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Assay Detail

CHEMBL926729

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Functional
Antitrypanosomal activity against Trypanosoma brucei
ChEMBL ↗
58
Total Activities
58
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei
Confidence 1 — Organism
Curated By Intermediate

Target

Trypanosoma brucei (CHEMBL612849) ↗
Type ORGANISM
Organism Trypanosoma brucei

Publication

Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
Mallari JP, Shelat AA, Obrien T, Caffrey CR, Kosinski A, Connelly M, Harbut M, Greenbaum D, McKerrow JH, Guy RK.
J Med Chem (2008) 51 : 545 -552
PubMed 18173229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.16 7.70
EC50 9 6.23 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35241 DIMINAZENE 2.0 1 7.70
CHEMBL400542 — — 1 7.22
CHEMBL254412 — — 1 6.96
CHEMBL265502 SURAMIN 3.0 1 6.89
CHEMBL254618 — — 1 6.82
CHEMBL255038 — — 1 6.75
CHEMBL254619 — — 1 6.66
CHEMBL429121 — — 1 6.62
CHEMBL400664 — — 1 6.58
CHEMBL252933 — — 1 6.58
CHEMBL252363 — — 1 6.57
CHEMBL252121 — — 1 6.57
CHEMBL252934 — — 1 6.51
CHEMBL400543 — — 1 6.50
CHEMBL399094 — — 1 6.48
CHEMBL400522 — — 1 6.47
CHEMBL400095 — — 1 6.41
CHEMBL399026 — — 1 6.40
CHEMBL254828 — — 1 6.38
CHEMBL251959 — — 1 6.36
CHEMBL254617 — — 1 6.35
CHEMBL400248 — — 1 6.32
CHEMBL398504 — — 1 6.30
CHEMBL254827 — — 1 6.27
CHEMBL400096 — — 1 6.26
CHEMBL251973 — — 1 6.25
CHEMBL398505 — — 1 6.22
CHEMBL400663 — — 1 6.22
CHEMBL399027 — — 1 6.16
CHEMBL252157 — — 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35241 DIMINAZENE IC50 = 20.0 nM 7.70
CHEMBL400542 — IC50 = 60.0 nM 7.22
CHEMBL254412 — IC50 = 110.0 nM 6.96
CHEMBL265502 SURAMIN IC50 = 130.0 nM 6.89
CHEMBL254618 — IC50 = 150.0 nM 6.82
CHEMBL255038 — IC50 = 180.0 nM 6.75
CHEMBL254619 — IC50 = 220.0 nM 6.66
CHEMBL429121 — EC50 = 240.0 nM 6.62
CHEMBL400664 — EC50 = 260.0 nM 6.58
CHEMBL252933 — IC50 = 260.0 nM 6.58
CHEMBL252363 — IC50 = 270.0 nM 6.57
CHEMBL252121 — IC50 = 270.0 nM 6.57
CHEMBL252934 — IC50 = 310.0 nM 6.51
CHEMBL400543 — IC50 = 320.0 nM 6.50
CHEMBL399094 — IC50 = 330.0 nM 6.48
CHEMBL400522 — IC50 = 340.0 nM 6.47
CHEMBL400095 — EC50 = 390.0 nM 6.41
CHEMBL399026 — EC50 = 400.0 nM 6.40
CHEMBL254828 — IC50 = 420.0 nM 6.38
CHEMBL251959 — IC50 = 440.0 nM 6.36
CHEMBL254617 — IC50 = 450.0 nM 6.35
CHEMBL400248 — IC50 = 480.0 nM 6.32
CHEMBL398504 — IC50 = 500.0 nM 6.30
CHEMBL254827 — IC50 = 540.0 nM 6.27
CHEMBL400096 — EC50 = 550.0 nM 6.26
CHEMBL251973 — EC50 = 560.0 nM 6.25
CHEMBL400663 — IC50 = 600.0 nM 6.22
CHEMBL398505 — IC50 = 600.0 nM 6.22
CHEMBL399027 — IC50 = 700.0 nM 6.16
CHEMBL252157 — IC50 = 700.0 nM 6.16
CHEMBL252729 — IC50 = 800.0 nM 6.10
CHEMBL252362 — IC50 = 800.0 nM 6.10
CHEMBL255080 — IC50 = 850.0 nM 6.07
CHEMBL251923 — IC50 = 900.0 nM 6.05
CHEMBL255087 — EC50 = 900.0 nM 6.05
CHEMBL255086 — EC50 = 1000.0 nM 6.00
CHEMBL398311 — IC50 = 1100.0 nM 5.96
CHEMBL436637 — IC50 = 1100.0 nM 5.96
CHEMBL254227 — IC50 = 1100.0 nM 5.96
CHEMBL253611 — IC50 = 1200.0 nM 5.92
CHEMBL399513 — IC50 = 1300.0 nM 5.89
CHEMBL252360 — IC50 = 1400.0 nM 5.85
CHEMBL253829 — IC50 = 1500.0 nM 5.82
CHEMBL252158 — IC50 = 1500.0 nM 5.82
CHEMBL398708 — IC50 = 1500.0 nM 5.82
CHEMBL252156 — IC50 = 1500.0 nM 5.82
CHEMBL400453 — IC50 = 1700.0 nM 5.77
CHEMBL255079 — IC50 = 1700.0 nM 5.77
CHEMBL400454 — IC50 = 2000.0 nM 5.70
CHEMBL252558 — IC50 = 2200.0 nM 5.66