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Assay Detail

CHEMBL3117337

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Binding
Inhibition of full-length human PDE4D2 assessed as cAMP hydrolysis preincubated for 20 mins followed by cAMP addition measured after 30 mins
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of the 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives as highly selective PDE4B inhibitors.
Goto T, Shiina A, Murata T, Tomii M, Yamazaki T, Yoshida K, Yoshino T, Suzuki O, Sogawa Y, Mizukami K, Takagi N, Yoshitomi T, Etori M, Tsuchida H, Mikkaichi T, Nakao N, Takahashi M, Takahashi H, Sasaki S.
Bioorg Med Chem Lett (2014) 24 : 893 -899
PubMed 24412069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.05 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385756 — — 1 6.75
CHEMBL3112613 — — 1 6.55
CHEMBL3114943 — — 1 6.54
CHEMBL3114926 — — 1 6.54
CHEMBL3114921 — — 1 6.52
CHEMBL3114945 — — 1 6.40
CHEMBL3114925 — — 1 6.38
CHEMBL3114933 — — 1 6.37
CHEMBL3114944 — — 1 6.36
CHEMBL3114941 — — 1 6.28
CHEMBL2385749 — — 1 6.26
CHEMBL3114953 — — 1 6.25
CHEMBL3114950 — — 1 6.24
CHEMBL3114958 — — 1 6.22
CHEMBL3114952 — — 1 6.22
CHEMBL3114948 — — 1 6.21
CHEMBL3114923 — — 1 6.17
CHEMBL3114942 — — 1 6.10
CHEMBL3114928 — — 1 6.10
CHEMBL3114957 — — 1 6.09
CHEMBL3114936 — — 1 6.07
CHEMBL3114929 — — 1 6.00
CHEMBL3114947 — — 1 6.00
CHEMBL3114924 — — 1 6.00
CHEMBL3114946 — — 1 5.96
CHEMBL3114938 — — 1 5.92
CHEMBL3114956 — — 1 5.89
CHEMBL2385573 — — 1 5.89
CHEMBL3114954 — — 1 5.89
CHEMBL3114951 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385756 — IC50 = 180.0 nM 6.75
CHEMBL3112613 — IC50 = 280.0 nM 6.55
CHEMBL3114943 — IC50 = 290.0 nM 6.54
CHEMBL3114926 — IC50 = 290.0 nM 6.54
CHEMBL3114921 — IC50 = 300.0 nM 6.52
CHEMBL3114945 — IC50 = 400.0 nM 6.40
CHEMBL3114925 — IC50 = 420.0 nM 6.38
CHEMBL3114933 — IC50 = 430.0 nM 6.37
CHEMBL3114944 — IC50 = 440.0 nM 6.36
CHEMBL3114941 — IC50 = 520.0 nM 6.28
CHEMBL2385749 — IC50 = 550.0 nM 6.26
CHEMBL3114953 — IC50 = 560.0 nM 6.25
CHEMBL3114950 — IC50 = 580.0 nM 6.24
CHEMBL3114958 — IC50 = 600.0 nM 6.22
CHEMBL3114952 — IC50 = 600.0 nM 6.22
CHEMBL3114948 — IC50 = 620.0 nM 6.21
CHEMBL3114923 — IC50 = 680.0 nM 6.17
CHEMBL3114942 — IC50 = 790.0 nM 6.10
CHEMBL3114928 — IC50 = 790.0 nM 6.10
CHEMBL3114957 — IC50 = 810.0 nM 6.09
CHEMBL3114936 — IC50 = 860.0 nM 6.07
CHEMBL3114929 — IC50 = 1000.0 nM 6.00
CHEMBL3114924 — IC50 = 1000.0 nM 6.00
CHEMBL3114947 — IC50 = 1000.0 nM 6.00
CHEMBL3114946 — IC50 = 1100.0 nM 5.96
CHEMBL3114938 — IC50 = 1200.0 nM 5.92
CHEMBL3114956 — IC50 = 1300.0 nM 5.89
CHEMBL2385573 — IC50 = 1300.0 nM 5.89
CHEMBL3114954 — IC50 = 1300.0 nM 5.89
CHEMBL3114951 — IC50 = 1300.0 nM 5.89
CHEMBL3114940 — IC50 = 1300.0 nM 5.89
CHEMBL3114949 — IC50 = 1300.0 nM 5.89
CHEMBL3114955 — IC50 = 1400.0 nM 5.85
CHEMBL3114934 — IC50 = 1500.0 nM 5.82
CHEMBL3114931 — IC50 = 1600.0 nM 5.80
CHEMBL3114927 — IC50 = 1800.0 nM 5.75
CHEMBL3114935 — IC50 = 2100.0 nM 5.68
CHEMBL3114932 — IC50 = 2200.0 nM 5.66
CHEMBL3114922 — IC50 = 3400.0 nM 5.47
CHEMBL3114939 — IC50 = 3400.0 nM 5.47
CHEMBL3114937 — IC50 = 3800.0 nM 5.42
CHEMBL3114930 — IC50 = 7400.0 nM 5.13