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Assay Detail

CHEMBL760476

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

Binding
Inhibition of Purine nucleoside phosphorylase was evaluated against the enzyme from calf spleen in 50 mM phosphate
21
Total Activities
21
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 21 6.55 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352454 1 9.80
CHEMBL79784 1 7.10
CHEMBL310364 1 6.82
CHEMBL351815 1 6.82
CHEMBL285627 1 6.80
CHEMBL311300 PELDESINE 2.0 1 6.72
CHEMBL354926 1 6.72
CHEMBL310202 1 6.68
CHEMBL159908 1 6.66
CHEMBL160043 1 6.60
CHEMBL349615 1 6.57
CHEMBL159960 1 6.57
CHEMBL82087 1 6.56
CHEMBL351205 1 6.50
CHEMBL79410 1 6.42
CHEMBL162751 1 6.18
CHEMBL159471 1 6.13
CHEMBL309679 1 5.70
CHEMBL81731 1 5.64
CHEMBL81966 1 5.60
CHEMBL158599 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352454 IC50 = 0.16 nM 9.80
CHEMBL79784 IC50 = 80.0 nM 7.10
CHEMBL310364 IC50 = 150.0 nM 6.82
CHEMBL351815 IC50 = 150.0 nM 6.82
CHEMBL285627 IC50 = 160.0 nM 6.80
CHEMBL311300 PELDESINE IC50 = 190.0 nM 6.72
CHEMBL354926 IC50 = 190.0 nM 6.72
CHEMBL310202 IC50 = 210.0 nM 6.68
CHEMBL159908 IC50 = 220.0 nM 6.66
CHEMBL160043 IC50 = 250.0 nM 6.60
CHEMBL349615 IC50 = 270.0 nM 6.57
CHEMBL159960 IC50 = 270.0 nM 6.57
CHEMBL82087 IC50 = 274.0 nM 6.56
CHEMBL351205 IC50 = 313.0 nM 6.50
CHEMBL79410 IC50 = 380.0 nM 6.42
CHEMBL162751 IC50 = 660.0 nM 6.18
CHEMBL159471 IC50 = 740.0 nM 6.13
CHEMBL309679 IC50 = 2000.0 nM 5.70
CHEMBL81731 IC50 = 2300.0 nM 5.64
CHEMBL81966 IC50 = 2520.0 nM 5.60
CHEMBL158599 IC50 = 10000.0 nM 5.00