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Assay Detail

CHEMBL1048427

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Functional
Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by alamar blue assay
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei rhodesiense (CHEMBL612348) ↗
Type ORGANISM
Organism Trypanosoma brucei rhodesiense

Publication

Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.
Fotie J, Kaiser M, Delfín DA, Manley J, Reid CS, Paris JM, Wenzler T, Maes L, Mahasenan KV, Li C, Werbovetz KA.
J Med Chem (2010) 53 : 966 -982
PubMed 20047276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 6.40 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565456 — — 1 8.15
CHEMBL166 MELARSOPROL 3.0 1 8.10
CHEMBL565457 — — 1 7.89
CHEMBL566743 — — 1 7.85
CHEMBL571471 — — 1 7.82
CHEMBL583463 — — 1 7.77
CHEMBL566744 — — 1 7.64
CHEMBL571256 — — 1 7.55
CHEMBL570129 — — 1 7.55
CHEMBL565717 — — 1 7.48
CHEMBL569180 — — 1 7.41
CHEMBL570816 — — 1 7.39
CHEMBL568969 — — 1 7.39
CHEMBL571035 — — 1 7.32
CHEMBL585919 — — 1 7.32
CHEMBL569179 — — 1 7.28
CHEMBL568047 — — 1 7.27
CHEMBL575019 — — 1 7.24
CHEMBL570583 — — 1 7.21
CHEMBL566963 — — 1 7.00
CHEMBL568268 — — 1 6.89
CHEMBL575018 — — 1 6.85
CHEMBL583579 — — 1 6.77
CHEMBL569418 — — 1 6.75
CHEMBL576463 — — 1 6.75
CHEMBL575017 — — 1 6.70
CHEMBL569417 — — 1 6.58
CHEMBL576699 — — 1 6.52
CHEMBL570825 — — 1 6.50
CHEMBL577468 — — 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565456 — IC50 = 7.0 nM 8.15
CHEMBL166 MELARSOPROL IC50 = 8.0 nM 8.10
CHEMBL565457 — IC50 = 13.0 nM 7.89
CHEMBL566743 — IC50 = 14.0 nM 7.85
CHEMBL571471 — IC50 = 15.0 nM 7.82
CHEMBL583463 — IC50 = 17.0 nM 7.77
CHEMBL566744 — IC50 = 23.0 nM 7.64
CHEMBL571256 — IC50 = 28.0 nM 7.55
CHEMBL570129 — IC50 = 28.0 nM 7.55
CHEMBL565717 — IC50 = 33.0 nM 7.48
CHEMBL569180 — IC50 = 39.0 nM 7.41
CHEMBL570816 — IC50 = 41.0 nM 7.39
CHEMBL568969 — IC50 = 41.0 nM 7.39
CHEMBL585919 — IC50 = 48.0 nM 7.32
CHEMBL571035 — IC50 = 48.0 nM 7.32
CHEMBL569179 — IC50 = 53.0 nM 7.28
CHEMBL568047 — IC50 = 54.0 nM 7.27
CHEMBL575019 — IC50 = 58.0 nM 7.24
CHEMBL570583 — IC50 = 61.0 nM 7.21
CHEMBL566963 — IC50 = 100.0 nM 7.00
CHEMBL568268 — IC50 = 130.0 nM 6.89
CHEMBL575018 — IC50 = 140.0 nM 6.85
CHEMBL583579 — IC50 = 170.0 nM 6.77
CHEMBL569418 — IC50 = 180.0 nM 6.75
CHEMBL576463 — IC50 = 180.0 nM 6.75
CHEMBL575017 — IC50 = 200.0 nM 6.70
CHEMBL569417 — IC50 = 260.0 nM 6.58
CHEMBL576699 — IC50 = 300.0 nM 6.52
CHEMBL570825 — IC50 = 320.0 nM 6.50
CHEMBL577468 — IC50 = 340.0 nM 6.47
CHEMBL578555 — IC50 = 340.0 nM 6.47
CHEMBL565506 — IC50 = 360.0 nM 6.44
CHEMBL571034 — IC50 = 390.0 nM 6.41
CHEMBL570817 — IC50 = 670.0 nM 6.17
CHEMBL575020 — IC50 = 780.0 nM 6.11
CHEMBL568726 — IC50 = 1100.0 nM 5.96
CHEMBL565673 — IC50 = 1400.0 nM 5.85
CHEMBL565672 — IC50 = 3600.0 nM 5.44
CHEMBL579228 — IC50 = 3700.0 nM 5.43
CHEMBL575230 — IC50 = 4100.0 nM 5.39
CHEMBL578831 — IC50 = 4400.0 nM 5.36
CHEMBL571251 — IC50 = 4500.0 nM 5.35
CHEMBL565505 — IC50 = 5200.0 nM 5.28
CHEMBL577328 — IC50 = 5300.0 nM 5.28
CHEMBL579024 — IC50 = 5300.0 nM 5.28
CHEMBL565455 — IC50 = 8800.0 nM 5.06
CHEMBL585745 — IC50 = 11000.0 nM 4.96
CHEMBL577467 — IC50 = 13000.0 nM 4.89
CHEMBL571472 — IC50 = 57000.0 nM 4.24
CHEMBL568943 — IC50 = 63000.0 nM 4.20