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Assay Detail

CHEMBL4324304

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

Binding
Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells after 1 hr by electromobility shift assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).
Ward RA, Anderton MJ, Bethel P, Breed J, Cook C, Davies EJ, Dobson A, Dong Z, Fairley G, Farrington P, Feron L, Flemington V, Gibbons FD, Graham MA, Greenwood R, Hanson L, Hopcroft P, Howells R, Hudson J, James M, Jones CD, Jones CR, Li Y, Lamont S, Lewis R, Lindsay N, McCabe J, McGuire T, Rawlins P, Roberts K, Sandin L, Simpson I, Swallow S, Tang J, Tomkinson G, Tonge M, Wang Z, Zhai B.
J Med Chem (2019) 62 : 11004 -11018
PubMed 31710489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4482864 TIZATERKIB 1.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4482864 TIZATERKIB IC50 = 1000.0 nM 6.00