Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2380185

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

Binding
Inhibition of human CDK2/Cyclin A2 using PKTPKKAKKL as substrate by PK/LDH spectrophotometric analysis
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

CDK2/Cyclin A2 (CHEMBL3038469) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.
Schonbrunn E, Betzi S, Alam R, Martin MP, Becker A, Han H, Francis R, Chakrasali R, Jakkaraj S, Kazi A, Sebti SM, Cubitt CL, Gebhard AW, Hazlehurst LA, Tash JS, Georg GI.
J Med Chem (2013) 56 : 3768 -3782
PubMed 23600925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 5.03 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2377849 — — 1 5.89
CHEMBL2377839 — — 1 5.85
CHEMBL2377815 — — 1 5.82
CHEMBL2377840 — — 1 5.80
CHEMBL2377848 — — 1 5.70
CHEMBL2377841 — — 1 5.66
CHEMBL2377830 — — 1 5.55
CHEMBL2377863 — — 1 5.54
CHEMBL2377860 — — 1 5.51
CHEMBL565033 — — 1 5.51
CHEMBL2377816 — — 1 5.46
CHEMBL2377827 — — 1 5.46
CHEMBL2377828 — — 1 5.40
CHEMBL2377814 — — 1 5.32
CHEMBL2377813 — — 1 5.32
CHEMBL2377861 — — 1 5.30
CHEMBL2377846 — — 1 5.24
CHEMBL2377812 — — 1 5.13
CHEMBL2377826 — — 1 5.11
CHEMBL2377810 — — 1 5.06
CHEMBL2377847 — — 1 5.05
CHEMBL2377859 — — 1 4.92
CHEMBL2377845 — — 1 4.82
CHEMBL2377862 — — 1 4.82
CHEMBL2377811 — — 1 4.82
CHEMBL2377687 — — 1 4.77
CHEMBL2377842 — — 1 4.77
CHEMBL2377686 — — 1 4.60
CHEMBL2377684 — — 1 4.50
CHEMBL2377857 — — 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2377849 — IC50 = 1300.0 nM 5.89
CHEMBL2377839 — IC50 = 1400.0 nM 5.85
CHEMBL2377815 — IC50 = 1500.0 nM 5.82
CHEMBL2377840 — IC50 = 1600.0 nM 5.80
CHEMBL2377848 — IC50 = 2000.0 nM 5.70
CHEMBL2377841 — IC50 = 2200.0 nM 5.66
CHEMBL2377830 — IC50 = 2800.0 nM 5.55
CHEMBL2377863 — IC50 = 2900.0 nM 5.54
CHEMBL2377860 — IC50 = 3100.0 nM 5.51
CHEMBL565033 — IC50 = 3100.0 nM 5.51
CHEMBL2377816 — IC50 = 3500.0 nM 5.46
CHEMBL2377827 — IC50 = 3500.0 nM 5.46
CHEMBL2377828 — IC50 = 4000.0 nM 5.40
CHEMBL2377813 — IC50 = 4800.0 nM 5.32
CHEMBL2377814 — IC50 = 4800.0 nM 5.32
CHEMBL2377861 — IC50 = 5000.0 nM 5.30
CHEMBL2377846 — IC50 = 5700.0 nM 5.24
CHEMBL2377812 — IC50 = 7400.0 nM 5.13
CHEMBL2377826 — IC50 = 7800.0 nM 5.11
CHEMBL2377810 — IC50 = 8800.0 nM 5.06
CHEMBL2377847 — IC50 = 8900.0 nM 5.05
CHEMBL2377859 — IC50 = 12000.0 nM 4.92
CHEMBL2377845 — IC50 = 15000.0 nM 4.82
CHEMBL2377862 — IC50 = 15000.0 nM 4.82
CHEMBL2377811 — IC50 = 15000.0 nM 4.82
CHEMBL2377687 — IC50 = 17000.0 nM 4.77
CHEMBL2377842 — IC50 = 17000.0 nM 4.77
CHEMBL2377686 — IC50 = 25000.0 nM 4.60
CHEMBL2377684 — IC50 = 32000.0 nM 4.50
CHEMBL2377857 — IC50 = 33000.0 nM 4.48
CHEMBL2377858 — IC50 = 35000.0 nM 4.46
CHEMBL2377856 — IC50 = 37000.0 nM 4.43
CHEMBL2377855 — IC50 = 41000.0 nM 4.39
CHEMBL2377824 — IC50 = 43000.0 nM 4.37
CHEMBL2377853 — IC50 = 49000.0 nM 4.31
CHEMBL2377685 — IC50 = 82000.0 nM 4.09
CHEMBL453920 — IC50 = 95000.0 nM 4.02
CHEMBL2377837 — IC50 = 99000.0 nM 4.00
CHEMBL2377834 — IC50 > 100000.0 nM -
CHEMBL2377843 — IC50 > 100000.0 nM -
CHEMBL570537 — IC50 > 100000.0 nM -
CHEMBL2377835 — IC50 > 100000.0 nM -
CHEMBL2377832 — IC50 > 100000.0 nM -
CHEMBL2377833 — IC50 > 100000.0 nM -
CHEMBL2375384 — IC50 > 100000.0 nM -
CHEMBL2377852 — IC50 > 100000.0 nM -
CHEMBL2377851 — IC50 > 100000.0 nM -
CHEMBL2377683 — IC50 > 100000.0 nM -
CHEMBL2377850 — IC50 > 100000.0 nM -
CHEMBL2377854 — IC50 > 100000.0 nM -