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Assay Detail

CHEMBL3804505

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms incubated for 48 hrs by alamar blue assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics.
Scott FJ, Khalaf AI, Giordani F, Wong PE, Duffy S, Barrett M, Avery VM, Suckling CJ.
Eur J Med Chem (2016) 116 : 116 -125
PubMed 27060763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.46 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35241 DIMINAZENE 2.0 1 8.30
CHEMBL3799766 1 8.27
CHEMBL338227 1 8.17
CHEMBL3797456 1 8.14
CHEMBL3798543 1 7.72
CHEMBL395187 1 7.40
CHEMBL3797687 1 6.77
CHEMBL394377 1 6.75
CHEMBL396361 1 6.75
CHEMBL3798852 1 6.68
CHEMBL3798718 1 6.66
CHEMBL126486 1 6.55
CHEMBL237235 1 6.52
CHEMBL394275 1 6.42
CHEMBL391515 1 6.41
CHEMBL3798709 1 6.40
CHEMBL236563 1 6.21
CHEMBL236564 1 6.20
CHEMBL3800015 1 6.15
CHEMBL3798376 1 6.14
CHEMBL95965 1 6.10
CHEMBL3798328 1 6.10
CHEMBL3797620 1 6.01
CHEMBL3797790 1 5.66
CHEMBL3800142 1 5.40
CHEMBL3800571 1 5.31
CHEMBL235083 1 5.30
CHEMBL3797682 1 4.57
CHEMBL3798993 1 4.32
CHEMBL397524 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35241 DIMINAZENE IC50 = 5.0 nM 8.30
CHEMBL3799766 IC50 = 5.4 nM 8.27
CHEMBL338227 IC50 = 6.8 nM 8.17
CHEMBL3797456 IC50 = 7.3 nM 8.14
CHEMBL3798543 IC50 = 19.0 nM 7.72
CHEMBL395187 IC50 = 40.0 nM 7.40
CHEMBL3797687 IC50 = 170.0 nM 6.77
CHEMBL394377 IC50 = 180.0 nM 6.75
CHEMBL396361 IC50 = 180.0 nM 6.75
CHEMBL3798852 IC50 = 210.0 nM 6.68
CHEMBL3798718 IC50 = 220.0 nM 6.66
CHEMBL126486 IC50 = 280.0 nM 6.55
CHEMBL237235 IC50 = 300.0 nM 6.52
CHEMBL394275 IC50 = 380.0 nM 6.42
CHEMBL391515 IC50 = 390.0 nM 6.41
CHEMBL3798709 IC50 = 400.0 nM 6.40
CHEMBL236563 IC50 = 620.0 nM 6.21
CHEMBL236564 IC50 = 630.0 nM 6.20
CHEMBL3800015 IC50 = 710.0 nM 6.15
CHEMBL3798376 IC50 = 730.0 nM 6.14
CHEMBL95965 IC50 = 790.0 nM 6.10
CHEMBL3798328 IC50 = 790.0 nM 6.10
CHEMBL3797620 IC50 = 970.0 nM 6.01
CHEMBL3797790 IC50 = 2200.0 nM 5.66
CHEMBL3800142 IC50 = 4000.0 nM 5.40
CHEMBL3800571 IC50 = 4900.0 nM 5.31
CHEMBL235083 IC50 = 5000.0 nM 5.30
CHEMBL3797682 IC50 = 27000.0 nM 4.57
CHEMBL3798993 IC50 = 48000.0 nM 4.32
CHEMBL397524 IC50 > 75000.0 nM -
CHEMBL236153 IC50 > 75000.0 nM -
CHEMBL235938 IC50 > 75000.0 nM -
CHEMBL235026 IC50 > 75000.0 nM -