD2149  [10]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C131(0.53)  LDD2150  [10]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C131(0.26)  LDD2151  [10]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C131(2.42)  LDD2153  [10]
 LDCM0628  OTUB2-COV-1 HEK-293T C163(0.96); C163(0.73)  LDD2207  [50]
 LDCM0131  RA190 MM1.R C293(1.23)  LDD0304  [51]
 LDCM0021  THZ1 HeLa S3 C163(1.11); C293(1.05); C185(0.94)  LDD0460  [16]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock cognate 71 kDa protein (HSPA8) Heat shock protein 70 family P11142
L-lactate dehydrogenase A chain (LDHA) LDH family P00338
L-lactate dehydrogenase B chain (LDHB) LDH family P07195

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nadh Small molecular drug DB00157
Nicotinamide Small molecular drug DB02701
Stiripentol Small molecular drug DB09118
Artenimol . DB11638
Copper . DB09130
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dcr-phxc Small interfering RNA DZ8DF0
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Oxamic Acid Small molecular drug DB03940
Etheno-nad . DB02483

References

1 Development of Novel Irreversible Pyruvate Kinase M2 Inhibitors. J Med Chem. 2019 Sep 26;62(18):8497-8510. doi: 10.1021/acs.jmedchem.9b00763. Epub 2019 Sep 16.
2 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
3 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
4 Small-Molecule Activity-Based Probe for Monitoring Ubiquitin C-Terminal Hydrolase L1 (UCHL1) Activity in Live Cells and Zebrafish Embryos. J Am Chem Soc. 2020 Sep 30;142(39):16825-16841. doi: 10.1021/jacs.0c07726. Epub 2020 Sep 18.
Mass spectrometry data entry: PXD021557 , PXD015828
5 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.
6 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.
7 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
8 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.
9 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.
10 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
11 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
12 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
13 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
14 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.
15 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
16 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
17 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
18 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
19 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.
20 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.
21 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.
22 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
23 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.
24 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
25 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
26 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
27 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
28 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
29 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
30 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
31 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.
32 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
33 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
34 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
35 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
36 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
37 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.
38 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.
39 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.
40 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.
41 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
42 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
43 Mapping the protein interaction landscape for fully functionalized small-molecule probes in human cells. J Am Chem Soc. 2014 Jul 30;136(30):10777-82. doi: 10.1021/ja505517t. Epub 2014 Jul 21.
44 Evaluation of fully-functionalized diazirine tags for chemical proteomic applications. Chem Sci. 2021 May 7;12(22):7839-7847. doi: 10.1039/d1sc01360b.
Mass spectrometry data entry: PXD025652
45 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094
46 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.
47 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
48 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
49 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
50 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.
51 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.