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Assay Detail

CHEMBL807794

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

Functional
Log IC50 brucei Trypomastigotes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Activity of bisphosphonates against Trypanosoma brucei rhodesiense.
Martin MB, Sanders JM, Kendrick H, de Luca-Fradley K, Lewis JC, Grimley JS, Van Brussel EM, Olsen JR, Meints GA, Burzynska A, Kafarski P, Croft SL, Oldfield E.
J Med Chem (2002) 45 : 2904 -2914
PubMed 12086478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.15 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52251 (OCTYLAMINO)METHYLENEDIPHOSPHONIC ACID 1 5.77
CHEMBL416301 1 5.70
CHEMBL298852 1 5.10
CHEMBL54004 1 4.69
CHEMBL55214 NERIDRONIC ACID 3.0 1 4.50
CHEMBL834 PAMIDRONIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52251 (OCTYLAMINO)METHYLENEDIPHOSPHONIC ACID IC50 = 1698.24 nM 5.77
CHEMBL416301 IC50 = 1995.26 nM 5.70
CHEMBL298852 IC50 = 7943.28 nM 5.10
CHEMBL54004 IC50 = 20417.38 nM 4.69
CHEMBL55214 NERIDRONIC ACID IC50 = 31622.78 nM 4.50
CHEMBL834 PAMIDRONIC ACID IC50 < 100000.0 nM -