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Assay Detail

CHEMBL4274072

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

Binding
Substrate activity at recombinant type-1 nitroreductase in promastigote stage of Leishmania donovani MHOM/SD/62/1S-CL2D LdBOB assessed as inhibition of parasite growth after 72 hrs by resazurin dye based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Leishmania donovani
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.
Fersing C, Boudot C, Pedron J, Hutter S, Primas N, Castera-Ducros C, Bourgeade-Delmas S, Sournia-Saquet A, Moreau A, Cohen A, Stigliani JL, Pratviel G, Crozet MD, Wyllie S, Fairlamb A, Valentin A, Rathelot P, Azas N, Courtioux B, Verhaeghe P, Vanelle P.
Eur J Med Chem (2018) 157 : 115 -126
PubMed 30092366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.24 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4277324 1 7.40
CHEMBL4290387 1 7.16
CHEMBL2441910 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4277324 IC50 = 40.0 nM 7.40
CHEMBL4290387 IC50 = 70.0 nM 7.16
CHEMBL2441910 IC50 = 70.0 nM 7.16