Protein Information

General Information of the Protein

Protein ID	PT01305
Protein Name	3',5'-cyclic-AMP phosphodiesterase 4B
Secondarily Protein Name	DPDE4 PDE32 cAMP-specific phosphodiesterase 4B
Gene Name	PDE4B
Secondarily Gene Name	DPDE4
Sequence	MKKSRSVMTVMADDNVKDYFECSLSKSYSSSSNTLGIDLWRGRRCCSGNLQLPPLSQRQSERARTPEGDGISRPTTLPLTTLPSIAITTVSQECFDVENGPSPGRSPLDPQASSSAGLVLHATFPGHSQRRESFLYRSDSDYDLSPKAMSRNSSLPSEQHGDDLIVTPFAQVLASLRSVRNNFTILTNLHGTSNKRSPAASQPPVSRVNPQEESYQKLAMETLEELDWCLDQLETIQTYRSVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEYISNTFLDKQNDVEIPSPTQKDREKKKKQQLMTQISGVKKLMHSSSLNNTSISRFGVNTENEDHLAKELEDLNKWGLNIFNVAGYSHNRPLTCIMYAIFQERDLLKTFRISSDTFITYMMTLEDHYHSDVAYHNSLHAADVAQSTHVLLSTPALDAVFTDLEILAAIFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEEHCDIFMNLTKKQRQTLRKMVIDMVLATDMSKHMSLLADLKTMVETKKVTSSGVLLLDNYTDRIQVLRNMVHCADLSNPTKSLELYRQWTDRIMEEFFQQGDKERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVQPDAQDILDTLEDNRNWYQSMIPQSPSPPLDEQNRDCQGLMEKFQFELTLDEEDSEGPEKEGEGHSYFSSTKTLCVIDPENRDSLGETDIDIATEDKSPVDT Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Phosphodiesterase > Phosphodiesterase 4 > Phosphodiesterase 4B
Function	Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes (PubMed:15260978). May be involved in mediating central nervous system effects of therapeutic agents ranging from antidepressants to antiasthmatic and anti-inflammatory agents. Show/Hide
Uniprot ID	Primary ID: Q07343 Secondarily ID: A5YW33 O15443 Q13945 Q5TEK4 Q5TEK5 Q5TEK6 Show/Hide
Ensembl ID	ENSG00000184588
HGNC ID	HGNC:8781
Subcellular Location	Cytoplasm Cell membrane

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 = 389 nM Bioactivity Info	TI LI LO TS
2	Ki = 5.6 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 = 6700 nM Bioactivity Info	TI LI LO TS
2	Ki = 41 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 = 13200 nM Bioactivity Info	TI LI LO TS
2	Ki = 2600 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 = 77 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 = 210 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 = 222 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 = 238 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 = 241 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 = 413 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 = 432 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 = 977 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 = 1000 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 = 1030 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 = 1440 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 = 1900 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 = 2010 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 = 2700 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 = 2700 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 = 4300 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 = 4400 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 = 4440 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 = 4900 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 = 5080 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 = 5200 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 = 5500 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 = 14000 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 = 26200 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 = 52200 nM Bioactivity Info	TI LI LO TS

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
CP0035728 Compound Info	3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide Show/Hide	C17H14Cl2F2N2O3	13
1	IC50 = 0.15 nM
2	IC50 = 0.2 nM
3	IC50 = 0.3981 nM
4	IC50 = 0.4 nM
5	IC50 = 0.49 nM
6	IC50 = 0.69 nM
7	IC50 = 0.7 nM
8	IC50 = 0.8 nM
9	IC50 = 0.84 nM
10	IC50 = 0.9 nM
11	IC50 = 1 nM
12	IC50 = 1.1 nM
13	IC50 = 1.3 nM
CP0014732 Compound Info	(4aS,8aR)-2-cycloheptyl-4-[4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl]-4a,5,8,8a-tetrahydrophthalazin-1-one Show/Hide	C33H40N6O4	2
1	IC50 = 0.5012 nM
2	IC50 = 0.631 nM
CP0140985 Compound Info	2-(4-(2-(5-chlorothiophen-2-yl)-5-ethyl-6-methylpyrimidin-4-ylamino)phenyl)acetic acid Show/Hide	C19H18ClN3O2S	2
1	IC50 = 15 nM
2	IC50 = 55 nM
CP0037308 Compound Info	(R,S)-Rolipram Show/Hide	C16H21NO3	27
1	IC50 = 20 nM
2	IC50 = 34 nM
3	IC50 = 35.7 nM
4	IC50 = 50 nM
5	IC50 = 52 nM
6	IC50 = 80 nM
7	IC50 = 86 nM
8	IC50 = 97.9 nM
9	IC50 = 100 nM
10	IC50 = 210 nM
11	IC50 = 220 nM
12	IC50 = 231 nM
13	IC50 = 320 nM
14	IC50 = 534 nM
15	IC50 = 550 nM
16	IC50 = 901 nM
17	IC50 = 940 nM
18	IC50 = 1040 nM
19	IC50 = 1100 nM
20	IC50 = 1120 nM
21	IC50 = 2000 nM
22	IC50 = 4000 nM
23	IC50 = 11370 nM
24	IC50 = 16000 nM
25	Ki = 220 nM
26	Ki = 221 nM
27	Ki = 223.87 nM
CP0137839 Compound Info	(S)-N-(2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-1,3-dioxoisoindolin-4-yl)acetamide Show/Hide	C22H24N2O7S	2
1	IC50 = 27 nM
2	IC50 = 74 nM
CP0046380 Compound Info	(-)-rolipram Show/Hide	C16H21NO3	3
1	IC50 = 39.81 nM
2	IC50 = 231 nM
3	IC50 = 500 nM
CP0069130 Compound Info	(Ibudilast)1-(2-Isopropyl-pyrazolo[1,5-a]pyridin-3-yl)-2-methyl-propan-1-one Show/Hide	C14H18N2O	2
1	IC50 = 65 nM
2	IC50 = 5000 nM
CP0060152 Compound Info	N-(2-chlorophenyl)-3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzamide Show/Hide	C18H16ClF2NO3	1
1	IC50 = 166 nM
CP0114701 Compound Info	4-[[4-(3-chlorophenyl)-6-ethyl-1,3,5-triazin-2-yl]amino]benzoic acid Show/Hide	C18H15ClN4O2	1
1	IC50 = 241 nM
CP0114700 Compound Info	2-[4-[[4-(3-chlorophenyl)-6-ethyl-1,3,5-triazin-2-yl]amino]phenyl]acetic acid Show/Hide	C19H17ClN4O2	1
1	IC50 = 781 nM
CP0114698 Compound Info	2-[4-[[4-(3-chlorophenyl)-6-ethyl-1,3,5-triazin-2-yl]amino]phenyl]propanoic acid Show/Hide	C20H19ClN4O2	1
1	IC50 = 1090 nM
CP0075844 Compound Info	6-cyclopentyloxy-7-methoxy-N-(2-methoxyphenyl)-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C29H30N2O4	1
1	IC50 = 1360 nM
CP0153850 Compound Info	6-cyclopentyloxy-7-methoxy-1-phenyl-N-[2-(trifluoromethoxy)phenyl]-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C29H27F3N2O4	1
1	IC50 = 1650 nM
CP0083426 Compound Info	N,N,2-trimethyl-5-nitrobenzenesulfonamide Show/Hide	C9H12N2O4S	1
1	IC50 = 1800 nM
CP0075843 Compound Info	6-cyclopentyloxy-N-(2-fluorophenyl)-7-methoxy-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C28H27FN2O3	1
1	IC50 = 6360 nM
CP0459229 Compound Info	N-(2-chlorophenyl)-6-cyclopentyloxy-7-methoxy-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C28H27ClN2O3	1
1	IC50 = 7530 nM
CP0243354 Compound Info	methyl 2-[(6-cyclopentyloxy-7-methoxy-1-phenyl-3,4-dihydroisoquinoline-3-carbonyl)amino]acetate Show/Hide	C25H28N2O5	1
1	IC50 = 10390 nM
CP0479250 Compound Info	6-cyclopentyloxy-7-methoxy-1-phenyl-N-pyridin-2-yl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C27H27N3O3	1
1	IC50 = 12620 nM
CP0059743 Compound Info	1-methyl-3-(2-methylpropyl)-2,3,6,7-tetrahydro-1H-purine-2,6-dione Show/Hide	C10H14N4O2	2
1	IC50 = 14310 nM
2	IC50 = 28200 nM
CP0204479 Compound Info	6-cyclopentyloxy-N-(2,6-difluorophenyl)-7-methoxy-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C28H26F2N2O3	1
1	IC50 = 17860 nM
CP0455611 Compound Info	6-cyclopentyloxy-7-methoxy-N,1-diphenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C28H28N2O3	1
1	IC50 = 19320 nM
CP0153867 Compound Info	6-cyclopentyloxy-7-methoxy-1-phenyl-N-(1,3,4-thiadiazol-2-yl)-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C24H24N4O3S	1
1	IC50 = 20890 nM
CP0243355 Compound Info	6-cyclopentyloxy-7-methoxy-N-(4-methoxyphenyl)-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C29H30N2O4	1
1	IC50 = 29360 nM
CP0157080 Compound Info	6-cyclopentyloxy-7-methoxy-N-(4-methylphenyl)-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C29H30N2O3	1
1	IC50 = 36480 nM
CP0204478 Compound Info	6-cyclopentyloxy-7-methoxy-N-(3-nitrophenyl)-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C28H27N3O5	1
1	IC50 = 41580 nM
CP0354719 Compound Info	N-(3-chlorophenyl)-6-cyclopentyloxy-7-methoxy-1-phenyl-3,4-dihydroisoquinoline-3-carboxamide Show/Hide	C28H27ClN2O3	1
1	IC50 = 43160 nM
CP0234672 Compound Info	4-[5-[(4aR,8aS)-4-oxo-3-propan-2-yl-4a,5,8,8a-tetrahydrophthalazin-1-yl]-2-methoxyphenyl]-N-(2-amino-2-oxoethyl)benzamide Show/Hide	C27H30N4O4	1
1	Ki = 1995.26 nM

Clinical Information about the Protein

Target 1 ( Phosphodiesterase 4B (PDE4B) )

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

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han