Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2330147

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

Binding
Inhibition of Trypanosoma brucei full length PDEB1 expressed in insect SF21 cells using cAMP as substrate by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Class 1 phosphodiesterase PDEB1 (CHEMBL2010636)
Type SINGLE PROTEIN
Organism Trypanosoma brucei

Publication

Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure.
Jansen C, Wang H, Kooistra AJ, de Graaf C, Orrling KM, Tenor H, Seebeck T, Bailey D, de Esch IJ, Ke H, Leurs R.
J Med Chem (2013) 56 : 2087 -2096
PubMed 23409953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.14 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326941 1 8.40
CHEMBL2326942 1 5.00
CHEMBL2326943 1 4.92
CHEMBL1382213 1 4.89
CHEMBL2326944 1 4.39
CHEMBL2326945 1 4.27
CHEMBL2326946 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326941 IC50 = 4.0 nM 8.40
CHEMBL2326942 IC50 = 10000.0 nM 5.00
CHEMBL2326943 IC50 = 12000.0 nM 4.92
CHEMBL1382213 IC50 = 13000.0 nM 4.89
CHEMBL2326944 IC50 = 41000.0 nM 4.39
CHEMBL2326945 IC50 = 54000.0 nM 4.27
CHEMBL2326946 IC50 = 75000.0 nM 4.12