Protein Information

General Information of the Protein

Protein ID	PT01538
Protein Name	3',5'-cyclic-AMP phosphodiesterase 4D
Secondarily Protein Name	DPDE3 PDE43 cAMP-specific phosphodiesterase 4D
Gene Name	PDE4D
Secondarily Gene Name	DPDE3
Sequence	MEAEGSSAPARAGSGEGSDSAGGATLKAPKHLWRHEQHHQYPLRQPQFRLLHPHHHLPPPPPPSPQPQPQCPLQPPPPPPLPPPPPPPGAARGRYASSGATGRVRHRGYSDTERYLYCRAMDRTSYAVETGHRPGLKKSRMSWPSSFQGLRRFDVDNGTSAGRSPLDPMTSPGSGLILQANFVHSQRRESFLYRSDSDYDLSPKSMSRNSSIASDIHGDDLIVTPFAQVLASLRTVRNNFAALTNLQDRAPSKRSPMCNQPSINKATITEEAYQKLASETLEELDWCLDQLETLQTRHSVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEFISNTFLDKQHEVEIPSPTQKEKEKKKRPMSQISGVKKLMHSSSLTNSSIPRFGVKTEQEDVLAKELEDVNKWGLHVFRIAELSGNRPLTVIMHTIFQERDLLKTFKIPVDTLITYLMTLEDHYHADVAYHNNIHAADVVQSTHVLLSTPALEAVFTDLEILAAIFASAIHDVDHPGVSNQFLINTNSELALMYNDSSVLENHHLAVGFKLLQEENCDIFQNLTKKQRQSLRKMVIDIVLATDMSKHMNLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLQNMVHCADLSNPTKPLQLYRQWTDRIMEEFFRQGDRERERGMEISPMCDKHNASVEKSQVGFIDYIVHPLWETWADLVHPDAQDILDTLEDNREWYQSTIPQSPSPAPDDPEEGRQGQTEKFQFELTLEEDGESDTEKDSGSQVEEDTSCSDSKTLCTQDSESTEIPLDEQVEEEAVGEEEESQPEACVIDDRSPDT Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Phosphodiesterase > Phosphodiesterase 4 > Phosphodiesterase 4D
Function	Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. Show/Hide
Uniprot ID	Primary ID: Q08499 Secondarily ID: O43433 Q13549 Q13550 Q13551 Q7Z2L8 Q8IV84 Q8IVA9 Q8IVD2 Q8IVD3 Q96HL4 Q9HCX7 Show/Hide
Ensembl ID	ENSG00000113448
HGNC ID	HGNC:8783
Subcellular Location	Apical cell membrane Cytoplasm Membrane Cytoplasm Cytoskeleton Cytoplasm Cytoskeleton Microtubule organizing center Centrosome

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: CL000011 , CHO

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0325271 Compound Info	(4-(3-(4-(3-nitrophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)(pyrazin-2-yl)methanone Show/Hide	C28H27N9O3	2
1	IC50 = 4900 nM Bioactivity Info	TI LI LO TS
2	Ki = 147 nM Bioactivity Info	TI LI LO TS
CP0479945 Compound Info	4-phenyl-N-(3-(4-(pyrimidin-2-yl)piperazin-1-yl)propyl)pyridazino[4,5-b]indolizin-1-amine Show/Hide	C27H28N8	2
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
2	Ki = 59000 nM Bioactivity Info	TI LI LO TS
CP0502806 Compound Info	(4-(3-(4-phenylpyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)(pyrazin-2-yl)methanone Show/Hide	C28H28N8O	2
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS
2	Ki = 8370 nM Bioactivity Info	TI LI LO TS
CP0502810 Compound Info	4-(3-nitrophenyl)-N-(3-(4-(pyrimidin-2-yl)piperazin-1-yl)propyl)pyridazino[4,5-b]indolizin-1-amine Show/Hide	C27H27N9O2	1
1	Ki = 2400 nM Bioactivity Info	TI LI LO TS
CP0504539 Compound Info	3-(1-(3-(4-(pyrimidin-2-yl)piperazin-1-yl)propylamino)pyridazino[4,5-b]indolizin-4-yl)benzonitrile Show/Hide	C28H27N9	1
1	Ki = 3350 nM Bioactivity Info	TI LI LO TS
CP0514006 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyrazin-2-yl)methanone Show/Hide	C26H29N9O3	1
1	Ki = 4440 nM Bioactivity Info	TI LI LO TS
CP0504529 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyridin-2-yl)methanone Show/Hide	C27H30N8O3	1
1	Ki = 11500 nM Bioactivity Info	TI LI LO TS
CP0514005 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(thiazol-5-yl)methanone Show/Hide	C25H28N8O3S	1
1	Ki = 12700 nM Bioactivity Info	TI LI LO TS
CP0506240 Compound Info	4-(3-chlorophenyl)-N-(3-(4-(pyrimidin-2-yl)piperazin-1-yl)propyl)pyridazino[4,5-b]indolizin-1-amine Show/Hide	C27H27ClN8	1
1	Ki = 14200 nM Bioactivity Info	TI LI LO TS
CP0506241 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyridin-3-yl)methanone Show/Hide	C27H30N8O3	1
1	Ki = 15300 nM Bioactivity Info	TI LI LO TS
CP0479941 Compound Info	4-(3-bromophenyl)-N-(3-(4-(pyrimidin-2-yl)piperazin-1-yl)propyl)pyridazino[4,5-b]indolizin-1-amine Show/Hide	C27H27BrN8	1
1	Ki = 17500 nM Bioactivity Info	TI LI LO TS
CP0524331 Compound Info	(4-(3-(4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)(pyridin-2-yl)methanone Show/Hide	C29H28FN7O	1
1	Ki = 18000 nM Bioactivity Info	TI LI LO TS
CP0479947 Compound Info	(4-(3-(4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)(pyridin-3-yl)methanone Show/Hide	C29H28FN7O	1
1	Ki = 19000 nM Bioactivity Info	TI LI LO TS
CP0469057 Compound Info	(4-(3-(4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)(phenyl)methanone Show/Hide	C30H29FN6O	1
1	Ki = 22200 nM Bioactivity Info	TI LI LO TS
CP0901742 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(1,2,3-thiadiazol-4-yl)methanone Show/Hide	C24H27N9O3S	1
1	Ki = 48600 nM Bioactivity Info	TI LI LO TS
CP0504530 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyridazin-4-yl)methanone Show/Hide	C26H29N9O3	1
1	Ki = 51200 nM Bioactivity Info	TI LI LO TS
CP0508359 Compound Info	4-(3-methylphenyl)-N-[3-(4-pyrimidin-2-ylpiperazin-1-yl)propyl]pyridazino[4,5-b]indolizin-1-amine Show/Hide	C28H30N8	1
1	Ki = 54400 nM Bioactivity Info	TI LI LO TS
CP0479942 Compound Info	cyclopentyl-[4-[3-[[4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-yl]amino]propyl]piperazin-1-yl]methanone Show/Hide	C29H33FN6O	1
1	Ki = 61000 nM Bioactivity Info	TI LI LO TS
CP0479946 Compound Info	(4-(3-(4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)(1-methyl-1H-pyrrol-2-yl)methanone Show/Hide	C29H30FN7O	1
1	Ki = 65000 nM Bioactivity Info	TI LI LO TS
CP0521450 Compound Info	(4-(3-(7-(3-chlorophenyl)-1,2-dimethyl-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyrimidin-2-yl)methanone Show/Hide	C26H29ClN8O	1
1	Ki = 80900 nM Bioactivity Info	TI LI LO TS
CP0504538 Compound Info	4-(3-fluorophenyl)-N-(3-(4-(pyrimidin-2-yl)piperazin-1-yl)propyl)pyridazino[4,5-b]indolizin-1-amine Show/Hide	C27H27FN8	1
1	Ki = 83000 nM Bioactivity Info	TI LI LO TS
CP0469058 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyridin-4-yl)methanone Show/Hide	C27H30N8O3	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS
CP0479944 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyrimidin-2-yl)methanone Show/Hide	C26H29N9O3	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS
CP0504528 Compound Info	1-(4-(3-(4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)propan-1-one Show/Hide	C26H29FN6O	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS
CP0507695 Compound Info	1-(4-(3-(4-(3-fluorophenyl)pyridazino[4,5-b]indolizin-1-ylamino)propyl)piperazin-1-yl)ethanone Show/Hide	C25H27FN6O	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS
CP0508357 Compound Info	(4-(3-(7-(3-fluorophenyl)-1,2-dimethyl-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyrimidin-2-yl)methanone Show/Hide	C26H29FN8O	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS
CP0518712 Compound Info	(4-(3-(1,2-dimethyl-7-(3-nitrophenyl)-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(isoxazol-5-yl)methanone Show/Hide	C25H28N8O4	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS
CP0524332 Compound Info	(4-(3-(1,2-dimethyl-7-phenyl-1H-pyrrolo[3,2-d]pyridazin-4-ylamino)propyl)piperazin-1-yl)(pyrimidin-2-yl)methanone Show/Hide	C26H30N8O	1
1	Ki > 100000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000018 , HL-60

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000100 , U-937

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0037308 Compound Info	(R,S)-Rolipram Show/Hide	C16H21NO3	25
1	IC50 = 0.80618 nM
2	IC50 = 31.6 nM
3	IC50 = 33 nM
4	IC50 = 50 nM
5	IC50 = 60 nM
6	IC50 = 79 nM
7	IC50 = 80 nM
8	IC50 = 82 nM
9	IC50 = 82.5 nM
10	IC50 = 130 nM
11	IC50 = 140 nM
12	IC50 = 160 nM
13	IC50 = 200 nM
14	IC50 = 240 nM
15	IC50 = 320 nM
16	IC50 = 403 nM
17	IC50 = 550 nM
18	IC50 = 590 nM
19	IC50 = 610 nM
20	IC50 = 621 nM
21	IC50 = 622 nM
22	IC50 = 880 nM
23	IC50 = 1000 nM
24	IC50 = 4310 nM
25	Ki = 58.9 nM
CP0016899 Compound Info	(R)-2-(4-fluorophenoxy)-N-(1-(thiophen-2-yl)ethyl)nicotinamide Show/Hide	C18H15FN2O2S	1
1	IC50 = 4 nM
CP0064315 Compound Info	2-[4-[[2-(3-chlorophenyl)-6-(trifluoromethyl)pyridin-4-yl]methyl]phenyl]acetic acid Show/Hide	C21H15ClF3NO2	1
1	IC50 = 7.8 nM
CP0203819 Compound Info	7-(3'-Cyclopropylmethoxy-4'-difluoromethoxyphenyl)-2-pyridin-3-yl-pyrazolo[1,5-a]pyrimidine Show/Hide	C22H18F2N4O2	1
1	IC50 = 27 nM
CP0137839 Compound Info	(S)-N-(2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide Show/Hide	C22H24N2O7S	3
1	IC50 = 33 nM
2	IC50 = 74 nM
3	IC50 = 540 nM
CP0317792 Compound Info	7-(3'-Cyclopropylmethoxy-4'-difluoromethoxyphenyl)-2-(1-oxypyridin-3-yl)-pyrazolo[1,5-a]pyrimidine Show/Hide	C22H18F2N4O3	1
1	IC50 = 42 nM
CP0069130 Compound Info	(Ibudilast)1-(2-Isopropyl-pyrazolo[1,5-a]pyridin-3-yl)-2-methyl-propan-1-one Show/Hide	C14H18N2O	1
1	IC50 = 166 nM
CP0277281 Compound Info	(cis)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one Show/Hide	C16H18N2O3	1
1	IC50 = 213 nM
CP0859215 Compound Info	3-(10-Oxo-4,8-diphenyl-10H-pyrano[4',3':3,4]pyrazolo[1,5-a]pyrimidin-7-yl)benzamide Show/Hide	C28H18N4O3	1
1	IC50 = 2840 nM

Clinical Information about the Protein

Target 1 ( Phosphodiesterase 4D (PDE4D) )

Target Type	Successful Target
Disease	11 Target-related Diseases				11
1	Spasm [ICD-11: MB47.3]
2	Cognitive impairment [ICD-11: 6D71]
3	Atopic dermatitis [ICD-11: EA80]
4	Alzheimer disease [ICD-11: 8A20]
5	Crohn disease [ICD-11: DD70]
6	Psoriasis vulgaris [ICD-11: EA90]
7	Asthma [ICD-11: CA23]
8	Rheumatoid arthritis [ICD-11: FA20]
9	Chronic obstructive pulmonary disease [ICD-11: CA22]
10	Multiple sclerosis [ICD-11: 8A40]
11	Peripheral vascular disease [ICD-11: BD4Z]
Approved Drug(s)	1 Approved Drug				1
1	Papaverine	Drug Info	Approved	Spasm
Clinical Trial Drug(s)	10 Clinical Trial Drugs				10
1	DENBUFYLLINE	Drug Info	Phase 3	Cognitive impairment
2	AN-2898	Drug Info	Phase 2	Atopic dermatitis
3	BPN14770	Drug Info	Phase 2	Alzheimer disease
4	CC-1088	Drug Info	Phase 2	Crohn disease
5	HT-0712	Drug Info	Phase 2	Cognitive impairment
6	MK-0873	Drug Info	Phase 2	Psoriasis vulgaris
7	Oglemilast	Drug Info	Phase 2	Asthma
8	Piclamilast	Drug Info	Phase 2	Rheumatoid arthritis
9	TOFIMILAST	Drug Info	Phase 2	Chronic obstructive pulmonary disease
10	Ronomilast	Drug Info	Phase 1	Chronic obstructive pulmonary disease
Discontinued Drug(s)	6 Discontinued Drugs				6
1	CDP840	Drug Info	Discontinued in Phase 2	Chronic obstructive pulmonary disease
2	CI-1018	Drug Info	Discontinued in Phase 2	Asthma
3	Daxalipram	Drug Info	Discontinued in Phase 2	Multiple sclerosis
4	YM-976	Drug Info	Discontinued in Phase 1	Asthma
5	GW-3600	Drug Info	Terminated	Asthma
6	Torbafylline	Drug Info	Terminated	Peripheral vascular disease

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han