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Assay Detail

CHEMBL764553

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Binding
Inhibition of rolipram binding to phosphodiesterase 4
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.
Ukita T, Sugahara M, Terakawa Y, Kuroda T, Wada K, Nakata A, Kikkawa H, Ikezawa K, Naito K.
Bioorg Med Chem Lett (2003) 13 : 2347 -2350
PubMed 12824031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.49 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.07
CHEMBL556179 1 8.85
CHEMBL554636 1 8.85
CHEMBL553502 1 8.82
CHEMBL544766 1 8.77
CHEMBL542299 1 8.74
CHEMBL543016 1 8.52
CHEMBL542650 1 8.51
CHEMBL536568 1 8.46
CHEMBL63 ROLIPRAM 2.0 1 8.42
CHEMBL545700 1 8.27
CHEMBL539265 1 8.19
CHEMBL553278 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST Ki = 0.85 nM 9.07
CHEMBL556179 Ki = 1.4 nM 8.85
CHEMBL554636 Ki = 1.4 nM 8.85
CHEMBL553502 Ki = 1.5 nM 8.82
CHEMBL544766 Ki = 1.7 nM 8.77
CHEMBL542299 Ki = 1.8 nM 8.74
CHEMBL543016 Ki = 3.0 nM 8.52
CHEMBL542650 Ki = 3.1 nM 8.51
CHEMBL536568 Ki = 3.5 nM 8.46
CHEMBL63 ROLIPRAM Ki = 3.8 nM 8.42
CHEMBL545700 Ki = 5.4 nM 8.27
CHEMBL539265 Ki = 6.5 nM 8.19
CHEMBL553278 Ki = 120.0 nM 6.92