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Assay Detail

CHEMBL845182

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

Functional
Inhibition of progression of cells from G1 into S-phase by BrdU incorporation assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
Bramson HN, Corona J, Davis ST, Dickerson SH, Edelstein M, Frye SV, Gampe RT, Harris PA, Hassell A, Holmes WD, Hunter RN, Lackey KE, Lovejoy B, Luzzio MJ, Montana V, Rocque WJ, Rusnak D, Shewchuk L, Veal JM, Walker DH, Kuyper LF.
J Med Chem (2001) 44 : 4339 -4358
PubMed 11728181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.67 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL409892 GW305178X 1 6.54
CHEMBL1964245 1 6.19
CHEMBL271136 1 5.96
CHEMBL391229 1 5.82
CHEMBL411426 1 5.75
CHEMBL269883 GW416981X 1 5.64
CHEMBL1276446 1 5.58
CHEMBL1964244 1 5.48
CHEMBL1964250 1 5.27
CHEMBL1964242 1 5.11
CHEMBL1964260 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL409892 GW305178X IC50 = 290.0 nM 6.54
CHEMBL1964245 IC50 = 650.0 nM 6.19
CHEMBL271136 IC50 = 1100.0 nM 5.96
CHEMBL391229 IC50 = 1500.0 nM 5.82
CHEMBL411426 IC50 = 1800.0 nM 5.75
CHEMBL269883 GW416981X IC50 = 2300.0 nM 5.64
CHEMBL1276446 IC50 = 2600.0 nM 5.58
CHEMBL1964244 IC50 = 3300.0 nM 5.48
CHEMBL1964250 IC50 = 5400.0 nM 5.27
CHEMBL1964242 IC50 = 7800.0 nM 5.11
CHEMBL1964260 IC50 = 8300.0 nM 5.08