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Assay Detail

CHEMBL1031298

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Binding
Inhibition of GSK3-beta
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glycogen synthase kinase-3 beta (CHEMBL262)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of the potent aurora inhibitor MK-0457 (VX-680).
Bebbington D, Binch H, Charrier JD, Everitt S, Fraysse D, Golec J, Kay D, Knegtel R, Mak C, Mazzei F, Miller A, Mortimore M, O'Donnell M, Patel S, Pierard F, Pinder J, Pollard J, Ramaya S, Robinson D, Rutherford A, Studley J, Westcott J.
Bioorg Med Chem Lett (2009) 19 : 3586 -3592
PubMed 19447622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.91 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL551633 1 8.10
CHEMBL549668 1 7.77
CHEMBL359482 1 7.66
CHEMBL552038 1 7.62
CHEMBL562416 1 7.48
CHEMBL562157 1 7.36
CHEMBL564459 1 7.32
CHEMBL565205 1 7.29
CHEMBL552033 1 7.17
CHEMBL549536 1 7.14
CHEMBL561834 1 6.95
CHEMBL552500 1 6.91
CHEMBL562415 1 6.90
CHEMBL549322 1 6.77
CHEMBL551634 1 6.67
CHEMBL550825 1 6.51
CHEMBL561421 1 6.47
CHEMBL560158 1 6.22
CHEMBL484950 1 5.99
CHEMBL564290 1 5.93
CHEMBL564449 1 5.88
CHEMBL564941 1 5.82
CHEMBL559900 1 -
CHEMBL556460 1 -
CHEMBL552385 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL551633 Ki = 8.0 nM 8.10
CHEMBL549668 Ki = 17.0 nM 7.77
CHEMBL359482 Ki = 22.0 nM 7.66
CHEMBL552038 Ki = 24.0 nM 7.62
CHEMBL562416 Ki = 33.0 nM 7.48
CHEMBL562157 Ki = 44.0 nM 7.36
CHEMBL564459 Ki = 48.0 nM 7.32
CHEMBL565205 Ki = 51.0 nM 7.29
CHEMBL552033 Ki = 67.0 nM 7.17
CHEMBL549536 Ki = 73.0 nM 7.14
CHEMBL561834 Ki = 113.0 nM 6.95
CHEMBL552500 Ki = 124.0 nM 6.91
CHEMBL562415 Ki = 126.0 nM 6.90
CHEMBL549322 Ki = 171.0 nM 6.77
CHEMBL551634 Ki = 216.0 nM 6.67
CHEMBL550825 Ki = 312.0 nM 6.51
CHEMBL561421 Ki = 338.0 nM 6.47
CHEMBL560158 Ki = 605.0 nM 6.22
CHEMBL484950 Ki = 1034.0 nM 5.99
CHEMBL564290 Ki = 1168.0 nM 5.93
CHEMBL564449 Ki = 1314.0 nM 5.88
CHEMBL564941 Ki = 1500.0 nM 5.82
CHEMBL559900 Ki > 150.0 nM -
CHEMBL556460 Ki > 4000.0 nM -
CHEMBL552385 Ki > 15.0 nM -