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Assay Detail

CHEMBL3625869

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Functional
Antitrypanosomal activity against Trypanosoma brucei brucei BSF427 VSG118 bloodstream forms incubated for 69 hrs by resazurin dye based assay
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851) ↗
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.
Cleghorn LA, Albrecht S, Stojanovski L, Simeons FR, Norval S, Kime R, Collie IT, De Rycker M, Campbell L, Hallyburton I, Frearson JA, Wyatt PG, Read KD, Gilbert IH.
J Med Chem (2015) 58 : 7695 -7706
PubMed 26418485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 53 6.45 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623020 — — 1 7.70
CHEMBL3621224 — — 1 7.54
CHEMBL3623019 — — 1 7.52
CHEMBL3623005 — — 1 7.52
CHEMBL3623014 — — 1 7.52
CHEMBL3623022 — — 1 7.52
CHEMBL3623040 — — 1 7.40
CHEMBL3623037 — — 1 7.40
CHEMBL3623016 — — 1 7.40
CHEMBL3623021 — — 1 7.40
CHEMBL3623023 — — 1 7.30
CHEMBL3623031 — — 1 7.30
CHEMBL3623038 — — 1 7.22
CHEMBL3623043 — — 1 7.16
CHEMBL3623029 — — 1 7.10
CHEMBL3623044 — — 1 7.10
CHEMBL3623042 — — 1 7.10
CHEMBL3623039 — — 1 7.10
CHEMBL3623025 — — 1 7.10
CHEMBL3623033 — — 1 7.05
CHEMBL3623041 — — 1 7.05
CHEMBL3623030 — — 1 6.96
CHEMBL3431063 — — 1 6.96
CHEMBL3623027 — — 1 6.96
CHEMBL3431060 — — 1 6.66
CHEMBL3623045 — — 1 6.62
CHEMBL3431059 — — 1 6.51
CHEMBL3623018 — — 1 6.41
CHEMBL3623015 — — 1 6.40
CHEMBL3623035 — — 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623020 — EC50 = 20.0 nM 7.70
CHEMBL3621224 — EC50 = 29.0 nM 7.54
CHEMBL3623005 — EC50 = 30.0 nM 7.52
CHEMBL3623014 — EC50 = 30.0 nM 7.52
CHEMBL3623022 — EC50 = 30.0 nM 7.52
CHEMBL3623019 — EC50 = 30.0 nM 7.52
CHEMBL3623021 — EC50 = 40.0 nM 7.40
CHEMBL3623016 — EC50 = 40.0 nM 7.40
CHEMBL3623040 — EC50 = 40.0 nM 7.40
CHEMBL3623037 — EC50 = 40.0 nM 7.40
CHEMBL3623023 — EC50 = 50.0 nM 7.30
CHEMBL3623031 — EC50 = 50.0 nM 7.30
CHEMBL3623038 — EC50 = 60.0 nM 7.22
CHEMBL3623043 — EC50 = 70.0 nM 7.16
CHEMBL3623025 — EC50 = 80.0 nM 7.10
CHEMBL3623044 — EC50 = 80.0 nM 7.10
CHEMBL3623042 — EC50 = 80.0 nM 7.10
CHEMBL3623039 — EC50 = 80.0 nM 7.10
CHEMBL3623029 — EC50 = 80.0 nM 7.10
CHEMBL3623033 — EC50 = 90.0 nM 7.05
CHEMBL3623041 — EC50 = 90.0 nM 7.05
CHEMBL3623030 — EC50 = 110.0 nM 6.96
CHEMBL3431063 — EC50 = 110.0 nM 6.96
CHEMBL3623027 — EC50 = 110.0 nM 6.96
CHEMBL3431060 — EC50 = 220.0 nM 6.66
CHEMBL3623045 — EC50 = 240.0 nM 6.62
CHEMBL3431059 — EC50 = 310.0 nM 6.51
CHEMBL3623018 — EC50 = 390.0 nM 6.41
CHEMBL3623015 — EC50 = 400.0 nM 6.40
CHEMBL3623035 — EC50 = 410.0 nM 6.39
CHEMBL3623046 — EC50 = 440.0 nM 6.36
CHEMBL3431058 — EC50 = 450.0 nM 6.35
CHEMBL3623594 — EC50 = 460.0 nM 6.34
CHEMBL3623008 — EC50 = 650.0 nM 6.19
CHEMBL3623007 — EC50 = 660.0 nM 6.18
CHEMBL3623026 — EC50 = 770.0 nM 6.11
CHEMBL3623047 — EC50 = 920.0 nM 6.04
CHEMBL3623009 — EC50 = 990.0 nM 6.00
CHEMBL3623017 — EC50 = 1100.0 nM 5.96
CHEMBL3623036 — EC50 = 1500.0 nM 5.82
CHEMBL3623013 — EC50 = 1900.0 nM 5.72
CHEMBL3623028 — EC50 = 2300.0 nM 5.64
CHEMBL3623006 — EC50 = 2900.0 nM 5.54
CHEMBL3623032 — EC50 = 5400.0 nM 5.27
CHEMBL3623010 — EC50 = 13000.0 nM 4.89
CHEMBL3623049 — EC50 = 19000.0 nM 4.72
CHEMBL3623034 — EC50 = 19000.0 nM 4.72
CHEMBL3623048 — EC50 = 36000.0 nM 4.44
CHEMBL3623050 — EC50 = 37000.0 nM 4.43
CHEMBL3623012 — EC50 = 41000.0 nM 4.39