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Assay Detail

CHEMBL4397899

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

Binding
Inhibition of recombinant human PDE4D catalytic domain using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay
14
Total Activities
14
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

Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Zhang X, Dong G, Li H, Chen W, Li J, Feng C, Gu Z, Zhu F, Zhang R, Li M, Tang W, Liu H, Xu Y.
J Med Chem (2019) 62 : 5579 -5593
PubMed 31099559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.91 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4532140 1 7.01
CHEMBL4543264 1 6.89
CHEMBL4527894 1 6.62
CHEMBL4592339 1 6.60
CHEMBL4520636 1 6.57
CHEMBL4556365 1 6.29
CHEMBL4466435 1 6.19
CHEMBL4443701 1 6.16
CHEMBL4536368 1 6.09
CHEMBL4445498 1 5.43
CHEMBL4572934 1 5.37
CHEMBL4440925 1 4.68
CHEMBL4525913 1 4.58
CHEMBL4455732 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4532140 IC50 = 98.0 nM 7.01
CHEMBL4543264 IC50 = 130.0 nM 6.89
CHEMBL4527894 IC50 = 240.0 nM 6.62
CHEMBL4592339 IC50 = 250.0 nM 6.60
CHEMBL4520636 IC50 = 270.0 nM 6.57
CHEMBL4556365 IC50 = 510.0 nM 6.29
CHEMBL4466435 IC50 = 650.0 nM 6.19
CHEMBL4443701 IC50 = 700.0 nM 6.16
CHEMBL4536368 IC50 = 820.0 nM 6.09
CHEMBL4445498 IC50 = 3710.0 nM 5.43
CHEMBL4572934 IC50 = 4300.0 nM 5.37
CHEMBL4440925 IC50 = 20700.0 nM 4.68
CHEMBL4525913 IC50 = 26100.0 nM 4.58
CHEMBL4455732 IC50 = 58500.0 nM 4.23