Protein Information

General Information of the Protein

Protein ID	PT01875
Protein Name	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Gene Name	PDE10A
Sequence	MASLEEPLAPRPQGPLPAAGDEPGCGPGKLRPEPRLSAAGGGSAAGPGPAPEWPGRGRAERAAPPRPPLSSAGRPSPAGGPGALSARGGGCGWVAARAPLALAFSSRVPSSSPSFFYFWPPPPPPPPSFLPSSSAFHLPVRLPGREGAAAAAAAGGGGDAGGGGGGGQEAAPLSVPTSSSHRGGGGSGGGRRRLFLSPALQGLLLPARAGPRPPPPPRLPLGQAARRAGSPGFPGAGPGGGGQTPRRPQGASFALAAAAALLFGSDMEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGPITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Phosphodiesterase > Phosphodiesterase 10 > Phosphodiesterase 10A
Function	Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides (PubMed:10373451, PubMed:10393245, PubMed:16330539, PubMed:27058447, PubMed:17389385). Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate (PubMed:10373451, PubMed:10393245, PubMed:27058447, PubMed:17389385). 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 (PubMed:27058447). Show/Hide
Uniprot ID	Primary ID: Q9Y233 Secondarily ID: A0A3F2YP58 Q6FHX1 Q9HCP9 Q9NTV4 Q9ULW9 Q9Y5T1 Show/Hide
Ensembl ID	ENSG00000112541
HGNC ID	HGNC:8772
Subcellular Location	Cytoplasm Cytosol

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000192 , AD-293

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0400720 Compound Info	US9200001, 13 Show/Hide	C27H25N7O2	1
1	Ki = 0.01 nM Bioactivity Info	TI LI LO TS
CP0472525 Compound Info	US8785467, 1-27 Show/Hide	C21H23ClN6OS	1
1	Ki = 0.02 nM Bioactivity Info	TI LI LO TS
CP0521287 Compound Info	US9062059, 2-27 Show/Hide	C21H21N7OS	1
1	Ki = 0.02 nM Bioactivity Info	TI LI LO TS
CP0521535 Compound Info	US9200001, 2 Show/Hide	C28H24N6O2	1
1	Ki = 0.023 nM Bioactivity Info	TI LI LO TS
CP0506743 Compound Info	US9200001, 16 Show/Hide	C27H27N7O2	1
1	Ki = 0.027 nM Bioactivity Info	TI LI LO TS
CP0859111 Compound Info	US9200001, 25 Show/Hide	C27H27N7O2	1
1	Ki = 0.027 nM Bioactivity Info	TI LI LO TS
CP0521536 Compound Info	US9200001, 8 Show/Hide	C27H27N7O2	1
1	Ki = 0.028 nM Bioactivity Info	TI LI LO TS
CP0563887 Compound Info	US9062059, 1-2 Show/Hide	C19H22N6O	1
1	Ki = 0.03 nM Bioactivity Info	TI LI LO TS
CP0452638 Compound Info	US8785467, 1-32 Show/Hide	C21H21ClN6O2S	1
1	Ki = 0.04 nM Bioactivity Info	TI LI LO TS
CP0488810 Compound Info	US9062059, 2-3 Show/Hide	C20H24N6O	1
1	Ki = 0.04 nM Bioactivity Info	TI LI LO TS
CP0475394 Compound Info	US8975261, I-42 Show/Hide	C24H20N6O	1
1	Ki = 0.04 nM Bioactivity Info	TI LI LO TS
CP0411005 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-2-(3-imidazo[1,2-a]pyridin-2-ylpropoxy)-5-methylpyrimidin-4-amine Show/Hide	C21H23ClN6OS	1
1	Ki = 0.047 nM Bioactivity Info	TI LI LO TS
CP0575642 Compound Info	US9062059, 2-53 Show/Hide	C18H21N7O2S	1
1	Ki = 0.05 nM Bioactivity Info	TI LI LO TS
CP0384996 Compound Info	2-[3-(1,3-benzothiazol-2-yl)propoxy]-6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methylpyrimidin-4-amine Show/Hide	C21H22ClN5OS2	1
1	Ki = 0.055 nM Bioactivity Info	TI LI LO TS
CP0549907 Compound Info	US9200001, 15 Show/Hide	C26H26N8O2	1
1	Ki = 0.056 nM Bioactivity Info	TI LI LO TS
CP0557971 Compound Info	US9200001, 34 Show/Hide	C28H27N7O2	1
1	Ki = 0.068 nM Bioactivity Info	TI LI LO TS
CP0419269 Compound Info	US9200001, 7 Show/Hide	C27H23N7O2	1
1	Ki = 0.073 nM Bioactivity Info	TI LI LO TS
CP0424181 Compound Info	US9062059, 9-2 Show/Hide	C21H24N6OS	1
1	Ki = 0.08 nM Bioactivity Info	TI LI LO TS
CP0549912 Compound Info	US9200001, 61 Show/Hide	C20H18N8	1
1	Ki = 0.085 nM Bioactivity Info	TI LI LO TS
CP0488812 Compound Info	US9062059, 3-25 Show/Hide	C20H22FN7OS	1
1	Ki = 0.09 nM Bioactivity Info	TI LI LO TS
CP0548843 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-[3-(1,8-naphthyridin-2-yl)propoxy]pyrimidin-4-amine Show/Hide	C22H23ClN6OS	1
1	Ki = 0.11 nM Bioactivity Info	TI LI LO TS
CP0549908 Compound Info	US9200001, 20 Show/Hide	C25H26N6O2	1
1	Ki = 0.11 nM Bioactivity Info	TI LI LO TS
CP0429119 Compound Info	US9200001, 5 Show/Hide	C25H28N6O2	1
1	Ki = 0.14 nM Bioactivity Info	TI LI LO TS
CP0549910 Compound Info	US9200001, 50 Show/Hide	C17H20N6	1
1	Ki = 0.14 nM Bioactivity Info	TI LI LO TS
CP0517411 Compound Info	US8975261, I-31 Show/Hide	C21H25N3O3	1
1	Ki = 0.15 nM Bioactivity Info	TI LI LO TS
CP0549909 Compound Info	US9200001, 49 Show/Hide	C24H24N6	1
1	Ki = 0.21 nM Bioactivity Info	TI LI LO TS
CP0563314 Compound Info	US9200001, 35 Show/Hide	C26H28N6O2	1
1	Ki = 0.21 nM Bioactivity Info	TI LI LO TS
CP0542955 Compound Info	US8975261, I-36 Show/Hide	C22H24N4O3	1
1	Ki = 0.22 nM Bioactivity Info	TI LI LO TS
CP0442232 Compound Info	US8975261, LL3 Show/Hide	C23H23N5O3	1
1	Ki = 0.23 nM Bioactivity Info	TI LI LO TS
CP0475393 Compound Info	US8975261, MM4 Show/Hide	C19H21N5O2	1
1	Ki = 0.25 nM Bioactivity Info	TI LI LO TS
CP0532985 Compound Info	US8975261, I-39 Show/Hide	C22H24N4O2	1
1	Ki = 0.34 nM Bioactivity Info	TI LI LO TS
CP0541118 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-(3-quinoxalin-2-ylpropoxy)pyrimidin-4-amine Show/Hide	C22H23ClN6OS	1
1	Ki = 0.37 nM Bioactivity Info	TI LI LO TS
CP0402514 Compound Info	US9200001, 133 Show/Hide	C24H28N8	1
1	Ki = 0.37 nM Bioactivity Info	TI LI LO TS
CP0521541 Compound Info	US9200001, 69 Show/Hide	C20H21N7S	1
1	Ki = 0.37 nM Bioactivity Info	TI LI LO TS
CP0426303 Compound Info	US9200001, 43 Show/Hide	C26H28N6O3	1
1	Ki = 0.39 nM Bioactivity Info	TI LI LO TS
CP0555251 Compound Info	US9200001, 92 Show/Hide	C21H23N7	1
1	Ki = 0.4 nM Bioactivity Info	TI LI LO TS
CP0549922 Compound Info	US9200001, 136 Show/Hide	C23H25N7O	1
1	Ki = 0.42 nM Bioactivity Info	TI LI LO TS
CP0418121 Compound Info	US9200001, 91 Show/Hide	C21H23N7O	1
1	Ki = 0.49 nM Bioactivity Info	TI LI LO TS
CP0524431 Compound Info	US9062059, 3-13 Show/Hide	C18H20FN7O2S	1
1	Ki = 0.5 nM Bioactivity Info	TI LI LO TS
CP0566294 Compound Info	US9200001, 42 Show/Hide	C26H29N7O2	1
1	Ki = 0.5 nM Bioactivity Info	TI LI LO TS
CP0518970 Compound Info	US9200001, 63 Show/Hide	C21H23N7O	1
1	Ki = 0.54 nM Bioactivity Info	TI LI LO TS
CP0557579 Compound Info	US9200001, 134 Show/Hide	C23H25FN8	1
1	Ki = 0.58 nM Bioactivity Info	TI LI LO TS
CP0506772 Compound Info	US9062059, 2-4 Show/Hide	C24H26N6O	1
1	Ki = 0.6 nM Bioactivity Info	TI LI LO TS
CP0475395 Compound Info	US8975261, TT1 Show/Hide	C22H22N4O2	1
1	Ki = 0.6 nM Bioactivity Info	TI LI LO TS
CP0518980 Compound Info	US9200001, 113 Show/Hide	C22H25N7O	1
1	Ki = 0.62 nM Bioactivity Info	TI LI LO TS
CP0518971 Compound Info	US9200001, 66 Show/Hide	C23H27N7O2	1
1	Ki = 0.63 nM Bioactivity Info	TI LI LO TS
CP0412256 Compound Info	US9200001, 112 Show/Hide	C22H23N7	1
1	Ki = 0.68 nM Bioactivity Info	TI LI LO TS
CP0413235 Compound Info	US9200001, 132 Show/Hide	C22H22F2N8	1
1	Ki = 0.75 nM Bioactivity Info	TI LI LO TS
CP0559641 Compound Info	US9200001, 62 Show/Hide	C20H22N8	1
1	Ki = 0.77 nM Bioactivity Info	TI LI LO TS
CP0464473 Compound Info	US8975261, I-57 Show/Hide	C19H20N4O2S	1
1	Ki = 0.78 nM Bioactivity Info	TI LI LO TS
CP0442234 Compound Info	US8975261, I-73 Show/Hide	C21H22N4O2	1
1	Ki = 0.8 nM Bioactivity Info	TI LI LO TS
CP0561323 Compound Info	US9200001, 14 Show/Hide	C27H23N7O2	1
1	Ki = 0.82 nM Bioactivity Info	TI LI LO TS
CP0555254 Compound Info	US9200001, 137 Show/Hide	C24H27N7O	1
1	Ki = 0.84 nM Bioactivity Info	TI LI LO TS
CP0518981 Compound Info	US9200001, 131 Show/Hide	C22H25N7O	1
1	Ki = 0.88 nM Bioactivity Info	TI LI LO TS
CP0559642 Compound Info	US9200001, 67 Show/Hide	C23H27N7O2	1
1	Ki = 0.9 nM Bioactivity Info	TI LI LO TS
CP0518976 Compound Info	US9200001, 83 Show/Hide	C21H23N7	1
1	Ki = 0.96 nM Bioactivity Info	TI LI LO TS
CP0488813 Compound Info	US9062059, 8-8 Show/Hide	C23H23N7OS	1
1	Ki = 1 nM Bioactivity Info	TI LI LO TS
CP0426304 Compound Info	US9200001, 65 Show/Hide	C22H25N7O2	1
1	Ki = 1.08 nM Bioactivity Info	TI LI LO TS
CP0521539 Compound Info	US9200001, 64 Show/Hide	C21H23N7O2	1
1	Ki = 1.09 nM Bioactivity Info	TI LI LO TS
CP0488814 Compound Info	US9062059, 12-2 Show/Hide	C19H21N5O2	1
1	Ki = 1.1 nM Bioactivity Info	TI LI LO TS
CP0506932 Compound Info	US9062059, 3-8 Show/Hide	C18H19FN6OS	1
1	Ki = 1.1 nM Bioactivity Info	TI LI LO TS
CP0490791 Compound Info	US9200001, 135 Show/Hide	C23H26N8O	1
1	Ki = 1.1 nM Bioactivity Info	TI LI LO TS
CP0527313 Compound Info	US9200001, 97 Show/Hide	C24H27N7O	1
1	Ki = 1.1 nM Bioactivity Info	TI LI LO TS
CP0566301 Compound Info	US9200001, 120 Show/Hide	C23H25N7O	1
1	Ki = 1.1 nM Bioactivity Info	TI LI LO TS
CP0490789 Compound Info	US9200001, 119 Show/Hide	C21H23N7	1
1	Ki = 1.2 nM Bioactivity Info	TI LI LO TS
CP0506732 Compound Info	US9200001, 114 Show/Hide	C21H24N8	1
1	Ki = 1.2 nM Bioactivity Info	TI LI LO TS
CP0521546 Compound Info	US9200001, 122 Show/Hide	C21H22FN7O	1
1	Ki = 1.2 nM Bioactivity Info	TI LI LO TS
CP0549919 Compound Info	US9200001, 116 Show/Hide	C23H26N8	1
1	Ki = 1.2 nM Bioactivity Info	TI LI LO TS
CP0521545 Compound Info	US9200001, 111 Show/Hide	C20H21N7O	1
1	Ki = 1.3 nM Bioactivity Info	TI LI LO TS
CP0564913 Compound Info	US9200001, 138 Show/Hide	C23H25N7O2	1
1	Ki = 1.3 nM Bioactivity Info	TI LI LO TS
CP0484147 Compound Info	US9200001, 86 Show/Hide	C21H23N7O	1
1	Ki = 1.4 nM Bioactivity Info	TI LI LO TS
CP0518979 Compound Info	US9200001, 109 Show/Hide	C20H18F3N7	1
1	Ki = 1.4 nM Bioactivity Info	TI LI LO TS
CP0521538 Compound Info	US9200001, 37 Show/Hide	C20H21N7	1
1	Ki = 1.4 nM Bioactivity Info	TI LI LO TS
CP0569134 Compound Info	US9200001, 124 Show/Hide	C21H20F3N7O	1
1	Ki = 1.5 nM Bioactivity Info	TI LI LO TS
CP0488815 Compound Info	US9062059, 16-4 Show/Hide	C19H20N8OS	1
1	Ki = 1.6 nM Bioactivity Info	TI LI LO TS
CP0521288 Compound Info	US9062059, 3-11 Show/Hide	C22H25N5OS	1
1	Ki = 1.6 nM Bioactivity Info	TI LI LO TS
CP0518643 Compound Info	US9200001, 130 Show/Hide	C20H20N8O	1
1	Ki = 1.6 nM Bioactivity Info	TI LI LO TS
CP0518969 Compound Info	US9200001, 56 Show/Hide	C22H25N7	1
1	Ki = 1.7 nM Bioactivity Info	TI LI LO TS
CP0566300 Compound Info	US9200001, 118 Show/Hide	C23H28N8	1
1	Ki = 1.7 nM Bioactivity Info	TI LI LO TS
CP0520239 Compound Info	US9200001, 115 Show/Hide	C22H26N8	1
1	Ki = 1.9 nM Bioactivity Info	TI LI LO TS
CP0401026 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine Show/Hide	C18H20ClN5OS	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0418120 Compound Info	US9200001, 88 Show/Hide	C19H18BrN7	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0566302 Compound Info	US9200001, 126 Show/Hide	C23H27N9	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0442846 Compound Info	US9200001, 95 Show/Hide	C22H25N7O	1
1	Ki = 2.1 nM Bioactivity Info	TI LI LO TS
CP0570846 Compound Info	US8975261, RR4 Show/Hide	C25H28N4O3	1
1	Ki = 2.5 nM Bioactivity Info	TI LI LO TS
CP0549918 Compound Info	US9200001, 79 Show/Hide	C25H29N7	1
1	Ki = 2.5 nM Bioactivity Info	TI LI LO TS
CP0960896 Compound Info	US9200001, 89 Show/Hide	C19H19N7	1
1	Ki = 2.6 nM Bioactivity Info	TI LI LO TS
CP0516742 Compound Info	US9200001, 106 Show/Hide	C22H25N7	1
1	Ki = 2.8 nM Bioactivity Info	TI LI LO TS
CP0550298 Compound Info	US9200001, 85 Show/Hide	C22H23N7	1
1	Ki = 2.9 nM Bioactivity Info	TI LI LO TS
CP0412206 Compound Info	US9200001, 93 Show/Hide	C20H20FN7	1
1	Ki = 3.1 nM Bioactivity Info	TI LI LO TS
CP0520240 Compound Info	US9200001, 121 Show/Hide	C24H29N9	1
1	Ki = 3.1 nM Bioactivity Info	TI LI LO TS
CP0536197 Compound Info	US8975261, I-54 Show/Hide	C17H20N6O	1
1	Ki = 3.2 nM Bioactivity Info	TI LI LO TS
CP0559638 Compound Info	US9200001, 4 Show/Hide	C24H26N6O4	1
1	Ki = 3.3 nM Bioactivity Info	TI LI LO TS
CP0575640 Compound Info	US9062059, 2-17 Show/Hide	C20H22F2N6O	1
1	Ki = 3.5 nM Bioactivity Info	TI LI LO TS
CP0518966 Compound Info	US9200001, 36 Show/Hide	C20H21N7	1
1	Ki = 3.5 nM Bioactivity Info	TI LI LO TS
CP0488811 Compound Info	US9062059, 3-19 Show/Hide	C17H17ClFN7OS	1
1	Ki = 3.6 nM Bioactivity Info	TI LI LO TS
CP0575638 Compound Info	US9062059, 2-14 Show/Hide	C20H24N6O2	1
1	Ki = 3.6 nM Bioactivity Info	TI LI LO TS
CP0424179 Compound Info	US9062059, 2-37 Show/Hide	C20H22N6OS	1
1	Ki = 3.8 nM Bioactivity Info	TI LI LO TS
CP0424180 Compound Info	US9062059, 2-58 Show/Hide	C19H21ClN6OS	1
1	Ki = 3.9 nM Bioactivity Info	TI LI LO TS
CP0484148 Compound Info	US9200001, 96 Show/Hide	C25H30N8	1
1	Ki = 3.9 nM Bioactivity Info	TI LI LO TS
CP0479038 Compound Info	US8975261, I-55 Show/Hide	C20H21N5O2S	1
1	Ki = 4.2 nM Bioactivity Info	TI LI LO TS
CP0506731 Compound Info	US9200001, 98 Show/Hide	C22H25N7O	1
1	Ki = 4.2 nM Bioactivity Info	TI LI LO TS
CP0549920 Compound Info	US9200001, 123 Show/Hide	C19H20N8	1
1	Ki = 4.2 nM Bioactivity Info	TI LI LO TS
CP0065329 Compound Info	6-chloro-2-cyclopropyl-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methylpyrimidin-4-amine Show/Hide	C14H17ClN4S	1
1	Ki = 4.8 nM Bioactivity Info	TI LI LO TS
CP0380358 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-propoxypyrimidin-4-amine Show/Hide	C14H19ClN4OS	1
1	Ki = 5.1 nM Bioactivity Info	TI LI LO TS
CP0575643 Compound Info	US9062059, 14-3 Show/Hide	C21H23N5O	1
1	Ki = 5.3 nM Bioactivity Info	TI LI LO TS
CP0412207 Compound Info	US9200001, 94 Show/Hide	C20H21N7O	1
1	Ki = 5.3 nM Bioactivity Info	TI LI LO TS
CP0425571 Compound Info	US9200001, 101 Show/Hide	C23H25N7O	1
1	Ki = 5.8 nM Bioactivity Info	TI LI LO TS
CP0518972 Compound Info	US9200001, 70 Show/Hide	C25H29N7O	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0520241 Compound Info	US9200001, 127 Show/Hide	C21H20N6	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0920562 Compound Info	US9200001, 41 Show/Hide	C19H19N7	1
1	Ki = 6.8 nM Bioactivity Info	TI LI LO TS
CP0407754 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-2-methoxy-5-methylpyrimidin-4-amine Show/Hide	C12H15ClN4OS	1
1	Ki = 8.5 nM Bioactivity Info	TI LI LO TS
CP0549320 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-(2-phenylethoxy)pyrimidin-4-amine Show/Hide	C19H21ClN4OS	1
1	Ki = 9 nM Bioactivity Info	TI LI LO TS
CP0449951 Compound Info	US9200001, 77 Show/Hide	C19H19N7	1
1	Ki = 9 nM Bioactivity Info	TI LI LO TS
CP0897309 Compound Info	US9200001, 68 Show/Hide	C19H18FN7	1
1	Ki = 9.2 nM Bioactivity Info	TI LI LO TS
CP0559640 Compound Info	US9200001, 29 Show/Hide	C23H25N7O2S	1
1	Ki = 9.8 nM Bioactivity Info	TI LI LO TS
CP0520531 Compound Info	US9200001, 74 Show/Hide	C25H24N8	1
1	Ki = 9.9 nM Bioactivity Info	TI LI LO TS
CP0541117 Compound Info	6-chloro-2-cyclopropyl-N-[(2-methoxy-1,3-thiazol-5-yl)methyl]-5-methylpyrimidin-4-amine Show/Hide	C13H15ClN4OS	1
1	Ki = 10 nM Bioactivity Info	TI LI LO TS
CP0425570 Compound Info	US9200001, 87 Show/Hide	C22H26N8	1
1	Ki = 10.6 nM Bioactivity Info	TI LI LO TS
CP0458412 Compound Info	2-[4-chloro-6-[(2,4-dimethyl-1,3-thiazol-5-yl)methylamino]-5-methylpyrimidin-2-yl]oxyethanol Show/Hide	C13H17ClN4O2S	1
1	Ki = 12 nM Bioactivity Info	TI LI LO TS
CP0418119 Compound Info	US9200001, 81 Show/Hide	C24H22N8	1
1	Ki = 12.8 nM Bioactivity Info	TI LI LO TS
CP0530572 Compound Info	US9200001, 75 Show/Hide	C24H27N7O	1
1	Ki = 13 nM Bioactivity Info	TI LI LO TS
CP0559643 Compound Info	US9200001, 73 Show/Hide	C25H24N8	1
1	Ki = 13.1 nM Bioactivity Info	TI LI LO TS
CP0559434 Compound Info	US9200001, 52 Show/Hide	C26H25N7	1
1	Ki = 13.4 nM Bioactivity Info	TI LI LO TS
CP0563958 Compound Info	US9200001, 71 Show/Hide	C22H25N7	1
1	Ki = 13.6 nM Bioactivity Info	TI LI LO TS
CP0564912 Compound Info	US9200001, 100 Show/Hide	C23H27N7	1
1	Ki = 13.8 nM Bioactivity Info	TI LI LO TS
CP0555252 Compound Info	US9200001, 108 Show/Hide	C20H21N7	1
1	Ki = 14.2 nM Bioactivity Info	TI LI LO TS
CP0563290 Compound Info	US9200001, 72 Show/Hide	C23H28N8	1
1	Ki = 14.2 nM Bioactivity Info	TI LI LO TS
CP0954491 Compound Info	US9200001, 53 Show/Hide	C19H18FN7	1
1	Ki = 14.2 nM Bioactivity Info	TI LI LO TS
CP0905975 Compound Info	US9200001, 55 Show/Hide	C20H21N7	1
1	Ki = 16.8 nM Bioactivity Info	TI LI LO TS
CP0487282 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(2-methyl-1,3-thiazol-4-yl)methyl]pyrimidin-4-amine Show/Hide	C13H15ClN4S	1
1	Ki = 18 nM Bioactivity Info	TI LI LO TS
CP0518973 Compound Info	US9200001, 76 Show/Hide	C25H24N8	1
1	Ki = 18.3 nM Bioactivity Info	TI LI LO TS
CP0484783 Compound Info	US9200001, 110 Show/Hide	C21H22N6	1
1	Ki = 18.4 nM Bioactivity Info	TI LI LO TS
CP0521547 Compound Info	US9200001, 125 Show/Hide	C19H19N7O	1
1	Ki = 19 nM Bioactivity Info	TI LI LO TS
CP0859092 Compound Info	US9200001, 54 Show/Hide	C19H17F2N7	1
1	Ki = 25.1 nM Bioactivity Info	TI LI LO TS
CP0384994 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(2-methyl-1,3-thiazol-5-yl)methyl]pyrimidin-4-amine Show/Hide	C13H15ClN4S	1
1	Ki = 26 nM Bioactivity Info	TI LI LO TS
CP0954494 Compound Info	US9200001, 59 Show/Hide	C20H21N7O	1
1	Ki = 30.5 nM Bioactivity Info	TI LI LO TS
CP0954492 Compound Info	US9200001, 57 Show/Hide	C19H18ClN7	1
1	Ki = 30.7 nM Bioactivity Info	TI LI LO TS
CP0954493 Compound Info	US9200001, 58 Show/Hide	C20H21N7	1
1	Ki = 34.9 nM Bioactivity Info	TI LI LO TS
CP0530523 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(1-methylpyrazol-4-yl)methyl]pyrimidin-4-amine Show/Hide	C13H16ClN5	1
1	Ki = 37 nM Bioactivity Info	TI LI LO TS
CP0541116 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidin-4-amine Show/Hide	C13H15ClN4O	1
1	Ki = 38 nM Bioactivity Info	TI LI LO TS
CP0555253 Compound Info	US9200001, 128 Show/Hide	C19H19N7	1
1	Ki = 38 nM Bioactivity Info	TI LI LO TS
CP0954596 Compound Info	US9200001, 90 Show/Hide	C19H19N7	1
1	Ki = 38 nM Bioactivity Info	TI LI LO TS
CP0559433 Compound Info	US9200001, 51 Show/Hide	C25H23N7	1
1	Ki = 38.8 nM Bioactivity Info	TI LI LO TS
CP0506773 Compound Info	US9062059, 2-47 Show/Hide	C21H25N5OS	1
1	Ki = 41.7 nM Bioactivity Info	TI LI LO TS
CP0447801 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(5-methyl-1,2-oxazol-3-yl)methyl]pyrimidin-4-amine Show/Hide	C13H15ClN4O	1
1	Ki = 51 nM Bioactivity Info	TI LI LO TS
CP0868828 Compound Info	US9200001, 60 Show/Hide	C20H19F2N7O	1
1	Ki = 58.2 nM Bioactivity Info	TI LI LO TS
CP0518978 Compound Info	US9200001, 107 Show/Hide	C19H23N7	1
1	Ki = 60.7 nM Bioactivity Info	TI LI LO TS
CP0569476 Compound Info	US8975261, SS1 Show/Hide	C20H24F2N4O2	1
1	Ki = 60.8 nM Bioactivity Info	TI LI LO TS
CP0549906 Compound Info	US9200001, 9 Show/Hide	C24H23N7OS	1
1	Ki = 62 nM Bioactivity Info	TI LI LO TS
CP0518977 Compound Info	US9200001, 99 Show/Hide	C19H19N7	1
1	Ki = 73 nM Bioactivity Info	TI LI LO TS
CP0559639 Compound Info	US9200001, 27 Show/Hide	C23H25N7O3	1
1	Ki = 88 nM Bioactivity Info	TI LI LO TS
CP0419271 Compound Info	US9200001, 40 Show/Hide	C15H17N7S	1
1	Ki = 124 nM Bioactivity Info	TI LI LO TS
CP0549323 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(6-methylpyridin-3-yl)methyl]pyrimidin-4-amine Show/Hide	C15H17ClN4	1
1	Ki = 130 nM Bioactivity Info	TI LI LO TS
CP0538109 Compound Info	6-chloro-2-cyclopropyl-N-(2-fluoroprop-2-enyl)-5-methylpyrimidin-4-amine Show/Hide	C11H13ClFN3	1
1	Ki = 180 nM Bioactivity Info	TI LI LO TS
CP0541826 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-(pyridin-4-ylmethyl)pyrimidin-4-amine Show/Hide	C14H15ClN4	1
1	Ki = 200 nM Bioactivity Info	TI LI LO TS
CP0543547 Compound Info	6-chloro-2-cyclopropyl-N,5-dimethyl-N-[(1-methylpyrazol-4-yl)methyl]pyrimidin-4-amine Show/Hide	C14H18ClN5	1
1	Ki = 220 nM Bioactivity Info	TI LI LO TS
CP0429120 Compound Info	US9200001, 24 Show/Hide	C23H25N7O3	1
1	Ki = 248 nM Bioactivity Info	TI LI LO TS
CP0483994 Compound Info	6-chloro-2-(2-cyclohexylethoxy)-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methylpyrimidin-4-amine Show/Hide	C19H27ClN4OS	1
1	Ki = 400 nM Bioactivity Info	TI LI LO TS
CP0384993 Compound Info	6-chloro-2-cyclopropyl-N,5-dimethyl-N-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidin-4-amine Show/Hide	C14H17ClN4O	1
1	Ki = 540 nM Bioactivity Info	TI LI LO TS
CP0384995 Compound Info	6-chloro-N-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-5-methyl-2-(2-piperidin-2-ylethoxy)pyrimidin-4-amine Show/Hide	C18H26ClN5OS	1
1	Ki = 590 nM Bioactivity Info	TI LI LO TS
CP0456160 Compound Info	6-chloro-2-cyclopropyl-N-(furan-3-ylmethyl)-5-methylpyrimidin-4-amine Show/Hide	C13H14ClN3O	1
1	Ki = 680 nM Bioactivity Info	TI LI LO TS
CP0534501 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-(1,2-oxazol-3-ylmethyl)pyrimidin-4-amine Show/Hide	C12H13ClN4O	1
1	Ki = 810 nM Bioactivity Info	TI LI LO TS
CP0541157 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-propylpyrimidin-4-amine Show/Hide	C11H16ClN3	1
1	Ki = 880 nM Bioactivity Info	TI LI LO TS
CP0380357 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-(1-pyridin-4-ylethyl)pyrimidin-4-amine Show/Hide	C15H17ClN4	1
1	Ki = 890 nM Bioactivity Info	TI LI LO TS
CP0425558 Compound Info	US9200001, 39 Show/Hide	C15H17N7O	1
1	Ki = 918 nM Bioactivity Info	TI LI LO TS
CP0472523 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-(pyridin-3-ylmethyl)pyrimidin-4-amine Show/Hide	C14H15ClN4	1
1	Ki = 1000 nM Bioactivity Info	TI LI LO TS
CP0548841 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-(1,3-thiazol-5-ylmethyl)pyrimidin-4-amine Show/Hide	C12H13ClN4S	1
1	Ki = 1000 nM Bioactivity Info	TI LI LO TS
CP0456159 Compound Info	6-chloro-2-cyclopropyl-N-ethyl-5-methylpyrimidin-4-amine Show/Hide	C10H14ClN3	1
1	Ki = 1200 nM Bioactivity Info	TI LI LO TS
CP0563568 Compound Info	5-(6-chloro-2-cyclopropyl-5-methylpyrimidin-4-yl)-2-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine Show/Hide	C15H17ClN4S	1
1	Ki = 1300 nM Bioactivity Info	TI LI LO TS
CP0450580 Compound Info	N-benzyl-6-chloro-2-cyclopropyl-5-methylpyrimidin-4-amine Show/Hide	C15H16ClN3	1
1	Ki = 1400 nM Bioactivity Info	TI LI LO TS
CP0380356 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[2-(1-methylpyrazol-4-yl)ethyl]pyrimidin-4-amine Show/Hide	C14H18ClN5	1
1	Ki = 1500 nM Bioactivity Info	TI LI LO TS
CP0541155 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(4-methyl-1,3-thiazol-5-yl)methyl]pyrimidin-4-amine Show/Hide	C13H15ClN4S	1
1	Ki = 1600 nM Bioactivity Info	TI LI LO TS
CP0534416 Compound Info	4-chloro-2-cyclopropyl-5-methyl-6-piperidin-1-ylpyrimidine Show/Hide	C13H18ClN3	1
1	Ki = 2100 nM Bioactivity Info	TI LI LO TS
CP0433366 Compound Info	6-chloro-2-cyclopropyl-5-methylpyrimidin-4-amine Show/Hide	C8H10ClN3	1
1	Ki = 2200 nM Bioactivity Info	TI LI LO TS
CP0512530 Compound Info	6-chloro-N-cyclopentyl-2-cyclopropyl-5-methylpyrimidin-4-amine Show/Hide	C13H18ClN3	1
1	Ki = 2800 nM Bioactivity Info	TI LI LO TS
CP0534417 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-propan-2-ylpyrimidin-4-amine Show/Hide	C11H16ClN3	1
1	Ki = 3600 nM Bioactivity Info	TI LI LO TS
CP0563236 Compound Info	4-chloro-2-cyclopropyl-5-methyl-6-piperazin-1-ylpyrimidine Show/Hide	C12H17ClN4	1
1	Ki = 4600 nM Bioactivity Info	TI LI LO TS
CP0528892 Compound Info	4-chloro-2-cyclopropyl-5-methyl-6-pyrrolidin-1-ylpyrimidine Show/Hide	C12H16ClN3	1
1	Ki = 5300 nM Bioactivity Info	TI LI LO TS
CP0384901 Compound Info	6-chloro-2-cyclopropyl-5-methyl-N-[(4-methyl-1,3-thiazol-2-yl)methyl]pyrimidin-4-amine Show/Hide	C13H15ClN4S	1
1	Ki = 6800 nM Bioactivity Info	TI LI LO TS
CP0452650 Compound Info	4,6-dichloro-2-cyclopropyl-5-methylpyrimidine Show/Hide	C8H8Cl2N2	1
1	Ki = 8700 nM Bioactivity Info	TI LI LO TS
CP0449952 Compound Info	US9200001, 84 Show/Hide	C29H36N8O2	1
1	Ki > 75 nM Bioactivity Info	TI LI LO TS
CP0503976 Compound Info	US9200001, 80 Show/Hide	C19H20N8	1
1	Ki > 75 nM Bioactivity Info	TI LI LO TS
CP0518975 Compound Info	US9200001, 78 Show/Hide	C19H19N7O	1
1	Ki > 75 nM Bioactivity Info	TI LI LO TS
CP0530573 Compound Info	US9200001, 105 Show/Hide	C18H19N9S	1
1	Ki > 75 nM Bioactivity Info	TI LI LO TS
CP0550297 Compound Info	US9200001, 82 Show/Hide	C24H22N8	1
1	Ki > 75 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000001 , Jurkat

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0046376 Compound Info	PF-2545920 Show/Hide	C25H20N4O	6
1	IC50 = 0.18 nM
2	IC50 = 0.3 nM
3	IC50 = 0.37 nM
4	IC50 = 1.26 nM
5	IC50 = 1.68 nM
6	IC50 = 2.6 nM
CP0139294 Compound Info	1-(2-chlorophenyl)-6,8-dimethoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H15ClN4O2	1
1	IC50 = 0.28 nM
CP0268614 Compound Info	US9464076, 38 Show/Hide	C28H29N3O4S	1
1	IC50 = 0.42 nM
CP0190119 Compound Info	US9464076, 87 Show/Hide	C24H23N2O7PS	1
1	IC50 = 0.99 nM
CP0139291 Compound Info	6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H14F3N5O	1
1	IC50 = 1.48 nM
CP0265225 Compound Info	US9464076, 2 Show/Hide	C26H24N2O4S	1
1	IC50 = 2.6 nM
CP0301299 Compound Info	8-fluoro-1-(3-fluoro-2-methylphenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H14F2N4O	1
1	IC50 = 3.55 nM
CP0278606 Compound Info	(R)-2-[3-cyano-2-(2'-ethoxy-biphenyl-4-yl)-6-fluoro-quinolin-4-ylamino]-propionic acid Show/Hide	C27H22FN3O3	1
1	IC50 = 8 nM
CP0102239 Compound Info	5-((1H-benzo[d]imidazol-2-yl)methylthio)-2-methyl-[1,2,4]triazolo[1,5-c]quinazoline Show/Hide	C18H14N6S	1
1	IC50 = 12 nM
CP0138175 Compound Info	US9464076, 8 Show/Hide	C25H22N2O4S	1
1	IC50 = 13 nM
CP0304264 Compound Info	3-(2-chlorophenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene Show/Hide	C16H12ClN5O	1
1	IC50 = 13.1 nM
CP0083432 Compound Info	1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoquinoline Show/Hide	C20H21NO4	7
1	IC50 = 21 nM
2	IC50 = 36 nM
3	IC50 = 38 nM
4	IC50 = 40 nM
5	IC50 = 92.3 nM
6	IC50 = 97 nM
7	IC50 = 210 nM
CP0075285 Compound Info	2-methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazine Show/Hide	C15H18N4O	1
1	IC50 = 32 nM
CP0179223 Compound Info	2-Methyl-5-(2-(1-methyl-4-phenyl-1H-imidazol-2-yl)-ethyl)pyrazolo[1,5-c]quinazoline Show/Hide	C23H21N5	1
1	IC50 = 50 nM
CP0117968 Compound Info	(R)-6,7-Dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrolidin-1-yl]-quinazoline Show/Hide	C22H21N5O3	2
1	IC50 = 64 nM
2	Ki = 4 nM
CP0010658 Compound Info	5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one Show/Hide	C22H30N6O4S	4
1	IC50 = 3100 nM
2	IC50 = 5400 nM
3	IC50 = 6800 nM
4	IC50 > 10000 nM
CP0000847 Compound Info	(2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione Show/Hide	C22H19N3O4	1
1	IC50 > 10000 nM

Clinical Information about the Protein

Target 1 ( Phosphodiesterase 10A (PDE10) )

Target Type	Clinical trial Target
Disease	3 Target-related Diseases				3
1	Schizophrenia [ICD-11: 6A20]
2	Irritable bowel syndrome [ICD-11: DD91.0]
3	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s)	4 Clinical Trial Drugs				4
1	PF-02545920	Drug Info	Phase 2	Schizophrenia
2	Tofisopam	Drug Info	Phase 2	Irritable bowel syndrome
3	AMG 579	Drug Info	Phase 1	Schizophrenia
4	PBF-999	Drug Info	Phase 1	Solid tumour/cancer

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT02512	cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	Rattus norvegicus, Rat	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han