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Assay Detail

CHEMBL2176528

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

Binding
Inhibition of PDE4 in human PBMC assessed as inhibition of LPS-induced TNFalpha production incubated for 10 mins prior to LPS-challenge measured after 20 hrs by sandwich ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Press NJ, Taylor RJ, Fullerton JD, Tranter P, McCarthy C, Keller TH, Arnold N, Beer D, Brown L, Cheung R, Christie J, Denholm A, Haberthuer S, Hatto JD, Keenan M, Mercer MK, Oakman H, Sahri H, Tuffnell AR, Tweed M, Tyler JW, Wagner T, Fozard JR, Trifilieff A.
J Med Chem (2012) 55 : 7472 -7479
PubMed 22889281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.73 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172376 1 7.72
CHEMBL2172373 1 7.28
CHEMBL2172375 1 7.28
CHEMBL77826 1 7.17
CHEMBL2172374 1 6.90
CHEMBL2172372 1 6.82
CHEMBL2172369 1 6.27
CHEMBL2172368 1 6.11
CHEMBL2172370 1 6.07
CHEMBL2172366 1 5.71
CHEMBL2172367 1 -
CHEMBL2172371 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172376 IC50 = 19.0 nM 7.72
CHEMBL2172373 IC50 = 52.0 nM 7.28
CHEMBL2172375 IC50 = 53.0 nM 7.28
CHEMBL77826 IC50 = 67.6 nM 7.17
CHEMBL2172374 IC50 = 126.0 nM 6.90
CHEMBL2172372 IC50 = 151.0 nM 6.82
CHEMBL2172369 IC50 = 541.0 nM 6.27
CHEMBL2172368 IC50 = 769.0 nM 6.11
CHEMBL2172370 IC50 = 851.0 nM 6.07
CHEMBL2172366 IC50 = 1930.0 nM 5.71
CHEMBL2172367 IC50 - -
CHEMBL2172371 IC50 - -