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Assay Detail

CHEMBL1648845

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

Functional
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
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

Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation.
Reid CS, Patrick DA, He S, Fotie J, Premalatha K, Tidwell RR, Wang MZ, Liu Q, Gershkovich P, Wasan KM, Wenzler T, Brun R, Werbovetz KA.
Bioorg Med Chem (2011) 19 : 513 -523
PubMed 21112788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.99 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.89
CHEMBL35241 DIMINAZENE 2.0 1 8.24
CHEMBL166 MELARSOPROL 3.0 1 8.00
CHEMBL1644656 1 7.96
CHEMBL566743 1 7.92
CHEMBL1644658 1 7.89
CHEMBL1644660 1 7.85
CHEMBL1644655 1 7.60
CHEMBL1644664 1 7.38
CHEMBL1644659 1 7.29
CHEMBL1644661 1 7.14
CHEMBL265502 SURAMIN 3.0 1 6.92
CHEMBL1644657 1 6.55
CHEMBL1644667 1 5.35
CHEMBL1644665 1 5.05
CHEMBL1644653 1 4.39
CHEMBL1644662 1 4.37
CHEMBL61 PODOFILOX 4.0 1 -
CHEMBL1644666 1 -
CHEMBL1644663 1 -
CHEMBL1644654 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 1.3 nM 8.89
CHEMBL35241 DIMINAZENE IC50 = 5.8 nM 8.24
CHEMBL166 MELARSOPROL IC50 = 9.9 nM 8.00
CHEMBL1644656 IC50 = 11.0 nM 7.96
CHEMBL566743 IC50 = 12.0 nM 7.92
CHEMBL1644658 IC50 = 13.0 nM 7.89
CHEMBL1644660 IC50 = 14.0 nM 7.85
CHEMBL1644655 IC50 = 25.0 nM 7.60
CHEMBL1644664 IC50 = 42.0 nM 7.38
CHEMBL1644659 IC50 = 51.0 nM 7.29
CHEMBL1644661 IC50 = 72.0 nM 7.14
CHEMBL265502 SURAMIN IC50 = 120.0 nM 6.92
CHEMBL1644657 IC50 = 280.0 nM 6.55
CHEMBL1644667 IC50 = 4500.0 nM 5.35
CHEMBL1644665 IC50 = 9000.0 nM 5.05
CHEMBL1644653 IC50 = 41000.0 nM 4.39
CHEMBL1644662 IC50 = 43000.0 nM 4.37
CHEMBL61 PODOFILOX IC50 - -
CHEMBL1644666 IC50 - -
CHEMBL1644663 IC50 - -
CHEMBL1644654 IC50 = 140000.0 nM -