TABLE 2

PDE4 inhibitors tested for their selectivity against different PDE4 subtypes

Compound	Study	PDE4 Form	Construct Category	IC₅₀
				nM
A-33	Naganuma et al., 2009	PDE4B	cat dom + C terminus	15
		PDE4D	cat dom + C terminus	1700
	Hagen et al., 2014	PDE4B1	Long	55
		PDE4D7	Long	1997
CDP840	Perry et al., 1998	PDE4A4	Long	3.5
		PDE4B3	Long	3.8
		PDE4C2	Long	30
		PDE4D3	Long	2.6
	Aoki et al., 2001b	PDE4A4	Long	27
		PDE4B1	Long	10
		PDE4C1	Long	63
		PDE4D3	Long	14
Cilomilast	Huang et al., 2007	PDE4A	Truncated (supershort)	42.9
		PDE4B	Truncated (supershort)	40.7
		PDE4C	Truncated (supershort)	160
		PDE4D	Truncated (supershort)	6.9
	Asaka et al., 2010	PDE4A1	Supershort	62
		PDE4B1	Long	56
		PDE4C1	Long	302
		PDE4D3	Long	19
	Pruniaux et al., 2010	PDE4A4	Long	34
		PDE4B2	Short	70
		PDE4C2	Long	238
		PDE4D3	Long	7
	Huang et al., 2006	PDE4A	Truncated (supershort)	37
		PDE4B	Truncated (supershort)	34
		PDE4C	Truncated (supershort)	133
		PDE4D	Truncated (supershort)	7
CI-1044	Pruniaux et al., 2010	PDE4A4	Long	290
		PDE4B2	Short	80
		PDE4C2	Long	560
		PDE4D3	Long	90
CT-2450	Robichaud et al., 2002b	PDE4A	Truncated (supershort)	0.9
		PDE4B	Truncated (supershort)	0.7
		PDE4C	Truncated (supershort)	1.6
		PDE4D	Truncated (supershort)	0.5
EPPA-1	Davis et al., 2009	PDE4A4	Long	93.0
		PDE4B2	Short	45.7
		PDE4C1	Long	142.2
		PDE4D3	Long	35.1
GEBR4d	Brullo et al., 2020	PDE4B2	Short	550
		PDE4D3	Long	1050
GEBR5d	Brullo et al., 2020	PDE4B2	Short	550
		PDE4D3	Long	1220
GPD-1116	Nose et al., 2016	PDE4A4	Long	100
		PDE4B2	Short	500
		PDE4C2	Long	100
		PDE4D3	Long	50
GPD-1133	Nose et al., 2016	PDE4A4	Long	40
		PDE4B2	Short	200
		PDE4C2	Long	63
		PDE4D3	Long	50
Ibudilast	Huang et al., 2006	PDE4A	Truncated (supershort)	54
		PDE4B	Truncated (supershort)	65
		PDE4C	Truncated (supershort)	239
		PDE4D	Truncated (supershort)	166
L-454.560	Huang et al., 2007	PDE4A	Truncated (supershort)	1.6
		PDE4B	Truncated (supershort)	0.5
		PDE4C	Truncated (supershort)	9.1
		PDE4D	Truncated (supershort)	1.2
L-826,141	Claveau et al., 2004	PDE4A	Truncated (supershort)	1.26
		PDE4B	Truncated (supershort)	0.38
		PDE4C	Truncated (supershort)	2.38
		PDE4D	Truncated (supershort)	0.26
Moexipril	Cameron et al., 2013	PDE4A4	Long	160
		PDE4B2	Short	38
		PDE4D5	Long	230
PMNPQ	Bureau et al., 2006	PDE4A	Truncated (supershort)	0.1
		PDE4B	Truncated (supershort)	0.1
		PDE4C	Truncated (supershort)	0.1
		PDE4D	Truncated (supershort)	0.1
Roflumilast	Nose et al., 2016	PDE4A4	Long	0.17
		PDE4B2	Short	0.27
		PDE4C2	Long	1
		PDE4D3	Long	0.15
	Claveau et al., 2004	PDE4A	Truncated (supershort)	0.16
		PDE4B	Truncated (supershort)	0.11
		PDE4C	Truncated (supershort)	0.61
		PDE4D	Truncated (supershort)	0.11
	Huang et al., 2007	PDE4A	Truncated (supershort)	0.16
		PDE4B	Truncated (supershort)	0.11
		PDE4C	Truncated (supershort)	0.61
		PDE4D	Truncated (supershort)	0.11
Roflumilast N-oxide	Claveau et al., 2004	PDE4A	Truncated (supershort)	0.58
		PDE4B	Truncated (supershort)	0.37
		PDE4C	Truncated (supershort)	3.2
		PDE4D	Truncated (supershort)	0.31
	Huang et al., 2007	PDE4A	Truncated (supershort)	0.58
		PDE4B	Truncated (supershort)	0.37
		PDE4C	Truncated (supershort)	3.2
		PDE4D	Truncated (supershort)	0.31
Rolipram	Aoki et al., 2001b	PDE4A4	Long	690
		PDE4B1	Long	270
		PDE4C1	Long	1900
		PDE4D3	Long	260
	Asaka et al., 2010	PDE4A1	Supershort	565
		PDE4B1	Long	402
		PDE4C1	Long	888
		PDE4D3	Long	234
R-rolipram	Claveau et al., 2004	PDE4A	Truncated (supershort)	4.8
		PDE4B	Truncated (supershort)	5.4
		PDE4C	Truncated (supershort)	40.5
		PDE4D	Truncated (supershort)	3.9
	Perry et al., 1998	PDE4A4	Long	84.4
		PDE4B3	Long	69
		PDE4C2	Long	612
		PDE4D3	Long	84.3
RP73401	Aoki et al., 2001b	PDE4A4	Long	0.9
		PDE4B1	Long	0.32
		PDE4C1	Long	4.8
		PDE4D3	Long	0.42
TAS-203	Asaka et al., 2010	PDE4A1	Supershort	47
		PDE4B1	Long	35
		PDE4C1	Long	227
		PDE4D3	Long	43
UFM24	Tsai et al., 2017	PDE4A1	Supershort	7510
		PDE4B2	Short	8580
		PDE4C1	Long	1750
		PDE4D2	Supershort	3530
YM976	Aoki et al., 2001b	PDE4A4	Long	3.5
		PDE4B1	Long	1
		PDE4C1	Long	13
		PDE4D3	Long	1.7
9	Hagen et al., 2014	PDE4B1	Long	770
		PDE4D7	Long	5611
29	Hagen et al., 2014	PDE4B1	Long	165
		PDE4D7	Long	7
5	Skoumbourdis et al., 2009	PDE4A1	Supershort	12.9
		PDE4B1	Long	48.2
		PDE4B2	Short	37.2
		PDE4C1	Long	452
		PDE4D2	Supershort	49.2
10	Skoumbourdis et al., 2009	PDE4A1	Supershort	0.26
		PDE4B1	Long	2.3
		PDE4B2	Short	1.6
		PDE4C1	Long	46
		PDE4D2	Supershort	1.9
18	Skoumbourdis et al., 2009	PDE4A1	Supershort	0.6
		PDE4B1	Long	4.1
		PDE4B2	Short	2.9
		PDE4C1	Long	106
		PDE4D2	Supershort	2.1
11r	Tang et al., 2019	PDE4B1	Long	340
		PDE4D7	Long	380
16a	Huang et al., 2019	PDE4B1	Long	293
		PDE4D7	Long	312
44	Goto et al., 2014	PDE4B2	Short	4.6
		PDE4D2	Supershort	620
5a	Brullo et al., 2014	PDE4B2	Short	1600
		PDE4D3	Long	660
10b	Brullo et al., 2014	PDE4B2	Short	18,000
		PDE4D4	Long	210
1	Purushothaman et al., 2018	PDE4A4	Long	45
		PDE4B1	Long	31
		PDE4C1	Long	77
		PDE4D7	Long	220
2	Purushothaman et al., 2018	PDE4A4	Long	152
		PDE4B1	Long	15
		PDE4C1	Long	57
		PDE4D7	Long	108
A	Manning et al., 1999	PDE4A4	Long	6.46
		PDE4B2	Short	14.13
		PDE4D3	Long	39.81
B	Manning et al., 1999	PDE4A4	Long	100.00
		PDE4B2	Short	77.62
		PDE4D3	Long	13.49
C	Manning et al., 1999	PDE4A4	Long	33.11
		PDE4B2	Short	30.20
		PDE4D3	Long	295.12
D	Manning et al., 1999	PDE4A4	Long	1318.26
		PDE4B2	Short	316.23
		PDE4D3	Long	257.04
E	Manning et al., 1999	PDE4A4	Long	208.93
		PDE4B2	Short	173.78
		PDE4D3	Long	36.31
F	Manning et al., 1999	PDE4A4	Long	63.10
		PDE4B2	Short	57.54
		PDE4D3	Long	11.75
G	Manning et al., 1999	PDE4A4	Long	588.84
		PDE4B2	Short	389.05
		PDE4D3	Long	54.95
H	Manning et al., 1999	PDE4A4	Long	1.23
		PDE4B2	Short	1.51
		PDE4D3	Long	10.96
I	Manning et al., 1999	PDE4A4	Long	0.25
		PDE4B2	Short	0.69
		PDE4D3	Long	4.17
J	Manning et al., 1999	PDE4A4	Long	0.27
		PDE4B2	Short	1.35
		PDE4D3	Long	3.98

cat dom, catalytic domain.