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Assay Detail

CHEMBL1103822

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

Binding
Inhibition of CDK2/cyclin E
17
Total Activities
17
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

5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.
Choi SJ, Lee JE, Jeong SY, Im I, Lee SD, Lee EJ, Lee SK, Kwon SM, Ahn SG, Yoon JH, Han SY, Kim JI, Kim YC.
J Med Chem (2010) 53 : 3696 -3706
PubMed 20361800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.61 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1087073 1 8.77
CHEMBL1087075 1 8.74
CHEMBL1088704 1 8.72
CHEMBL1086662 1 8.65
CHEMBL1098686 1 8.28
CHEMBL369303 1 8.13
CHEMBL1087074 1 8.10
CHEMBL1086683 1 8.08
CHEMBL1086701 1 8.06
CHEMBL1086950 1 8.00
CHEMBL1099029 1 7.96
CHEMBL1086811 1 7.63
CHEMBL1086700 1 7.22
CHEMBL1086951 1 7.12
CHEMBL1087739 1 5.53
CHEMBL1099039 1 5.38
CHEMBL1087740 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1087073 IC50 = 1.71 nM 8.77
CHEMBL1087075 IC50 = 1.83 nM 8.74
CHEMBL1088704 IC50 = 1.91 nM 8.72
CHEMBL1086662 IC50 = 2.25 nM 8.65
CHEMBL1098686 IC50 = 5.27 nM 8.28
CHEMBL369303 IC50 = 7.35 nM 8.13
CHEMBL1087074 IC50 = 8.01 nM 8.10
CHEMBL1086683 IC50 = 8.32 nM 8.08
CHEMBL1086701 IC50 = 8.68 nM 8.06
CHEMBL1086950 IC50 = 10.1 nM 8.00
CHEMBL1099029 IC50 = 11.1 nM 7.96
CHEMBL1086811 IC50 = 23.5 nM 7.63
CHEMBL1086700 IC50 = 60.3 nM 7.22
CHEMBL1086951 IC50 = 76.2 nM 7.12
CHEMBL1087739 IC50 = 2950.0 nM 5.53
CHEMBL1099039 IC50 = 4120.0 nM 5.38
CHEMBL1087740 IC50 = 8620.0 nM 5.06