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Assay Detail

CHEMBL5586012

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

Functional
Antitrypanosomal activity against bloodstream trypomastigote form of Trypanosoma brucei Lister 427 assessed as reduction in parasite growth incubated for 72 hrs by alamar blue dye based fluorescence analysis
34
Total Activities
34
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

Revisiting the dipeptidyl carboxypeptidase inhibitor captopril as a source of pan anti-trypanosomatid agents.
Garsi JB, Hocine S, Hensienne R, Moitessier M, Denton H, Major LL, Smith TK, Hanessian S.
Bioorg Med Chem Lett (2024) 110 : 129883 -129883
PubMed 39013490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 34 5.00 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.70
CHEMBL5597520 1 5.84
CHEMBL5597846 1 5.72
CHEMBL5596772 1 5.71
CHEMBL5596985 1 5.61
CHEMBL5596379 1 5.39
CHEMBL5591156 1 5.23
CHEMBL5596170 1 5.23
CHEMBL5596663 1 5.16
CHEMBL5596153 1 5.12
CHEMBL5590596 1 5.01
CHEMBL5597345 1 5.01
CHEMBL5598023 1 5.00
CHEMBL5596953 1 4.91
CHEMBL5596255 1 4.91
CHEMBL5596086 1 4.88
CHEMBL5598194 1 4.83
CHEMBL5597972 1 4.82
CHEMBL305938 1 4.78
CHEMBL5590274 1 4.69
CHEMBL1560 CAPTOPRIL 4.0 1 4.64
CHEMBL5596258 1 4.58
CHEMBL5596792 1 4.55
CHEMBL10962 1 4.55
CHEMBL5596950 1 4.48
CHEMBL5597935 1 4.42
CHEMBL5597849 1 4.41
CHEMBL242863 1 4.39
CHEMBL5597720 1 4.23
CHEMBL5598285 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE EC50 = 2.0 nM 8.70
CHEMBL5597520 EC50 = 1440.0 nM 5.84
CHEMBL5597846 EC50 = 1920.0 nM 5.72
CHEMBL5596772 EC50 = 1950.0 nM 5.71
CHEMBL5596985 EC50 = 2460.0 nM 5.61
CHEMBL5596379 EC50 = 4110.0 nM 5.39
CHEMBL5591156 EC50 = 5940.0 nM 5.23
CHEMBL5596170 EC50 = 5900.0 nM 5.23
CHEMBL5596663 EC50 = 6900.0 nM 5.16
CHEMBL5596153 EC50 = 7520.0 nM 5.12
CHEMBL5590596 EC50 = 9850.0 nM 5.01
CHEMBL5597345 EC50 = 9700.0 nM 5.01
CHEMBL5598023 EC50 = 9900.0 nM 5.00
CHEMBL5596953 EC50 = 12200.0 nM 4.91
CHEMBL5596255 EC50 = 12400.0 nM 4.91
CHEMBL5596086 EC50 = 13200.0 nM 4.88
CHEMBL5598194 EC50 = 14800.0 nM 4.83
CHEMBL5597972 EC50 = 15200.0 nM 4.82
CHEMBL305938 EC50 = 16700.0 nM 4.78
CHEMBL5590274 EC50 = 20300.0 nM 4.69
CHEMBL1560 CAPTOPRIL EC50 = 22900.0 nM 4.64
CHEMBL5596258 EC50 = 26300.0 nM 4.58
CHEMBL5596792 EC50 = 28200.0 nM 4.55
CHEMBL10962 EC50 = 28400.0 nM 4.55
CHEMBL5596950 EC50 = 32900.0 nM 4.48
CHEMBL5597935 EC50 = 38000.0 nM 4.42
CHEMBL5597849 EC50 = 38600.0 nM 4.41
CHEMBL242863 EC50 = 40800.0 nM 4.39
CHEMBL5597720 EC50 = 58300.0 nM 4.23
CHEMBL5598285 EC50 = 61500.0 nM 4.21
CHEMBL5596359 EC50 = 96700.0 nM 4.01
CHEMBL5597628 EC50 = 106000.0 nM -
CHEMBL5597271 EC50 > 200000.0 nM -
CHEMBL5597141 EC50 > 200000.0 nM -