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Assay Detail

CHEMBL5679158

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

Binding
Binding affinity to recombinant human GST tagged Ckh1 phosphorylation expressed in baculovirus Insect cell assessed as inhibition constant incubated for 20 mins in presence of ATP by topcount reader based analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Insect cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.
Zabludoff SD, Deng C, Grondine MR, Sheehy AM, Ashwell S, Caleb BL, Green S, Haye HR, Horn CL, Janetka JW, Liu D, Mouchet E, Ready S, Rosenthal JL, Queva C, Schwartz GK, Taylor KJ, Tse AN, Walker GE, White AM.
Mol Cancer Ther (2008) 7 : 2955 -2966
PubMed 18790776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.44 8.44

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2041933 AZD-7762 1.0 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041933 AZD-7762 Ki = 3.6 nM 8.44