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Assay Detail

CHEMBL2175364

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

Binding
Inhibition of Trypanosoma brucei His-tagged catalytic domains of TbrPDEB1 expressed in Escherichia coli BL21 assessed as conversion of cAMP to AMP after 20 mins by PDELight assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Orrling KM, Jansen C, Vu XL, Balmer V, Bregy P, Shanmugham A, England P, Bailey D, Cos P, Maes L, Adams E, van den Bogaart E, Chatelain E, Ioset JR, van de Stolpe A, Zorg S, Veerman J, Seebeck T, Sterk GJ, de Esch IJ, Leurs R.
J Med Chem (2012) 55 : 8745 -8756
PubMed 22963052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.26 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171452 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171452 IC50 = 55.0 nM 7.26