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Assay Detail

CHEMBL770309

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Binding
Inhibitory activity against calf spleen purine nucleoside phosphorylase (PNP) using inosine as substrate at a concentration of 10 uM.
29
Total Activities
29
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 29 7.28 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309907 1 8.40
CHEMBL55675 1 8.07
CHEMBL79460 1 8.05
CHEMBL56593 1 8.04
CHEMBL55454 1 8.03
CHEMBL79410 1 7.97
CHEMBL81839 1 7.96
CHEMBL310202 1 7.96
CHEMBL56540 1 7.94
CHEMBL299952 1 7.88
CHEMBL311300 PELDESINE 2.0 1 7.87
CHEMBL79784 1 7.81
CHEMBL82087 1 7.78
CHEMBL81055 1 7.73
CHEMBL310364 1 7.72
CHEMBL79865 1 7.59
CHEMBL285627 1 7.45
CHEMBL83158 1 7.42
CHEMBL81966 1 7.19
CHEMBL78808 1 7.18
CHEMBL309679 1 7.08
CHEMBL81731 1 6.96
CHEMBL79132 1 6.83
CHEMBL54489 1 6.47
CHEMBL301203 1 6.06
CHEMBL292132 1 6.05
CHEMBL8040 8-AMINOGUANINE 1 6.01
CHEMBL311528 1 4.99
CHEMBL415041 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309907 Ki = 4.0 nM 8.40
CHEMBL55675 Ki = 8.5 nM 8.07
CHEMBL79460 Ki = 9.0 nM 8.05
CHEMBL56593 Ki = 9.1 nM 8.04
CHEMBL55454 Ki = 9.4 nM 8.03
CHEMBL79410 Ki = 10.6 nM 7.97
CHEMBL81839 Ki = 10.9 nM 7.96
CHEMBL310202 Ki = 11.0 nM 7.96
CHEMBL56540 Ki = 11.4 nM 7.94
CHEMBL299952 Ki = 13.2 nM 7.88
CHEMBL311300 PELDESINE Ki = 13.5 nM 7.87
CHEMBL79784 Ki = 15.6 nM 7.81
CHEMBL82087 Ki = 16.5 nM 7.78
CHEMBL81055 Ki = 18.7 nM 7.73
CHEMBL310364 Ki = 18.9 nM 7.72
CHEMBL79865 Ki = 25.4 nM 7.59
CHEMBL285627 Ki = 35.7 nM 7.45
CHEMBL83158 Ki = 37.8 nM 7.42
CHEMBL81966 Ki = 65.0 nM 7.19
CHEMBL78808 Ki = 66.7 nM 7.18
CHEMBL309679 Ki = 84.0 nM 7.08
CHEMBL81731 Ki = 109.1 nM 6.96
CHEMBL79132 Ki = 148.8 nM 6.83
CHEMBL54489 Ki = 335.3 nM 6.47
CHEMBL301203 Ki = 862.0 nM 6.06
CHEMBL292132 Ki = 885.0 nM 6.05
CHEMBL8040 8-AMINOGUANINE Ki = 982.0 nM 6.01
CHEMBL311528 Ki = 10321.0 nM 4.99
CHEMBL415041 Ki = 24645.0 nM 4.61