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Assay Detail

CHEMBL3108259

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as growth inhibition after 70 hrs by Alamar blue assay
27
Total Activities
27
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

Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
Patrick DA, Bakunov SA, Bakunova SM, Wenzler T, Brun R, Tidwell RR.
Bioorg Med Chem (2014) 22 : 559 -576
PubMed 24268543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.34 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217053 1 8.74
CHEMBL3216615 1 8.57
CHEMBL24057 FURAMIDINE -1.0 1 8.52
CHEMBL55 PENTAMIDINE 4.0 1 8.52
CHEMBL3216167 1 8.43
CHEMBL166 MELARSOPROL 3.0 1 8.40
CHEMBL3216850 1 8.23
CHEMBL3217270 1 8.21
CHEMBL3215723 1 8.14
CHEMBL3217055 1 7.92
CHEMBL3217057 1 7.87
CHEMBL3216848 1 7.84
CHEMBL3217049 1 7.80
CHEMBL3105253 1 7.72
CHEMBL3217052 1 7.62
CHEMBL3217056 1 7.30
CHEMBL3215961 1 7.28
CHEMBL3216614 1 7.19
CHEMBL3217274 1 6.74
CHEMBL3217269 1 6.68
CHEMBL3105271 1 6.31
CHEMBL3215955 1 6.23
CHEMBL3215722 1 6.22
CHEMBL3216376 1 5.78
CHEMBL3216170 1 5.47
CHEMBL3217058 1 5.24
CHEMBL3215956 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217053 IC50 = 1.8 nM 8.74
CHEMBL3216615 IC50 = 2.7 nM 8.57
CHEMBL24057 FURAMIDINE IC50 = 3.0 nM 8.52
CHEMBL55 PENTAMIDINE IC50 = 3.0 nM 8.52
CHEMBL3216167 IC50 = 3.7 nM 8.43
CHEMBL166 MELARSOPROL IC50 = 4.0 nM 8.40
CHEMBL3216850 IC50 = 5.9 nM 8.23
CHEMBL3217270 IC50 = 6.2 nM 8.21
CHEMBL3215723 IC50 = 7.2 nM 8.14
CHEMBL3217055 IC50 = 12.1 nM 7.92
CHEMBL3217057 IC50 = 13.6 nM 7.87
CHEMBL3216848 IC50 = 14.4 nM 7.84
CHEMBL3217049 IC50 = 16.0 nM 7.80
CHEMBL3105253 IC50 = 19.1 nM 7.72
CHEMBL3217052 IC50 = 23.9 nM 7.62
CHEMBL3217056 IC50 = 50.5 nM 7.30
CHEMBL3215961 IC50 = 52.8 nM 7.28
CHEMBL3216614 IC50 = 64.3 nM 7.19
CHEMBL3217274 IC50 = 183.0 nM 6.74
CHEMBL3217269 IC50 = 207.0 nM 6.68
CHEMBL3105271 IC50 = 492.0 nM 6.31
CHEMBL3215955 IC50 = 583.0 nM 6.23
CHEMBL3215722 IC50 = 596.0 nM 6.22
CHEMBL3216376 IC50 = 1670.0 nM 5.78
CHEMBL3216170 IC50 = 3380.0 nM 5.47
CHEMBL3217058 IC50 = 5710.0 nM 5.24
CHEMBL3215956 IC50 = 6120.0 nM 5.21