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Assay Detail

CHEMBL4313830

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

Functional
Antitrypanosomal activity against Trypanosoma brucei bloodstream form assessed as parasite growth inhibition incubated for 72 hrs by resazurin dye based assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
Borsari C, Jiménez-Antón MD, Eick J, Bifeld E, Torrado JJ, Olías-Molero AI, Corral MJ, Santarem N, Baptista C, Severi L, Gul S, Wolf M, Kuzikov M, Ellinger B, Reinshagen J, Witt G, Linciano P, Tait A, Costantino L, Luciani R, Tejera Nevado P, Zander-Dinse D, Franco CH, Ferrari S, Moraes CB, Cordeiro-da-Silva A, Ponterini G, Clos J, Alunda JM, Costi MP.
Eur J Med Chem (2019) 183 : 111676 -111676
PubMed 31542713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 39 5.65 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110 BENZNIDAZOLE 4.0 1 7.80
CHEMBL4450031 1 6.40
CHEMBL4464312 1 6.10
CHEMBL4567447 1 5.89
CHEMBL4441917 1 5.89
CHEMBL4473268 1 5.85
CHEMBL4469979 1 5.82
CHEMBL4447054 1 5.82
CHEMBL4565781 1 5.77
CHEMBL4439246 1 5.70
CHEMBL4575467 1 5.68
CHEMBL4458341 1 5.58
CHEMBL4539604 1 5.55
CHEMBL4439388 1 5.52
CHEMBL4590171 1 5.52
CHEMBL4592506 1 5.51
CHEMBL4448565 1 5.51
CHEMBL4453866 1 5.48
CHEMBL4588892 1 5.47
CHEMBL4592720 1 5.43
CHEMBL4575126 1 5.41
CHEMBL4541910 1 5.35
CHEMBL4446646 1 5.31
CHEMBL4471364 1 5.31
CHEMBL4448476 1 5.27
CHEMBL4444621 1 5.24
CHEMBL125 MILTEFOSINE 4.0 1 4.47
CHEMBL4531258 1 -
CHEMBL4465877 1 -
CHEMBL4459417 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110 BENZNIDAZOLE EC50 = 16.0 nM 7.80
CHEMBL4450031 EC50 = 400.0 nM 6.40
CHEMBL4464312 EC50 = 800.0 nM 6.10
CHEMBL4567447 EC50 = 1300.0 nM 5.89
CHEMBL4441917 EC50 = 1300.0 nM 5.89
CHEMBL4473268 EC50 = 1400.0 nM 5.85
CHEMBL4469979 EC50 = 1500.0 nM 5.82
CHEMBL4447054 EC50 = 1500.0 nM 5.82
CHEMBL4565781 EC50 = 1700.0 nM 5.77
CHEMBL4439246 EC50 = 2000.0 nM 5.70
CHEMBL4575467 EC50 = 2100.0 nM 5.68
CHEMBL4458341 EC50 = 2600.0 nM 5.58
CHEMBL4539604 EC50 = 2800.0 nM 5.55
CHEMBL4439388 EC50 = 3000.0 nM 5.52
CHEMBL4590171 EC50 = 3000.0 nM 5.52
CHEMBL4592506 EC50 = 3100.0 nM 5.51
CHEMBL4448565 EC50 = 3100.0 nM 5.51
CHEMBL4453866 EC50 = 3300.0 nM 5.48
CHEMBL4588892 EC50 = 3400.0 nM 5.47
CHEMBL4592720 EC50 = 3700.0 nM 5.43
CHEMBL4575126 EC50 = 3900.0 nM 5.41
CHEMBL4541910 EC50 = 4500.0 nM 5.35
CHEMBL4446646 EC50 = 4900.0 nM 5.31
CHEMBL4471364 EC50 = 4900.0 nM 5.31
CHEMBL4448476 EC50 = 5340.0 nM 5.27
CHEMBL4444621 EC50 = 5700.0 nM 5.24
CHEMBL125 MILTEFOSINE EC50 = 34000.0 nM 4.47
CHEMBL4567834 EC50 - -
CHEMBL4538581 EC50 - -
CHEMBL4457377 EC50 - -
CHEMBL4520438 EC50 - -
CHEMBL4563463 EC50 - -
CHEMBL4519474 EC50 - -
CHEMBL4438959 EC50 - -
CHEMBL4445329 EC50 - -
CHEMBL4450073 EC50 - -
CHEMBL4459417 EC50 - -
CHEMBL4465877 EC50 - -
CHEMBL4531258 EC50 - -