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Assay Detail

CHEMBL3381604

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Functional
Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs
ChEMBL ↗
78
Total Activities
78
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

From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
Venkatraj M, Ariën KK, Heeres J, Joossens J, Dirié B, Lyssens S, Michiels J, Cos P, Lewi PJ, Vanham G, Maes L, Van der Veken P, Augustyns K.
Bioorg Med Chem (2014) 22 : 5241 -5248
PubMed 25199582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 78 5.60 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3338053 — — 1 7.82
CHEMBL265502 SURAMIN 3.0 1 7.70
CHEMBL166 MELARSOPROL 3.0 1 7.52
CHEMBL3338050 — — 1 7.30
CHEMBL470025 — — 1 6.92
CHEMBL3338009 — — 1 6.68
CHEMBL3338054 — — 1 6.68
CHEMBL3338032 — — 1 6.38
CHEMBL302791 — — 1 6.28
CHEMBL3338027 — — 1 6.23
CHEMBL71659 — — 1 6.11
CHEMBL3338052 — — 1 6.10
CHEMBL72529 — — 1 6.02
CHEMBL421114 — — 1 5.95
CHEMBL71521 — — 1 5.93
CHEMBL69503 — — 1 5.86
CHEMBL3338039 — — 1 5.84
CHEMBL3338029 — — 1 5.81
CHEMBL3338028 — — 1 5.81
CHEMBL3338033 — — 1 5.78
CHEMBL3338034 — — 1 5.73
CHEMBL3338013 — — 1 5.70
CHEMBL3338051 — — 1 5.69
CHEMBL3338030 — — 1 5.69
CHEMBL3338038 — — 1 5.67
CHEMBL3338007 — — 1 5.63
CHEMBL3338044 — — 1 5.58
CHEMBL3338010 — — 1 5.54
CHEMBL3338049 — — 1 5.45
CHEMBL3338042 — — 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3338053 — IC50 = 15.0 nM 7.82
CHEMBL265502 SURAMIN IC50 = 20.0 nM 7.70
CHEMBL166 MELARSOPROL IC50 = 30.0 nM 7.52
CHEMBL3338050 — IC50 = 50.0 nM 7.30
CHEMBL470025 — IC50 = 120.0 nM 6.92
CHEMBL3338009 — IC50 = 210.0 nM 6.68
CHEMBL3338054 — IC50 = 210.0 nM 6.68
CHEMBL3338032 — IC50 = 420.0 nM 6.38
CHEMBL302791 — IC50 = 520.0 nM 6.28
CHEMBL3338027 — IC50 = 590.0 nM 6.23
CHEMBL71659 — IC50 = 780.0 nM 6.11
CHEMBL3338052 — IC50 = 790.0 nM 6.10
CHEMBL72529 — IC50 = 960.0 nM 6.02
CHEMBL421114 — IC50 = 1130.0 nM 5.95
CHEMBL71521 — IC50 = 1170.0 nM 5.93
CHEMBL69503 — IC50 = 1370.0 nM 5.86
CHEMBL3338039 — IC50 = 1450.0 nM 5.84
CHEMBL3338029 — IC50 = 1540.0 nM 5.81
CHEMBL3338028 — IC50 = 1540.0 nM 5.81
CHEMBL3338033 — IC50 = 1680.0 nM 5.78
CHEMBL3338034 — IC50 = 1880.0 nM 5.73
CHEMBL3338013 — IC50 = 1990.0 nM 5.70
CHEMBL3338051 — IC50 = 2030.0 nM 5.69
CHEMBL3338030 — IC50 = 2050.0 nM 5.69
CHEMBL3338038 — IC50 = 2120.0 nM 5.67
CHEMBL3338007 — IC50 = 2330.0 nM 5.63
CHEMBL3338044 — IC50 = 2610.0 nM 5.58
CHEMBL3338010 — IC50 = 2860.0 nM 5.54
CHEMBL3338049 — IC50 = 3520.0 nM 5.45
CHEMBL3338042 — IC50 = 4100.0 nM 5.39
CHEMBL3338018 — IC50 = 4160.0 nM 5.38
CHEMBL3338026 — IC50 = 4470.0 nM 5.35
CHEMBL3338021 — IC50 = 4470.0 nM 5.35
CHEMBL74174 — IC50 = 4840.0 nM 5.32
CHEMBL3338040 — IC50 = 5180.0 nM 5.29
CHEMBL3338045 — IC50 = 5200.0 nM 5.28
CHEMBL3338048 — IC50 = 5200.0 nM 5.28
CHEMBL3338043 — IC50 = 5320.0 nM 5.27
CHEMBL3338041 — IC50 = 5510.0 nM 5.26
CHEMBL3338020 — IC50 = 6150.0 nM 5.21
CHEMBL3338024 — IC50 = 6440.0 nM 5.19
CHEMBL3338025 — IC50 = 6840.0 nM 5.17
CHEMBL3338023 — IC50 = 7010.0 nM 5.15
CHEMBL578061 — IC50 = 7270.0 nM 5.14
CHEMBL3337998 — IC50 = 7190.0 nM 5.14
CHEMBL3338015 — IC50 = 8060.0 nM 5.09
CHEMBL3338046 — IC50 = 9120.0 nM 5.04
CHEMBL3338019 — IC50 = 11600.0 nM 4.94
CHEMBL3338017 — IC50 = 11610.0 nM 4.93
CHEMBL3338031 — IC50 = 12160.0 nM 4.92