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Assay Detail

CHEMBL3376833

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

Binding
Inhibition of recombinant Trypanosoma brucei PTR1 using dihydrobiopterin and NADPH by spectrophotometric assay
71
Total Activities
71
Compounds Tested
2
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

Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1.
Khalaf AI, Huggan JK, Suckling CJ, Gibson CL, Stewart K, Giordani F, Barrett MP, Wong PE, Barrack KL, Hunter WN.
J Med Chem (2014) 57 : 6479 -6494
PubMed 25007262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 59 6.14 6.87
Ki(app) 12 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318913 1 6.87
CHEMBL3318208 1 6.86
CHEMBL3318212 1 6.80
CHEMBL3318495 1 6.72
CHEMBL3318494 1 6.70
CHEMBL3318922 1 6.70
CHEMBL3318815 1 6.64
CHEMBL3318211 1 6.64
CHEMBL3318213 1 6.62
CHEMBL3318821 1 6.62
CHEMBL3318812 1 6.60
CHEMBL3318804 1 6.58
CHEMBL567351 1 6.57
CHEMBL3318920 1 6.54
CHEMBL3318916 1 6.54
CHEMBL3318921 1 6.52
CHEMBL3318822 1 6.52
CHEMBL3318801 1 6.50
CHEMBL3318214 1 6.46
CHEMBL3318206 1 6.46
CHEMBL3318803 1 6.40
CHEMBL3318819 1 6.33
CHEMBL3318802 1 6.32
CHEMBL3318810 1 6.30
CHEMBL3318806 1 6.25
CHEMBL3318914 1 6.24
CHEMBL3318911 1 6.24
CHEMBL3318820 1 6.23
CHEMBL3318207 1 6.14
CHEMBL3318811 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318913 Ki = 135.0 nM 6.87
CHEMBL3318208 Ki = 137.0 nM 6.86
CHEMBL3318212 Ki = 160.0 nM 6.80
CHEMBL3318495 Ki = 190.0 nM 6.72
CHEMBL3318494 Ki = 200.0 nM 6.70
CHEMBL3318922 Ki = 200.0 nM 6.70
CHEMBL3318815 Ki = 230.0 nM 6.64
CHEMBL3318211 Ki = 230.0 nM 6.64
CHEMBL3318213 Ki = 240.0 nM 6.62
CHEMBL3318821 Ki = 240.0 nM 6.62
CHEMBL3318812 Ki = 250.0 nM 6.60
CHEMBL3318804 Ki = 260.0 nM 6.58
CHEMBL567351 Ki = 270.0 nM 6.57
CHEMBL3318916 Ki = 290.0 nM 6.54
CHEMBL3318920 Ki = 290.0 nM 6.54
CHEMBL3318921 Ki = 300.0 nM 6.52
CHEMBL3318822 Ki = 300.0 nM 6.52
CHEMBL3318801 Ki = 320.0 nM 6.50
CHEMBL3318214 Ki = 350.0 nM 6.46
CHEMBL3318206 Ki = 350.0 nM 6.46
CHEMBL3318803 Ki = 400.0 nM 6.40
CHEMBL3318819 Ki = 470.0 nM 6.33
CHEMBL3318802 Ki = 480.0 nM 6.32
CHEMBL3318810 Ki = 500.0 nM 6.30
CHEMBL3318806 Ki = 560.0 nM 6.25
CHEMBL3318914 Ki = 580.0 nM 6.24
CHEMBL3318911 Ki = 580.0 nM 6.24
CHEMBL3318820 Ki = 590.0 nM 6.23
CHEMBL3318207 Ki = 731.0 nM 6.14
CHEMBL3318811 Ki = 760.0 nM 6.12
CHEMBL3318493 Ki = 800.0 nM 6.10
CHEMBL3318816 Ki = 950.0 nM 6.02
CHEMBL3318809 Ki = 1060.0 nM 5.97
CHEMBL3318808 Ki = 1170.0 nM 5.93
CHEMBL3318496 Ki = 1200.0 nM 5.92
CHEMBL3318498 Ki = 1200.0 nM 5.92
CHEMBL3318497 Ki = 1300.0 nM 5.89
CHEMBL3318915 Ki = 1280.0 nM 5.89
CHEMBL3318210 Ki = 3317.0 nM 5.48
CHEMBL3318486 Ki = 4200.0 nM 5.38
CHEMBL3318209 Ki = 4900.0 nM 5.31
CHEMBL3318499 Ki = 7300.0 nM 5.14
CHEMBL3318487 Ki = 8600.0 nM 5.07
CHEMBL3318491 Ki = 8800.0 nM 5.06
CHEMBL3319008 Ki = 50000.0 nM 4.30
CHEMBL3318488 Ki = 75000.0 nM 4.12
CHEMBL3319009 Ki(app) - -
CHEMBL3318490 Ki > 100000.0 nM -
CHEMBL3318489 Ki > 100000.0 nM -
CHEMBL3318823 Ki(app) - -