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Assay Detail

CHEMBL973273

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900
31
Total Activities
16
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

Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity.
Schlapper C, Seebacher W, Kaiser M, Brun R, Saf R, Weis R.
Eur J Med Chem (2008) 43 : 800 -807
PubMed 17698258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.56 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.41
CHEMBL459423 2 6.21
CHEMBL459437 2 6.07
CHEMBL460449 2 6.02
CHEMBL459436 2 5.97
CHEMBL518332 2 5.95
CHEMBL518167 2 5.84
CHEMBL518622 2 5.82
CHEMBL518623 2 5.78
CHEMBL518333 2 5.75
CHEMBL219419 2 5.60
CHEMBL374245 2 5.53
CHEMBL516462 2 5.51
CHEMBL516624 2 5.47
CHEMBL375980 2 5.27
CHEMBL459424 2 4.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 3.9 nM 8.41
CHEMBL459423 IC50 = 620.0 nM 6.21
CHEMBL459437 IC50 = 860.0 nM 6.07
CHEMBL460449 IC50 = 960.0 nM 6.02
CHEMBL459436 IC50 = 1060.0 nM 5.97
CHEMBL459423 IC50 = 1070.0 nM 5.97
CHEMBL518332 IC50 = 1120.0 nM 5.95
CHEMBL518167 IC50 = 1440.0 nM 5.84
CHEMBL518622 IC50 = 1520.0 nM 5.82
CHEMBL518332 IC50 = 1530.0 nM 5.82
CHEMBL518623 IC50 = 1680.0 nM 5.78
CHEMBL518333 IC50 = 1760.0 nM 5.75
CHEMBL459436 IC50 = 2040.0 nM 5.69
CHEMBL219419 IC50 = 2530.0 nM 5.60
CHEMBL374245 IC50 = 2950.0 nM 5.53
CHEMBL516462 IC50 = 3120.0 nM 5.51
CHEMBL518623 IC50 = 3160.0 nM 5.50
CHEMBL516624 IC50 = 3350.0 nM 5.47
CHEMBL518167 IC50 = 3490.0 nM 5.46
CHEMBL374245 IC50 = 3640.0 nM 5.44
CHEMBL219419 IC50 = 4260.0 nM 5.37
CHEMBL460449 IC50 = 4950.0 nM 5.30
CHEMBL375980 IC50 = 5340.0 nM 5.27
CHEMBL459437 IC50 = 6270.0 nM 5.20
CHEMBL375980 IC50 = 13140.0 nM 4.88
CHEMBL516462 IC50 = 14990.0 nM 4.82
CHEMBL518622 IC50 = 15940.0 nM 4.80
CHEMBL516624 IC50 = 16920.0 nM 4.77
CHEMBL518333 IC50 = 37580.0 nM 4.42
CHEMBL459424 IC50 = 70940.0 nM 4.15
CHEMBL459424 IC50 - -