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Assay Detail

CHEMBL4394716

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

Functional
Inhibition of human MV411 cells incubated for 72 hrs by cellTiter 96 aqueous one solution reagent based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MV4-11
Confidence 1 — Organism
Curated By Autocuration

Target

MV4-11 (CHEMBL613835)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.
Tong L, Song P, Jiang K, Xu L, Jin T, Wang P, Hu X, Fang S, Gao A, Zhou Y, Liu T, Li J, Hu Y.
Eur J Med Chem (2019) 173 : 44 -62
PubMed 30986571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.26 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3544911 PREXASERTIB 2.0 1 8.40
CHEMBL4448921 1 7.41
CHEMBL4444269 1 7.40
CHEMBL4470089 1 7.36
CHEMBL4562902 1 7.19
CHEMBL4456833 1 6.97
CHEMBL3039517 RABUSERTIB 2.0 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3544911 PREXASERTIB IC50 = 4.0 nM 8.40
CHEMBL4448921 IC50 = 39.0 nM 7.41
CHEMBL4444269 IC50 = 40.0 nM 7.40
CHEMBL4470089 IC50 = 44.0 nM 7.36
CHEMBL4562902 IC50 = 64.0 nM 7.19
CHEMBL4456833 IC50 = 107.0 nM 6.97
CHEMBL3039517 RABUSERTIB IC50 = 869.0 nM 6.06