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Assay Detail

CHEMBL760057

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

Binding
Inhibition of purine nucleoside phosphorylase against the enzyme from calf spleen in 1 mM phosphate
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Spleen
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Purine nucleoside phosphorylase (CHEMBL2935)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Structure-based design of inhibitors of purine nucleoside phosphorylase. 1. 9-(arylmethyl) derivatives of 9-deazaguanine.
Montgomery JA, Niwas S, Rose JD, Secrist JA, Babu YS, Bugg CE, Erion MD, Guida WC, Ealick SE.
J Med Chem (1993) 36 : 55 -69
PubMed 8421291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.58 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159640 1 10.17
CHEMBL162255 1 9.80
CHEMBL159758 1 9.20
CHEMBL345655 1 7.96
CHEMBL160043 1 7.77
CHEMBL310364 1 7.70
CHEMBL351815 1 7.68
CHEMBL349615 1 7.64
CHEMBL159908 1 7.62
CHEMBL79410 1 7.60
CHEMBL311300 PELDESINE 2.0 1 7.60
CHEMBL79784 1 7.60
CHEMBL354926 1 7.44
CHEMBL310202 1 7.29
CHEMBL159960 1 7.24
CHEMBL82087 1 7.16
CHEMBL162751 1 7.09
CHEMBL351205 1 7.08
CHEMBL81966 1 6.92
CHEMBL159471 1 6.83
CHEMBL285627 1 6.80
CHEMBL158599 1 6.62
CHEMBL81731 1 6.58
CHEMBL309679 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL159640 IC50 = 0.067 nM 10.17
CHEMBL162255 IC50 = 0.16 nM 9.80
CHEMBL159758 IC50 = 0.63 nM 9.20
CHEMBL345655 IC50 = 11.0 nM 7.96
CHEMBL160043 IC50 = 17.0 nM 7.77
CHEMBL310364 IC50 = 20.0 nM 7.70
CHEMBL351815 IC50 = 21.0 nM 7.68
CHEMBL349615 IC50 = 23.0 nM 7.64
CHEMBL159908 IC50 = 24.0 nM 7.62
CHEMBL79410 IC50 = 25.0 nM 7.60
CHEMBL311300 PELDESINE IC50 = 25.0 nM 7.60
CHEMBL79784 IC50 = 25.0 nM 7.60
CHEMBL354926 IC50 = 36.0 nM 7.44
CHEMBL310202 IC50 = 51.0 nM 7.29
CHEMBL159960 IC50 = 57.0 nM 7.24
CHEMBL82087 IC50 = 70.0 nM 7.16
CHEMBL162751 IC50 = 82.0 nM 7.09
CHEMBL351205 IC50 = 83.0 nM 7.08
CHEMBL81966 IC50 = 120.0 nM 6.92
CHEMBL159471 IC50 = 147.0 nM 6.83
CHEMBL285627 IC50 = 160.0 nM 6.80
CHEMBL158599 IC50 = 240.0 nM 6.62
CHEMBL81731 IC50 = 260.0 nM 6.58
CHEMBL309679 IC50 = 270.0 nM 6.57