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Assay Detail

CHEMBL5737554

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Binding
LanthaScreen LanthaScreen: CDK2 (cyclin E1): IC50 values of compounds against CDK2 (cyclin E1) were determined by LanthaScreen™ Eu Kinase Binding Assay at Invitrogen Life Technologies (Grand Island, N.Y.)) where total reaction volume was 16 μL/well in low volume, white 384-well plate (#784207, Greiner). 0.16 μL of 100× test compound in 100% DMSO (at specific solutions) were mixed with 3.84 μL of Kinase Buffer (50 mM HEPES pH 7.5, 0.01% BRIJ-35, 10 mM MgCl2, 1 mM EGTA), 8.0 μL of 2× Kinase (2.5 nM)/Antibody (Eu-anti-GST, 2 nM) Mixture and 4.0 μL of 4× Tracer (Tracer 236, 100 nM). The plates were shaken for 30 seconds, and incubated for 60 minutes at room temperature. The plates were read on fluorescence plate reader with Dual emission at 615 nm and 665 nm.
3
Total Activities
1
Compounds Tested
3
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

Heterocyclic compounds as kinase inhibitors
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.14 8.14
kon 1 - -
k_off 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5803114 3 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5803114 IC50 = 7.2 nM 8.14
CHEMBL5803114 kon = - -
CHEMBL5803114 k_off = - s-1 -