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Assay Detail

CHEMBL2175363

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

Binding
Inhibition of Trypanosoma brucei recombinant TbrPDEB2 expressed in yeast assessed as reduction of [3H]-cAMP hydrolysis by scintillation proximity assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.14 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171452 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171452 IC50 = 72.0 nM 7.14