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Assay Detail

CHEMBL657123

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

Binding
In vitro inhibition of human CDK2/cyclin E.
17
Total Activities
17
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

1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases.
Misra RN, Rawlins DB, Xiao HY, Shan W, Bursuker I, Kellar KA, Mulheron JG, Sack JS, Tokarski JS, Kimball SD, Webster KR.
Bioorg Med Chem Lett (2003) 13 : 1133 -1136
PubMed 12643928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.10 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14619 SQ-67563 1 6.96
CHEMBL428690 ALVOCIDIB 3.0 1 6.77
CHEMBL279405 1 6.75
CHEMBL418540 1 6.75
CHEMBL277795 1 6.62
CHEMBL14593 1 6.55
CHEMBL14327 1 6.28
CHEMBL279590 1 6.18
CHEMBL14709 1 5.43
CHEMBL276336 1 5.36
CHEMBL278709 1 4.82
CHEMBL278941 1 4.77
CHEMBL277160 1 -
CHEMBL277354 1 -
CHEMBL14799 1 -
CHEMBL14124 1 -
CHEMBL14856 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14619 SQ-67563 IC50 = 110.0 nM 6.96
CHEMBL428690 ALVOCIDIB IC50 = 170.0 nM 6.77
CHEMBL279405 IC50 = 180.0 nM 6.75
CHEMBL418540 IC50 = 180.0 nM 6.75
CHEMBL277795 IC50 = 240.0 nM 6.62
CHEMBL14593 IC50 = 280.0 nM 6.55
CHEMBL14327 IC50 = 520.0 nM 6.28
CHEMBL279590 IC50 = 660.0 nM 6.18
CHEMBL14709 IC50 = 3700.0 nM 5.43
CHEMBL276336 IC50 = 4400.0 nM 5.36
CHEMBL278709 IC50 = 15000.0 nM 4.82
CHEMBL278941 IC50 = 17000.0 nM 4.77
CHEMBL277160 IC50 > 25000.0 nM -
CHEMBL277354 IC50 > 25000.0 nM -
CHEMBL14799 IC50 > 25000.0 nM -
CHEMBL14124 IC50 > 25000.0 nM -
CHEMBL14856 IC50 > 25000.0 nM -