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Assay Detail

CHEMBL768611

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

Binding
Inhibition of human Phosphodiesterase 4B
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.
Brackeen MF, Cowan DJ, Stafford JA, Schoenen FJ, Veal JM, Domanico PL, Rose D, Strickland AB, Verghese M, Feldman PL.
J Med Chem (1995) 38 : 4848 -4854
PubMed 7490734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.66 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL144649 1 7.57
CHEMBL144499 1 7.20
CHEMBL144823 1 7.16
CHEMBL63 ROLIPRAM 2.0 1 6.66
CHEMBL144491 1 6.55
CHEMBL343244 1 6.47
CHEMBL423743 1 6.35
CHEMBL144633 1 6.23
CHEMBL18701 RO-201724 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL144649 Ki = 27.0 nM 7.57
CHEMBL144499 Ki = 63.0 nM 7.20
CHEMBL144823 Ki = 70.0 nM 7.16
CHEMBL63 ROLIPRAM Ki = 221.0 nM 6.66
CHEMBL144491 Ki = 282.0 nM 6.55
CHEMBL343244 Ki = 338.0 nM 6.47
CHEMBL423743 Ki = 447.0 nM 6.35
CHEMBL144633 Ki = 583.0 nM 6.23
CHEMBL18701 RO-201724 Ki = 1930.0 nM 5.71