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Assay Detail

CHEMBL869006

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Binding
Inhibition of Trypanosoma brucei rhodesiense rhodesain
ChEMBL ↗
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei rhodesiense
Confidence 9 — Direct single protein target
Curated By Expert

Target

Rhodesain (CHEMBL4188) ↗
Type SINGLE PROTEIN
Organism Trypanosoma brucei rhodesiense

Publication

Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
Vicik R, Hoerr V, Glaser M, Schultheis M, Hansell E, McKerrow JH, Holzgrabe U, Caffrey CR, Ponte-Sucre A, Moll H, Stich A, Schirmeister T.
Bioorg Med Chem Lett (2006) 16 : 2753 -2757
PubMed 16516467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 5.93 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205707 — — 1 7.00
CHEMBL208156 — — 1 6.52
CHEMBL383647 — — 1 6.30
CHEMBL379649 — — 1 6.30
CHEMBL206415 — — 1 6.22
CHEMBL379406 — — 1 6.22
CHEMBL379355 — — 1 6.22
CHEMBL208297 — — 1 6.16
CHEMBL379571 — — 1 6.16
CHEMBL377676 — — 1 6.16
CHEMBL206922 — — 1 6.10
CHEMBL439510 — — 1 6.10
CHEMBL208129 — — 1 6.10
CHEMBL382431 — — 1 6.05
CHEMBL207526 — — 1 6.00
CHEMBL207070 — — 1 6.00
CHEMBL208263 — — 1 5.96
CHEMBL184629 — — 1 5.96
CHEMBL382388 — — 1 5.96
CHEMBL379509 — — 1 5.92
CHEMBL380076 — — 1 5.92
CHEMBL377650 — — 1 5.85
CHEMBL380337 — — 1 5.80
CHEMBL382910 — — 1 5.80
CHEMBL208418 — — 1 5.72
CHEMBL207092 — — 1 5.72
CHEMBL377947 — — 1 5.72
CHEMBL378288 — — 1 5.64
CHEMBL378902 — — 1 5.55
CHEMBL379944 — — 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205707 — Ki = 100.0 nM 7.00
CHEMBL208156 — Ki = 300.0 nM 6.52
CHEMBL383647 — Ki = 500.0 nM 6.30
CHEMBL379649 — Ki = 500.0 nM 6.30
CHEMBL206415 — Ki = 600.0 nM 6.22
CHEMBL379406 — Ki = 600.0 nM 6.22
CHEMBL379355 — Ki = 600.0 nM 6.22
CHEMBL208297 — Ki = 700.0 nM 6.16
CHEMBL379571 — Ki = 700.0 nM 6.16
CHEMBL377676 — Ki = 700.0 nM 6.16
CHEMBL206922 — Ki = 800.0 nM 6.10
CHEMBL439510 — Ki = 800.0 nM 6.10
CHEMBL208129 — Ki = 800.0 nM 6.10
CHEMBL382431 — Ki = 900.0 nM 6.05
CHEMBL207070 — Ki = 1000.0 nM 6.00
CHEMBL207526 — Ki = 1000.0 nM 6.00
CHEMBL382388 — Ki = 1100.0 nM 5.96
CHEMBL208263 — Ki = 1100.0 nM 5.96
CHEMBL184629 — Ki = 1100.0 nM 5.96
CHEMBL379509 — Ki = 1200.0 nM 5.92
CHEMBL380076 — Ki = 1200.0 nM 5.92
CHEMBL377650 — Ki = 1400.0 nM 5.85
CHEMBL380337 — Ki = 1600.0 nM 5.80
CHEMBL382910 — Ki = 1600.0 nM 5.80
CHEMBL208418 — Ki = 1900.0 nM 5.72
CHEMBL207092 — Ki = 1900.0 nM 5.72
CHEMBL377947 — Ki = 1900.0 nM 5.72
CHEMBL378288 — Ki = 2300.0 nM 5.64
CHEMBL378902 — Ki = 2800.0 nM 5.55
CHEMBL379944 — Ki = 3100.0 nM 5.51
CHEMBL207797 — Ki = 3100.0 nM 5.51
CHEMBL207838 — Ki = 3100.0 nM 5.51
CHEMBL377682 — Ki = 3100.0 nM 5.51
CHEMBL441354 — Ki = 3300.0 nM 5.48
CHEMBL380077 — Ki = 3900.0 nM 5.41
CHEMBL377234 — Ki = 5000.0 nM 5.30
CHEMBL290960 NIFURTIMOX Ki - — -