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Assay Detail

CHEMBL1837597

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

Functional
Antitrypanosomal activity against blood stream form Trypanosoma brucei brucei by resazurin fluorescence-based viability assay
19
Total Activities
19
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

Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: discovery, synthesis, and characterization of their binding mode by protein crystallography.
Patterson S, Alphey MS, Jones DC, Shanks EJ, Street IP, Frearson JA, Wyatt PG, Gilbert IH, Fairlamb AH.
J Med Chem (2011) 54 : 6514 -6530
PubMed 21851087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.43 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836572 1 6.36
CHEMBL1836574 1 6.26
CHEMBL1836603 1 6.14
CHEMBL1836575 1 6.12
CHEMBL1836376 1 5.89
CHEMBL1836615 1 5.85
CHEMBL1836611 1 5.82
CHEMBL1836606 1 5.70
CHEMBL1836380 1 5.57
CHEMBL1836378 1 5.36
CHEMBL1836570 1 5.25
CHEMBL1836371 1 5.19
CHEMBL1836567 1 5.00
CHEMBL1836571 1 4.92
CHEMBL1836562 1 4.89
CHEMBL1836365 1 4.89
CHEMBL1836368 1 4.85
CHEMBL1836559 1 4.72
CHEMBL1836554 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836572 EC50 = 440.0 nM 6.36
CHEMBL1836574 EC50 = 550.0 nM 6.26
CHEMBL1836603 EC50 = 730.0 nM 6.14
CHEMBL1836575 EC50 = 750.0 nM 6.12
CHEMBL1836376 EC50 = 1300.0 nM 5.89
CHEMBL1836615 EC50 = 1400.0 nM 5.85
CHEMBL1836611 EC50 = 1500.0 nM 5.82
CHEMBL1836606 EC50 = 2000.0 nM 5.70
CHEMBL1836380 EC50 = 2700.0 nM 5.57
CHEMBL1836378 EC50 = 4400.0 nM 5.36
CHEMBL1836570 EC50 = 5600.0 nM 5.25
CHEMBL1836371 EC50 = 6400.0 nM 5.19
CHEMBL1836567 EC50 = 10000.0 nM 5.00
CHEMBL1836571 EC50 = 12000.0 nM 4.92
CHEMBL1836562 EC50 = 13000.0 nM 4.89
CHEMBL1836365 EC50 = 13000.0 nM 4.89
CHEMBL1836368 EC50 = 14000.0 nM 4.85
CHEMBL1836559 EC50 = 19000.0 nM 4.72
CHEMBL1836554 EC50 = 40000.0 nM 4.40