Details of the Target

General Information of Target

Target ID LDTP01018
Target Name High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A (PDE8A)
Gene Name PDE8A
Gene ID 5151
Synonyms
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A; EC 3.1.4.53
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSG
KKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACF
LDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGF
TRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYA
NPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNI
QQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSL
DVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLE
ILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPIS
LDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRS
WLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDH
PGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQG
IIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRM
LIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQIS
FIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Cyclic nucleotide phosphodiesterase family, PDE8 subfamily
Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in maintaining basal levels of the cyclic nucleotide and/or in the cAMP regulation of germ cell development. Binding to RAF1 reduces RAF1 'Ser-259' inhibitory-phosphorylation and stimulates RAF1-dependent EGF-activated ERK-signaling. Protects against cell death induced by hydrogen peroxide and staurosporine.
TTD ID
T05904
Uniprot ID
O60658
DrugMap ID
TTIS4OW
Ensemble ID
ENST00000310298.8
HGNC ID
HGNC:8793
ChEMBL ID
CHEMBL4640

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL148 SNV: p.H510R .
EFO27 Deletion: p.K269RfsTer8 .
HCC15 SNV: p.I147V .
Ishikawa (Heraklio) 02 ER SNV: p.E426A .
KNS81FD Insertion: p.A103SfsTer4 .
NCIH1993 SNV: p.A22E .
OZ SNV: p.A48S .
RKO SNV: p.T604A DBIA    Probe Info 
SUPT1 SNV: p.G815E .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
AHL-Pu-1
 Probe Info  		C338(4.60)  LDD0168  [1]
DBIA
 Probe Info  		C279(1.26); C119(1.01)  LDD0080  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0162  [3]
WYneO
 Probe Info  		N.A.  LDD0022  [4]
IPM
 Probe Info  		C338(0.00); C326(0.00)  LDD2156  [5]
TFBX
 Probe Info  		N.A.  LDD0148  [6]
VSF
 Probe Info  		N.A.  LDD0007  [4]
NAIA_5
 Probe Info  		N.A.  LDD2223  [7]
PAL-AfBPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C376
 Probe Info  		7.26  LDD2036  [8]
C378
 Probe Info  		5.86  LDD2037  [8]
C380
 Probe Info  		6.15  LDD2039  [8]
C386
 Probe Info  		7.26  LDD2045  [8]
C429
 Probe Info  		18.51  LDD2084  [8]
C431
 Probe Info  		28.64  LDD2086  [8]
OEA-DA
 Probe Info  		20.00  LDD0046  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C338(4.60)  LDD0168  [1]
 LDCM0026  4SU-RNA+native RNA HEK-293T C338(3.09)  LDD0169  [1]
 LDCM0214  AC1 HEK-293T C772(1.06); C326(0.79)  LDD1507  [10]
 LDCM0215  AC10 HEK-293T C772(0.97); C326(0.99)  LDD1508  [10]
 LDCM0216  AC100 HEK-293T C724(0.74)  LDD0814  [2]
 LDCM0217  AC101 HEK-293T C724(0.97)  LDD0815  [2]
 LDCM0218  AC102 HEK-293T C724(1.08)  LDD0816  [2]
 LDCM0219  AC103 HEK-293T C724(1.46)  LDD0817  [2]
 LDCM0220  AC104 HEK-293T C724(1.17)  LDD0818  [2]
 LDCM0221  AC105 HEK-293T C724(0.61)  LDD0819  [2]
 LDCM0222  AC106 HEK-293T C724(1.15)  LDD0820  [2]
 LDCM0223  AC107 HEK-293T C724(0.92)  LDD0821  [2]
 LDCM0224  AC108 HEK-293T C724(0.83)  LDD0822  [2]
 LDCM0225  AC109 HEK-293T C724(1.29)  LDD0823  [2]
 LDCM0227  AC110 HEK-293T C724(1.18)  LDD0825  [2]
 LDCM0228  AC111 HEK-293T C724(1.81)  LDD0826  [2]
 LDCM0229  AC112 HEK-293T C724(1.18)  LDD0827  [2]
 LDCM0237  AC12 HEK-293T C338(1.09); C772(1.06)  LDD1510  [10]
 LDCM0246  AC128 HEK-293T C724(0.85)  LDD0844  [2]
 LDCM0247  AC129 HEK-293T C724(1.00)  LDD0845  [2]
 LDCM0249  AC130 HEK-293T C724(0.92)  LDD0847  [2]
 LDCM0250  AC131 HEK-293T C724(0.92)  LDD0848  [2]
 LDCM0251  AC132 HEK-293T C724(1.03)  LDD0849  [2]
 LDCM0252  AC133 HEK-293T C724(1.15)  LDD0850  [2]
 LDCM0253  AC134 HEK-293T C724(1.23)  LDD0851  [2]
 LDCM0254  AC135 HEK-293T C724(1.04)  LDD0852  [2]
 LDCM0255  AC136 HEK-293T C724(1.16)  LDD0853  [2]
 LDCM0256  AC137 HEK-293T C724(1.30)  LDD0854  [2]
 LDCM0257  AC138 HEK-293T C724(1.37)  LDD0855  [2]
 LDCM0258  AC139 HEK-293T C724(1.30)  LDD0856  [2]
 LDCM0259  AC14 HEK-293T C772(1.04)  LDD1512  [10]
 LDCM0260  AC140 HEK-293T C724(1.20)  LDD0858  [2]
 LDCM0261  AC141 HEK-293T C724(1.46)  LDD0859  [2]
 LDCM0262  AC142 HEK-293T C724(1.16)  LDD0860  [2]
 LDCM0263  AC143 HEK-293T C724(1.23)  LDD0861  [2]
 LDCM0264  AC144 HEK-293T C724(1.43)  LDD0862  [2]
 LDCM0265  AC145 HEK-293T C724(1.35)  LDD0863  [2]
 LDCM0266  AC146 HEK-293T C724(1.51)  LDD0864  [2]
 LDCM0267  AC147 HEK-293T C724(1.70)  LDD0865  [2]
 LDCM0268  AC148 HEK-293T C724(1.29)  LDD0866  [2]
 LDCM0269  AC149 HEK-293T C724(0.96)  LDD0867  [2]
 LDCM0271  AC150 HEK-293T C724(1.24)  LDD0869  [2]
 LDCM0272  AC151 HEK-293T C724(1.29)  LDD0870  [2]
 LDCM0273  AC152 HEK-293T C724(1.26)  LDD0871  [2]
 LDCM0274  AC153 HEK-293T C724(1.28)  LDD0872  [2]
 LDCM0621  AC154 HEK-293T C724(1.18)  LDD2162  [2]
 LDCM0622  AC155 HEK-293T C724(1.19)  LDD2163  [2]
 LDCM0623  AC156 HEK-293T C724(1.58)  LDD2164  [2]
 LDCM0624  AC157 HEK-293T C724(1.90)  LDD2165  [2]
 LDCM0276  AC17 HEK-293T C772(1.07); C326(0.97)  LDD1515  [10]
 LDCM0277  AC18 HEK-293T C772(0.91); C326(1.04)  LDD1516  [10]
 LDCM0279  AC2 HEK-293T C772(1.02); C326(1.08)  LDD1518  [10]
 LDCM0280  AC20 HEK-293T C338(1.00); C772(1.01)  LDD1519  [10]
 LDCM0282  AC22 HEK-293T C772(0.97)  LDD1521  [10]
 LDCM0285  AC25 HEK-293T C772(0.90); C326(0.89)  LDD1524  [10]
 LDCM0286  AC26 HEK-293T C772(1.02); C326(1.01)  LDD1525  [10]
 LDCM0288  AC28 HEK-293T C338(0.96); C772(0.98)  LDD1527  [10]
 LDCM0291  AC30 HEK-293T C772(0.94)  LDD1530  [10]
 LDCM0294  AC33 HEK-293T C772(1.01); C326(0.91)  LDD1533  [10]
 LDCM0295  AC34 HEK-293T C772(1.01); C326(1.07)  LDD1534  [10]
 LDCM0297  AC36 HEK-293T C338(0.94); C772(1.02)  LDD1536  [10]
 LDCM0299  AC38 HEK-293T C772(0.99)  LDD1538  [10]
 LDCM0301  AC4 HEK-293T C338(1.04); C772(0.93)  LDD1540  [10]
 LDCM0303  AC41 HEK-293T C772(1.06); C326(0.87)  LDD1542  [10]
 LDCM0304  AC42 HEK-293T C772(1.03); C326(1.09)  LDD1543  [10]
 LDCM0306  AC44 HEK-293T C338(1.09); C772(1.06)  LDD1545  [10]
 LDCM0308  AC46 HEK-293T C724(1.10)  LDD0906  [2]
 LDCM0309  AC47 HEK-293T C724(0.99)  LDD0907  [2]
 LDCM0310  AC48 HEK-293T C724(1.02)  LDD0908  [2]
 LDCM0311  AC49 HEK-293T C724(1.12)  LDD0909  [2]
 LDCM0313  AC50 HEK-293T C724(0.98)  LDD0911  [2]
 LDCM0314  AC51 HEK-293T C724(1.17)  LDD0912  [2]
 LDCM0315  AC52 HEK-293T C724(1.10)  LDD0913  [2]
 LDCM0316  AC53 HEK-293T C724(0.91)  LDD0914  [2]
 LDCM0317  AC54 HEK-293T C724(1.17)  LDD0915  [2]
 LDCM0318  AC55 HEK-293T C724(1.23)  LDD0916  [2]
 LDCM0319  AC56 HEK-293T C724(1.09)  LDD0917  [2]
 LDCM0320  AC57 HEK-293T C724(0.95)  LDD0918  [2]
 LDCM0321  AC58 HEK-293T C724(0.83)  LDD0919  [2]
 LDCM0322  AC59 HEK-293T C724(0.82)  LDD0920  [2]
 LDCM0323  AC6 HEK-293T C772(1.08)  LDD1562  [10]
 LDCM0324  AC60 HEK-293T C724(0.89)  LDD0922  [2]
 LDCM0325  AC61 HEK-293T C724(1.14)  LDD0923  [2]
 LDCM0326  AC62 HEK-293T C724(0.86)  LDD0924  [2]
 LDCM0327  AC63 HEK-293T C724(0.97)  LDD0925  [2]
 LDCM0328  AC64 HEK-293T C724(0.85)  LDD0926  [2]
 LDCM0329  AC65 HEK-293T C724(1.06)  LDD0927  [2]
 LDCM0330  AC66 HEK-293T C724(0.80)  LDD0928  [2]
 LDCM0331  AC67 HEK-293T C724(0.92)  LDD0929  [2]
 LDCM0332  AC68 HEK-293T C724(0.90)  LDD0930  [2]
 LDCM0333  AC69 HEK-293T C724(0.88)  LDD0931  [2]
 LDCM0335  AC70 HEK-293T C724(1.03)  LDD0933  [2]
 LDCM0336  AC71 HEK-293T C724(1.10)  LDD0934  [2]
 LDCM0337  AC72 HEK-293T C724(0.91)  LDD0935  [2]
 LDCM0338  AC73 HEK-293T C724(1.17)  LDD0936  [2]
 LDCM0339  AC74 HEK-293T C724(2.02)  LDD0937  [2]
 LDCM0340  AC75 HEK-293T C724(1.17)  LDD0938  [2]
 LDCM0341  AC76 HEK-293T C724(0.96)  LDD0939  [2]
 LDCM0342  AC77 HEK-293T C724(1.03)  LDD0940  [2]
 LDCM0343  AC78 HEK-293T C724(1.07)  LDD0941  [2]
 LDCM0344  AC79 HEK-293T C724(1.14)  LDD0942  [2]
 LDCM0346  AC80 HEK-293T C724(1.19)  LDD0944  [2]
 LDCM0347  AC81 HEK-293T C724(1.09)  LDD0945  [2]
 LDCM0348  AC82 HEK-293T C724(1.50)  LDD0946  [2]
 LDCM0365  AC98 HEK-293T C724(1.13)  LDD0963  [2]
 LDCM0366  AC99 HEK-293T C724(0.73)  LDD0964  [2]
 LDCM0356  AKOS034007680 HEK-293T C772(1.00); C326(0.90)  LDD1570  [10]
 LDCM0632  CL-Sc Hep-G2 C338(2.96); C279(0.83); C119(0.81)  LDD2227  [7]
 LDCM0367  CL1 HEK-293T C772(1.05); C528(1.00)  LDD1571  [10]
 LDCM0368  CL10 HEK-293T C772(1.07)  LDD1572  [10]
 LDCM0369  CL100 HEK-293T C772(0.98); C326(1.11)  LDD1573  [10]
 LDCM0370  CL101 HEK-293T C772(0.91); C528(0.99)  LDD1574  [10]
 LDCM0371  CL102 HEK-293T C772(1.06)  LDD1575  [10]
 LDCM0372  CL103 HEK-293T C772(0.96)  LDD1576  [10]
 LDCM0373  CL104 HEK-293T C772(1.12); C326(1.07)  LDD1577  [10]
 LDCM0374  CL105 HEK-293T C772(0.99); C528(1.00)  LDD1578  [10]
 LDCM0375  CL106 HEK-293T C772(1.05)  LDD1579  [10]
 LDCM0376  CL107 HEK-293T C772(0.96)  LDD1580  [10]
 LDCM0377  CL108 HEK-293T C772(1.07); C326(1.04)  LDD1581  [10]
 LDCM0378  CL109 HEK-293T C772(0.95); C528(0.99)  LDD1582  [10]
 LDCM0380  CL110 HEK-293T C772(0.88)  LDD1584  [10]
 LDCM0381  CL111 HEK-293T C772(0.88)  LDD1585  [10]
 LDCM0382  CL112 HEK-293T C772(1.17); C326(1.05)  LDD1586  [10]
 LDCM0383  CL113 HEK-293T C772(1.21); C528(1.09)  LDD1587  [10]
 LDCM0384  CL114 HEK-293T C772(0.91)  LDD1588  [10]
 LDCM0385  CL115 HEK-293T C772(0.91)  LDD1589  [10]
 LDCM0386  CL116 HEK-293T C772(0.98); C326(1.11)  LDD1590  [10]
 LDCM0387  CL117 HEK-293T C772(0.98); C528(1.19)  LDD1591  [10]
 LDCM0388  CL118 HEK-293T C772(1.12)  LDD1592  [10]
 LDCM0389  CL119 HEK-293T C772(1.00)  LDD1593  [10]
 LDCM0391  CL120 HEK-293T C772(1.14); C326(1.06)  LDD1595  [10]
 LDCM0392  CL121 HEK-293T C724(1.11)  LDD0990  [2]
 LDCM0393  CL122 HEK-293T C724(1.09)  LDD0991  [2]
 LDCM0394  CL123 HEK-293T C724(0.98)  LDD0992  [2]
 LDCM0395  CL124 HEK-293T C724(1.25)  LDD0993  [2]
 LDCM0396  CL125 HEK-293T C724(0.99)  LDD0994  [2]
 LDCM0397  CL126 HEK-293T C724(0.93)  LDD0995  [2]
 LDCM0398  CL127 HEK-293T C724(0.81)  LDD0996  [2]
 LDCM0399  CL128 HEK-293T C724(1.00)  LDD0997  [2]
 LDCM0400  CL13 HEK-293T C772(1.03); C528(1.24)  LDD1604  [10]
 LDCM0401  CL14 HEK-293T C772(1.02)  LDD1605  [10]
 LDCM0402  CL15 HEK-293T C772(0.93)  LDD1606  [10]
 LDCM0403  CL16 HEK-293T C724(1.02)  LDD1001  [2]
 LDCM0404  CL17 HEK-293T C724(1.00)  LDD1002  [2]
 LDCM0405  CL18 HEK-293T C724(1.08)  LDD1003  [2]
 LDCM0406  CL19 HEK-293T C724(1.07)  LDD1004  [2]
 LDCM0407  CL2 HEK-293T C772(0.84)  LDD1611  [10]
 LDCM0408  CL20 HEK-293T C724(1.08)  LDD1006  [2]
 LDCM0409  CL21 HEK-293T C724(1.52)  LDD1007  [2]
 LDCM0410  CL22 HEK-293T C724(1.05)  LDD1008  [2]
 LDCM0411  CL23 HEK-293T C724(1.08)  LDD1009  [2]
 LDCM0412  CL24 HEK-293T C724(0.96)  LDD1010  [2]
 LDCM0413  CL25 HEK-293T C724(1.23)  LDD1011  [2]
 LDCM0414  CL26 HEK-293T C724(0.88)  LDD1012  [2]
 LDCM0415  CL27 HEK-293T C724(0.97)  LDD1013  [2]
 LDCM0416  CL28 HEK-293T C724(1.02)  LDD1014  [2]
 LDCM0417  CL29 HEK-293T C724(0.95)  LDD1015  [2]
 LDCM0418  CL3 HEK-293T C772(0.99)  LDD1622  [10]
 LDCM0419  CL30 HEK-293T C724(1.23)  LDD1017  [2]
 LDCM0421  CL32 HEK-293T C338(1.04); C772(1.10)  LDD1625  [10]
 LDCM0423  CL34 HEK-293T C772(1.18)  LDD1627  [10]
 LDCM0426  CL37 HEK-293T C772(0.92); C528(0.96)  LDD1630  [10]
 LDCM0428  CL39 HEK-293T C772(0.89)  LDD1632  [10]
 LDCM0429  CL4 HEK-293T C772(1.07); C326(1.07)  LDD1633  [10]
 LDCM0430  CL40 HEK-293T C772(0.98); C326(1.28)  LDD1634  [10]
 LDCM0431  CL41 HEK-293T C772(0.96); C326(0.97)  LDD1635  [10]
 LDCM0432  CL42 HEK-293T C772(1.00); C326(1.07)  LDD1636  [10]
 LDCM0434  CL44 HEK-293T C338(1.10); C772(0.99)  LDD1638  [10]
 LDCM0436  CL46 HEK-293T C772(1.15)  LDD1640  [10]
 LDCM0439  CL49 HEK-293T C772(1.00); C528(1.12)  LDD1643  [10]
 LDCM0440  CL5 HEK-293T C772(0.95); C326(0.90)  LDD1644  [10]
 LDCM0441  CL50 HEK-293T C772(0.96)  LDD1645  [10]
 LDCM0443  CL52 HEK-293T C772(1.23); C326(1.00)  LDD1646  [10]
 LDCM0444  CL53 HEK-293T C772(1.02); C326(0.84)  LDD1647  [10]
 LDCM0445  CL54 HEK-293T C772(0.95); C326(1.01)  LDD1648  [10]
 LDCM0447  CL56 HEK-293T C338(1.06); C772(1.04)  LDD1650  [10]
 LDCM0449  CL58 HEK-293T C772(1.17)  LDD1652  [10]
 LDCM0451  CL6 HEK-293T C772(0.87); C326(0.97)  LDD1654  [10]
 LDCM0453  CL61 HEK-293T C772(1.09); C528(1.00)  LDD1656  [10]
 LDCM0454  CL62 HEK-293T C772(1.02)  LDD1657  [10]
 LDCM0455  CL63 HEK-293T C772(0.97)  LDD1658  [10]
 LDCM0456  CL64 HEK-293T C772(1.24); C326(0.98)  LDD1659  [10]
 LDCM0457  CL65 HEK-293T C772(1.04); C326(0.89)  LDD1660  [10]
 LDCM0458  CL66 HEK-293T C772(1.02); C326(1.15)  LDD1661  [10]
 LDCM0460  CL68 HEK-293T C338(1.02); C772(1.03)  LDD1663  [10]
 LDCM0463  CL70 HEK-293T C772(1.12)  LDD1666  [10]
 LDCM0466  CL73 HEK-293T C772(0.92); C528(1.27)  LDD1669  [10]
 LDCM0467  CL74 HEK-293T C772(1.00)  LDD1670  [10]
 LDCM0469  CL76 HEK-293T C772(1.03); C326(0.93)  LDD1672  [10]
 LDCM0470  CL77 HEK-293T C772(1.04); C326(0.90)  LDD1673  [10]
 LDCM0471  CL78 HEK-293T C772(1.02); C326(0.97)  LDD1674  [10]
 LDCM0473  CL8 HEK-293T C338(1.15); C772(0.83)  LDD1676  [10]
 LDCM0474  CL80 HEK-293T C338(0.99); C772(1.04)  LDD1677  [10]
 LDCM0476  CL82 HEK-293T C772(1.05)  LDD1679  [10]
 LDCM0479  CL85 HEK-293T C772(1.05); C528(1.17)  LDD1682  [10]
 LDCM0480  CL86 HEK-293T C772(0.94)  LDD1683  [10]
 LDCM0481  CL87 HEK-293T C772(0.83)  LDD1684  [10]
 LDCM0482  CL88 HEK-293T C772(1.04); C326(1.01)  LDD1685  [10]
 LDCM0483  CL89 HEK-293T C772(0.96); C326(0.94)  LDD1686  [10]
 LDCM0485  CL90 HEK-293T C772(1.02); C326(1.36)  LDD1688  [10]
 LDCM0487  CL92 HEK-293T C338(0.94); C772(0.94)  LDD1690  [10]
 LDCM0489  CL94 HEK-293T C772(0.97)  LDD1692  [10]
 LDCM0492  CL97 HEK-293T C772(0.75); C528(1.10)  LDD1695  [10]
 LDCM0493  CL98 HEK-293T C772(0.93)  LDD1696  [10]
 LDCM0494  CL99 HEK-293T C772(0.88)  LDD1697  [10]
 LDCM0495  E2913 HEK-293T C772(0.91)  LDD1698  [10]
 LDCM0468  Fragment33 HEK-293T C772(1.07)  LDD1671  [10]
 LDCM0427  Fragment51 HEK-293T C772(0.89)  LDD1631  [10]
 LDCM0022  KB02 HCT 116 C279(1.26); C119(1.01)  LDD0080  [2]
 LDCM0023  KB03 HCT 116 C279(1.22); C119(1.33)  LDD0081  [2]
 LDCM0024  KB05 HCT 116 C279(1.65); C119(1.05)  LDD0082  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Caffeine Small molecular drug DB00201
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
3-isobutyl-1-methyl-7h-xanthine Small molecular drug DB07954
Trapidil Small molecular drug DB09283
Pf-04957325 . D04TZA
Pf-4957325-00 . D0TE9G
Patented
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ac1m1sp5 Small molecular drug D0Z7YQ
Bc11-28 Small molecular drug D0SH7F
Us8846654, 11 Small molecular drug D0EF6R
Us8846654, 251 Small molecular drug D0A5JS
Us8846654, 294 Small molecular drug D05SRL
Us9493447, 1001 Small molecular drug D0EN2M

References

1 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
2 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
3 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
4 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
5 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
6 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
7 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
8 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
9 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
10 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