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Assay Detail

CHEMBL5522136

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

Binding
Inhibition of human PDE4D catalytic domain (T86 to S413 residues) expressed in Escherichia coli BL21 (DE3) using [3H]-cAMP/cGMP as substrate incubated for 10 mins by MicroBeta scintillation proximity assay
23
Total Activities
23
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 Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model.
Gu C, Liu J, Qian F, Yu W, Huang D, Shen J, Feng C, Chen K, Li Y, Jiang X, Xu Y, Zhang L.
J Med Chem (2024) 67 : 4855 -4869
PubMed 38489246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.82 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5562344 1 6.77
CHEMBL5560091 1 6.54
CHEMBL1991200 1 5.94
CHEMBL484785 CRISABOROLE 4.0 1 5.94
CHEMBL464374 1 5.89
CHEMBL5561298 1 5.89
CHEMBL5562065 1 5.55
CHEMBL1971313 1 5.49
CHEMBL5549963 1 5.26
CHEMBL5563938 1 4.90
CHEMBL1977166 1 -
CHEMBL5563004 1 -
CHEMBL5562424 1 -
CHEMBL5556061 1 -
CHEMBL5561279 1 -
CHEMBL5555586 1 -
CHEMBL5560239 1 -
CHEMBL2261308 1 -
CHEMBL5560387 1 -
CHEMBL5562969 1 -
CHEMBL5560423 1 -
CHEMBL5557916 1 -
CHEMBL5566327 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5562344 IC50 = 170.0 nM 6.77
CHEMBL5560091 IC50 = 290.0 nM 6.54
CHEMBL1991200 IC50 = 1140.0 nM 5.94
CHEMBL484785 CRISABOROLE IC50 = 1140.0 nM 5.94
CHEMBL464374 IC50 = 1290.0 nM 5.89
CHEMBL5561298 IC50 = 1280.0 nM 5.89
CHEMBL5562065 IC50 = 2820.0 nM 5.55
CHEMBL1971313 IC50 = 3260.0 nM 5.49
CHEMBL5549963 IC50 = 5480.0 nM 5.26
CHEMBL5563938 IC50 = 12590.0 nM 4.90
CHEMBL1977166 IC50 - -
CHEMBL5563004 IC50 - -
CHEMBL5562424 IC50 - -
CHEMBL5556061 IC50 - -
CHEMBL5561279 IC50 - -
CHEMBL5555586 IC50 - -
CHEMBL5560239 IC50 - -
CHEMBL2261308 IC50 - -
CHEMBL5560387 IC50 - -
CHEMBL5562969 IC50 - -
CHEMBL5560423 IC50 - -
CHEMBL5557916 IC50 - -
CHEMBL5566327 IC50 - -