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Assay Detail

CHEMBL1104157

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

Binding
Inhibition of PKAalpha assessed as decrease in NADH absorbance at 340 nm in the presence of
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

cAMP-dependent protein kinase catalytic subunit alpha (CHEMBL4101)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.
Bandarage U, Hare B, Parsons J, Pham L, Marhefka C, Bemis G, Tang Q, Moody CS, Rodems S, Shah S, Adams C, Bravo J, Charonnet E, Savic V, Come JH, Green J.
Bioorg Med Chem Lett (2009) 19 : 5191 -5194
PubMed 19632115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.05 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1080071 1 7.47
CHEMBL1078930 1 6.42
CHEMBL1079294 1 6.27
CHEMBL1078929 1 6.22
CHEMBL1079295 1 6.14
CHEMBL365286 GW549034X 1 6.02
CHEMBL1079040 1 5.96
CHEMBL1079243 1 5.92
CHEMBL1078426 1 5.89
CHEMBL1078820 1 5.85
CHEMBL1080970 1 5.82
CHEMBL1080072 1 5.60
CHEMBL1079135 1 5.58
CHEMBL1079032 1 5.55
CHEMBL1077670 1 -
CHEMBL1078717 1 -
CHEMBL1080245 1 -
CHEMBL1080073 1 -
CHEMBL1082061 1 -
CHEMBL1078245 1 -
CHEMBL1078155 1 -
CHEMBL1078539 1 -
CHEMBL1078538 1 -
CHEMBL1078537 1 -
CHEMBL1078427 1 -
CHEMBL1079293 1 -
CHEMBL1079208 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1080071 Ki = 34.0 nM 7.47
CHEMBL1078930 Ki = 380.0 nM 6.42
CHEMBL1079294 Ki = 540.0 nM 6.27
CHEMBL1078929 Ki = 600.0 nM 6.22
CHEMBL1079295 Ki = 720.0 nM 6.14
CHEMBL365286 GW549034X Ki = 960.0 nM 6.02
CHEMBL1079040 Ki = 1100.0 nM 5.96
CHEMBL1079243 Ki = 1200.0 nM 5.92
CHEMBL1078426 Ki = 1300.0 nM 5.89
CHEMBL1078820 Ki = 1400.0 nM 5.85
CHEMBL1080970 Ki = 1500.0 nM 5.82
CHEMBL1080072 Ki = 2500.0 nM 5.60
CHEMBL1079135 Ki = 2600.0 nM 5.58
CHEMBL1079032 Ki = 2800.0 nM 5.55
CHEMBL1077670 Ki > 3300.0 nM -
CHEMBL1078717 Ki > 4000.0 nM -
CHEMBL1080245 Ki > 3300.0 nM -
CHEMBL1080073 Ki > 3300.0 nM -
CHEMBL1082061 Ki > 3300.0 nM -
CHEMBL1078245 Ki > 4000.0 nM -
CHEMBL1078155 Ki - -
CHEMBL1078539 Ki > 5000.0 nM -
CHEMBL1078538 Ki > 5000.0 nM -
CHEMBL1078537 Ki > 5000.0 nM -
CHEMBL1078427 Ki > 5000.0 nM -
CHEMBL1079293 Ki > 3300.0 nM -
CHEMBL1079208 Ki > 3300.0 nM -