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Assay Detail

CHEMBL5370872

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

Functional
Antileishmanial activity against promastigote stage of Leishmania infantum MHOM/BR/1974/PP75 infected in human THP-1 cells assessed as parasite growth inhibition incubated for 72 hrs by microplate reader analysis
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania infantum
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

Leishmania infantum (CHEMBL612848)
Type ORGANISM
Organism Leishmania infantum

Publication

Hit-to-lead optimization of a pyrazinylpiperazine series against Leishmania infantum and Leishmania braziliensis.
Jacques Dit Lapierre TJW, Cruz MGFML, Brito NPF, Resende DM, Souza FO, Pilau EJ, da Silva MFB, Neves BJ, Murta SMF, Rezende Júnior CO.
Eur J Med Chem (2023) 256 : 115445 -115445
PubMed 37156183 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 4.97 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267345 AMPHOTERICIN B 4.0 1 6.60
CHEMBL5407179 1 5.72
CHEMBL5402532 1 5.55
CHEMBL5436490 1 5.54
CHEMBL5437482 1 5.51
CHEMBL5397842 1 5.48
CHEMBL5406357 1 5.48
CHEMBL5416460 1 5.46
CHEMBL5396330 1 5.35
CHEMBL5396842 1 5.29
CHEMBL5418830 1 5.28
CHEMBL5398251 1 5.24
CHEMBL5414096 1 5.21
CHEMBL5426223 1 5.14
CHEMBL5400035 1 5.12
CHEMBL5430423 1 4.97
CHEMBL3431258 1 4.92
CHEMBL5428957 1 4.85
CHEMBL5394006 1 4.80
CHEMBL5416563 1 4.66
CHEMBL5429046 1 4.60
CHEMBL5419956 1 4.58
CHEMBL5430852 1 4.56
CHEMBL5434127 1 4.46
CHEMBL5431973 1 4.45
CHEMBL5402709 1 4.36
CHEMBL5428270 1 4.26
CHEMBL5398366 1 4.23
CHEMBL5438033 1 4.20
CHEMBL5412591 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267345 AMPHOTERICIN B IC50 = 250.0 nM 6.60
CHEMBL5407179 IC50 = 1900.0 nM 5.72
CHEMBL5402532 IC50 = 2800.0 nM 5.55
CHEMBL5436490 IC50 = 2900.0 nM 5.54
CHEMBL5437482 IC50 = 3100.0 nM 5.51
CHEMBL5397842 IC50 = 3300.0 nM 5.48
CHEMBL5406357 IC50 = 3300.0 nM 5.48
CHEMBL5416460 IC50 = 3500.0 nM 5.46
CHEMBL5396330 IC50 = 4500.0 nM 5.35
CHEMBL5396842 IC50 = 5100.0 nM 5.29
CHEMBL5418830 IC50 = 5300.0 nM 5.28
CHEMBL5398251 IC50 = 5800.0 nM 5.24
CHEMBL5414096 IC50 = 6200.0 nM 5.21
CHEMBL5426223 IC50 = 7300.0 nM 5.14
CHEMBL5400035 IC50 = 7500.0 nM 5.12
CHEMBL5430423 IC50 = 10800.0 nM 4.97
CHEMBL3431258 IC50 = 11900.0 nM 4.92
CHEMBL5428957 IC50 = 14200.0 nM 4.85
CHEMBL5394006 IC50 = 15900.0 nM 4.80
CHEMBL5416563 IC50 = 21900.0 nM 4.66
CHEMBL5429046 IC50 = 25300.0 nM 4.60
CHEMBL5419956 IC50 = 26400.0 nM 4.58
CHEMBL5430852 IC50 = 27500.0 nM 4.56
CHEMBL5434127 IC50 = 34300.0 nM 4.46
CHEMBL5431973 IC50 = 35200.0 nM 4.45
CHEMBL5402709 IC50 = 43600.0 nM 4.36
CHEMBL5428270 IC50 = 55300.0 nM 4.26
CHEMBL5398366 IC50 = 58800.0 nM 4.23
CHEMBL5438033 IC50 = 63100.0 nM 4.20
CHEMBL5412591 IC50 = 64800.0 nM 4.19
CHEMBL5429051 IC50 = 84500.0 nM 4.07
CHEMBL5439730 IC50 = 280500.0 nM -
CHEMBL5438796 IC50 = 221000.0 nM -
CHEMBL5433944 IC50 = 141700.0 nM -
CHEMBL5411027 IC50 = 127800.0 nM -
CHEMBL5425292 IC50 = 7431000.0 nM -
CHEMBL5407537 IC50 = 105200.0 nM -
CHEMBL5413093 IC50 = 112700.0 nM -
CHEMBL5430658 IC50 = 175800.0 nM -
CHEMBL5416541 IC50 = 156700.0 nM -
CHEMBL5430403 IC50 = 112500.0 nM -
CHEMBL1877859 IC50 = 122300.0 nM -