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Assay Detail

CHEMBL3376834

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

Functional
Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 after 48 hrs by Alamar blue assay
31
Total Activities
31
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

Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1.
Khalaf AI, Huggan JK, Suckling CJ, Gibson CL, Stewart K, Giordani F, Barrett MP, Wong PE, Barrack KL, Hunter WN.
J Med Chem (2014) 57 : 6479 -6494
PubMed 25007262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.22 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319009 1 6.89
CHEMBL3319008 1 6.80
CHEMBL3319007 1 6.33
CHEMBL3318495 1 6.19
CHEMBL3318926 1 5.99
CHEMBL3318490 1 5.98
CHEMBL3318925 1 5.73
CHEMBL3318924 1 5.69
CHEMBL3318211 1 5.22
CHEMBL3318489 1 5.14
CHEMBL3318494 1 5.11
CHEMBL3319010 1 5.05
CHEMBL3318491 1 4.84
CHEMBL3318802 1 4.84
CHEMBL3318497 1 4.60
CHEMBL3318803 1 4.39
CHEMBL3318498 1 4.27
CHEMBL3318210 1 4.21
CHEMBL3318212 1 4.14
CHEMBL3318487 1 4.10
CHEMBL3318804 1 4.03
CHEMBL3318801 1 -
CHEMBL567351 1 -
CHEMBL3318496 1 -
CHEMBL3318207 1 -
CHEMBL3318208 1 -
CHEMBL3318209 1 -
CHEMBL3318206 1 -
CHEMBL3318493 1 -
CHEMBL3318213 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319009 IC50 = 130.0 nM 6.89
CHEMBL3319008 IC50 = 160.0 nM 6.80
CHEMBL3319007 IC50 = 470.0 nM 6.33
CHEMBL3318495 IC50 = 650.0 nM 6.19
CHEMBL3318926 IC50 = 1016.0 nM 5.99
CHEMBL3318490 IC50 = 1040.0 nM 5.98
CHEMBL3318925 IC50 = 1857.0 nM 5.73
CHEMBL3318924 IC50 = 2038.0 nM 5.69
CHEMBL3318211 IC50 = 6030.0 nM 5.22
CHEMBL3318489 IC50 = 7300.0 nM 5.14
CHEMBL3318494 IC50 = 7750.0 nM 5.11
CHEMBL3319010 IC50 = 8820.0 nM 5.05
CHEMBL3318491 IC50 = 14330.0 nM 4.84
CHEMBL3318802 IC50 = 14470.0 nM 4.84
CHEMBL3318497 IC50 = 25110.0 nM 4.60
CHEMBL3318803 IC50 = 41010.0 nM 4.39
CHEMBL3318498 IC50 = 53340.0 nM 4.27
CHEMBL3318210 IC50 = 62360.0 nM 4.21
CHEMBL3318212 IC50 = 72520.0 nM 4.14
CHEMBL3318487 IC50 = 80060.0 nM 4.10
CHEMBL3318804 IC50 = 93520.0 nM 4.03
CHEMBL3318801 IC50 = 170000.0 nM -
CHEMBL567351 IC50 = 7620000.0 nM -
CHEMBL3318496 IC50 = 125000.0 nM -
CHEMBL3318207 IC50 - -
CHEMBL3318208 IC50 - -
CHEMBL3318209 IC50 = 2440000.0 nM -
CHEMBL3318206 IC50 - -
CHEMBL3318493 IC50 = 139000.0 nM -
CHEMBL3318213 IC50 = 170000.0 nM -
CHEMBL3318492 IC50 = 340000.0 nM -