Details of the Target

General Information of Target

Target ID LDTP05761
Target Name 5'-AMP-activated protein kinase catalytic subunit alpha-1 (PRKAA1)
Gene Name PRKAA1
Gene ID 5562
Synonyms
AMPK1; 5'-AMP-activated protein kinase catalytic subunit alpha-1; AMPK subunit alpha-1; EC 2.7.11.1; Acetyl-CoA carboxylase kinase; ACACA kinase; Hydroxymethylglutaryl-CoA reductase kinase; HMGCR kinase; EC 2.7.11.31; Tau-protein kinase PRKAA1; EC 2.7.11.26
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRRLSSWRKMATAEKQKHDGRVKIGHYILGDTLGVGTFGKVKVGKHELTGHKVAVKILNR
QKIRSLDVVGKIRREIQNLKLFRHPHIIKLYQVISTPSDIFMVMEYVSGGELFDYICKNG
RLDEKESRRLFQQILSGVDYCHRHMVVHRDLKPENVLLDAHMNAKIADFGLSNMMSDGEF
LRTSCGSPNYAAPEVISGRLYAGPEVDIWSSGVILYALLCGTLPFDDDHVPTLFKKICDG
IFYTPQYLNPSVISLLKHMLQVDPMKRATIKDIREHEWFKQDLPKYLFPEDPSYSSTMID
DEALKEVCEKFECSEEEVLSCLYNRNHQDPLAVAYHLIIDNRRIMNEAKDFYLATSPPDS
FLDDHHLTRPHPERVPFLVAETPRARHTLDELNPQKSKHQGVRKAKWHLGIRSQSRPNDI
MAEVCRAIKQLDYEWKVVNPYYLRVRRKNPVTSTYSKMSLQLYQVDSRTYLLDFRSIDDE
ITEAKSGTATPQRSGSVSNYRSCQRSDSDAEAQGKSSEVSLTSSVTSLDSSPVDLTPRPG
SHTIEFFEMCANLIKILAQ
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CAMK Ser/Thr protein kinase family, SNF1 subfamily
Subcellular location
Cytoplasm
Function
Catalytic subunit of AMP-activated protein kinase (AMPK), an energy sensor protein kinase that plays a key role in regulating cellular energy metabolism. In response to reduction of intracellular ATP levels, AMPK activates energy-producing pathways and inhibits energy-consuming processes: inhibits protein, carbohydrate and lipid biosynthesis, as well as cell growth and proliferation. AMPK acts via direct phosphorylation of metabolic enzymes, and by longer-term effects via phosphorylation of transcription regulators. Regulates lipid synthesis by phosphorylating and inactivating lipid metabolic enzymes such as ACACA, ACACB, GYS1, HMGCR and LIPE; regulates fatty acid and cholesterol synthesis by phosphorylating acetyl-CoA carboxylase (ACACA and ACACB) and hormone-sensitive lipase (LIPE) enzymes, respectively. Promotes lipolysis of lipid droplets by mediating phosphorylation of isoform 1 of CHKA (CHKalpha2). Regulates insulin-signaling and glycolysis by phosphorylating IRS1, PFKFB2 and PFKFB3. AMPK stimulates glucose uptake in muscle by increasing the translocation of the glucose transporter SLC2A4/GLUT4 to the plasma membrane, possibly by mediating phosphorylation of TBC1D4/AS160. Regulates transcription and chromatin structure by phosphorylating transcription regulators involved in energy metabolism such as CRTC2/TORC2, FOXO3, histone H2B, HDAC5, MEF2C, MLXIPL/ChREBP, EP300, HNF4A, p53/TP53, SREBF1, SREBF2 and PPARGC1A. Acts as a key regulator of glucose homeostasis in liver by phosphorylating CRTC2/TORC2, leading to CRTC2/TORC2 sequestration in the cytoplasm. In response to stress, phosphorylates 'Ser-36' of histone H2B (H2BS36ph), leading to promote transcription. Acts as a key regulator of cell growth and proliferation by phosphorylating FNIP1, TSC2, RPTOR, WDR24 and ATG1/ULK1: in response to nutrient limitation, negatively regulates the mTORC1 complex by phosphorylating RPTOR component of the mTORC1 complex and by phosphorylating and activating TSC2. Also phosphorylates and inhibits GATOR2 subunit WDR24 in response to nutrient limitation, leading to suppress glucose-mediated mTORC1 activation. In response to energetic stress, phosphorylates FNIP1, inactivating the non-canonical mTORC1 signaling, thereby promoting nuclear translocation of TFEB and TFE3, and inducing transcription of lysosomal or autophagy genes. In response to nutrient limitation, promotes autophagy by phosphorylating and activating ATG1/ULK1. In that process also activates WDR45/WIPI4. Phosphorylates CASP6, thereby preventing its autoprocessing and subsequent activation. In response to nutrient limitation, phosphorylates transcription factor FOXO3 promoting FOXO3 mitochondrial import. Also acts as a regulator of cellular polarity by remodeling the actin cytoskeleton; probably by indirectly activating myosin. AMPK also acts as a regulator of circadian rhythm by mediating phosphorylation of CRY1, leading to destabilize it. May regulate the Wnt signaling pathway by phosphorylating CTNNB1, leading to stabilize it. Also has tau-protein kinase activity: in response to amyloid beta A4 protein (APP) exposure, activated by CAMKK2, leading to phosphorylation of MAPT/TAU; however the relevance of such data remains unclear in vivo. Also phosphorylates CFTR, EEF2K, KLC1, NOS3 and SLC12A1. Regulates hepatic lipogenesis. Activated via SIRT3, represses sterol regulatory element-binding protein (SREBP) transcriptional activities and ATP-consuming lipogenesis to restore cellular energy balance.
Uniprot ID
Q13131
Ensemble ID
ENST00000354209.7
HGNC ID
HGNC:9376
ChEMBL ID
CHEMBL4045

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HS578T SNV: p.R447M DBIA    Probe Info 
LN229 SNV: p.P450A DBIA    Probe Info 
P31FUJ SNV: p.H142R DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 30 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
A-EBA
 Probe Info  		17.47  LDD0215  [2]
TH211
 Probe Info  		Y190(9.51); Y247(5.75)  LDD0260  [3]
ONAyne
 Probe Info  		K398(5.26)  LDD0275  [4]
OPA-S-S-alkyne
 Probe Info  		K56(14.48)  LDD3494  [5]
Probe 1
 Probe Info  		Y463(18.68); Y500(12.11)  LDD3495  [6]
JZ128-DTB
 Probe Info  		N.A.  LDD0462  [7]
BTD
 Probe Info  		C425(0.24)  LDD2096  [8]
DA-P3
 Probe Info  		12.37  LDD0183  [9]
AHL-Pu-1
 Probe Info  		C238(2.25)  LDD0168  [10]
DBIA
 Probe Info  		C185(7.46)  LDD0209  [11]
HHS-475
 Probe Info  		Y27(0.58); Y243(1.16)  LDD0264  [12]
ATP probe
 Probe Info  		K40(0.00); K42(0.00)  LDD0199  [13]
4-Iodoacetamidophenylacetylene
 Probe Info  		C238(0.00); C141(0.00); C425(0.00); C185(0.00)  LDD0038  [14]
IA-alkyne
 Probe Info  		C425(0.00); C185(0.00)  LDD0032  [15]
Lodoacetamide azide
 Probe Info  		C238(0.00); C141(0.00); C425(0.00); C185(0.00)  LDD0037  [14]
ATP probe
 Probe Info  		N.A.  LDD0035  [16]
IPM
 Probe Info  		N.A.  LDD0025  [17]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [17]
NAIA_4
 Probe Info  		C238(0.00); C425(0.00)  LDD2226  [18]
TFBX
 Probe Info  		C425(0.00); C185(0.00)  LDD0027  [17]
KY-26
 Probe Info  		N.A.  LDD0301  [19]
ENE
 Probe Info  		N.A.  LDD0006  [20]
NHS
 Probe Info  		K40(0.00); K80(0.00)  LDD0010  [20]
SF
 Probe Info  		N.A.  LDD0028  [21]
STPyne
 Probe Info  		N.A.  LDD0009  [20]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [22]
Acrolein
 Probe Info  		C141(0.00); C425(0.00)  LDD0217  [23]
AOyne
 Probe Info  		15.00  LDD0443  [24]
NAIA_5
 Probe Info  		C141(0.00); C117(0.00); C425(0.00)  LDD2223  [18]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C425(1.26)  LDD2117  [8]
 LDCM0025  4SU-RNA HEK-293T C238(2.25)  LDD0168  [10]
 LDCM0026  4SU-RNA+native RNA HEK-293T C185(2.10); C238(3.53)  LDD0169  [10]
 LDCM0214  AC1 HEK-293T C425(0.89); C185(1.04); C141(1.02); C238(1.13)  LDD1507  [25]
 LDCM0215  AC10 HEK-293T C425(1.21); C185(1.06); C141(0.98); C238(1.12)  LDD1508  [25]
 LDCM0226  AC11 HEK-293T C185(1.14); C141(0.93); C238(1.07)  LDD1509  [25]
 LDCM0237  AC12 HEK-293T C425(1.14); C185(1.12); C141(1.04); C238(1.04)  LDD1510  [25]
 LDCM0259  AC14 HEK-293T C185(1.05); C141(1.07); C238(1.04)  LDD1512  [25]
 LDCM0270  AC15 HEK-293T C425(1.04); C185(1.05); C141(1.02); C238(1.09)  LDD1513  [25]
 LDCM0276  AC17 HEK-293T C425(0.92); C185(1.09); C141(1.05); C238(1.02)  LDD1515  [25]
 LDCM0277  AC18 HEK-293T C425(0.90); C185(1.19); C141(0.91); C238(1.03)  LDD1516  [25]
 LDCM0278  AC19 HEK-293T C185(1.18); C141(0.87); C238(0.83)  LDD1517  [25]
 LDCM0279  AC2 HEK-293T C425(0.99); C185(1.03); C141(1.02); C238(1.07)  LDD1518  [25]
 LDCM0280  AC20 HEK-293T C425(1.12); C185(1.13); C141(0.97); C238(1.08)  LDD1519  [25]
 LDCM0281  AC21 HEK-293T C185(1.04); C141(1.09); C238(0.97)  LDD1520  [25]
 LDCM0282  AC22 HEK-293T C185(0.96); C141(0.90); C238(1.08)  LDD1521  [25]
 LDCM0283  AC23 HEK-293T C425(1.11); C185(1.00); C141(1.07); C238(1.07)  LDD1522  [25]
 LDCM0284  AC24 HEK-293T C425(1.11); C185(0.91); C141(0.97); C238(1.09)  LDD1523  [25]
 LDCM0285  AC25 HEK-293T C425(0.94); C185(1.00); C141(0.98); C238(1.01)  LDD1524  [25]
 LDCM0286  AC26 HEK-293T C425(1.04); C185(1.02); C141(0.81); C238(1.13)  LDD1525  [25]
 LDCM0287  AC27 HEK-293T C185(1.21); C141(1.02); C238(1.04)  LDD1526  [25]
 LDCM0288  AC28 HEK-293T C425(1.08); C185(1.16); C141(1.20); C238(1.04)  LDD1527  [25]
 LDCM0289  AC29 HEK-293T C185(1.10); C141(1.03); C238(1.11)  LDD1528  [25]
 LDCM0290  AC3 HEK-293T C185(1.21); C141(0.97); C238(1.07)  LDD1529  [25]
 LDCM0291  AC30 HEK-293T C185(0.94); C141(0.90); C238(1.12)  LDD1530  [25]
 LDCM0292  AC31 HEK-293T C425(1.06); C185(1.10); C141(1.02); C238(1.03)  LDD1531  [25]
 LDCM0293  AC32 HEK-293T C425(1.03); C185(0.92); C141(1.05); C238(1.06)  LDD1532  [25]
 LDCM0294  AC33 HEK-293T C425(0.97); C185(1.09); C141(1.04); C238(1.01)  LDD1533  [25]
 LDCM0295  AC34 HEK-293T C425(0.90); C185(1.17); C141(0.98); C238(1.05)  LDD1534  [25]
 LDCM0296  AC35 HEK-293T C185(1.12); C141(1.03); C238(1.04)  LDD1535  [25]
 LDCM0297  AC36 HEK-293T C425(1.20); C185(1.04); C141(0.97); C238(0.99)  LDD1536  [25]
 LDCM0298  AC37 HEK-293T C185(1.04); C141(1.17); C238(1.07)  LDD1537  [25]
 LDCM0299  AC38 HEK-293T C185(1.02); C141(0.87); C238(0.98)  LDD1538  [25]
 LDCM0300  AC39 HEK-293T C425(1.05); C185(1.15); C141(1.06); C238(1.10)  LDD1539  [25]
 LDCM0301  AC4 HEK-293T C425(1.10); C185(1.09); C141(1.27); C238(0.99)  LDD1540  [25]
 LDCM0302  AC40 HEK-293T C425(1.08); C185(0.86); C141(1.12); C238(1.04)  LDD1541  [25]
 LDCM0303  AC41 HEK-293T C425(0.97); C185(1.07); C141(1.06); C238(1.11)  LDD1542  [25]
 LDCM0304  AC42 HEK-293T C425(1.05); C185(1.12); C141(0.99); C238(1.05)  LDD1543  [25]
 LDCM0305  AC43 HEK-293T C185(1.07); C141(0.86); C238(1.01)  LDD1544  [25]
 LDCM0306  AC44 HEK-293T C425(1.09); C185(1.02); C141(1.14); C238(1.10)  LDD1545  [25]
 LDCM0307  AC45 HEK-293T C185(1.05); C141(1.14); C238(1.01)  LDD1546  [25]
 LDCM0308  AC46 HEK-293T C185(1.00); C141(1.00); C238(1.08)  LDD1547  [25]
 LDCM0309  AC47 HEK-293T C425(1.06); C185(0.83); C141(1.03); C238(1.00)  LDD1548  [25]
 LDCM0310  AC48 HEK-293T C425(1.14); C185(0.93); C141(1.07); C238(1.12)  LDD1549  [25]
 LDCM0311  AC49 HEK-293T C425(0.92); C185(1.08); C141(1.06); C238(1.13)  LDD1550  [25]
 LDCM0312  AC5 HEK-293T C185(0.92); C141(1.06); C238(1.08)  LDD1551  [25]
 LDCM0313  AC50 HEK-293T C425(0.94); C185(1.06); C141(1.10); C238(1.14)  LDD1552  [25]
 LDCM0314  AC51 HEK-293T C185(1.28); C141(1.00); C238(1.05)  LDD1553  [25]
 LDCM0315  AC52 HEK-293T C425(1.12); C185(1.10); C141(1.07); C238(0.99)  LDD1554  [25]
 LDCM0316  AC53 HEK-293T C185(1.02); C141(1.14); C238(1.03)  LDD1555  [25]
 LDCM0317  AC54 HEK-293T C185(1.04); C141(1.01); C238(0.96)  LDD1556  [25]
 LDCM0318  AC55 HEK-293T C425(0.99); C185(1.08); C141(1.03); C238(1.06)  LDD1557  [25]
 LDCM0319  AC56 HEK-293T C425(1.06); C185(0.81); C141(0.99); C238(1.18)  LDD1558  [25]
 LDCM0320  AC57 HEK-293T C425(0.96); C185(1.12); C141(0.96); C238(0.98)  LDD1559  [25]
 LDCM0321  AC58 HEK-293T C425(1.11); C185(1.08); C141(0.90); C238(1.04)  LDD1560  [25]
 LDCM0322  AC59 HEK-293T C185(1.14); C141(0.96); C238(1.20)  LDD1561  [25]
 LDCM0323  AC6 HEK-293T C185(1.06); C141(0.94); C238(1.04)  LDD1562  [25]
 LDCM0324  AC60 HEK-293T C425(1.02); C185(1.02); C141(1.19); C238(1.00)  LDD1563  [25]
 LDCM0325  AC61 HEK-293T C185(1.05); C141(1.06); C238(1.01)  LDD1564  [25]
 LDCM0326  AC62 HEK-293T C185(1.01); C141(0.95); C238(1.10)  LDD1565  [25]
 LDCM0327  AC63 HEK-293T C425(1.01); C185(1.20); C141(1.05); C238(1.12)  LDD1566  [25]
 LDCM0328  AC64 HEK-293T C425(1.00); C185(0.84); C141(1.03); C238(1.05)  LDD1567  [25]
 LDCM0334  AC7 HEK-293T C425(1.04); C185(0.99); C141(1.12); C238(1.00)  LDD1568  [25]
 LDCM0345  AC8 HEK-293T C425(1.13); C185(0.82); C141(1.02); C238(0.94)  LDD1569  [25]
 LDCM0248  AKOS034007472 HEK-293T C185(0.96); C141(1.08); C238(1.07)  LDD1511  [25]
 LDCM0356  AKOS034007680 HEK-293T C425(0.97); C185(0.98); C141(0.92); C238(1.03)  LDD1570  [25]
 LDCM0275  AKOS034007705 HEK-293T C425(1.04); C185(0.98); C141(1.11); C238(1.18)  LDD1514  [25]
 LDCM0156  Aniline NCI-H1299 11.67  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C185(1.76); C117(1.38)  LDD2214  [26]
 LDCM0108  Chloroacetamide HeLa C141(0.00); C425(0.00)  LDD0222  [23]
 LDCM0632  CL-Sc Hep-G2 C141(1.27); C425(1.05)  LDD2227  [18]
 LDCM0367  CL1 HEK-293T C425(0.96); C185(0.89); C141(0.96); C238(1.05)  LDD1571  [25]
 LDCM0368  CL10 HEK-293T C185(1.08); C141(1.10); C238(0.88)  LDD1572  [25]
 LDCM0369  CL100 HEK-293T C425(0.99); C185(0.97); C141(1.04); C238(1.04)  LDD1573  [25]
 LDCM0370  CL101 HEK-293T C425(1.05); C185(0.98); C141(0.94); C238(0.99)  LDD1574  [25]
 LDCM0371  CL102 HEK-293T C425(1.00); C185(1.10); C141(0.94); C238(0.98)  LDD1575  [25]
 LDCM0372  CL103 HEK-293T C425(0.99); C185(0.97); C141(1.21); C238(0.98)  LDD1576  [25]
 LDCM0373  CL104 HEK-293T C425(1.14); C185(0.97); C141(0.76); C238(1.02)  LDD1577  [25]
 LDCM0374  CL105 HEK-293T C425(1.08); C185(1.07); C141(0.91); C238(1.00)  LDD1578  [25]
 LDCM0375  CL106 HEK-293T C425(1.06); C185(1.02); C141(1.19); C238(0.95)  LDD1579  [25]
 LDCM0376  CL107 HEK-293T C425(1.02); C185(1.02); C141(0.92); C238(0.93)  LDD1580  [25]
 LDCM0377  CL108 HEK-293T C425(0.98); C185(1.07); C141(0.83); C238(1.08)  LDD1581  [25]
 LDCM0378  CL109 HEK-293T C425(0.95); C185(1.01); C141(1.03); C238(1.08)  LDD1582  [25]
 LDCM0379  CL11 HEK-293T C425(1.21); C185(0.91); C141(1.17); C238(1.00)  LDD1583  [25]
 LDCM0380  CL110 HEK-293T C425(0.99); C185(1.06); C141(0.92); C238(0.93)  LDD1584  [25]
 LDCM0381  CL111 HEK-293T C425(0.93); C185(1.04); C141(0.95); C238(0.93)  LDD1585  [25]
 LDCM0382  CL112 HEK-293T C425(1.18); C185(1.07); C141(0.92); C238(0.96)  LDD1586  [25]
 LDCM0383  CL113 HEK-293T C425(1.03); C185(1.01); C141(1.06); C238(0.97)  LDD1587  [25]
 LDCM0384  CL114 HEK-293T C425(1.07); C185(1.02); C141(1.00); C238(0.87)  LDD1588  [25]
 LDCM0385  CL115 HEK-293T C425(0.98); C185(1.07); C141(0.96); C238(0.97)  LDD1589  [25]
 LDCM0386  CL116 HEK-293T C425(1.09); C185(0.98); C141(0.97); C238(0.94)  LDD1590  [25]
 LDCM0387  CL117 HEK-293T C425(0.88); C185(1.03); C141(0.93); C238(1.01)  LDD1591  [25]
 LDCM0388  CL118 HEK-293T C425(1.12); C185(1.05); C141(0.83); C238(0.94)  LDD1592  [25]
 LDCM0389  CL119 HEK-293T C425(0.92); C185(1.04); C141(1.28); C238(0.99)  LDD1593  [25]
 LDCM0390  CL12 HEK-293T C425(1.16); C185(0.94); C141(1.11); C238(1.11)  LDD1594  [25]
 LDCM0391  CL120 HEK-293T C425(1.17); C185(1.09); C141(0.79); C238(1.01)  LDD1595  [25]
 LDCM0392  CL121 HEK-293T C425(1.03); C185(1.01); C141(1.10); C238(1.02)  LDD1596  [25]
 LDCM0393  CL122 HEK-293T C425(1.12); C185(1.03); C141(1.04); C238(0.95)  LDD1597  [25]
 LDCM0394  CL123 HEK-293T C425(1.03); C185(0.93); C141(0.94); C238(0.97)  LDD1598  [25]
 LDCM0395  CL124 HEK-293T C425(1.14); C185(1.05); C141(0.83); C238(1.11)  LDD1599  [25]
 LDCM0396  CL125 HEK-293T C425(0.94); C185(1.08); C141(1.01); C238(1.10)  LDD1600  [25]
 LDCM0397  CL126 HEK-293T C425(0.98); C185(1.03); C141(1.04); C238(1.02)  LDD1601  [25]
 LDCM0398  CL127 HEK-293T C425(0.98); C185(1.07); C141(1.05); C238(1.00)  LDD1602  [25]
 LDCM0399  CL128 HEK-293T C425(1.02); C185(0.93); C141(0.74); C238(1.13)  LDD1603  [25]
 LDCM0400  CL13 HEK-293T C425(1.00); C185(1.12); C141(0.31); C238(1.06)  LDD1604  [25]
 LDCM0401  CL14 HEK-293T C425(1.13); C185(1.04); C141(0.92); C238(0.90)  LDD1605  [25]
 LDCM0402  CL15 HEK-293T C425(1.02); C185(1.31); C141(1.19); C238(0.96)  LDD1606  [25]
 LDCM0403  CL16 HEK-293T C425(1.18); C185(1.06); C141(0.86); C238(1.03)  LDD1607  [25]
 LDCM0404  CL17 HEK-293T C425(0.99); C185(1.17); C141(0.78); C238(0.89)  LDD1608  [25]
 LDCM0405  CL18 HEK-293T C425(1.17); C185(1.15); C141(1.09); C238(1.03)  LDD1609  [25]
 LDCM0406  CL19 HEK-293T C185(0.87); C141(0.83); C238(0.97)  LDD1610  [25]
 LDCM0407  CL2 HEK-293T C425(1.11); C185(1.06); C141(0.89); C238(1.04)  LDD1611  [25]
 LDCM0408  CL20 HEK-293T C425(1.09); C185(1.17); C141(1.19); C238(0.97)  LDD1612  [25]
 LDCM0409  CL21 HEK-293T C185(1.14); C141(1.20); C238(1.04)  LDD1613  [25]
 LDCM0410  CL22 HEK-293T C185(1.01); C141(0.97); C238(0.94)  LDD1614  [25]
 LDCM0411  CL23 HEK-293T C425(1.10); C185(0.99); C141(1.16); C238(0.95)  LDD1615  [25]
 LDCM0412  CL24 HEK-293T C425(1.25); C185(1.00); C141(1.10); C238(1.21)  LDD1616  [25]
 LDCM0413  CL25 HEK-293T C425(1.04); C185(1.16); C141(0.95); C238(1.02)  LDD1617  [25]
 LDCM0414  CL26 HEK-293T C425(0.95); C185(1.01); C141(1.05); C238(0.89)  LDD1618  [25]
 LDCM0415  CL27 HEK-293T C425(1.13); C185(1.01); C141(0.97); C238(0.95)  LDD1619  [25]
 LDCM0416  CL28 HEK-293T C425(1.15); C185(0.89); C141(0.84); C238(1.04)  LDD1620  [25]
 LDCM0417  CL29 HEK-293T C425(0.94); C185(1.19); C141(1.04); C238(1.30)  LDD1621  [25]
 LDCM0418  CL3 HEK-293T C425(1.09); C185(0.97); C141(0.97); C238(1.02)  LDD1622  [25]
 LDCM0419  CL30 HEK-293T C425(1.18); C185(1.04); C141(0.99); C238(1.01)  LDD1623  [25]
 LDCM0420  CL31 HEK-293T C185(1.04); C141(0.90); C238(0.92)  LDD1624  [25]
 LDCM0421  CL32 HEK-293T C425(1.20); C185(1.04); C141(1.11); C238(0.93)  LDD1625  [25]
 LDCM0422  CL33 HEK-293T C185(1.10); C141(1.39); C238(0.93)  LDD1626  [25]
 LDCM0423  CL34 HEK-293T C185(1.02); C141(0.89); C238(0.86)  LDD1627  [25]
 LDCM0424  CL35 HEK-293T C425(1.04); C185(1.04); C141(1.18); C238(0.92)  LDD1628  [25]
 LDCM0425  CL36 HEK-293T C425(1.16); C185(0.81); C141(0.99); C238(1.00)  LDD1629  [25]
 LDCM0426  CL37 HEK-293T C425(1.05); C185(0.98); C141(0.95); C238(1.04)  LDD1630  [25]
 LDCM0428  CL39 HEK-293T C425(1.00); C185(0.96); C141(1.07); C238(0.91)  LDD1632  [25]
 LDCM0429  CL4 HEK-293T C425(0.98); C185(1.03); C141(0.87); C238(1.10)  LDD1633  [25]
 LDCM0430  CL40 HEK-293T C425(1.18); C185(1.00); C141(0.79); C238(1.03)  LDD1634  [25]
 LDCM0431  CL41 HEK-293T C425(1.02); C185(1.02); C141(1.06); C238(1.02)  LDD1635  [25]
 LDCM0432  CL42 HEK-293T C425(1.11); C185(1.00); C141(0.94); C238(0.94)  LDD1636  [25]
 LDCM0433  CL43 HEK-293T C185(0.81); C141(0.92); C238(1.09)  LDD1637  [25]
 LDCM0434  CL44 HEK-293T C425(1.32); C185(1.16); C141(1.14); C238(0.91)  LDD1638  [25]
 LDCM0435  CL45 HEK-293T C185(1.06); C141(1.11); C238(0.88)  LDD1639  [25]
 LDCM0436  CL46 HEK-293T C185(0.95); C141(0.94); C238(0.84)  LDD1640  [25]
 LDCM0437  CL47 HEK-293T C425(1.09); C185(1.06); C141(1.09); C238(0.95)  LDD1641  [25]
 LDCM0438  CL48 HEK-293T C425(1.22); C185(0.95); C141(1.08); C238(1.29)  LDD1642  [25]
 LDCM0439  CL49 HEK-293T C425(0.92); C185(0.93); C141(0.94); C238(1.14)  LDD1643  [25]
 LDCM0440  CL5 HEK-293T C425(0.97); C185(1.04); C141(1.10); C238(1.14)  LDD1644  [25]
 LDCM0441  CL50 HEK-293T C425(1.12); C185(0.98); C141(0.91); C238(0.92)  LDD1645  [25]
 LDCM0443  CL52 HEK-293T C425(1.11); C185(1.01); C141(0.91); C238(0.99)  LDD1646  [25]
 LDCM0444  CL53 HEK-293T C425(1.00); C185(1.04); C141(1.05); C238(1.01)  LDD1647  [25]
 LDCM0445  CL54 HEK-293T C425(1.05); C185(1.13); C141(1.03); C238(1.05)  LDD1648  [25]
 LDCM0446  CL55 HEK-293T C185(0.82); C141(0.88); C238(1.07)  LDD1649  [25]
 LDCM0447  CL56 HEK-293T C425(1.11); C185(1.04); C141(1.06); C238(0.89)  LDD1650  [25]
 LDCM0448  CL57 HEK-293T C185(1.13); C141(1.08); C238(0.98)  LDD1651  [25]
 LDCM0449  CL58 HEK-293T C185(0.94); C141(0.96); C238(0.92)  LDD1652  [25]
 LDCM0450  CL59 HEK-293T C425(1.13); C185(0.96); C141(1.09); C238(0.94)  LDD1653  [25]
 LDCM0451  CL6 HEK-293T C425(0.95); C185(1.08); C141(1.08); C238(0.84)  LDD1654  [25]
 LDCM0452  CL60 HEK-293T C425(1.04); C185(0.90); C141(1.10); C238(1.25)  LDD1655  [25]
 LDCM0453  CL61 HEK-293T C425(0.95); C185(0.85); C141(1.00); C238(1.13)  LDD1656  [25]
 LDCM0454  CL62 HEK-293T C425(1.12); C185(0.98); C141(0.95); C238(1.08)  LDD1657  [25]
 LDCM0455  CL63 HEK-293T C425(1.13); C185(0.94); C141(1.11); C238(0.96)  LDD1658  [25]
 LDCM0456  CL64 HEK-293T C425(1.13); C185(1.02); C141(0.87); C238(1.05)  LDD1659  [25]
 LDCM0457  CL65 HEK-293T C425(0.97); C185(1.05); C141(0.89); C238(1.02)  LDD1660  [25]
 LDCM0458  CL66 HEK-293T C425(1.16); C185(1.14); C141(0.79); C238(0.95)  LDD1661  [25]
 LDCM0459  CL67 HEK-293T C185(0.93); C141(0.95); C238(1.06)  LDD1662  [25]
 LDCM0460  CL68 HEK-293T C425(1.18); C185(1.06); C141(1.02); C238(0.93)  LDD1663  [25]
 LDCM0461  CL69 HEK-293T C185(1.05); C141(1.09); C238(0.96)  LDD1664  [25]
 LDCM0462  CL7 HEK-293T C185(0.84); C141(0.87); C238(1.01)  LDD1665  [25]
 LDCM0463  CL70 HEK-293T C185(0.99); C141(0.95); C238(0.84)  LDD1666  [25]
 LDCM0464  CL71 HEK-293T C425(1.01); C185(0.98); C141(0.95); C238(0.96)  LDD1667  [25]
 LDCM0465  CL72 HEK-293T C425(1.32); C185(0.84); C141(1.04); C238(1.09)  LDD1668  [25]
 LDCM0466  CL73 HEK-293T C425(0.99); C185(1.32); C141(1.02); C238(1.11)  LDD1669  [25]
 LDCM0467  CL74 HEK-293T C425(1.08); C185(0.96); C141(1.65); C238(0.96)  LDD1670  [25]
 LDCM0469  CL76 HEK-293T C425(1.07); C185(1.01); C141(0.82); C238(1.14)  LDD1672  [25]
 LDCM0470  CL77 HEK-293T C425(0.96); C185(1.08); C141(1.04); C238(1.04)  LDD1673  [25]
 LDCM0471  CL78 HEK-293T C425(1.03); C185(1.07); C141(1.14); C238(0.95)  LDD1674  [25]
 LDCM0472  CL79 HEK-293T C185(0.89); C141(0.93); C238(1.01)  LDD1675  [25]
 LDCM0473  CL8 HEK-293T C425(1.13); C185(1.15); C141(1.12); C238(0.88)  LDD1676  [25]
 LDCM0474  CL80 HEK-293T C425(1.26); C185(1.07); C141(1.02); C238(0.96)  LDD1677  [25]
 LDCM0475  CL81 HEK-293T C185(1.00); C141(1.07); C238(0.90)  LDD1678  [25]
 LDCM0476  CL82 HEK-293T C185(0.87); C141(0.95); C238(0.94)  LDD1679  [25]
 LDCM0477  CL83 HEK-293T C425(1.02); C185(0.85); C141(0.98); C238(0.98)  LDD1680  [25]
 LDCM0478  CL84 HEK-293T C425(1.18); C185(0.89); C141(0.90); C238(1.08)  LDD1681  [25]
 LDCM0479  CL85 HEK-293T C425(0.99); C185(0.92); C141(0.94); C238(1.14)  LDD1682  [25]
 LDCM0480  CL86 HEK-293T C425(1.08); C185(1.01); C141(1.03); C238(1.05)  LDD1683  [25]
 LDCM0481  CL87 HEK-293T C425(1.06); C185(1.03); C141(1.05); C238(1.01)  LDD1684  [25]
 LDCM0482  CL88 HEK-293T C425(1.10); C185(0.87); C141(0.91); C238(1.22)  LDD1685  [25]
 LDCM0483  CL89 HEK-293T C425(0.98); C185(1.13); C141(1.15); C238(1.03)  LDD1686  [25]
 LDCM0484  CL9 HEK-293T C185(1.15); C141(1.04); C238(0.93)  LDD1687  [25]
 LDCM0485  CL90 HEK-293T C425(1.05); C185(1.16); C141(1.07); C238(0.89)  LDD1688  [25]
 LDCM0486  CL91 HEK-293T C185(1.07); C141(0.96); C238(1.04)  LDD1689  [25]
 LDCM0487  CL92 HEK-293T C425(1.17); C185(0.95); C141(1.08); C238(0.90)  LDD1690  [25]
 LDCM0488  CL93 HEK-293T C185(0.98); C141(1.14); C238(1.02)  LDD1691  [25]
 LDCM0489  CL94 HEK-293T C185(0.99); C141(0.95); C238(0.98)  LDD1692  [25]
 LDCM0490  CL95 HEK-293T C425(1.04); C185(1.09); C141(1.05); C238(0.91)  LDD1693  [25]
 LDCM0491  CL96 HEK-293T C425(1.06); C185(0.93); C141(1.08); C238(1.09)  LDD1694  [25]
 LDCM0492  CL97 HEK-293T C425(0.85); C185(0.98); C141(0.88); C238(1.00)  LDD1695  [25]
 LDCM0493  CL98 HEK-293T C425(0.94); C185(1.17); C141(0.86); C238(0.87)  LDD1696  [25]
 LDCM0494  CL99 HEK-293T C425(0.98); C185(0.98); C141(0.87); C238(0.92)  LDD1697  [25]
 LDCM0495  E2913 HEK-293T C425(0.99); C185(0.93); C141(1.25); C238(0.94)  LDD1698  [25]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C141(2.55)  LDD1702  [8]
 LDCM0031  Epigallocatechin gallate HEK-293T 12.37  LDD0183  [9]
 LDCM0468  Fragment33 HEK-293T C425(0.99); C185(1.02); C141(1.13); C238(0.91)  LDD1671  [25]
 LDCM0427  Fragment51 HEK-293T C425(1.06); C185(1.10); C141(0.75); C238(0.91)  LDD1631  [25]
 LDCM0116  HHS-0101 DM93 Y27(0.58); Y243(1.16)  LDD0264  [12]
 LDCM0117  HHS-0201 DM93 Y27(0.97)  LDD0265  [12]
 LDCM0118  HHS-0301 DM93 Y27(0.90); Y243(1.35)  LDD0266  [12]
 LDCM0119  HHS-0401 DM93 Y243(1.03); Y27(1.31)  LDD0267  [12]
 LDCM0120  HHS-0701 DM93 Y243(1.02); Y27(1.33)  LDD0268  [12]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [7]
 LDCM0022  KB02 HEK-293T C185(0.87); C141(0.96); C238(0.94)  LDD1492  [25]
 LDCM0023  KB03 Jurkat C185(7.46)  LDD0209  [11]
 LDCM0024  KB05 COLO792 C253(3.35)  LDD3310  [27]
 LDCM0109  NEM HeLa N.A.  LDD0224  [23]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C425(0.24)  LDD2096  [8]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C425(0.86)  LDD2123  [8]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C425(1.16)  LDD2136  [8]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C425(1.41)  LDD2146  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
5'-AMP-activated protein kinase subunit beta-1 (PRKAB1) 5'-AMP-activated protein kinase beta subunit family Q9Y478
5'-AMP-activated protein kinase subunit beta-2 (PRKAB2) 5'-AMP-activated protein kinase beta subunit family O43741
5'-AMP-activated protein kinase subunit gamma-1 (PRKAG1) 5'-AMP-activated protein kinase gamma subunit family P54619
Zinc finger protein RFP (TRIM27) TRIM/RBCC family P14373
E3 SUMO-protein ligase ZBED1 (ZBED1) . O96006
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein CDX-4 (CDX4) Caudal homeobox family O14627
Zinc finger protein Aiolos (IKZF3) Ikaros C2H2-type zinc-finger protein family Q9UKT9
DNA-binding protein RFX6 (RFX6) RFX family Q8HWS3
THAP domain-containing protein 1 (THAP1) THAP1 family Q9NVV9
TSC22 domain family protein 4 (TSC22D4) TSC-22/Dip/Bun family Q9Y3Q8
Class E basic helix-loop-helix protein 40 (BHLHE40) . O14503
Homeobox-containing protein 1 (HMBOX1) . Q6NT76
Other
Click To Hide/Show 19 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Abl interactor 2 (ABI2) ABI family Q9NYB9
Afadin- and alpha-actinin-binding protein (SSX2IP) ADIP family Q9Y2D8
Golgin subfamily A member 2 (GOLGA2) GOLGA2 family Q08379
Keratin, type I cytoskeletal 40 (KRT40) Intermediate filament family Q6A162
Microtubule-associated tumor suppressor candidate 2 (MTUS2) MTUS1 family Q5JR59
Paraneoplastic antigen-like protein 5 (PNMA5) PNMA family Q96PV4
RIMS-binding protein 3A (RIMBP3) RIMBP family Q9UFD9
Ropporin-1A (ROPN1) Ropporin family Q9HAT0
Vacuolar protein sorting-associated protein 37B (VPS37B) VPS37 family Q9H9H4
Vacuolar protein sorting-associated protein 52 homolog (VPS52) VPS52 family Q8N1B4
TLE family member 5 (TLE5) WD repeat Groucho/TLE family Q08117
Transcriptional coactivator YAP1 (YAP1) YAP1 family P46937
Thyroid receptor-interacting protein 6 (TRIP6) Zyxin/ajuba family Q15654
Fibrinogen silencer-binding protein (FSBP) . O95073
INO80 complex subunit E (INO80E) . Q8NBZ0
Lethal(3)malignant brain tumor-like protein 3 (L3MBTL3) . Q96JM7
Polyhomeotic-like protein 2 (PHC2) . Q8IXK0
RNA-binding protein with multiple splicing (RBPMS) . Q93062
UBX domain-containing protein 11 (UBXN11) . Q5T124

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
Acetylsalicylic Acid Small molecular drug DB00945
Adenosine Phosphate Small molecular drug DB00131
Fostamatinib Small molecular drug DB12010
Phenformin Small molecular drug DB00914
Topiramate Small molecular drug DB00273
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atp Small molecular drug DB00171

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 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
3 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
4 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
5 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
6 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
7 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.
8 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
9 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
10 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
11 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
12 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.
13 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
14 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
15 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
16 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
17 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
18 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
19 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
20 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
21 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
22 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
23 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.
24 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.
25 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
26 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.
27 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