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Assay Detail

CHEMBL1013499

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Binding
Inhibition of bovine spleen adenosine deaminase type 9 by spectrophotometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Spleen
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors.
La Motta C, Sartini S, Mugnaini L, Salerno S, Simorini F, Taliani S, Marini AM, Da Settimo F, Lavecchia A, Novellino E, Antonioli L, Fornai M, Blandizzi C, Del Tacca M.
J Med Chem (2009) 52 : 1681 -1692
PubMed 19226143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.19 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459780 1 9.80
CHEMBL517884 1 9.29
CHEMBL461038 1 9.02
CHEMBL459570 1 8.94
CHEMBL296435 (+)-EHNA 1 8.94
CHEMBL460200 1 8.70
CHEMBL459771 1 8.62
CHEMBL471837 1 7.90
CHEMBL472461 1 7.81
CHEMBL459569 1 7.55
CHEMBL461039 1 7.32
CHEMBL472462 1 7.07
CHEMBL513249 1 6.97
CHEMBL470158 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459780 Ki = 0.16 nM 9.80
CHEMBL517884 Ki = 0.51 nM 9.29
CHEMBL461038 Ki = 0.96 nM 9.02
CHEMBL459570 Ki = 1.15 nM 8.94
CHEMBL296435 (+)-EHNA Ki = 1.14 nM 8.94
CHEMBL460200 Ki = 2.01 nM 8.70
CHEMBL459771 Ki = 2.42 nM 8.62
CHEMBL471837 Ki = 12.65 nM 7.90
CHEMBL472461 Ki = 15.56 nM 7.81
CHEMBL459569 Ki = 28.27 nM 7.55
CHEMBL461039 Ki = 47.91 nM 7.32
CHEMBL472462 Ki = 85.7 nM 7.07
CHEMBL513249 Ki = 108.0 nM 6.97
CHEMBL470158 Ki = 186.0 nM 6.73