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Assay Detail

CHEMBL4016699

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

Binding
Inhibition of full length human C-terminal His6-tagged CDK2/N-terminal GST-tagged CyclinE expressed in baculovirus infected sf21 cells after 10 mins in presence of [gamma32P]ATP by beta counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of a Water-Soluble Indirubin Derivative as Potent Inhibitor of Insulin-like Growth Factor 1 Receptor through Structural Modification of the Parent Natural Molecule.
Cheng X, Merz KH, Vatter S, Zeller J, Muehlbeyer S, Thommet A, Christ J, Wölfl S, Eisenbrand G.
J Med Chem (2017) 60 : 4949 -4962
PubMed 28557430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.46 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065365 1 7.37
CHEMBL1830064 1 7.27
CHEMBL4085289 1 7.05
CHEMBL1276317 1 6.68
CHEMBL1802727 1 6.64
CHEMBL14762 SELICICLIB 2.0 1 6.21
CHEMBL4100748 1 6.04
CHEMBL4100916 1 5.77
CHEMBL1276127 INDIRUBIN 2.0 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065365 IC50 = 43.0 nM 7.37
CHEMBL1830064 IC50 = 54.0 nM 7.27
CHEMBL4085289 IC50 = 90.0 nM 7.05
CHEMBL1276317 IC50 = 210.0 nM 6.68
CHEMBL1802727 IC50 = 230.0 nM 6.64
CHEMBL14762 SELICICLIB IC50 = 620.0 nM 6.21
CHEMBL4100748 IC50 = 920.0 nM 6.04
CHEMBL4100916 IC50 = 1700.0 nM 5.77
CHEMBL1276127 INDIRUBIN IC50 = 7500.0 nM 5.12