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Assay Detail

CHEMBL760593

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

Binding
Inhibitory activity against Phosphodiesterase type IV (PDE4) obtained from guinea-pig macrophage was evaluated
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
Hulme C, Moriarty K, Miller B, Mathew R, Ramanjulu M, Cox P, Souness J, Page KM, Uhl J, Travis J, Huang FC, Labaudiniere R, Djuric SW.
Bioorg Med Chem Lett (1998) 8 : 1867 -1872
PubMed 9873449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.25 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54988 1 8.49
CHEMBL293775 1 8.30
CHEMBL55046 1 8.28
CHEMBL53710 1 7.92
CHEMBL55867 1 7.82
CHEMBL301201 1 7.75
CHEMBL54361 1 7.60
CHEMBL55203 1 7.60
CHEMBL301448 1 7.38
CHEMBL52712 1 7.35
CHEMBL54590 1 7.34
CHEMBL300395 1 7.28
CHEMBL53559 1 7.22
CHEMBL429356 1 7.16
CHEMBL292925 1 7.10
CHEMBL299332 1 7.00
CHEMBL417930 1 6.73
CHEMBL445354 1 6.70
CHEMBL54767 1 6.66
CHEMBL56406 1 6.52
CHEMBL63 ROLIPRAM 2.0 1 6.50
CHEMBL294831 1 6.42
CHEMBL53373 1 5.54
CHEMBL300129 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54988 IC50 = 3.2 nM 8.49
CHEMBL293775 IC50 = 5.0 nM 8.30
CHEMBL55046 IC50 = 5.2 nM 8.28
CHEMBL53710 IC50 = 12.0 nM 7.92
CHEMBL55867 IC50 = 15.0 nM 7.82
CHEMBL301201 IC50 = 18.0 nM 7.75
CHEMBL54361 IC50 = 25.0 nM 7.60
CHEMBL55203 IC50 = 25.0 nM 7.60
CHEMBL301448 IC50 = 42.0 nM 7.38
CHEMBL52712 IC50 = 45.0 nM 7.35
CHEMBL54590 IC50 = 46.0 nM 7.34
CHEMBL300395 IC50 = 52.0 nM 7.28
CHEMBL53559 IC50 = 60.0 nM 7.22
CHEMBL429356 IC50 = 70.0 nM 7.16
CHEMBL292925 IC50 = 80.0 nM 7.10
CHEMBL299332 IC50 = 100.0 nM 7.00
CHEMBL417930 IC50 = 187.0 nM 6.73
CHEMBL445354 IC50 = 200.0 nM 6.70
CHEMBL54767 IC50 = 220.0 nM 6.66
CHEMBL56406 IC50 = 300.0 nM 6.52
CHEMBL63 ROLIPRAM IC50 = 320.0 nM 6.50
CHEMBL294831 IC50 = 380.0 nM 6.42
CHEMBL53373 IC50 = 2900.0 nM 5.54
CHEMBL300129 IC50 > 10000.0 nM -