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Assay Detail

CHEMBL4057136

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei TC221 after 72 hrs by alamar blue assay
38
Total Activities
38
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

Bistacrines as potential antitrypanosomal agents.
Schmidt I, Göllner S, Fuß A, Stich A, Kucharski A, Schirmeister T, Katzowitsch E, Bruhn H, Miliu A, Krauth-Siegel RL, Holzgrabe U.
Bioorg Med Chem (2017) 25 : 4526 -4531
PubMed 28698054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.73 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066464 1 8.00
CHEMBL3815015 1 6.85
CHEMBL386423 1 6.82
CHEMBL424707 1 6.80
CHEMBL4103108 1 6.68
CHEMBL4084963 1 6.60
CHEMBL4102912 1 6.60
CHEMBL73800 1 6.48
CHEMBL4078832 1 6.38
CHEMBL32823 1 6.23
CHEMBL75274 1 6.18
CHEMBL3814557 1 6.17
CHEMBL4063546 1 6.16
CHEMBL3814548 1 6.15
CHEMBL73160 1 6.15
CHEMBL3813885 1 6.14
CHEMBL4095162 1 6.06
CHEMBL211313 1 5.68
CHEMBL4105680 1 5.47
CHEMBL3813881 1 5.47
CHEMBL3815079 1 5.46
CHEMBL4070827 1 5.46
CHEMBL4098222 1 5.43
CHEMBL4078037 1 5.43
CHEMBL4071169 1 5.32
CHEMBL213377 1 5.29
CHEMBL378006 1 5.25
CHEMBL179732 1 5.19
CHEMBL4102299 1 4.99
CHEMBL4097935 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066464 IC50 = 10.0 nM 8.00
CHEMBL3815015 IC50 = 140.0 nM 6.85
CHEMBL386423 IC50 = 150.0 nM 6.82
CHEMBL424707 IC50 = 160.0 nM 6.80
CHEMBL4103108 IC50 = 210.0 nM 6.68
CHEMBL4084963 IC50 = 250.0 nM 6.60
CHEMBL4102912 IC50 = 250.0 nM 6.60
CHEMBL73800 IC50 = 330.0 nM 6.48
CHEMBL4078832 IC50 = 420.0 nM 6.38
CHEMBL32823 IC50 = 590.0 nM 6.23
CHEMBL75274 IC50 = 660.0 nM 6.18
CHEMBL3814557 IC50 = 680.0 nM 6.17
CHEMBL4063546 IC50 = 700.0 nM 6.16
CHEMBL3814548 IC50 = 710.0 nM 6.15
CHEMBL73160 IC50 = 710.0 nM 6.15
CHEMBL3813885 IC50 = 720.0 nM 6.14
CHEMBL4095162 IC50 = 880.0 nM 6.06
CHEMBL211313 IC50 = 2100.0 nM 5.68
CHEMBL3813881 IC50 = 3400.0 nM 5.47
CHEMBL4105680 IC50 = 3400.0 nM 5.47
CHEMBL3815079 IC50 = 3500.0 nM 5.46
CHEMBL4070827 IC50 = 3500.0 nM 5.46
CHEMBL4098222 IC50 = 3700.0 nM 5.43
CHEMBL4078037 IC50 = 3700.0 nM 5.43
CHEMBL4071169 IC50 = 4800.0 nM 5.32
CHEMBL213377 IC50 = 5100.0 nM 5.29
CHEMBL378006 IC50 = 5600.0 nM 5.25
CHEMBL179732 IC50 = 6400.0 nM 5.19
CHEMBL4102299 IC50 = 10300.0 nM 4.99
CHEMBL4097935 IC50 = 13400.0 nM 4.87
CHEMBL59977 IC50 = 15100.0 nM 4.82
CHEMBL62084 IC50 = 16500.0 nM 4.78
CHEMBL292314 IC50 = 17100.0 nM 4.77
CHEMBL4068111 IC50 = 17200.0 nM 4.76
CHEMBL1626324 IC50 = 18000.0 nM 4.75
CHEMBL4078987 IC50 = 17600.0 nM 4.75
CHEMBL2094322 IC50 = 18100.0 nM 4.74
CHEMBL95 TACRINE IC50 = 18400.0 nM 4.74