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Assay Detail

CHEMBL829503

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

Binding
In vitro inhibition of bovine smooth muscle phosphodiesterase 4
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Muscle tissue
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.
Krier M, Araújo-Júnior JX, Schmitt M, Duranton J, Justiano-Basaran H, Lugnier C, Bourguignon JJ, Rognan D.
J Med Chem (2005) 48 : 3816 -3822
PubMed 15916433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.65 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195155 1 9.05
CHEMBL363562 1 7.70
CHEMBL195446 1 7.70
CHEMBL365177 1 7.22
CHEMBL434354 1 7.10
CHEMBL313842 ZARDAVERINE 2.0 1 6.10
CHEMBL372055 1 5.70
CHEMBL192124 1 5.10
CHEMBL192779 1 4.22
CHEMBL194551 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195155 IC50 = 0.9 nM 9.05
CHEMBL363562 IC50 = 20.0 nM 7.70
CHEMBL195446 IC50 = 20.0 nM 7.70
CHEMBL365177 IC50 = 60.0 nM 7.22
CHEMBL434354 IC50 = 80.0 nM 7.10
CHEMBL313842 ZARDAVERINE IC50 = 800.0 nM 6.10
CHEMBL372055 IC50 = 2000.0 nM 5.70
CHEMBL192124 IC50 = 8000.0 nM 5.10
CHEMBL192779 IC50 = 60000.0 nM 4.22
CHEMBL194551 IC50 > 10000.0 nM -