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Assay Detail

CHEMBL5115680

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

Functional
Antitrypanosomal activity against intracellularTrypanosoma cruzi amastigote
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease.
McGonagle K, Tarver GJ, Cantizani J, Cotillo I, Dodd PG, Ferguson L, Gilbert IH, Marco M, Miles T, Naylor C, Osuna-Cabello M, Paterson C, Read KD, Pinto EG, Riley J, Scullion P, Shishikura Y, Simeons F, Stojanovski L, Svensen N, Thomas J, Wyatt PG, Manzano P, De Rycker M, Thomas MG.
Eur J Med Chem (2022) 238 : 114421 -114421
PubMed 35594652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 47 5.43 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5171327 1 6.80
CHEMBL5187467 1 6.80
CHEMBL5181614 1 6.70
CHEMBL3546548 1 6.40
CHEMBL5195708 1 6.30
CHEMBL5186876 1 6.20
CHEMBL5186388 1 6.00
CHEMBL5187359 1 6.00
CHEMBL5179868 1 5.90
CHEMBL5204107 1 5.80
CHEMBL5200127 1 5.70
CHEMBL5205066 1 5.50
CHEMBL5206675 1 5.50
CHEMBL5185578 1 5.50
CHEMBL5185400 1 5.40
CHEMBL5195813 1 5.40
CHEMBL5205296 1 5.30
CHEMBL5174062 1 5.30
CHEMBL5208894 1 5.20
CHEMBL5198680 1 5.20
CHEMBL5198955 1 5.20
CHEMBL5195923 1 5.20
CHEMBL5205362 1 5.10
CHEMBL5197401 1 5.10
CHEMBL5191547 1 5.00
CHEMBL5173853 1 5.00
CHEMBL5173156 1 4.90
CHEMBL5196386 1 4.90
CHEMBL5205290 1 4.80
CHEMBL5177328 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5171327 EC50 = 158.49 nM 6.80
CHEMBL5187467 EC50 = 158.49 nM 6.80
CHEMBL5181614 EC50 = 199.53 nM 6.70
CHEMBL3546548 EC50 = 398.11 nM 6.40
CHEMBL5195708 EC50 = 501.19 nM 6.30
CHEMBL5186876 EC50 = 630.96 nM 6.20
CHEMBL5186388 EC50 = 1000.0 nM 6.00
CHEMBL5187359 EC50 = 1000.0 nM 6.00
CHEMBL5179868 EC50 = 1258.93 nM 5.90
CHEMBL5204107 EC50 = 1584.89 nM 5.80
CHEMBL5200127 EC50 = 1995.26 nM 5.70
CHEMBL5206675 EC50 = 3162.28 nM 5.50
CHEMBL5185578 EC50 = 3162.28 nM 5.50
CHEMBL5205066 EC50 = 3162.28 nM 5.50
CHEMBL5195813 EC50 = 3981.07 nM 5.40
CHEMBL5185400 EC50 = 3981.07 nM 5.40
CHEMBL5205296 EC50 = 5011.87 nM 5.30
CHEMBL5174062 EC50 = 5011.87 nM 5.30
CHEMBL5208894 EC50 = 6309.57 nM 5.20
CHEMBL5198680 EC50 = 6309.57 nM 5.20
CHEMBL5198955 EC50 = 6309.57 nM 5.20
CHEMBL5195923 EC50 = 6309.57 nM 5.20
CHEMBL5197401 EC50 = 7943.28 nM 5.10
CHEMBL5205362 EC50 = 7943.28 nM 5.10
CHEMBL5191547 EC50 = 10000.0 nM 5.00
CHEMBL5173853 EC50 = 10000.0 nM 5.00
CHEMBL5173156 EC50 = 12589.25 nM 4.90
CHEMBL5196386 EC50 = 12589.25 nM 4.90
CHEMBL5205290 EC50 = 15848.93 nM 4.80
CHEMBL5177328 EC50 = 15848.93 nM 4.80
CHEMBL5198768 EC50 = 15848.93 nM 4.80
CHEMBL5171508 EC50 = 15848.93 nM 4.80
CHEMBL5194318 EC50 = 19952.62 nM 4.70
CHEMBL5195384 EC50 = 25118.86 nM 4.60
CHEMBL5178331 EC50 = 50118.72 nM 4.30
CHEMBL5196051 EC50 > 50118.72 nM -
CHEMBL5184676 EC50 > 50118.72 nM -
CHEMBL5174453 EC50 > 50118.72 nM -
CHEMBL5204051 EC50 > 50118.72 nM -
CHEMBL5193764 EC50 > 50118.72 nM -
CHEMBL5185181 EC50 > 50118.72 nM -
CHEMBL5200858 EC50 > 50118.72 nM -
CHEMBL5194351 EC50 > 50118.72 nM -
CHEMBL5190564 EC50 > 50118.72 nM -
CHEMBL5195080 EC50 > 50118.72 nM -
CHEMBL5209474 EC50 > 50118.72 nM -
CHEMBL5178648 EC50 > 50118.72 nM -