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Assay Detail

CHEMBL666605

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

Binding
Inhibitory activity against baculovirus expressed Cyclin dependent kinase 2-cyclinE
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin E (CHEMBL2094126)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Kimball SD, Misra RN, Rawlins DB, Hunt JT, Xiao HY, Lu S, Qian L, Han WC, Shan W, Mitt T, Cai ZW, Poss MA, Zhu H, Sack JS, Tokarski JS, Chang CY, Pavletich N, Kamath A, Humphreys WG, Marathe P, Bursuker I, Kellar KA, Roongta U, Batorsky R, Mulheron JG, Bol D, Fairchild CR, Lee FY, Webster KR.
J Med Chem (2002) 45 : 3905 -3927
PubMed 12190313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 55 7.22 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL126997 1 8.70
CHEMBL340904 1 8.52
CHEMBL300936 1 8.52
CHEMBL126549 1 8.52
CHEMBL126328 1 8.40
CHEMBL126993 1 8.30
CHEMBL129396 1 8.30
CHEMBL295136 1 8.30
CHEMBL126630 1 8.30
CHEMBL2111846 1 8.22
CHEMBL129471 1 8.22
CHEMBL340794 1 7.96
CHEMBL263955 1 7.77
CHEMBL125401 1 7.70
CHEMBL126908 1 7.60
CHEMBL48796 1 7.58
CHEMBL340012 1 7.30
CHEMBL126600 1 7.30
CHEMBL2112653 1 7.22
CHEMBL420143 1 7.05
CHEMBL126782 1 6.85
CHEMBL129475 1 6.82
CHEMBL127929 1 6.77
CHEMBL129716 1 6.70
CHEMBL435992 1 6.60
CHEMBL428690 ALVOCIDIB 3.0 1 6.48
CHEMBL339246 1 6.47
CHEMBL125731 1 6.46
CHEMBL129555 1 6.44
CHEMBL340741 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL126997 IC50 = 2.0 nM 8.70
CHEMBL340904 IC50 = 3.0 nM 8.52
CHEMBL126549 IC50 = 3.0 nM 8.52
CHEMBL300936 IC50 = 3.0 nM 8.52
CHEMBL126328 IC50 = 4.0 nM 8.40
CHEMBL126993 IC50 = 5.0 nM 8.30
CHEMBL129396 IC50 = 5.0 nM 8.30
CHEMBL295136 IC50 = 5.0 nM 8.30
CHEMBL126630 IC50 = 5.0 nM 8.30
CHEMBL2111846 IC50 = 6.0 nM 8.22
CHEMBL129471 IC50 = 6.0 nM 8.22
CHEMBL340794 IC50 = 11.0 nM 7.96
CHEMBL263955 IC50 = 17.0 nM 7.77
CHEMBL125401 IC50 = 20.0 nM 7.70
CHEMBL126908 IC50 = 25.0 nM 7.60
CHEMBL48796 IC50 = 26.0 nM 7.58
CHEMBL340012 IC50 = 50.0 nM 7.30
CHEMBL126600 IC50 = 50.0 nM 7.30
CHEMBL2112653 IC50 = 60.0 nM 7.22
CHEMBL420143 IC50 = 90.0 nM 7.05
CHEMBL126782 IC50 = 140.0 nM 6.85
CHEMBL129475 IC50 = 150.0 nM 6.82
CHEMBL127929 IC50 = 170.0 nM 6.77
CHEMBL129716 IC50 = 200.0 nM 6.70
CHEMBL435992 IC50 = 250.0 nM 6.60
CHEMBL428690 ALVOCIDIB IC50 = 330.0 nM 6.48
CHEMBL339246 IC50 = 340.0 nM 6.47
CHEMBL125731 IC50 = 350.0 nM 6.46
CHEMBL129555 IC50 = 360.0 nM 6.44
CHEMBL340741 IC50 = 680.0 nM 6.17
CHEMBL339070 IC50 = 1740.0 nM 5.76
CHEMBL126458 IC50 = 1840.0 nM 5.74
CHEMBL129009 IC50 = 2810.0 nM 5.55
CHEMBL129107 IC50 = 4280.0 nM 5.37
CHEMBL126405 IC50 = 12580.0 nM 4.90
CHEMBL129466 IC50 > 1000.0 nM -
CHEMBL130020 IC50 > 1000.0 nM -
CHEMBL340400 IC50 > 25000.0 nM -
CHEMBL340796 IC50 > 25000.0 nM -
CHEMBL129763 IC50 > 1000.0 nM -
CHEMBL126934 IC50 > 1000.0 nM -
CHEMBL338401 IC50 > 25000.0 nM -
CHEMBL129532 IC50 > 1000.0 nM -
CHEMBL129584 IC50 > 25000.0 nM -
CHEMBL341286 IC50 > 1000.0 nM -
CHEMBL129563 IC50 > 1000.0 nM -
CHEMBL125352 IC50 > 1000.0 nM -
CHEMBL129213 IC50 > 25000.0 nM -
CHEMBL126459 IC50 > 1000.0 nM -
CHEMBL126788 IC50 > 1000.0 nM -