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Assay Detail

CHEMBL1107017

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

Binding
Inhibition of PDE4
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.
Zhang YK, Plattner JJ, Akama T, Baker SJ, Hernandez VS, Sanders V, Freund Y, Kimura R, Bu W, Hold KM, Lu XS.
Bioorg Med Chem Lett (2010) 20 : 2270 -2274
PubMed 20188549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.65 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093373 1 7.33
CHEMBL1093375 1 7.08
CHEMBL1090022 1 7.03
CHEMBL1093730 1 6.95
CHEMBL1093376 1 6.89
CHEMBL1089680 1 6.89
CHEMBL1093962 1 6.75
CHEMBL1093706 1 6.66
CHEMBL1093705 1 6.54
CHEMBL484785 CRISABOROLE 4.0 1 6.31
CHEMBL1093707 1 6.12
CHEMBL485358 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093373 IC50 = 47.0 nM 7.33
CHEMBL1093375 IC50 = 84.0 nM 7.08
CHEMBL1090022 IC50 = 94.5 nM 7.03
CHEMBL1093730 IC50 = 113.0 nM 6.95
CHEMBL1093376 IC50 = 130.0 nM 6.89
CHEMBL1089680 IC50 = 130.0 nM 6.89
CHEMBL1093962 IC50 = 180.0 nM 6.75
CHEMBL1093706 IC50 = 219.0 nM 6.66
CHEMBL1093705 IC50 = 287.0 nM 6.54
CHEMBL484785 CRISABOROLE IC50 = 490.0 nM 6.31
CHEMBL1093707 IC50 = 763.0 nM 6.12
CHEMBL485358 IC50 = 6420.0 nM 5.19