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Assay Detail

CHEMBL3413259

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

Functional
Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar Blue assay
22
Total Activities
22
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

Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
Papadopoulou MV, Bloomer WD, Lepesheva GI, Rosenzweig HS, Kaiser M, Aguilera-Venegas B, Wilkinson SR, Chatelain E, Ioset JR.
J Med Chem (2015) 58 : 1307 -1319
PubMed 25580906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.18 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.15
CHEMBL3410620 1 6.47
CHEMBL3410622 1 6.04
CHEMBL3410634 1 5.96
CHEMBL3410628 1 5.76
CHEMBL3410631 1 5.74
CHEMBL3410636 1 5.54
CHEMBL3407532 1 5.39
CHEMBL3410625 1 5.15
CHEMBL3410624 1 5.00
CHEMBL3410638 1 4.94
CHEMBL3410623 1 4.79
CHEMBL3410626 1 4.77
CHEMBL3410635 1 4.58
CHEMBL3410627 1 4.47
CHEMBL3410629 1 4.29
CHEMBL3410633 1 4.18
CHEMBL3410621 1 4.13
CHEMBL3410639 1 4.12
CHEMBL3410630 1 4.12
CHEMBL3410632 1 -
CHEMBL3410637 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 7.0 nM 8.15
CHEMBL3410620 IC50 = 336.0 nM 6.47
CHEMBL3410622 IC50 = 901.0 nM 6.04
CHEMBL3410634 IC50 = 1090.0 nM 5.96
CHEMBL3410628 IC50 = 1750.0 nM 5.76
CHEMBL3410631 IC50 = 1838.0 nM 5.74
CHEMBL3410636 IC50 = 2877.0 nM 5.54
CHEMBL3407532 IC50 = 4060.0 nM 5.39
CHEMBL3410625 IC50 = 7035.0 nM 5.15
CHEMBL3410624 IC50 = 10000.0 nM 5.00
CHEMBL3410638 IC50 = 11596.0 nM 4.94
CHEMBL3410623 IC50 = 16066.0 nM 4.79
CHEMBL3410626 IC50 = 17015.0 nM 4.77
CHEMBL3410635 IC50 = 26610.0 nM 4.58
CHEMBL3410627 IC50 = 34067.0 nM 4.47
CHEMBL3410629 IC50 = 51710.0 nM 4.29
CHEMBL3410633 IC50 = 65600.0 nM 4.18
CHEMBL3410621 IC50 = 73870.0 nM 4.13
CHEMBL3410639 IC50 = 76250.0 nM 4.12
CHEMBL3410630 IC50 = 76550.0 nM 4.12
CHEMBL3410632 IC50 = 153160.0 nM -
CHEMBL3410637 IC50 = 220860.0 nM -