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Assay Detail

CHEMBL808707

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

Functional
Inhibition of Trypanosoma rhodesiense (strain STIB900) was determined using blood stream from trypomastigotes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
Martin MB, Grimley JS, Lewis JC, Heath HT, Bailey BN, Kendrick H, Yardley V, Caldera A, Lira R, Urbina JA, Moreno SN, Docampo R, Croft SL, Oldfield E.
J Med Chem (2001) 44 : 909 -916
PubMed 11300872 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.95 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434024 1 6.66
CHEMBL55140 1 6.16
CHEMBL293522 1 5.77
CHEMBL55812 OLPADRONIC ACID 2.0 1 5.27
CHEMBL55358 1 5.11
CHEMBL923 RISEDRONIC ACID 4.0 1 5.07
CHEMBL301247 1 5.07
CHEMBL55359 1 4.70
CHEMBL56556 1 4.67
CHEMBL301471 1 4.55
CHEMBL55214 NERIDRONIC ACID 3.0 1 4.50
CHEMBL417932 1 4.40
CHEMBL299988 1 4.21
CHEMBL52761 1 4.04
CHEMBL299491 1 4.00
CHEMBL55886 1 -
CHEMBL834 PAMIDRONIC ACID 4.0 1 -
CHEMBL298771 1 -
CHEMBL870 ALENDRONIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434024 IC50 = 220.0 nM 6.66
CHEMBL55140 IC50 = 700.0 nM 6.16
CHEMBL293522 IC50 = 1700.0 nM 5.77
CHEMBL55812 OLPADRONIC ACID IC50 = 5400.0 nM 5.27
CHEMBL55358 IC50 = 7800.0 nM 5.11
CHEMBL923 RISEDRONIC ACID IC50 = 8600.0 nM 5.07
CHEMBL301247 IC50 = 8600.0 nM 5.07
CHEMBL55359 IC50 = 19800.0 nM 4.70
CHEMBL56556 IC50 = 21300.0 nM 4.67
CHEMBL301471 IC50 = 27900.0 nM 4.55
CHEMBL55214 NERIDRONIC ACID IC50 = 31700.0 nM 4.50
CHEMBL417932 IC50 = 40000.0 nM 4.40
CHEMBL299988 IC50 = 62400.0 nM 4.21
CHEMBL52761 IC50 = 92000.0 nM 4.04
CHEMBL299491 IC50 = 99800.0 nM 4.00
CHEMBL55886 IC50 > 200000.0 nM -
CHEMBL834 PAMIDRONIC ACID IC50 = 177000.0 nM -
CHEMBL298771 IC50 > 200000.0 nM -
CHEMBL870 ALENDRONIC ACID IC50 > 200000.0 nM -