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Assay Detail

CHEMBL4046302

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

Functional
Antitrypanosomal activity against Trypanosoma brucei Lister 427 bloodstream forms assessed as inhibition of parasite growth incubated for 48 hrs by ATP-bioluminescence cell viability assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Synthesis and evaluation of analogs of 5'-(((Z)-4-amino-2-butenyl)methylamino)-5'-deoxyadenosine (MDL 73811, or AbeAdo) - An inhibitor of S-adenosylmethionine decarboxylase with antitrypanosomal activity.
Brockway AJ, Volkov OA, Cosner CC, MacMillan KS, Wring SA, Richardson TE, Peel M, Phillips MA, De Brabander JK.
Bioorg Med Chem (2017) 25 : 5433 -5440
PubMed 28807574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.45 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL512274 1 8.74
CHEMBL381751 1 8.00
CHEMBL4092771 1 6.80
CHEMBL4100498 1 6.44
CHEMBL4084041 1 6.43
CHEMBL4094107 1 6.38
CHEMBL4073680 1 5.60
CHEMBL4087972 1 5.58
CHEMBL4073465 1 5.52
CHEMBL4062325 1 5.00
CHEMBL4085520 1 -
CHEMBL4103447 1 -
CHEMBL4102756 1 -
CHEMBL4078482 1 -
CHEMBL4076008 1 -
CHEMBL4086336 1 -
CHEMBL4083844 1 -
CHEMBL4080100 1 -
CHEMBL4091618 1 -
CHEMBL4063836 1 -
CHEMBL4091805 1 -
CHEMBL4065088 1 -
CHEMBL4101847 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL512274 EC50 = 1.8 nM 8.74
CHEMBL381751 EC50 = 10.0 nM 8.00
CHEMBL4092771 EC50 = 160.0 nM 6.80
CHEMBL4100498 EC50 = 360.0 nM 6.44
CHEMBL4084041 EC50 = 370.0 nM 6.43
CHEMBL4094107 EC50 = 420.0 nM 6.38
CHEMBL4073680 EC50 = 2500.0 nM 5.60
CHEMBL4087972 EC50 = 2600.0 nM 5.58
CHEMBL4073465 EC50 = 3000.0 nM 5.52
CHEMBL4062325 EC50 = 10000.0 nM 5.00
CHEMBL4085520 EC50 > 25000.0 nM -
CHEMBL4103447 EC50 > 25000.0 nM -
CHEMBL4102756 EC50 > 25000.0 nM -
CHEMBL4078482 EC50 > 25000.0 nM -
CHEMBL4076008 EC50 > 25000.0 nM -
CHEMBL4086336 EC50 > 25000.0 nM -
CHEMBL4083844 EC50 > 25000.0 nM -
CHEMBL4080100 EC50 > 25000.0 nM -
CHEMBL4091618 EC50 > 25000.0 nM -
CHEMBL4063836 EC50 > 25000.0 nM -
CHEMBL4091805 EC50 > 3000.0 nM -
CHEMBL4065088 EC50 > 25000.0 nM -
CHEMBL4101847 EC50 > 3000.0 nM -