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Assay Detail

CHEMBL5159178

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

Binding
Inhibition of His-tagged Trypanosoma brucei HGXPRT expressed in Escherichia coli BL21 (DE3) cells using PRib-PP as substrate by spectrophotometric assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Stereo-Defined Acyclic Nucleoside Phosphonates are Selective and Potent Inhibitors of Parasite 6-Oxopurine Phosphoribosyltransferases.
Klejch T, Keough DT, King G, Doleželová E, Česnek M, Buděšínský M, Zíková A, Janeba Z, Guddat LW, Hocková D.
J Med Chem (2022) 65 : 4030 -4057
PubMed 35175749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.47 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208021 1 7.70
CHEMBL5185227 1 7.70
CHEMBL5171024 1 7.52
CHEMBL5179417 1 7.52
CHEMBL5187896 1 7.40
CHEMBL5180101 1 7.22
CHEMBL5204284 1 7.00
CHEMBL5197487 1 7.00
CHEMBL5194527 1 6.70
CHEMBL5180136 1 6.60
CHEMBL5180341 1 6.35
CHEMBL5186759 1 6.22
CHEMBL5205733 1 5.70
CHEMBL5170511 1 5.70
CHEMBL5185264 1 5.22
CHEMBL5201462 1 5.05
CHEMBL5193549 1 4.92
CHEMBL5176444 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208021 Ki = 20.0 nM 7.70
CHEMBL5185227 Ki = 20.0 nM 7.70
CHEMBL5171024 Ki = 30.0 nM 7.52
CHEMBL5179417 Ki = 30.0 nM 7.52
CHEMBL5187896 Ki = 40.0 nM 7.40
CHEMBL5180101 Ki = 60.0 nM 7.22
CHEMBL5204284 Ki = 100.0 nM 7.00
CHEMBL5197487 Ki = 100.0 nM 7.00
CHEMBL5194527 Ki = 200.0 nM 6.70
CHEMBL5180136 Ki = 250.0 nM 6.60
CHEMBL5180341 Ki = 450.0 nM 6.35
CHEMBL5186759 Ki = 600.0 nM 6.22
CHEMBL5205733 Ki = 2000.0 nM 5.70
CHEMBL5170511 Ki = 2000.0 nM 5.70
CHEMBL5185264 Ki = 6000.0 nM 5.22
CHEMBL5201462 Ki = 9000.0 nM 5.05
CHEMBL5193549 Ki = 12000.0 nM 4.92
CHEMBL5176444 Ki = 14000.0 nM 4.85