Details of the Target

General Information of Target

Target ID LDTP13790
Target Name cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A)
Gene Name PDE10A
Gene ID 10846
Synonyms
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A; EC 3.1.4.17
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTFQASHRSAWGKSRKKNWQYEGPTQKLFLKRNNVSAPDGPSDPSISVSSEQSGAQQPPA
LQVERIVDKRKNKKGKTEYLVRWKGYDSEDDTWEPEQHLVNCEEYIHDFNRRHTEKQKES
TLTRTNRTSPNNARKQISRSTNSNFSKTSPKALVIGKDHESKNSQLFAASQKFRKNTAPS
LSSRKNMDLAKSGIKILVPKSPVKSRTAVDGFQSESPEKLDPVEQGQEDTVAPEVAAEKP
VGALLGPGAERARMGSRPRIHPLVPQVPGPVTAAMATGLAVNGKGTSPFMDALTANGTTN
IQTSVTGVTASKRKFIDDRRDQPFDKRLRFSVRQTESAYRYRDIVVRKQDGFTHILLSTK
SSENNSLNPEVMREVQSALSTAAADDSKLVLLSAVGSVFCCGLDFIYFIRRLTDDRKRES
TKMAEAIRNFVNTFIQFKKPIIVAVNGPAIGLGASILPLCDVVWANEKAWFQTPYTTFGQ
SPDGCSTVMFPKIMGGASANEMLLSGRKLTAQEACGKGLVSQVFWPGTFTQEVMVRIKEL
ASCNPVVLEESKALVRCNMKMELEQANERECEVLKKIWGSAQGMDSMLKYLQRKIDEF
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Cyclic nucleotide phosphodiesterase family
Subcellular location
Cytoplasm, cytosol
Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate. May play a critical role in regulating cAMP and cGMP levels in the striatum, a region of the brain that contributes to the control of movement and cognition.
TTD ID
T84133
Uniprot ID
Q9Y233
DrugMap ID
TTJW4LU
Ensemble ID
ENST00000539869.4
HGNC ID
HGNC:8772
ChEMBL ID
CHEMBL4409

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C436(2.51)  LDD3342  [1]
IPM
 Probe Info  		C287(9.92)  LDD1702  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C369(0.96)  LDD1508  [3]
 LDCM0270  AC15 HEK-293T C369(0.91)  LDD1513  [3]
 LDCM0277  AC18 HEK-293T C369(1.00)  LDD1516  [3]
 LDCM0279  AC2 HEK-293T C369(1.06)  LDD1518  [3]
 LDCM0283  AC23 HEK-293T C369(0.96)  LDD1522  [3]
 LDCM0284  AC24 HEK-293T C369(1.12)  LDD1523  [3]
 LDCM0286  AC26 HEK-293T C369(1.12)  LDD1525  [3]
 LDCM0292  AC31 HEK-293T C369(1.14)  LDD1531  [3]
 LDCM0293  AC32 HEK-293T C369(1.02)  LDD1532  [3]
 LDCM0295  AC34 HEK-293T C369(1.06)  LDD1534  [3]
 LDCM0300  AC39 HEK-293T C369(1.09)  LDD1539  [3]
 LDCM0302  AC40 HEK-293T C369(0.97)  LDD1541  [3]
 LDCM0304  AC42 HEK-293T C369(1.01)  LDD1543  [3]
 LDCM0309  AC47 HEK-293T C369(0.96)  LDD1548  [3]
 LDCM0310  AC48 HEK-293T C369(0.99)  LDD1549  [3]
 LDCM0313  AC50 HEK-293T C369(1.09)  LDD1552  [3]
 LDCM0318  AC55 HEK-293T C369(1.01)  LDD1557  [3]
 LDCM0319  AC56 HEK-293T C369(1.05)  LDD1558  [3]
 LDCM0321  AC58 HEK-293T C369(1.01)  LDD1560  [3]
 LDCM0327  AC63 HEK-293T C369(0.96)  LDD1566  [3]
 LDCM0328  AC64 HEK-293T C369(1.06)  LDD1567  [3]
 LDCM0334  AC7 HEK-293T C369(1.13)  LDD1568  [3]
 LDCM0345  AC8 HEK-293T C369(1.03)  LDD1569  [3]
 LDCM0275  AKOS034007705 HEK-293T C369(1.00)  LDD1514  [3]
 LDCM0379  CL11 HEK-293T C369(0.90)  LDD1583  [3]
 LDCM0390  CL12 HEK-293T C369(1.10)  LDD1594  [3]
 LDCM0405  CL18 HEK-293T C369(1.00)  LDD1609  [3]
 LDCM0411  CL23 HEK-293T C369(1.11)  LDD1615  [3]
 LDCM0412  CL24 HEK-293T C369(1.22)  LDD1616  [3]
 LDCM0419  CL30 HEK-293T C369(0.97)  LDD1623  [3]
 LDCM0424  CL35 HEK-293T C369(0.98)  LDD1628  [3]
 LDCM0425  CL36 HEK-293T C369(1.08)  LDD1629  [3]
 LDCM0432  CL42 HEK-293T C369(0.92)  LDD1636  [3]
 LDCM0437  CL47 HEK-293T C369(0.88)  LDD1641  [3]
 LDCM0438  CL48 HEK-293T C369(1.04)  LDD1642  [3]
 LDCM0445  CL54 HEK-293T C369(0.86)  LDD1648  [3]
 LDCM0450  CL59 HEK-293T C369(1.10)  LDD1653  [3]
 LDCM0451  CL6 HEK-293T C369(0.93)  LDD1654  [3]
 LDCM0452  CL60 HEK-293T C369(1.07)  LDD1655  [3]
 LDCM0458  CL66 HEK-293T C369(0.90)  LDD1661  [3]
 LDCM0464  CL71 HEK-293T C369(0.84)  LDD1667  [3]
 LDCM0465  CL72 HEK-293T C369(1.09)  LDD1668  [3]
 LDCM0471  CL78 HEK-293T C369(0.99)  LDD1674  [3]
 LDCM0477  CL83 HEK-293T C369(1.06)  LDD1680  [3]
 LDCM0478  CL84 HEK-293T C369(0.94)  LDD1681  [3]
 LDCM0485  CL90 HEK-293T C369(1.03)  LDD1688  [3]
 LDCM0490  CL95 HEK-293T C369(1.07)  LDD1693  [3]
 LDCM0491  CL96 HEK-293T C369(0.99)  LDD1694  [3]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C287(9.92)  LDD1702  [2]
 LDCM0022  KB02 786-O C297(2.48); C436(2.09)  LDD2247  [1]
 LDCM0023  KB03 786-O C297(2.66); C436(3.64)  LDD2664  [1]
 LDCM0024  KB05 NCI-H1155 C436(2.51)  LDD3342  [1]

The Interaction Atlas With This Target

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
Caffeine Small molecular drug DB00201
Dipyridamole Small molecular drug DB00975
Papaverine Small molecular drug DB01113
Triflusal Small molecular drug DB08814
Phase 2
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lu Af11167 Small molecular drug DC29HL
Pf-02545920 Small molecular drug D0OH2W
Tofisopam Small molecular drug DB82TO
Oms824 . D0U3QK
Tak-063 . D09UZL
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pbf-999 Small molecular drug DJ0P6A
Amg 579 . D0X0PP
Frm-6308 . D09GPI
Rg7203 . D0LB6D
Investigative
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mardepodect Small molecular drug DB08387
Trapidil Small molecular drug DB09283
2-({4-[4-(Pyridin-4-ylmethyl)-1h-pyrazol-3-yl]Phenoxy}Methyl)Quinoline . DB08384
2-{[4-(4-pyridin-4-yl-1h-pyrazol-3-yl)Phenoxy]Methyl}Quinoline . DB08386
45-bis(4-methoxyphenyl)-2-thiophen-2-yl-1h-imidazole . DB08383
67-dimethoxy-4-[(3r)-3-(2-naphthyloxy)Pyrrolidin-1-yl]Quinazoline . DB08389
Pq-10 . DB08391
Patented
Click To Hide/Show 31 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,2,4-triazole [4,3-a]Quinoxaline Derivative 1 Small molecular drug D09BDD
1,2,4-triazole [4,3-a]Quinoxaline Derivative 2 Small molecular drug D0RI3W
1,2,4-triazole [4,3-a]Quinoxaline Derivative 3 Small molecular drug D0J6KS
1-aryl-4-methyl-[1,2,4]Triazolo[4,3-a]Quinoxaline Derivative 3 Small molecular drug D0LI6Z
1-aryl-4-methyl-[1,2,4]Triazolo[4,3-a]Quinoxaline Derivative 4 Small molecular drug D0QE7X
1-aryl-4-methyl-[1,2,4]Triazolo[4,3-a]Quinoxaline Derivative 5 Small molecular drug D0X2UO
1-aryl-4-methyl-[1,2,4]Triazolo[4,3-a]Quinoxaline Derivative 6 Small molecular drug D0FV3G
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 1 Small molecular drug D0D4YR
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 2 Small molecular drug D00YOY
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 3 Small molecular drug D07EUB
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 4 Small molecular drug D07NRP
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 5 Small molecular drug D07ZTT
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 6 Small molecular drug D0PP8O
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 7 Small molecular drug D0JJ8K
Imidazo[5,1-c]Pyrido[2,3-e][1,2,4]Triazine Derivative 8 Small molecular drug D0J8YF
Imidazo[5,1-c][1,2,4]Benzotriazine Derivative 1 Small molecular drug D0QI8G
Imidazo[5,1-c][1,2,4]Benzotriazine Derivative 2 Small molecular drug D0I5UY
Imidazo[5,1-c][1,2,4]Benzotriazine Derivative 3 Small molecular drug D0MK7X
Imidazo[5,1-c][1,2,4]Benzotriazine Derivative 4 Small molecular drug D0L6AM
Pmid27321640-compound-58 Small molecular drug D02PFP
Pmid27321640-compound-59 Small molecular drug D09RWM
Pyrido[1,2,4]Triazolo[4,3-a]Pyrazine Derivative 1 Small molecular drug D0Z4IA
Pyrido[1,2,4]Triazolo[4,3-a]Pyrazine Derivative 2 Small molecular drug D0D0QT
Pyrido[1,2,4]Triazolo[4,3-a]Pyrazine Derivative 3 Small molecular drug D0SV1I
Pyrido[3,2-e][1,2,4]Triazolo[4,3-a]Pyrazine Derivative 1 Small molecular drug D01LSP
Pyrido[3,2-e][1,2,4]Triazolo[4,3-a]Pyrazine Derivative 2 Small molecular drug D0T8WU
Triazolo-pyridine Derivative 2 Small molecular drug D0U3KV
Triazolo-pyridine Derivative 3 Small molecular drug D0Z8VY
Triazolo-pyridine Derivative 4 Small molecular drug D05VBJ
Triazolo-pyridine Derivative 5 Small molecular drug D01ITP
Triazolo-pyridine Derivative 6 Small molecular drug D0A8EV

References

1 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
2 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
3 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