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Assay Detail

CHEMBL765474

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

Binding
Evaluated for its ability to inhibit PDE4A.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.
Charpiot B, Brun J, Donze I, Naef R, Stefani M, Mueller T.
Bioorg Med Chem Lett (1998) 8 : 2891 -2896
PubMed 9873643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.14 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97817 1 7.52
CHEMBL98662 1 7.16
CHEMBL97214 1 7.07
CHEMBL420454 1 6.89
CHEMBL96039 1 6.60
CHEMBL97785 1 6.30
CHEMBL99101 1 6.27
CHEMBL318444 1 6.20
CHEMBL96034 1 6.05
CHEMBL418785 1 5.89
CHEMBL420999 1 5.64
CHEMBL97866 1 5.54
CHEMBL95715 1 5.48
CHEMBL98730 1 5.48
CHEMBL95979 1 5.27
CHEMBL431806 1 4.85
CHEMBL97213 1 -
CHEMBL99470 1 -
CHEMBL319809 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97817 IC50 = 30.0 nM 7.52
CHEMBL98662 IC50 = 70.0 nM 7.16
CHEMBL97214 IC50 = 85.0 nM 7.07
CHEMBL420454 IC50 = 130.0 nM 6.89
CHEMBL96039 IC50 = 250.0 nM 6.60
CHEMBL97785 IC50 = 500.0 nM 6.30
CHEMBL99101 IC50 = 540.0 nM 6.27
CHEMBL318444 IC50 = 630.0 nM 6.20
CHEMBL96034 IC50 = 900.0 nM 6.05
CHEMBL418785 IC50 = 1300.0 nM 5.89
CHEMBL420999 IC50 = 2300.0 nM 5.64
CHEMBL97866 IC50 = 2900.0 nM 5.54
CHEMBL95715 IC50 = 3300.0 nM 5.48
CHEMBL98730 IC50 = 3300.0 nM 5.48
CHEMBL95979 IC50 = 5400.0 nM 5.27
CHEMBL431806 IC50 = 14000.0 nM 4.85
CHEMBL97213 IC50 > 10000.0 nM -
CHEMBL99470 IC50 > 100000.0 nM -
CHEMBL319809 IC50 > 100000.0 nM -