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Assay Detail

CHEMBL4429336

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

Functional
Antiparasitic activity against bloodstream form of Trypanosoma brucei 221 infected in mouse VSMC assessed as reduction in parasitic proliferation after 48 hrs by cell titer-glo based assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor.
Valenciano AL, Ramsey AC, Santos WL, Mackey ZB.
Bioorg Med Chem (2016) 24 : 4647 -4651
PubMed 27519462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.56 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103840 DINACICLIB 3.0 1 7.10
CHEMBL1236962 OMIPALISIB 2.0 1 6.96
CHEMBL296468 BMS-387032 1.0 1 6.92
CHEMBL1774055 1 6.92
CHEMBL488436 AZD-5438 1.0 1 6.68
CHEMBL4289017 PF-03814735 1.0 1 6.58
CHEMBL7064 1 6.24
CHEMBL564829 MILCICLIB 2.0 1 6.21
CHEMBL3218578 BGT-226 FREE BASE 2.0 1 6.02
CHEMBL1765602 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103840 DINACICLIB IC50 = 80.0 nM 7.10
CHEMBL1236962 OMIPALISIB IC50 = 111.0 nM 6.96
CHEMBL296468 BMS-387032 IC50 = 120.0 nM 6.92
CHEMBL1774055 IC50 = 120.0 nM 6.92
CHEMBL488436 AZD-5438 IC50 = 210.0 nM 6.68
CHEMBL4289017 PF-03814735 IC50 = 260.0 nM 6.58
CHEMBL7064 IC50 = 570.0 nM 6.24
CHEMBL564829 MILCICLIB IC50 = 610.0 nM 6.21
CHEMBL3218578 BGT-226 FREE BASE IC50 = 950.0 nM 6.02
CHEMBL1765602 IC50 = 1000.0 nM 6.00