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Assay Detail

CHEMBL666745

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Binding
Compound was evaluated for 50% inhibition of Cyclin-dependent kinase 4-cyclin D1
39
Total Activities
39
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 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 2. Probing the indeno ring substituent pattern.
Nugiel DA, Vidwans A, Etzkorn AM, Rossi KA, Benfield PA, Burton CR, Cox S, Doleniak D, Seitz SP.
J Med Chem (2002) 45 : 5224 -5232
PubMed 12431050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.31 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL345525 1 8.05
CHEMBL147038 1 7.92
CHEMBL147012 1 7.92
CHEMBL357770 1 7.92
CHEMBL149834 1 7.70
CHEMBL148580 1 7.58
CHEMBL148889 1 7.19
CHEMBL346164 1 7.18
CHEMBL346184 1 7.12
CHEMBL147084 1 7.09
CHEMBL151915 1 6.95
CHEMBL357491 1 6.90
CHEMBL434081 1 6.71
CHEMBL358281 1 6.51
CHEMBL147281 1 6.34
CHEMBL27275 1 6.32
CHEMBL149705 1 6.11
CHEMBL436078 1 6.06
CHEMBL151720 1 6.05
CHEMBL341835 1 6.04
CHEMBL147290 1 5.94
CHEMBL357330 1 4.70
CHEMBL151616 1 4.67
CHEMBL147254 1 4.64
CHEMBL357986 1 4.46
CHEMBL281470 1 4.35
CHEMBL355951 1 4.26
CHEMBL147523 1 4.10
CHEMBL148652 1 -
CHEMBL150529 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL345525 IC50 = 9.0 nM 8.05
CHEMBL147038 IC50 = 12.0 nM 7.92
CHEMBL357770 IC50 = 12.0 nM 7.92
CHEMBL147012 IC50 = 12.0 nM 7.92
CHEMBL149834 IC50 = 20.0 nM 7.70
CHEMBL148580 IC50 = 26.0 nM 7.58
CHEMBL148889 IC50 = 64.0 nM 7.19
CHEMBL346164 IC50 = 66.0 nM 7.18
CHEMBL346184 IC50 = 76.0 nM 7.12
CHEMBL147084 IC50 = 82.0 nM 7.09
CHEMBL151915 IC50 = 113.0 nM 6.95
CHEMBL357491 IC50 = 125.0 nM 6.90
CHEMBL434081 IC50 = 195.0 nM 6.71
CHEMBL358281 IC50 = 307.0 nM 6.51
CHEMBL147281 IC50 = 460.0 nM 6.34
CHEMBL27275 IC50 = 480.0 nM 6.32
CHEMBL149705 IC50 = 780.0 nM 6.11
CHEMBL436078 IC50 = 877.0 nM 6.06
CHEMBL151720 IC50 = 900.0 nM 6.05
CHEMBL341835 IC50 = 917.0 nM 6.04
CHEMBL147290 IC50 = 1150.0 nM 5.94
CHEMBL357330 IC50 = 20000.0 nM 4.70
CHEMBL151616 IC50 = 21500.0 nM 4.67
CHEMBL147254 IC50 = 23000.0 nM 4.64
CHEMBL357986 IC50 = 34500.0 nM 4.46
CHEMBL281470 IC50 = 45000.0 nM 4.35
CHEMBL355951 IC50 = 55500.0 nM 4.26
CHEMBL147523 IC50 = 80000.0 nM 4.10
CHEMBL149884 IC50 > 2300.0 nM -
CHEMBL151696 IC50 = 108000.0 nM -
CHEMBL424507 IC50 > 1400.0 nM -
CHEMBL149956 IC50 > 1000.0 nM -
CHEMBL355993 IC50 > 361000.0 nM -
CHEMBL357142 IC50 > 340000.0 nM -
CHEMBL149095 IC50 > 200000.0 nM -
CHEMBL151551 IC50 > 500.0 nM -
CHEMBL358390 IC50 > 1100.0 nM -
CHEMBL150529 IC50 > 1300.0 nM -
CHEMBL148652 IC50 > 150000.0 nM -