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Assay Detail

CHEMBL3396024

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

Functional
Cytotoxicity against human U2OS cells assessed as cell viability after 72 hrs by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U2OS
Confidence 1 — Organism
Curated By Autocuration

Target

U2OS (CHEMBL615023)
Type CELL-LINE
Organism Homo sapiens

Publication

Iterative conversion of cyclin binding groove peptides into druglike CDK inhibitors with antitumor activity.
Premnath PN, Craig SN, Liu S, Anderson EL, Grigoroudis AI, Kontopidis G, Perkins TL, Wyatt MD, Pittman DL, McInnes C.
J Med Chem (2015) 58 : 433 -442
PubMed 25454794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.40 4.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393784 1 4.74
CHEMBL3393783 1 4.51
CHEMBL3393788 1 4.22
CHEMBL3393786 1 4.12
CHEMBL3393787 1 -
CHEMBL3393785 1 -
CHEMBL3393782 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393784 IC50 = 18300.0 nM 4.74
CHEMBL3393783 IC50 = 30700.0 nM 4.51
CHEMBL3393788 IC50 = 60500.0 nM 4.22
CHEMBL3393786 IC50 = 75600.0 nM 4.12
CHEMBL3393787 IC50 = 108000.0 nM -
CHEMBL3393785 IC50 > 100000.0 nM -
CHEMBL3393782 IC50 > 100000.0 nM -