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Assay Detail

CHEMBL940738

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

Binding
Inhibition of PDE4B
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Kuang R, Shue HJ, Blythin DJ, Shih NY, Gu D, Chen X, Schwerdt J, Lin L, Ting PC, Zhu X, Aslanian R, Piwinski JJ, Xiao L, Prelusky D, Wu P, Zhang J, Zhang X, Celly CS, Minnicozzi M, Billah M, Wang P.
Bioorg Med Chem Lett (2007) 17 : 5150 -5154
PubMed 17683932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.57 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL250137 1 9.30
CHEMBL399385 1 9.00
CHEMBL251107 1 9.00
CHEMBL249933 1 8.92
CHEMBL399298 1 8.85
CHEMBL400976 1 8.80
CHEMBL437020 1 8.70
CHEMBL401345 1 8.66
CHEMBL249691 1 8.37
CHEMBL401121 1 7.77
CHEMBL401186 1 7.72
CHEMBL40200 1 7.70
CHEMBL399690 1 7.62
CHEMBL249486 1 7.51
CHEMBL399297 1 7.31
CHEMBL429484 1 7.28
CHEMBL250546 SCH-351591 1 7.22
CHEMBL401120 1 7.21
CHEMBL248683 1 7.12
CHEMBL251712 1 7.10
CHEMBL398454 1 7.06
CHEMBL249285 1 6.96
CHEMBL398254 1 6.51
CHEMBL400079 1 6.46
CHEMBL400276 1 6.41
CHEMBL251299 1 6.33
CHEMBL251298 1 6.33
CHEMBL399898 1 6.24
CHEMBL428415 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL250137 IC50 = 0.5 nM 9.30
CHEMBL399385 IC50 = 1.0 nM 9.00
CHEMBL251107 IC50 = 1.0 nM 9.00
CHEMBL249933 IC50 = 1.2 nM 8.92
CHEMBL399298 IC50 = 1.4 nM 8.85
CHEMBL400976 IC50 = 1.6 nM 8.80
CHEMBL437020 IC50 = 2.0 nM 8.70
CHEMBL401345 IC50 = 2.2 nM 8.66
CHEMBL249691 IC50 = 4.3 nM 8.37
CHEMBL401121 IC50 = 17.0 nM 7.77
CHEMBL401186 IC50 = 19.0 nM 7.72
CHEMBL40200 IC50 = 20.0 nM 7.70
CHEMBL399690 IC50 = 24.0 nM 7.62
CHEMBL249486 IC50 = 31.0 nM 7.51
CHEMBL399297 IC50 = 49.0 nM 7.31
CHEMBL429484 IC50 = 53.0 nM 7.28
CHEMBL250546 SCH-351591 IC50 = 60.0 nM 7.22
CHEMBL401120 IC50 = 62.0 nM 7.21
CHEMBL248683 IC50 = 76.0 nM 7.12
CHEMBL251712 IC50 = 80.0 nM 7.10
CHEMBL398454 IC50 = 88.0 nM 7.06
CHEMBL249285 IC50 = 110.0 nM 6.96
CHEMBL398254 IC50 = 310.0 nM 6.51
CHEMBL400079 IC50 = 350.0 nM 6.46
CHEMBL400276 IC50 = 390.0 nM 6.41
CHEMBL251299 IC50 = 470.0 nM 6.33
CHEMBL251298 IC50 = 470.0 nM 6.33
CHEMBL399898 IC50 = 580.0 nM 6.24
CHEMBL428415 IC50 = 670.0 nM 6.17