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Assay Detail

CHEMBL662528

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

Binding
Inhibition of cyclin-dependent kinase 2-cyclin A3 (CDK2)
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.
Hardcastle IR, Arris CE, Bentley J, Boyle FT, Chen Y, Curtin NJ, Endicott JA, Gibson AE, Golding BT, Griffin RJ, Jewsbury P, Menyerol J, Mesguiche V, Newell DR, Noble ME, Pratt DJ, Wang LZ, Whitfield HJ.
J Med Chem (2004) 47 : 3710 -3722
PubMed 15239650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.98 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319467 1 8.27
CHEMBL434217 1 8.15
CHEMBL122489 1 7.25
CHEMBL331123 1 7.16
CHEMBL123156 1 7.00
CHEMBL436560 1 6.89
CHEMBL122620 1 6.70
CHEMBL123337 1 6.70
CHEMBL123368 1 6.68
CHEMBL122850 1 6.52
CHEMBL124436 1 6.52
CHEMBL332198 1 6.40
CHEMBL435999 1 6.19
CHEMBL125091 1 6.10
CHEMBL122264 1 6.01
CHEMBL122365 1 5.92
CHEMBL123242 1 5.77
CHEMBL332550 1 5.77
CHEMBL122040 1 5.75
CHEMBL341273 1 5.64
CHEMBL338355 1 5.55
CHEMBL123140 1 5.55
CHEMBL332540 1 5.37
CHEMBL122900 1 5.30
CHEMBL124059 1 5.30
CHEMBL262367 1 5.17
CHEMBL122032 1 4.92
CHEMBL330894 1 4.28
CHEMBL121655 1 4.20
CHEMBL121941 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319467 IC50 = 5.4 nM 8.27
CHEMBL434217 IC50 = 7.0 nM 8.15
CHEMBL122489 IC50 = 56.0 nM 7.25
CHEMBL331123 IC50 = 70.0 nM 7.16
CHEMBL123156 IC50 = 100.0 nM 7.00
CHEMBL436560 IC50 = 130.0 nM 6.89
CHEMBL122620 IC50 = 200.0 nM 6.70
CHEMBL123337 IC50 = 200.0 nM 6.70
CHEMBL123368 IC50 = 210.0 nM 6.68
CHEMBL122850 IC50 = 300.0 nM 6.52
CHEMBL124436 IC50 = 300.0 nM 6.52
CHEMBL332198 IC50 = 400.0 nM 6.40
CHEMBL435999 IC50 = 650.0 nM 6.19
CHEMBL125091 IC50 = 800.0 nM 6.10
CHEMBL122264 IC50 = 970.0 nM 6.01
CHEMBL122365 IC50 = 1200.0 nM 5.92
CHEMBL123242 IC50 = 1700.0 nM 5.77
CHEMBL332550 IC50 = 1700.0 nM 5.77
CHEMBL122040 IC50 = 1800.0 nM 5.75
CHEMBL341273 IC50 = 2300.0 nM 5.64
CHEMBL338355 IC50 = 2800.0 nM 5.55
CHEMBL123140 IC50 = 2800.0 nM 5.55
CHEMBL332540 IC50 = 4300.0 nM 5.37
CHEMBL122900 IC50 = 5000.0 nM 5.30
CHEMBL124059 IC50 = 5000.0 nM 5.30
CHEMBL262367 IC50 = 6800.0 nM 5.17
CHEMBL122032 IC50 = 12000.0 nM 4.92
CHEMBL330894 IC50 = 52000.0 nM 4.28
CHEMBL121655 IC50 = 63000.0 nM 4.20
CHEMBL121941 IC50 = 64000.0 nM 4.19
CHEMBL340813 IC50 = 69000.0 nM 4.16