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Assay Detail

CHEMBL2349751

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

Binding
Inhibition of CDK2/Cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and in vitro biological evaluation of 2,6,9-trisubstituted purines targeting multiple cyclin-dependent kinases.
Zatloukal M, Jorda R, Gucký T, Řezníčková E, Voller J, Pospíšil T, Malínková V, Adamcová H, Kryštof V, Strnad M.
Eur J Med Chem (2013) 61 : 61 -72
PubMed 22770608 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.15 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2349194 1 8.03
CHEMBL2347577 1 7.93
CHEMBL2347575 1 7.88
CHEMBL2347574 1 7.72
CHEMBL2347578 1 7.72
CHEMBL2347579 1 7.70
CHEMBL2347580 1 7.70
CHEMBL2347576 1 7.61
CHEMBL2349193 1 7.60
CHEMBL2349188 1 7.51
CHEMBL1094304 OLOMOUCINE II 1 7.30
CHEMBL2349190 1 7.23
CHEMBL2349189 1 7.22
CHEMBL2349192 1 7.21
CHEMBL2347582 1 7.16
CHEMBL14762 SELICICLIB 2.0 1 6.75
CHEMBL2347584 1 6.66
CHEMBL2347583 1 6.58
CHEMBL2347585 1 6.47
CHEMBL2349191 1 6.20
CHEMBL2347581 1 6.10
CHEMBL76921 1 6.05
CHEMBL2347586 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2349194 IC50 = 9.4 nM 8.03
CHEMBL2347577 IC50 = 11.8 nM 7.93
CHEMBL2347575 IC50 = 13.1 nM 7.88
CHEMBL2347574 IC50 = 19.0 nM 7.72
CHEMBL2347578 IC50 = 19.0 nM 7.72
CHEMBL2347579 IC50 = 20.0 nM 7.70
CHEMBL2347580 IC50 = 20.0 nM 7.70
CHEMBL2347576 IC50 = 24.3 nM 7.61
CHEMBL2349193 IC50 = 25.0 nM 7.60
CHEMBL2349188 IC50 = 31.0 nM 7.51
CHEMBL1094304 OLOMOUCINE II IC50 = 50.0 nM 7.30
CHEMBL2349190 IC50 = 59.0 nM 7.23
CHEMBL2349189 IC50 = 60.0 nM 7.22
CHEMBL2349192 IC50 = 61.0 nM 7.21
CHEMBL2347582 IC50 = 70.0 nM 7.16
CHEMBL14762 SELICICLIB IC50 = 180.0 nM 6.75
CHEMBL2347584 IC50 = 220.0 nM 6.66
CHEMBL2347583 IC50 = 260.0 nM 6.58
CHEMBL2347585 IC50 = 340.0 nM 6.47
CHEMBL2349191 IC50 = 630.0 nM 6.20
CHEMBL2347581 IC50 = 790.0 nM 6.10
CHEMBL76921 IC50 = 890.0 nM 6.05
CHEMBL2347586 IC50 = 890.0 nM 6.05