Assay Detail

CHEMBL2174792

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Functional

Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB-900 after 72 hrs by fluorescence assay

ChEMBL ↗

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Target

Trypanosoma brucei rhodesiense (CHEMBL612348) ↗

Open DB target context

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Trypanosoma brucei rhodesiense (CHEMBL612348) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Trypanosoma brucei rhodesiense

CHEMBL612348

Anchored from Assay target.

Protein identity Trypanosoma brucei rhodesiense

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Trypanosoma brucei rhodesiense
Confidence	1 — Organism
Curated By	Autocuration

Target

Trypanosoma brucei rhodesiense (CHEMBL612348) ↗

Type	ORGANISM
Organism	Trypanosoma brucei rhodesiense

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	7.22	7.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2171452	—	—	1	7.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2171452	—	IC50	=	60.0	nM	7.22