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Assay Detail

CHEMBL4700085

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 infected in human HEK293 cells assessed as parasite growth inhibition measured after 48 hrs by alamar blue assay
49
Total Activities
49
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

Hit-to-lead optimization of novel benzimidazole phenylacetamides as broad spectrum trypanosomacides
McNamara, Nicole, Rahmani, Raphael, Sykes, Melissa L., Avery, Vicky M., Baell, Jonathan
RSC Med Chem (2020) 11 : 685 -695
PubMed 33479668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 5.54 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 7.85
CHEMBL469912 PUROMYCIN 2.0 1 7.42
CHEMBL380216 DIMINAZENE DIACETURATE 1 7.06
CHEMBL4758264 1 6.05
CHEMBL4743083 1 5.82
CHEMBL3431111 1 5.70
CHEMBL4747355 1 5.70
CHEMBL4796000 1 5.68
CHEMBL4785216 1 5.64
CHEMBL4800536 1 5.62
CHEMBL4777875 1 5.62
CHEMBL4784548 1 5.60
CHEMBL4778729 1 5.58
CHEMBL4746059 1 5.58
CHEMBL4777056 1 5.55
CHEMBL4787692 1 5.54
CHEMBL2098075 1 5.51
CHEMBL4781677 1 5.50
CHEMBL4748426 1 5.50
CHEMBL4756128 1 5.47
CHEMBL4743470 1 5.46
CHEMBL4746266 1 5.44
CHEMBL4746844 1 5.44
CHEMBL4777653 1 5.44
CHEMBL4760278 1 5.43
CHEMBL3235190 1 5.42
CHEMBL1443198 1 5.42
CHEMBL4791657 1 5.39
CHEMBL4795724 1 5.37
CHEMBL4795131 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 14.0 nM 7.85
CHEMBL469912 PUROMYCIN IC50 = 38.0 nM 7.42
CHEMBL380216 DIMINAZENE DIACETURATE IC50 = 87.0 nM 7.06
CHEMBL4758264 IC50 = 900.0 nM 6.05
CHEMBL4743083 IC50 = 1500.0 nM 5.82
CHEMBL3431111 IC50 = 2000.0 nM 5.70
CHEMBL4747355 IC50 = 2000.0 nM 5.70
CHEMBL4796000 IC50 = 2100.0 nM 5.68
CHEMBL4785216 IC50 = 2300.0 nM 5.64
CHEMBL4800536 IC50 = 2400.0 nM 5.62
CHEMBL4777875 IC50 = 2400.0 nM 5.62
CHEMBL4784548 IC50 = 2500.0 nM 5.60
CHEMBL4746059 IC50 = 2600.0 nM 5.58
CHEMBL4778729 IC50 = 2600.0 nM 5.58
CHEMBL4777056 IC50 = 2800.0 nM 5.55
CHEMBL4787692 IC50 = 2900.0 nM 5.54
CHEMBL2098075 IC50 = 3100.0 nM 5.51
CHEMBL4781677 IC50 = 3200.0 nM 5.50
CHEMBL4748426 IC50 = 3200.0 nM 5.50
CHEMBL4756128 IC50 = 3400.0 nM 5.47
CHEMBL4743470 IC50 = 3500.0 nM 5.46
CHEMBL4746266 IC50 = 3600.0 nM 5.44
CHEMBL4746844 IC50 = 3600.0 nM 5.44
CHEMBL4777653 IC50 = 3600.0 nM 5.44
CHEMBL4760278 IC50 = 3700.0 nM 5.43
CHEMBL1443198 IC50 = 3800.0 nM 5.42
CHEMBL3235190 IC50 = 3800.0 nM 5.42
CHEMBL4791657 IC50 = 4100.0 nM 5.39
CHEMBL4795724 IC50 = 4300.0 nM 5.37
CHEMBL4795131 IC50 = 4400.0 nM 5.36
CHEMBL4750809 IC50 = 4400.0 nM 5.36
CHEMBL4747847 IC50 = 4500.0 nM 5.35
CHEMBL4749436 IC50 = 5000.0 nM 5.30
CHEMBL4751320 IC50 = 5200.0 nM 5.28
CHEMBL4790719 IC50 = 5400.0 nM 5.27
CHEMBL4740748 IC50 = 5500.0 nM 5.26
CHEMBL4740712 IC50 = 7300.0 nM 5.14
CHEMBL4782335 IC50 = 9400.0 nM 5.03
CHEMBL4786189 IC50 = 11000.0 nM 4.96
CHEMBL4751949 IC50 = 14000.0 nM 4.85
CHEMBL4757252 IC50 = 15000.0 nM 4.82
CHEMBL4749669 IC50 = 16000.0 nM 4.80
CHEMBL4744411 IC50 = 19000.0 nM 4.72
CHEMBL4751511 IC50 > 83000.0 nM -
CHEMBL4790847 IC50 > 83000.0 nM -
CHEMBL4778352 IC50 > 83000.0 nM -
CHEMBL4788748 IC50 > 83000.0 nM -
CHEMBL4792087 IC50 > 83000.0 nM -
CHEMBL4743974 IC50 > 83000.0 nM -