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Assay Detail

CHEMBL661125

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

Binding
Inhibitory activity against human cyclin-dependent kinase 2 (CDK2)
ChEMBL ↗
94
Total Activities
94
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 2 (CHEMBL301) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 94 7.85 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1964259 — — 1 9.27
CHEMBL1964249 — — 1 9.00
CHEMBL411224 — — 1 8.92
CHEMBL445945 — — 1 8.82
CHEMBL270544 GW396574X — 1 8.82
CHEMBL409892 GW305178X — 1 8.80
CHEMBL271136 — — 1 8.77
CHEMBL429142 — — 1 8.72
CHEMBL411887 — — 1 8.70
CHEMBL409731 — — 1 8.68
CHEMBL271953 — — 1 8.68
CHEMBL269882 — — 1 8.66
CHEMBL269827 GW276655X — 1 8.64
CHEMBL411426 — — 1 8.60
CHEMBL270132 — — 1 8.60
CHEMBL1794055 GW589933X — 1 8.55
CHEMBL269883 GW416981X — 1 8.52
CHEMBL1964255 — — 1 8.48
CHEMBL271160 — — 1 8.47
CHEMBL1964251 — — 1 8.44
CHEMBL1964244 — — 1 8.37
CHEMBL410883 — — 1 8.35
CHEMBL1964250 — — 1 8.35
CHEMBL272667 — — 1 8.34
CHEMBL314397 — — 1 8.34
CHEMBL1964247 — — 1 8.34
CHEMBL1964246 — — 1 8.33
CHEMBL1964242 — — 1 8.25
CHEMBL1964253 — — 1 8.25
CHEMBL1964245 — — 1 8.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1964259 — IC50 = 0.54 nM 9.27
CHEMBL1964249 — IC50 = 1.0 nM 9.00
CHEMBL411224 — IC50 = 1.2 nM 8.92
CHEMBL445945 — IC50 = 1.5 nM 8.82
CHEMBL270544 GW396574X IC50 = 1.5 nM 8.82
CHEMBL409892 GW305178X IC50 = 1.6 nM 8.80
CHEMBL271136 — IC50 = 1.7 nM 8.77
CHEMBL429142 — IC50 = 1.9 nM 8.72
CHEMBL411887 — IC50 = 2.0 nM 8.70
CHEMBL409731 — IC50 = 2.1 nM 8.68
CHEMBL271953 — IC50 = 2.1 nM 8.68
CHEMBL269882 — IC50 = 2.2 nM 8.66
CHEMBL269827 GW276655X IC50 = 2.3 nM 8.64
CHEMBL411426 — IC50 = 2.5 nM 8.60
CHEMBL270132 — IC50 = 2.5 nM 8.60
CHEMBL1794055 GW589933X IC50 = 2.8 nM 8.55
CHEMBL269883 GW416981X IC50 = 3.0 nM 8.52
CHEMBL1964255 — IC50 = 3.3 nM 8.48
CHEMBL271160 — IC50 = 3.4 nM 8.47
CHEMBL1964251 — IC50 = 3.6 nM 8.44
CHEMBL1964244 — IC50 = 4.3 nM 8.37
CHEMBL410883 — IC50 = 4.5 nM 8.35
CHEMBL1964250 — IC50 = 4.5 nM 8.35
CHEMBL1964247 — IC50 = 4.6 nM 8.34
CHEMBL272667 — IC50 = 4.6 nM 8.34
CHEMBL314397 — IC50 = 4.6 nM 8.34
CHEMBL1964246 — IC50 = 4.7 nM 8.33
CHEMBL1964242 — IC50 = 5.6 nM 8.25
CHEMBL1964253 — IC50 = 5.6 nM 8.25
CHEMBL1964245 — IC50 = 5.6 nM 8.25
CHEMBL1234086 — IC50 = 5.7 nM 8.24
CHEMBL1964260 — IC50 = 5.7 nM 8.24
CHEMBL410072 GW301784X IC50 = 6.8 nM 8.17
CHEMBL407709 — IC50 = 7.1 nM 8.15
CHEMBL1964257 — IC50 = 7.5 nM 8.12
CHEMBL411425 — IC50 = 7.9 nM 8.10
CHEMBL408210 — IC50 = 8.9 nM 8.05
CHEMBL272165 GW300657X IC50 = 8.9 nM 8.05
CHEMBL1234087 — IC50 = 8.9 nM 8.05
CHEMBL272380 — IC50 = 9.3 nM 8.03
CHEMBL271952 — IC50 = 9.5 nM 8.02
CHEMBL2112297 — IC50 = 9.5 nM 8.02
CHEMBL1276446 — IC50 = 9.7 nM 8.01
CHEMBL409690 — IC50 = 10.0 nM 8.00
CHEMBL273060 — IC50 = 11.0 nM 7.96
CHEMBL272028 GW300660X IC50 = 12.0 nM 7.92
CHEMBL260103 — IC50 = 12.0 nM 7.92
CHEMBL411865 — IC50 = 12.0 nM 7.92
CHEMBL272833 — IC50 = 13.0 nM 7.89
CHEMBL411490 — IC50 = 13.0 nM 7.89