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Assay Detail

CHEMBL4395162

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

Binding
Inhibition of PDE4D (unknown origin)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

InCl<sub>3</sub> mediated heteroarylation of indoles and their derivatization via CH activation strategy: Discovery of 2-(1H-indol-3-yl)-quinoxaline derivatives as a new class of PDE4B selective inhibitors for arthritis and/or multiple sclerosis.
Sunke R, Bankala R, Thirupataiah B, Ramarao EVVS, Kumar JS, Doss HM, Medishetti R, Kulkarni P, Kapavarapu RK, Rasool M, Mudgal J, Mathew JE, Shenoy GG, Parsa KVL, Pal M.
Eur J Med Chem (2019) 174 : 198 -215
PubMed 31035240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.59 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193240 ROFLUMILAST 4.0 1 9.70
CHEMBL514800 APREMILAST 4.0 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193240 ROFLUMILAST IC50 = 0.2 nM 9.70
CHEMBL514800 APREMILAST IC50 = 33.0 nM 7.48