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Assay Detail

CHEMBL5535003

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PDE4D7 (unknown origin) using FAM-cyclic-3',5'-AMP as substrate incubated for 1 hrs by fluorescence polarization based IMAP assay
45
Total Activities
45
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

Discovery of 4-Ethoxy-6-chloro-5-azaindazoles as Novel PDE4 Inhibitors for the Treatment of Alcohol Use Disorder and Alcoholic Liver Diseases.
Zheng L, Aimaiti Z, Long L, Xia C, Wang W, Zhou ZZ.
J Med Chem (2024) 67 : 728 -753
PubMed 38156615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 7.26 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5563001 1 7.78
CHEMBL5567204 1 7.70
CHEMBL5590959 1 7.59
CHEMBL5570546 1 7.43
CHEMBL5575493 1 7.41
CHEMBL5568942 1 7.33
CHEMBL5566545 1 7.29
CHEMBL5563029 1 7.15
CHEMBL5574297 1 7.03
CHEMBL5592515 1 6.64
CHEMBL63 ROLIPRAM 2.0 1 6.49
CHEMBL5564470 1 -
CHEMBL5595928 1 -
CHEMBL5571738 1 -
CHEMBL5570756 1 -
CHEMBL5575915 1 -
CHEMBL5573041 1 -
CHEMBL5569037 1 -
CHEMBL5579659 1 -
CHEMBL5594433 1 -
CHEMBL5595427 1 -
CHEMBL5595032 1 -
CHEMBL5569925 1 -
CHEMBL5570980 1 -
CHEMBL5570240 1 -
CHEMBL5590059 1 -
CHEMBL5584181 1 -
CHEMBL5591926 1 -
CHEMBL5570894 1 -
CHEMBL5573189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5563001 IC50 = 16.6 nM 7.78
CHEMBL5567204 IC50 = 20.2 nM 7.70
CHEMBL5590959 IC50 = 25.6 nM 7.59
CHEMBL5570546 IC50 = 37.4 nM 7.43
CHEMBL5575493 IC50 = 38.7 nM 7.41
CHEMBL5568942 IC50 = 47.0 nM 7.33
CHEMBL5566545 IC50 = 51.7 nM 7.29
CHEMBL5563029 IC50 = 71.3 nM 7.15
CHEMBL5574297 IC50 = 92.7 nM 7.03
CHEMBL5592515 IC50 = 230.0 nM 6.64
CHEMBL63 ROLIPRAM IC50 = 326.0 nM 6.49
CHEMBL5595928 IC50 - -
CHEMBL5574788 IC50 - -
CHEMBL5564470 IC50 - -
CHEMBL5569279 IC50 - -
CHEMBL5571426 IC50 - -
CHEMBL5571695 IC50 - -
CHEMBL5574916 IC50 - -
CHEMBL5565223 IC50 - -
CHEMBL5570767 IC50 - -
CHEMBL5573894 IC50 - -
CHEMBL5575635 IC50 - -
CHEMBL5564007 IC50 - -
CHEMBL5568801 IC50 - -
CHEMBL5568706 IC50 - -
CHEMBL5589872 IC50 - -
CHEMBL5570403 IC50 - -
CHEMBL5574435 IC50 - -
CHEMBL5595032 IC50 - -
CHEMBL5573189 IC50 - -
CHEMBL5570894 IC50 - -
CHEMBL5591926 IC50 - -
CHEMBL5584181 IC50 - -
CHEMBL5590059 IC50 - -
CHEMBL5570240 IC50 - -
CHEMBL5570980 IC50 - -
CHEMBL5569925 IC50 - -
CHEMBL5571738 IC50 - -
CHEMBL5595427 IC50 - -
CHEMBL5594433 IC50 - -
CHEMBL5579659 IC50 - -
CHEMBL5569037 IC50 - -
CHEMBL5573041 IC50 - -
CHEMBL5575915 IC50 - -
CHEMBL5570756 IC50 - -