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Assay Detail

CHEMBL660784

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Binding
Inhibitory concentration against cyclin-dependent kinase 2
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cyclin-dependent kinase 2 (CHEMBL301)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.
Breault GA, Ellston RP, Green S, James SR, Jewsbury PJ, Midgley CJ, Pauptit RA, Minshull CA, Tucker JA, Pease JE.
Bioorg Med Chem Lett (2003) 13 : 2961 -2966
PubMed 12941312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.16 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419720 1 6.70
CHEMBL419534 1 6.52
CHEMBL100391 1 6.30
CHEMBL430507 1 6.16
CHEMBL101311 1 6.00
CHEMBL101810 1 6.00
CHEMBL322019 1 5.70
CHEMBL101468 1 5.70
CHEMBL101156 1 5.52
CHEMBL99689 1 5.40
CHEMBL99948 1 5.30
CHEMBL317629 1 5.30
CHEMBL101679 1 5.22
CHEMBL101019 1 5.16
CHEMBL103633 1 5.16
CHEMBL101473 1 5.10
CHEMBL101887 1 4.92
CHEMBL100664 1 4.82
CHEMBL430854 1 4.75
CHEMBL322640 1 4.66
CHEMBL100675 1 4.66
CHEMBL99687 1 4.58
CHEMBL100811 1 4.55
CHEMBL102047 1 4.47
CHEMBL101557 1 4.46
CHEMBL101052 1 4.44
CHEMBL328623 1 4.09
CHEMBL101868 1 4.07
CHEMBL99647 1 4.02
CHEMBL101779 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419720 IC50 = 200.0 nM 6.70
CHEMBL419534 IC50 = 300.0 nM 6.52
CHEMBL100391 IC50 = 500.0 nM 6.30
CHEMBL430507 IC50 = 700.0 nM 6.16
CHEMBL101311 IC50 = 1000.0 nM 6.00
CHEMBL101810 IC50 = 1000.0 nM 6.00
CHEMBL322019 IC50 = 2000.0 nM 5.70
CHEMBL101468 IC50 = 2000.0 nM 5.70
CHEMBL101156 IC50 = 3000.0 nM 5.52
CHEMBL99689 IC50 = 4000.0 nM 5.40
CHEMBL99948 IC50 = 5000.0 nM 5.30
CHEMBL317629 IC50 = 5000.0 nM 5.30
CHEMBL101679 IC50 = 6000.0 nM 5.22
CHEMBL101019 IC50 = 7000.0 nM 5.16
CHEMBL103633 IC50 = 7000.0 nM 5.16
CHEMBL101473 IC50 = 8000.0 nM 5.10
CHEMBL101887 IC50 = 12000.0 nM 4.92
CHEMBL100664 IC50 = 15000.0 nM 4.82
CHEMBL430854 IC50 = 18000.0 nM 4.75
CHEMBL100675 IC50 = 22000.0 nM 4.66
CHEMBL322640 IC50 = 22000.0 nM 4.66
CHEMBL99687 IC50 = 26000.0 nM 4.58
CHEMBL100811 IC50 = 28000.0 nM 4.55
CHEMBL102047 IC50 = 34000.0 nM 4.47
CHEMBL101557 IC50 = 35000.0 nM 4.46
CHEMBL101052 IC50 = 36000.0 nM 4.44
CHEMBL328623 IC50 = 81000.0 nM 4.09
CHEMBL101868 IC50 = 85000.0 nM 4.07
CHEMBL99647 IC50 = 95000.0 nM 4.02
CHEMBL101779 IC50 > 100000.0 nM -
CHEMBL98335 IC50 > 10000.0 nM -
CHEMBL102136 IC50 > 100000.0 nM -
CHEMBL318485 IC50 > 100000.0 nM -
CHEMBL318188 IC50 > 100000.0 nM -
CHEMBL102008 IC50 > 10000.0 nM -
CHEMBL318461 IC50 > 100000.0 nM -