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Assay Detail

CHEMBL873419

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

Binding
Inhibitory activity against calf spleen purine nucleoside phosphorylase (PNP) using 2-amino-6-mercapto-7-methyl purine ribonucleoside (MESG) as substrate.
27
Total Activities
27
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-activity relationships for a class of inhibitors of purine nucleoside phosphorylase.
Farutin V, Masterson L, Andricopulo AD, Cheng J, Riley B, Hakimi R, Frazer JW, Cordes EH.
J Med Chem (1999) 42 : 2422 -2431
PubMed 10395483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.61 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82087 1 8.77
CHEMBL311300 PELDESINE 2.0 1 8.51
CHEMBL56540 1 8.48
CHEMBL79784 1 8.46
CHEMBL310202 1 8.44
CHEMBL55454 1 8.41
CHEMBL310364 1 8.37
CHEMBL81839 1 8.34
CHEMBL81055 1 8.27
CHEMBL55675 1 8.22
CHEMBL56593 1 8.21
CHEMBL299952 1 8.19
CHEMBL81966 1 7.84
CHEMBL79865 1 7.77
CHEMBL83158 1 7.69
CHEMBL285627 1 7.68
CHEMBL309907 1 7.66
CHEMBL309679 1 7.50
CHEMBL81731 1 7.46
CHEMBL78808 1 7.45
CHEMBL79460 1 7.21
CHEMBL79132 1 7.17
CHEMBL54489 1 6.48
CHEMBL301203 1 6.30
CHEMBL8040 8-AMINOGUANINE 1 6.17
CHEMBL292132 1 6.12
CHEMBL311528 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82087 Ki = 1.7 nM 8.77
CHEMBL311300 PELDESINE Ki = 3.1 nM 8.51
CHEMBL56540 Ki = 3.3 nM 8.48
CHEMBL79784 Ki = 3.5 nM 8.46
CHEMBL310202 Ki = 3.6 nM 8.44
CHEMBL55454 Ki = 3.9 nM 8.41
CHEMBL310364 Ki = 4.3 nM 8.37
CHEMBL81839 Ki = 4.6 nM 8.34
CHEMBL81055 Ki = 5.4 nM 8.27
CHEMBL55675 Ki = 6.0 nM 8.22
CHEMBL56593 Ki = 6.2 nM 8.21
CHEMBL299952 Ki = 6.4 nM 8.19
CHEMBL81966 Ki = 14.4 nM 7.84
CHEMBL79865 Ki = 16.9 nM 7.77
CHEMBL83158 Ki = 20.3 nM 7.69
CHEMBL285627 Ki = 20.7 nM 7.68
CHEMBL309907 Ki = 22.0 nM 7.66
CHEMBL309679 Ki = 31.8 nM 7.50
CHEMBL81731 Ki = 35.0 nM 7.46
CHEMBL78808 Ki = 35.6 nM 7.45
CHEMBL79460 Ki = 61.0 nM 7.21
CHEMBL79132 Ki = 67.7 nM 7.17
CHEMBL54489 Ki = 332.7 nM 6.48
CHEMBL301203 Ki = 500.3 nM 6.30
CHEMBL8040 8-AMINOGUANINE Ki = 680.6 nM 6.17
CHEMBL292132 Ki = 766.0 nM 6.12
CHEMBL311528 Ki = 67501.0 nM 4.17