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Assay Detail

CHEMBL665281

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Binding
Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate
21
Total Activities
21
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 E (CHEMBL2094126)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.
Sanchez-Martinez C, Shih C, Zhu G, Li T, Brooks HB, Patel BK, Schultz RM, DeHahn TB, Spencer CD, Watkins SA, Ogg CA, Considine E, Dempsey JA, Zhang F.
Bioorg Med Chem Lett (2003) 13 : 3841 -3846
PubMed 14552792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.03 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62253 1 6.85
CHEMBL545295 1 6.80
CHEMBL126087 1 6.75
CHEMBL416056 1 6.58
CHEMBL301515 1 6.24
CHEMBL304428 1 6.17
CHEMBL268368 STAUROSPORINE AGLYCON 1 6.05
CHEMBL124620 1 5.82
CHEMBL341110 1 5.79
CHEMBL341035 1 5.73
CHEMBL53856 1 5.71
CHEMBL7463 GF-109203 1 4.99
CHEMBL266487 RO-316233 1 4.93
CHEMBL339948 1 -
CHEMBL127852 1 -
CHEMBL302234 1 -
CHEMBL123777 1 -
CHEMBL124033 1 -
CHEMBL293898 1 -
CHEMBL124072 1 -
CHEMBL16958 STAUROSPORINONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62253 IC50 = 140.0 nM 6.85
CHEMBL545295 IC50 = 160.0 nM 6.80
CHEMBL126087 IC50 = 180.0 nM 6.75
CHEMBL416056 IC50 = 260.0 nM 6.58
CHEMBL301515 IC50 = 580.0 nM 6.24
CHEMBL304428 IC50 = 680.0 nM 6.17
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 900.0 nM 6.05
CHEMBL124620 IC50 = 1500.0 nM 5.82
CHEMBL341110 IC50 = 1610.0 nM 5.79
CHEMBL341035 IC50 = 1880.0 nM 5.73
CHEMBL53856 IC50 = 1950.0 nM 5.71
CHEMBL7463 GF-109203 IC50 = 10180.0 nM 4.99
CHEMBL266487 RO-316233 IC50 = 11690.0 nM 4.93
CHEMBL339948 IC50 < 60.0 nM -
CHEMBL127852 IC50 > 1000.0 nM -
CHEMBL302234 IC50 > 1000.0 nM -
CHEMBL123777 IC50 > 1000.0 nM -
CHEMBL124033 IC50 > 10000.0 nM -
CHEMBL293898 IC50 > 200.0 nM -
CHEMBL124072 IC50 > 1000.0 nM -
CHEMBL16958 STAUROSPORINONE IC50 > 1000.0 nM -