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Assay Detail

CHEMBL4680485

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 blood stream forms after 72 hrs by resazurin dye based fluorescence assay
30
Total Activities
30
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-property studies of an imidazoquinoline chemotype with antitrypanosomal activity
Klug, Dana M., Diaz-Gonzalez, Rosario, DeLano, Travis J., Mavrogiannaki, Eftychia M., Buskes, Melissa J., Dalton, Raeann M., Fisher, John K., Schneider, Katherine M., Hilborne, Vivian, Fritsche, Melanie G., Simpson, Quillon J., Tear, Westley F., Devine, William G., Perez-Moreno, Guiomar, Ceballos-Perez, Gloria, Garcia-HernAndez, Raquel, Bosch-Navarrete, Cristina, Ruiz-Perez, Luis Miguel, Gamarro, Francisco, GonzAlez-Pacanowska, Dolores, Martinez-Martinez, Maria Santos, Manzano-Chinchon, Pilar, Navarro, Miguel, Pollastri, Michael P., Ferrins, Lori
RSC Med Chem (2020) 11 : 950 -959
PubMed 33479690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 6.33 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1879463 DACTOLISIB 3.0 1 8.70
CHEMBL4786814 1 8.20
CHEMBL4753757 1 8.10
CHEMBL4764546 1 8.10
CHEMBL4750442 1 7.80
CHEMBL4758874 1 7.70
CHEMBL4776376 1 7.70
CHEMBL4740571 1 7.40
CHEMBL4799228 1 6.80
CHEMBL4761576 1 6.80
CHEMBL4796633 1 6.20
CHEMBL4761919 1 6.10
CHEMBL4762633 1 6.10
CHEMBL4790031 1 6.10
CHEMBL4790499 1 5.90
CHEMBL4791712 1 5.90
CHEMBL4795660 1 5.80
CHEMBL4780547 1 5.80
CHEMBL4756094 1 5.80
CHEMBL4762558 1 5.70
CHEMBL4761457 1 5.60
CHEMBL4787851 1 5.20
CHEMBL4742777 1 5.20
CHEMBL4743077 1 5.00
CHEMBL3290295 1 5.00
CHEMBL4764775 1 4.90
CHEMBL4753533 1 4.90
CHEMBL4795669 1 4.60
CHEMBL4782388 1 -
CHEMBL4787117 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1879463 DACTOLISIB EC50 = 1.995 nM 8.70
CHEMBL4786814 EC50 = 6.31 nM 8.20
CHEMBL4753757 EC50 = 7.943 nM 8.10
CHEMBL4764546 EC50 = 7.943 nM 8.10
CHEMBL4750442 EC50 = 15.85 nM 7.80
CHEMBL4758874 EC50 = 19.95 nM 7.70
CHEMBL4776376 EC50 = 19.95 nM 7.70
CHEMBL4740571 EC50 = 39.81 nM 7.40
CHEMBL4799228 EC50 = 158.49 nM 6.80
CHEMBL4761576 EC50 = 158.49 nM 6.80
CHEMBL4796633 EC50 = 630.96 nM 6.20
CHEMBL4761919 EC50 = 794.33 nM 6.10
CHEMBL4762633 EC50 = 794.33 nM 6.10
CHEMBL4790031 EC50 = 794.33 nM 6.10
CHEMBL4790499 EC50 = 1258.93 nM 5.90
CHEMBL4791712 EC50 = 1258.93 nM 5.90
CHEMBL4795660 EC50 = 1584.89 nM 5.80
CHEMBL4780547 EC50 = 1584.89 nM 5.80
CHEMBL4756094 EC50 = 1584.89 nM 5.80
CHEMBL4762558 EC50 = 1995.26 nM 5.70
CHEMBL4761457 EC50 = 2511.89 nM 5.60
CHEMBL4787851 EC50 = 6309.57 nM 5.20
CHEMBL4742777 EC50 = 6309.57 nM 5.20
CHEMBL4743077 EC50 = 10000.0 nM 5.00
CHEMBL3290295 EC50 = 10000.0 nM 5.00
CHEMBL4764775 EC50 = 12589.25 nM 4.90
CHEMBL4753533 EC50 = 12589.25 nM 4.90
CHEMBL4795669 EC50 = 25118.86 nM 4.60
CHEMBL4782388 EC50 > 39810.72 nM -
CHEMBL4787117 EC50 < 1.995 nM -