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Assay Detail

CHEMBL5337178

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

Functional
Antitrypanosomal activity against Trypanosoma brucei assessed as inhibition of parasite growth incubated for 72 hrs by resazurin reagent fluorimetric analysis
22
Total Activities
20
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

Lead Optimization of the 5-Phenylpyrazolopyrimidinone NPD-2975 toward Compounds with Improved Antitrypanosomal Efficacy.
Zheng Y, van den Kerkhof M, Ibrahim M, De Esch IJP, Maes L, Sterk GJ, Caljon G, Leurs R.
J Med Chem (2024) 67 : 2849 -2863
PubMed 38330051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.35 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5409850 1 8.00
CHEMBL5432114 1 7.80
CHEMBL5422988 1 7.40
CHEMBL5417746 1 7.30
CHEMBL5411692 1 7.20
CHEMBL5411418 1 7.10
CHEMBL5440925 1 6.80
CHEMBL5428744 1 6.60
CHEMBL5414294 1 6.40
CHEMBL5428468 2 6.20
CHEMBL5433039 1 5.80
CHEMBL5413276 2 5.50
CHEMBL5438730 1 5.20
CHEMBL5399254 1 4.60
CHEMBL4568326 1 4.50
CHEMBL5413625 1 -
CHEMBL5412074 1 -
CHEMBL5440199 1 -
CHEMBL5429276 1 -
CHEMBL5420989 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5409850 IC50 = 10.0 nM 8.00
CHEMBL5432114 IC50 = 15.85 nM 7.80
CHEMBL5422988 IC50 = 39.81 nM 7.40
CHEMBL5417746 IC50 = 50.12 nM 7.30
CHEMBL5411692 IC50 = 63.1 nM 7.20
CHEMBL5411418 IC50 = 79.43 nM 7.10
CHEMBL5440925 IC50 = 158.49 nM 6.80
CHEMBL5428744 IC50 = 251.19 nM 6.60
CHEMBL5414294 IC50 = 398.11 nM 6.40
CHEMBL5428468 IC50 = 630.96 nM 6.20
CHEMBL5428468 IC50 = 800.0 nM 6.10
CHEMBL5433039 IC50 = 1584.89 nM 5.80
CHEMBL5413276 IC50 = 3162.28 nM 5.50
CHEMBL5413276 IC50 = 3200.0 nM 5.50
CHEMBL5438730 IC50 = 6309.57 nM 5.20
CHEMBL5399254 IC50 = 25118.86 nM 4.60
CHEMBL4568326 IC50 = 31622.78 nM 4.50
CHEMBL5413625 IC50 > 63095.73 nM -
CHEMBL5412074 IC50 > 63095.73 nM -
CHEMBL5440199 IC50 > 63095.73 nM -
CHEMBL5429276 IC50 > 10000.0 nM -
CHEMBL5420989 IC50 > 10000.0 nM -