Details of the Target

General Information of Target

Target ID LDTP04620
Target Name 5'-AMP-activated protein kinase catalytic subunit alpha-2 (PRKAA2)
Gene Name PRKAA2
Gene ID 5563
Synonyms
AMPK; AMPK2; 5'-AMP-activated protein kinase catalytic subunit alpha-2; AMPK subunit alpha-2; EC 2.7.11.1; Acetyl-CoA carboxylase kinase; ACACA kinase; Hydroxymethylglutaryl-CoA reductase kinase; HMGCR kinase; EC 2.7.11.31
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAEKQKHDGRVKIGHYVLGDTLGVGTFGKVKIGEHQLTGHKVAVKILNRQKIRSLDVVGK
IKREIQNLKLFRHPHIIKLYQVISTPTDFFMVMEYVSGGELFDYICKHGRVEEMEARRLF
QQILSAVDYCHRHMVVHRDLKPENVLLDAHMNAKIADFGLSNMMSDGEFLRTSCGSPNYA
APEVISGRLYAGPEVDIWSCGVILYALLCGTLPFDDEHVPTLFKKIRGGVFYIPEYLNRS
VATLLMHMLQVDPLKRATIKDIREHEWFKQDLPSYLFPEDPSYDANVIDDEAVKEVCEKF
ECTESEVMNSLYSGDPQDQLAVAYHLIIDNRRIMNQASEFYLASSPPSGSFMDDSAMHIP
PGLKPHPERMPPLIADSPKARCPLDALNTTKPKSLAVKKAKWHLGIRSQSKPYDIMAEVY
RAMKQLDFEWKVVNAYHLRVRRKNPVTGNYVKMSLQLYLVDNRSYLLDFKSIDDEVVEQR
SGSSTPQRSCSAAGLHRPRSSFDSTTAESHSLSGSLTGSLTGSTLSSVSPRLGSHTMDFF
EMCASLITTLAR
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. Involved in insulin receptor/INSR internalization. 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. 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 acts as a regulator of cellular polarity by remodeling the actin cytoskeleton; probably by indirectly activating myosin. Also phosphorylates CFTR, EEF2K, KLC1, NOS3 and SLC12A1. Plays an important role in the differential regulation of pro-autophagy (composed of PIK3C3, BECN1, PIK3R4 and UVRAG or ATG14) and non-autophagy (composed of PIK3C3, BECN1 and PIK3R4) complexes, in response to glucose starvation. Can inhibit the non-autophagy complex by phosphorylating PIK3C3 and can activate the pro-autophagy complex by phosphorylating BECN1. Upon glucose starvation, promotes ARF6 activation in a kinase-independent manner leading to cell migration. Upon glucose deprivation mediates the phosphorylation of ACSS2 at 'Ser-659', which exposes the nuclear localization signal of ACSS2, required for its interaction with KPNA1 and nuclear translocation.
Uniprot ID
P54646
Ensemble ID
ENST00000371244.9
HGNC ID
HGNC:9377
ChEMBL ID
CHEMBL2116

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 20 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K401(6.48); K45(4.55)  LDD0277  [1]
DBIA
 Probe Info  		C200(7.97)  LDD3310  [2]
DA-P3
 Probe Info  		4.36  LDD0179  [3]
AHL-Pu-1
 Probe Info  		C174(2.10)  LDD0169  [4]
HPAP
 Probe Info  		3.70  LDD0062  [5]
HHS-465
 Probe Info  		Y413(0.82)  LDD2237  [6]
AMP probe
 Probe Info  		N.A.  LDD0200  [7]
ATP probe
 Probe Info  		K45(0.00); K141(0.00); K60(0.00); K62(0.00)  LDD0199  [7]
IA-alkyne
 Probe Info  		C130(0.00); C490(0.00); C174(0.00); C543(0.00)  LDD0165  [8]
NAIA_4
 Probe Info  		N.A.  LDD2226  [9]
WYneN
 Probe Info  		C174(0.00); C382(0.00)  LDD0021  [10]
Compound 10
 Probe Info  		N.A.  LDD2216  [11]
Compound 11
 Probe Info  		N.A.  LDD2213  [11]
IPM
 Probe Info  		C382(0.00); C490(0.00); C174(0.00)  LDD0005  [10]
NPM
 Probe Info  		N.A.  LDD0016  [10]
TFBX
 Probe Info  		C174(0.00); C130(0.00)  LDD0148  [12]
VSF
 Probe Info  		C174(0.00); C382(0.00)  LDD0007  [10]
Phosphinate-6
 Probe Info  		C490(0.00); C382(0.00)  LDD0018  [13]
Acrolein
 Probe Info  		N.A.  LDD0217  [14]
AOyne
 Probe Info  		15.00  LDD0443  [15]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C004
 Probe Info  		9.99  LDD1714  [16]
C285
 Probe Info  		22.78  LDD1955  [16]
C289
 Probe Info  		28.64  LDD1959  [16]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA HEK-293T C174(2.10)  LDD0169  [4]
 LDCM0214  AC1 HEK-293T C490(1.39); C382(1.09); C130(1.01)  LDD1507  [17]
 LDCM0215  AC10 HEK-293T C382(1.10); C130(0.99)  LDD1508  [17]
 LDCM0226  AC11 HEK-293T C490(0.90); C382(1.08); C130(0.91)  LDD1509  [17]
 LDCM0237  AC12 HEK-293T C490(0.98); C382(1.10); C130(0.98)  LDD1510  [17]
 LDCM0259  AC14 HEK-293T C490(1.06); C382(1.09); C130(1.40)  LDD1512  [17]
 LDCM0270  AC15 HEK-293T C490(0.94); C382(1.07); C130(1.02)  LDD1513  [17]
 LDCM0276  AC17 HEK-293T C490(1.25); C382(1.11); C130(0.98)  LDD1515  [17]
 LDCM0277  AC18 HEK-293T C382(1.09); C130(1.05)  LDD1516  [17]
 LDCM0278  AC19 HEK-293T C490(1.13); C382(1.15); C130(0.83)  LDD1517  [17]
 LDCM0279  AC2 HEK-293T C382(1.02); C130(0.93)  LDD1518  [17]
 LDCM0280  AC20 HEK-293T C490(1.01); C382(1.01); C130(1.15)  LDD1519  [17]
 LDCM0281  AC21 HEK-293T C490(1.02); C382(1.03); C130(1.08)  LDD1520  [17]
 LDCM0282  AC22 HEK-293T C490(1.07); C382(1.06); C130(1.15)  LDD1521  [17]
 LDCM0283  AC23 HEK-293T C490(1.03); C382(1.07); C130(1.01)  LDD1522  [17]
 LDCM0284  AC24 HEK-293T C490(1.03); C382(0.99); C130(0.99)  LDD1523  [17]
 LDCM0285  AC25 HEK-293T C490(1.24); C382(1.17); C130(0.79)  LDD1524  [17]
 LDCM0286  AC26 HEK-293T C382(1.07); C130(1.00)  LDD1525  [17]
 LDCM0287  AC27 HEK-293T C490(0.98); C382(1.02); C130(0.88)  LDD1526  [17]
 LDCM0288  AC28 HEK-293T C490(0.96); C382(1.00); C130(1.25)  LDD1527  [17]
 LDCM0289  AC29 HEK-293T C490(1.00); C382(1.03); C130(1.01)  LDD1528  [17]
 LDCM0290  AC3 HEK-293T C490(0.99); C382(1.07); C130(0.97)  LDD1529  [17]
 LDCM0291  AC30 HEK-293T C490(1.02); C382(1.13); C130(0.99)  LDD1530  [17]
 LDCM0292  AC31 HEK-293T C490(1.06); C382(1.10); C130(1.00)  LDD1531  [17]
 LDCM0293  AC32 HEK-293T C490(1.05); C382(1.07); C130(0.89)  LDD1532  [17]
 LDCM0294  AC33 HEK-293T C490(1.55); C382(1.17); C130(1.06)  LDD1533  [17]
 LDCM0295  AC34 HEK-293T C382(1.01); C130(1.00)  LDD1534  [17]
 LDCM0296  AC35 HEK-293T C490(0.99); C382(1.11); C130(1.08)  LDD1535  [17]
 LDCM0297  AC36 HEK-293T C490(0.99); C382(1.04); C130(1.10)  LDD1536  [17]
 LDCM0298  AC37 HEK-293T C490(0.99); C382(1.02); C130(1.06)  LDD1537  [17]
 LDCM0299  AC38 HEK-293T C490(1.07); C382(1.05); C130(1.27)  LDD1538  [17]
 LDCM0300  AC39 HEK-293T C490(1.04); C382(1.03); C130(1.07)  LDD1539  [17]
 LDCM0301  AC4 HEK-293T C490(0.96); C382(1.01); C130(1.12)  LDD1540  [17]
 LDCM0302  AC40 HEK-293T C490(1.00); C382(1.07); C130(0.94)  LDD1541  [17]
 LDCM0303  AC41 HEK-293T C490(1.39); C382(1.12); C130(0.91)  LDD1542  [17]
 LDCM0304  AC42 HEK-293T C382(1.10); C130(1.09)  LDD1543  [17]
 LDCM0305  AC43 HEK-293T C490(0.94); C382(1.10); C130(0.98)  LDD1544  [17]
 LDCM0306  AC44 HEK-293T C490(0.95); C382(1.07); C130(1.35)  LDD1545  [17]
 LDCM0307  AC45 HEK-293T C490(1.05); C382(1.05); C130(1.15)  LDD1546  [17]
 LDCM0308  AC46 HEK-293T C490(0.96); C382(0.96); C130(1.07)  LDD1547  [17]
 LDCM0309  AC47 HEK-293T C490(0.98); C382(1.04); C130(1.03)  LDD1548  [17]
 LDCM0310  AC48 HEK-293T C490(1.02); C382(1.07); C130(1.03)  LDD1549  [17]
 LDCM0311  AC49 HEK-293T C490(1.24); C382(1.10); C130(1.15)  LDD1550  [17]
 LDCM0312  AC5 HEK-293T C490(1.01); C382(1.01); C130(1.07)  LDD1551  [17]
 LDCM0313  AC50 HEK-293T C382(1.04); C130(1.04)  LDD1552  [17]
 LDCM0314  AC51 HEK-293T C490(0.90); C382(1.08); C130(0.99)  LDD1553  [17]
 LDCM0315  AC52 HEK-293T C490(0.87); C382(1.03); C130(1.16)  LDD1554  [17]
 LDCM0316  AC53 HEK-293T C490(0.95); C382(1.00); C130(1.04)  LDD1555  [17]
 LDCM0317  AC54 HEK-293T C490(1.02); C382(1.03); C130(1.05)  LDD1556  [17]
 LDCM0318  AC55 HEK-293T C490(0.91); C382(1.02); C130(1.17)  LDD1557  [17]
 LDCM0319  AC56 HEK-293T C490(0.98); C382(1.11); C130(0.91)  LDD1558  [17]
 LDCM0320  AC57 HEK-293T C490(1.07); C382(1.09); C130(0.95)  LDD1559  [17]
 LDCM0321  AC58 HEK-293T C382(1.01); C130(1.08)  LDD1560  [17]
 LDCM0322  AC59 HEK-293T C490(0.84); C382(1.04); C130(0.97)  LDD1561  [17]
 LDCM0323  AC6 HEK-293T C490(1.04); C382(1.02); C130(1.21)  LDD1562  [17]
 LDCM0324  AC60 HEK-293T C490(0.97); C382(1.12); C130(1.20)  LDD1563  [17]
 LDCM0325  AC61 HEK-293T C490(0.95); C382(1.05); C130(1.09)  LDD1564  [17]
 LDCM0326  AC62 HEK-293T C490(0.92); C382(1.07); C130(1.21)  LDD1565  [17]
 LDCM0327  AC63 HEK-293T C490(0.93); C382(1.08); C130(1.02)  LDD1566  [17]
 LDCM0328  AC64 HEK-293T C490(0.91); C382(1.02); C130(1.03)  LDD1567  [17]
 LDCM0334  AC7 HEK-293T C490(0.98); C382(1.04); C130(1.05)  LDD1568  [17]
 LDCM0345  AC8 HEK-293T C490(1.05); C382(1.09); C130(1.02)  LDD1569  [17]
 LDCM0248  AKOS034007472 HEK-293T C490(0.99); C382(1.00); C130(0.93)  LDD1511  [17]
 LDCM0356  AKOS034007680 HEK-293T C490(1.38); C382(1.12); C130(1.04)  LDD1570  [17]
 LDCM0275  AKOS034007705 HEK-293T C490(0.99); C382(1.07); C130(1.00)  LDD1514  [17]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [14]
 LDCM0367  CL1 HEK-293T C490(1.02); C382(1.40); C130(1.00)  LDD1571  [17]
 LDCM0368  CL10 HEK-293T C490(1.03); C382(1.82); C130(1.26)  LDD1572  [17]
 LDCM0369  CL100 HEK-293T C490(1.01); C382(1.02); C130(0.87)  LDD1573  [17]
 LDCM0370  CL101 HEK-293T C490(1.11); C382(1.18); C130(1.13)  LDD1574  [17]
 LDCM0371  CL102 HEK-293T C490(0.83); C382(1.37); C130(0.92)  LDD1575  [17]
 LDCM0372  CL103 HEK-293T C490(1.06); C382(1.10); C130(0.92); C302(1.01)  LDD1576  [17]
 LDCM0373  CL104 HEK-293T C490(0.93); C382(0.99); C130(1.05)  LDD1577  [17]
 LDCM0374  CL105 HEK-293T C490(1.12); C382(1.17); C130(1.04)  LDD1578  [17]
 LDCM0375  CL106 HEK-293T C490(0.93); C382(1.17); C130(0.89)  LDD1579  [17]
 LDCM0376  CL107 HEK-293T C490(0.98); C382(1.03); C130(0.87); C302(0.80)  LDD1580  [17]
 LDCM0377  CL108 HEK-293T C490(0.92); C382(1.06); C130(1.06)  LDD1581  [17]
 LDCM0378  CL109 HEK-293T C490(1.08); C382(1.19); C130(1.02)  LDD1582  [17]
 LDCM0379  CL11 HEK-293T C490(0.89); C382(0.94); C130(0.93)  LDD1583  [17]
 LDCM0380  CL110 HEK-293T C490(0.90); C382(1.43); C130(0.91)  LDD1584  [17]
 LDCM0381  CL111 HEK-293T C490(1.05); C382(1.16); C130(1.06); C302(0.93)  LDD1585  [17]
 LDCM0382  CL112 HEK-293T C490(1.12); C382(1.14); C130(0.98)  LDD1586  [17]
 LDCM0383  CL113 HEK-293T C490(1.06); C382(1.08); C130(1.01)  LDD1587  [17]
 LDCM0384  CL114 HEK-293T C490(1.05); C382(1.30); C130(0.87)  LDD1588  [17]
 LDCM0385  CL115 HEK-293T C490(1.06); C382(1.09); C130(0.86); C302(1.08)  LDD1589  [17]
 LDCM0386  CL116 HEK-293T C490(1.07); C382(0.98); C130(0.96)  LDD1590  [17]
 LDCM0387  CL117 HEK-293T C490(0.98); C382(1.12); C130(1.00)  LDD1591  [17]
 LDCM0388  CL118 HEK-293T C490(0.91); C382(1.13); C130(1.00)  LDD1592  [17]
 LDCM0389  CL119 HEK-293T C490(1.02); C382(1.08); C130(0.82); C302(0.89)  LDD1593  [17]
 LDCM0390  CL12 HEK-293T C490(0.87); C382(0.90); C130(1.04)  LDD1594  [17]
 LDCM0391  CL120 HEK-293T C490(1.09); C382(1.05); C130(1.03)  LDD1595  [17]
 LDCM0392  CL121 HEK-293T C490(0.97); C382(1.15); C130(1.07)  LDD1596  [17]
 LDCM0393  CL122 HEK-293T C490(0.86); C382(1.16); C130(0.95)  LDD1597  [17]
 LDCM0394  CL123 HEK-293T C490(0.94); C382(1.59); C130(0.80); C302(0.79)  LDD1598  [17]
 LDCM0395  CL124 HEK-293T C490(0.99); C382(1.15); C130(1.07)  LDD1599  [17]
 LDCM0396  CL125 HEK-293T C490(0.87); C382(1.12); C130(1.12)  LDD1600  [17]
 LDCM0397  CL126 HEK-293T C490(0.79); C382(1.23); C130(1.00)  LDD1601  [17]
 LDCM0398  CL127 HEK-293T C490(0.86); C382(1.10); C130(0.89); C302(0.66)  LDD1602  [17]
 LDCM0399  CL128 HEK-293T C490(0.96); C382(0.97); C130(1.15)  LDD1603  [17]
 LDCM0400  CL13 HEK-293T C490(1.05); C382(1.25); C130(1.09)  LDD1604  [17]
 LDCM0401  CL14 HEK-293T C490(1.08); C382(1.33); C130(1.04)  LDD1605  [17]
 LDCM0402  CL15 HEK-293T C490(0.99); C382(1.46); C130(0.87); C302(0.93)  LDD1606  [17]
 LDCM0403  CL16 HEK-293T C490(0.86); C382(1.06); C130(0.95)  LDD1607  [17]
 LDCM0404  CL17 HEK-293T C490(1.12); C382(1.98); C130(0.84)  LDD1608  [17]
 LDCM0405  CL18 HEK-293T C382(1.06); C130(0.77)  LDD1609  [17]
 LDCM0406  CL19 HEK-293T C490(0.79); C382(1.10); C130(0.97)  LDD1610  [17]
 LDCM0407  CL2 HEK-293T C490(1.06); C382(1.27); C130(1.13)  LDD1611  [17]
 LDCM0408  CL20 HEK-293T C490(0.84); C382(1.11); C130(1.30)  LDD1612  [17]
 LDCM0409  CL21 HEK-293T C490(0.96); C382(1.53); C130(1.13)  LDD1613  [17]
 LDCM0410  CL22 HEK-293T C490(0.89); C382(0.78); C130(1.38)  LDD1614  [17]
 LDCM0411  CL23 HEK-293T C490(0.84); C382(0.74); C130(0.93)  LDD1615  [17]
 LDCM0412  CL24 HEK-293T C490(0.82); C382(0.70); C130(0.99)  LDD1616  [17]
 LDCM0413  CL25 HEK-293T C490(0.91); C382(1.15); C130(0.96)  LDD1617  [17]
 LDCM0414  CL26 HEK-293T C490(0.83); C382(1.04); C130(1.05)  LDD1618  [17]
 LDCM0415  CL27 HEK-293T C490(1.04); C382(1.01); C130(0.83); C302(1.08)  LDD1619  [17]
 LDCM0416  CL28 HEK-293T C490(1.06); C382(1.19); C130(0.93)  LDD1620  [17]
 LDCM0417  CL29 HEK-293T C490(1.22); C382(1.05); C130(0.88)  LDD1621  [17]
 LDCM0418  CL3 HEK-293T C490(0.97); C382(1.09); C130(0.93); C302(1.04)  LDD1622  [17]
 LDCM0419  CL30 HEK-293T C382(1.02); C130(0.95)  LDD1623  [17]
 LDCM0420  CL31 HEK-293T C490(0.83); C382(1.25); C130(0.84)  LDD1624  [17]
 LDCM0421  CL32 HEK-293T C490(0.87); C382(1.06); C130(1.27)  LDD1625  [17]
 LDCM0422  CL33 HEK-293T C490(0.86); C382(3.02); C130(0.91)  LDD1626  [17]
 LDCM0423  CL34 HEK-293T C490(0.85); C382(0.93); C130(1.06)  LDD1627  [17]
 LDCM0424  CL35 HEK-293T C490(0.88); C382(0.70); C130(0.88)  LDD1628  [17]
 LDCM0425  CL36 HEK-293T C490(0.96); C382(0.77); C130(1.16)  LDD1629  [17]
 LDCM0426  CL37 HEK-293T C490(0.96); C382(1.10); C130(1.14)  LDD1630  [17]
 LDCM0428  CL39 HEK-293T C490(1.02); C382(1.38); C130(0.90); C302(0.78)  LDD1632  [17]
 LDCM0429  CL4 HEK-293T C490(0.84); C382(1.17); C130(0.86)  LDD1633  [17]
 LDCM0430  CL40 HEK-293T C490(1.22); C382(0.98); C130(0.95)  LDD1634  [17]
 LDCM0431  CL41 HEK-293T C490(1.23); C382(1.15); C130(0.40)  LDD1635  [17]
 LDCM0432  CL42 HEK-293T C382(1.04); C130(1.16)  LDD1636  [17]
 LDCM0433  CL43 HEK-293T C490(0.91); C382(1.06); C130(0.91)  LDD1637  [17]
 LDCM0434  CL44 HEK-293T C490(0.99); C382(1.05); C130(1.34)  LDD1638  [17]
 LDCM0435  CL45 HEK-293T C490(0.94); C382(1.59); C130(1.05)  LDD1639  [17]
 LDCM0436  CL46 HEK-293T C490(0.95); C382(0.82); C130(0.96)  LDD1640  [17]
 LDCM0437  CL47 HEK-293T C490(0.89); C382(0.84); C130(0.98)  LDD1641  [17]
 LDCM0438  CL48 HEK-293T C490(0.86); C382(0.74); C130(0.99)  LDD1642  [17]
 LDCM0439  CL49 HEK-293T C490(0.97); C382(1.10); C130(1.12)  LDD1643  [17]
 LDCM0440  CL5 HEK-293T C490(1.27); C382(1.04); C130(1.03)  LDD1644  [17]
 LDCM0441  CL50 HEK-293T C490(0.95); C382(1.22); C130(0.96)  LDD1645  [17]
 LDCM0443  CL52 HEK-293T C490(1.05); C382(1.02); C130(0.97)  LDD1646  [17]
 LDCM0444  CL53 HEK-293T C490(1.28); C382(1.47); C130(0.86)  LDD1647  [17]
 LDCM0445  CL54 HEK-293T C382(1.74); C130(1.00)  LDD1648  [17]
 LDCM0446  CL55 HEK-293T C490(0.87); C382(1.05); C130(0.84)  LDD1649  [17]
 LDCM0447  CL56 HEK-293T C490(0.96); C382(1.31); C130(1.21)  LDD1650  [17]
 LDCM0448  CL57 HEK-293T C490(0.92); C382(1.41); C130(0.96)  LDD1651  [17]
 LDCM0449  CL58 HEK-293T C490(0.91); C382(1.03); C130(1.02)  LDD1652  [17]
 LDCM0450  CL59 HEK-293T C490(0.90); C382(0.78); C130(0.85)  LDD1653  [17]
 LDCM0451  CL6 HEK-293T C382(1.17); C130(0.97)  LDD1654  [17]
 LDCM0452  CL60 HEK-293T C490(0.89); C382(0.82); C130(0.64)  LDD1655  [17]
 LDCM0453  CL61 HEK-293T C490(0.90); C382(1.07); C130(1.00)  LDD1656  [17]
 LDCM0454  CL62 HEK-293T C490(0.88); C382(1.13); C130(1.08)  LDD1657  [17]
 LDCM0455  CL63 HEK-293T C490(1.00); C382(1.06); C130(0.82); C302(0.86)  LDD1658  [17]
 LDCM0456  CL64 HEK-293T C490(0.98); C382(1.40); C130(0.98)  LDD1659  [17]
 LDCM0457  CL65 HEK-293T C490(1.36); C382(1.04); C130(0.77)  LDD1660  [17]
 LDCM0458  CL66 HEK-293T C382(1.19); C130(0.97)  LDD1661  [17]
 LDCM0459  CL67 HEK-293T C490(0.85); C382(1.12); C130(1.08)  LDD1662  [17]
 LDCM0460  CL68 HEK-293T C490(0.90); C382(1.30); C130(1.06)  LDD1663  [17]
 LDCM0461  CL69 HEK-293T C490(0.87); C382(1.14); C130(1.09)  LDD1664  [17]
 LDCM0462  CL7 HEK-293T C490(0.71); C382(1.10); C130(1.03)  LDD1665  [17]
 LDCM0463  CL70 HEK-293T C490(0.97); C382(0.72); C130(1.18)  LDD1666  [17]
 LDCM0464  CL71 HEK-293T C490(0.80); C382(0.77); C130(1.00)  LDD1667  [17]
 LDCM0465  CL72 HEK-293T C490(0.92); C382(0.82); C130(1.05)  LDD1668  [17]
 LDCM0466  CL73 HEK-293T C490(0.99); C382(1.27); C130(0.92)  LDD1669  [17]
 LDCM0467  CL74 HEK-293T C490(0.90); C382(1.16); C130(1.15)  LDD1670  [17]
 LDCM0469  CL76 HEK-293T C490(1.01); C382(1.00); C130(0.97)  LDD1672  [17]
 LDCM0470  CL77 HEK-293T C490(1.02); C382(1.60); C130(0.87)  LDD1673  [17]
 LDCM0471  CL78 HEK-293T C382(0.94); C130(0.93)  LDD1674  [17]
 LDCM0472  CL79 HEK-293T C490(0.80); C382(1.10); C130(0.98)  LDD1675  [17]
 LDCM0473  CL8 HEK-293T C490(0.72); C382(3.74); C130(1.19)  LDD1676  [17]
 LDCM0474  CL80 HEK-293T C490(0.86); C382(1.05); C130(1.10)  LDD1677  [17]
 LDCM0475  CL81 HEK-293T C490(0.82); C382(0.91); C130(1.03)  LDD1678  [17]
 LDCM0476  CL82 HEK-293T C490(0.99); C382(0.75); C130(1.06)  LDD1679  [17]
 LDCM0477  CL83 HEK-293T C490(0.84); C382(0.81); C130(0.84)  LDD1680  [17]
 LDCM0478  CL84 HEK-293T C490(0.87); C382(0.89); C130(0.91)  LDD1681  [17]
 LDCM0479  CL85 HEK-293T C490(0.96); C382(1.09); C130(1.06)  LDD1682  [17]
 LDCM0480  CL86 HEK-293T C490(0.69); C382(1.17); C130(1.02)  LDD1683  [17]
 LDCM0481  CL87 HEK-293T C490(0.78); C382(1.15); C130(0.93); C302(0.89)  LDD1684  [17]
 LDCM0482  CL88 HEK-293T C490(0.82); C382(1.01); C130(0.93)  LDD1685  [17]
 LDCM0483  CL89 HEK-293T C490(0.96); C382(1.08); C130(1.10)  LDD1686  [17]
 LDCM0484  CL9 HEK-293T C490(0.81); C382(0.97); C130(1.22)  LDD1687  [17]
 LDCM0485  CL90 HEK-293T C382(2.69); C130(0.87)  LDD1688  [17]
 LDCM0486  CL91 HEK-293T C490(0.67); C382(1.10); C130(0.87)  LDD1689  [17]
 LDCM0487  CL92 HEK-293T C490(0.81); C382(1.66); C130(1.06)  LDD1690  [17]
 LDCM0488  CL93 HEK-293T C490(0.86); C382(1.26); C130(0.96)  LDD1691  [17]
 LDCM0489  CL94 HEK-293T C490(0.96); C382(0.95); C130(1.10)  LDD1692  [17]
 LDCM0490  CL95 HEK-293T C490(0.99); C382(0.40); C130(0.61)  LDD1693  [17]
 LDCM0491  CL96 HEK-293T C490(0.82); C382(1.09); C130(1.06)  LDD1694  [17]
 LDCM0492  CL97 HEK-293T C490(1.10); C382(1.24); C130(0.98)  LDD1695  [17]
 LDCM0493  CL98 HEK-293T C490(0.87); C382(1.19); C130(1.02)  LDD1696  [17]
 LDCM0494  CL99 HEK-293T C490(0.96); C382(1.36); C130(0.85); C302(0.85)  LDD1697  [17]
 LDCM0027  Dopamine HEK-293T 4.36  LDD0179  [3]
 LDCM0495  E2913 HEK-293T C490(1.12); C382(1.99); C130(0.85); C302(0.89)  LDD1698  [17]
 LDCM0625  F8 Ramos C174(1.36)  LDD2187  [18]
 LDCM0572  Fragment10 Ramos C174(1.40)  LDD2189  [18]
 LDCM0573  Fragment11 Ramos C174(0.62)  LDD2190  [18]
 LDCM0574  Fragment12 Ramos C174(1.13)  LDD2191  [18]
 LDCM0575  Fragment13 Ramos C174(0.97)  LDD2192  [18]
 LDCM0576  Fragment14 Ramos C174(0.71)  LDD2193  [18]
 LDCM0579  Fragment20 Ramos C174(1.01)  LDD2194  [18]
 LDCM0580  Fragment21 Ramos C174(1.06)  LDD2195  [18]
 LDCM0582  Fragment23 Ramos C174(0.83)  LDD2196  [18]
 LDCM0578  Fragment27 Ramos C174(0.77)  LDD2197  [18]
 LDCM0586  Fragment28 Ramos C174(1.14)  LDD2198  [18]
 LDCM0588  Fragment30 Ramos C174(1.14)  LDD2199  [18]
 LDCM0589  Fragment31 Ramos C174(0.80)  LDD2200  [18]
 LDCM0590  Fragment32 Ramos C174(1.74)  LDD2201  [18]
 LDCM0468  Fragment33 HEK-293T C490(0.95); C382(1.17); C130(0.87); C302(1.18)  LDD1671  [17]
 LDCM0596  Fragment38 Ramos C174(0.88)  LDD2203  [18]
 LDCM0566  Fragment4 Ramos C174(1.06)  LDD2184  [18]
 LDCM0427  Fragment51 HEK-293T C490(0.86); C382(1.07); C130(0.96)  LDD1631  [17]
 LDCM0610  Fragment52 Ramos C174(1.23)  LDD2204  [18]
 LDCM0614  Fragment56 Ramos C174(1.25)  LDD2205  [18]
 LDCM0569  Fragment7 Ramos C174(2.42)  LDD2186  [18]
 LDCM0571  Fragment9 Ramos C174(1.72)  LDD2188  [18]
 LDCM0022  KB02 HEK-293T C490(0.94); C382(0.92); C130(0.97)  LDD1492  [17]
 LDCM0023  KB03 HEK-293T C490(0.99); C382(0.96); C130(0.94)  LDD1497  [17]
 LDCM0024  KB05 COLO792 C200(7.97)  LDD3310  [2]
 LDCM0030  Luteolin HEK-293T 8.09  LDD0182  [3]
 LDCM0627  NUDT7-COV-1 HEK-293T C174(0.60)  LDD2206  [19]
 LDCM0628  OTUB2-COV-1 HEK-293T C174(0.91); C382(0.86)  LDD2207  [19]
 LDCM0014  Panhematin HEK-293T 3.70  LDD0062  [5]

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
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
Pachytene checkpoint protein 2 homolog (TRIP13) AAA ATPase family Q15645
Putative histone-lysine N-methyltransferase PRDM6 (PRDM6) Class V-like SAM-binding methyltransferase superfamily Q9NQX0
Superkiller complex protein 2 (SKIC2) Helicase family Q15477
Serine/threonine-protein kinase STK11 (STK11) CAMK Ser/Thr protein kinase family Q15831
Serine/threonine-protein kinase ULK1 (ULK1) Ser/Thr protein kinase family O75385
Dynamin-2 (DNM2) Dynamin/Fzo/YdjA family P50570
Kinesin-like protein KIFC3 (KIFC3) Kinesin family Q9BVG8
E3 ubiquitin-protein ligase CCNB1IP1 (CCNB1IP1) . Q9NPC3
NEDD4-like E3 ubiquitin-protein ligase WWP2 (WWP2) . O00308
pre-mRNA splicing regulator USH1G (USH1G) . Q495M9
Probable E3 ubiquitin-protein ligase makorin-3 (MKRN3) . Q13064
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Arrestin domain-containing protein 3 (ARRDC3) Arrestin family Q96B67
Wolframin (WFS1) . O76024
Transcription factor
Click To Hide/Show 12 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox protein CDX-4 (CDX4) Caudal homeobox family O14627
Zinc finger protein GLI1 (GLI1) GLI C2H2-type zinc-finger protein family P08151
Zinc finger protein Aiolos (IKZF3) Ikaros C2H2-type zinc-finger protein family Q9UKT9
Zinc finger and SCAN domain-containing protein 23 (ZSCAN23) Krueppel C2H2-type zinc-finger protein family Q3MJ62
Zinc finger protein 212 (ZNF212) Krueppel C2H2-type zinc-finger protein family Q9UDV6
Zinc finger protein 397 (ZNF397) Krueppel C2H2-type zinc-finger protein family Q8NF99
DNA-binding protein RFX6 (RFX6) RFX family Q8HWS3
TSC22 domain family protein 4 (TSC22D4) TSC-22/Dip/Bun family Q9Y3Q8
Homeobox-containing protein 1 (HMBOX1) . Q6NT76
Spermatogenesis- and oogenesis-specific basic helix-loop-helix-containing protein 1 (SOHLH1) . Q5JUK2
Transcription factor 4 (TCF4) . P15884
Zinc finger and BTB domain-containing protein 8A (ZBTB8A) . Q96BR9
Other
Click To Hide/Show 50 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Abl interactor 2 (ABI2) ABI family Q9NYB9
A-kinase anchor protein 8-like (AKAP8L) AKAP95 family Q9ULX6
Angiomotin-like protein 2 (AMOTL2) Angiomotin family Q9Y2J4
Calcium-binding and coiled-coil domain-containing protein 1 (CALCOCO1) CALCOCO family Q9P1Z2
Calcium-binding and coiled-coil domain-containing protein 2 (CALCOCO2) CALCOCO family Q13137
Neutrophil gelatinase-associated lipocalin (LCN2) Lipocalin family P80188
cAMP-dependent protein kinase type I-beta regulatory subunit (PRKAR1B) CAMP-dependent kinase regulatory chain family P31321
Coiled-coil domain-containing protein 172 (CCDC172) CCDC172 family P0C7W6
Cerebellar degeneration-related protein 2 (CDR2) CDR2 family Q01850
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
Segment polarity protein dishevelled homolog DVL-3 (DVL3) DSH family Q92997
GRB10-interacting GYF protein 1 (GIGYF1) GIGYF family O75420
Golgin subfamily A member 2 (GOLGA2) GOLGA2 family Q08379
Golgin subfamily A member 6A (GOLGA6A) GOLGA6 family Q9NYA3
Progranulin (GRN) Granulin family P28799
GRB2-related adapter protein 2 (GRAP2) GRB2/sem-5/DRK family O75791
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Keratin, type I cytoskeletal 16 (KRT16) Intermediate filament family P08779
Peripherin (PRPH) Intermediate filament family P41219
Keratin-associated protein 1-3 (KRTAP1-3) KRTAP type 1 family Q8IUG1
Keratin-associated protein 10-9 (KRTAP10-9) KRTAP type 10 family P60411
Leucine zipper putative tumor suppressor 2 (LZTS2) LZTS2 family Q9BRK4
Harmonin-binding protein USHBP1 (USHBP1) MCC family Q8N6Y0
MORF4 family-associated protein 1 (MRFAP1) MORF4 family-associated protein family Q9Y605
NGFI-A-binding protein 2 (NAB2) NAB family Q15742
Notch homolog 2 N-terminal-like protein A (NOTCH2NLA) NOTCH family Q7Z3S9
NUT family member 1 (NUTM1) NUT family Q86Y26
Dynein axonemal assembly factor 6 (DNAAF6) PIH1 family Q9NQM4
Protein sprouty homolog 1 (SPRY1) Sprouty family O43609
TRAF-interacting protein with FHA domain-containing protein A (TIFA) TIFA family Q96CG3
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
Thyroid receptor-interacting protein 6 (TRIP6) Zyxin/ajuba family Q15654
Aminoacyl tRNA synthase complex-interacting multifunctional protein 2 (AIMP2) . Q13155
Amyloid protein-binding protein 2 (APPBP2) . Q92624
Arginine vasopressin-induced protein 1 (AVPI1) . Q5T686
BTB/POZ domain-containing protein KCTD1 (KCTD1) . Q719H9
BTB/POZ domain-containing protein KCTD9 (KCTD9) . Q7L273
Lethal(3)malignant brain tumor-like protein 3 (L3MBTL3) . Q96JM7
MORN repeat-containing protein 3 (MORN3) . Q6PF18
Nuclear receptor-binding factor 2 (NRBF2) . Q96F24
Protein hinderin (KIAA1328) . Q86T90
RAS protein activator like-3 (RASAL3) . Q86YV0
RING finger protein 11 (RNF11) . Q9Y3C5
RNA-binding protein with multiple splicing (RBPMS) . Q93062
SERTA domain-containing protein 3 (SERTAD3) . Q9UJW9
SH3 and cysteine-rich domain-containing protein 2 (STAC2) . Q6ZMT1
Src-like-adapter 2 (SLA2) . Q9H6Q3
Zinc finger MYND domain-containing protein 12 (ZMYND12) . Q9H0C1

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 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
Topiramate Small molecular drug DB00273

References

1 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
2 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
3 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
4 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
5 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
6 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.
7 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.
8 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
9 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
10 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
11 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
12 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
13 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
14 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.
15 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.
16 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
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 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
19 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.