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Assay Detail

CHEMBL831686

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Binding
Inhibition of Cyclin-dependent kinase 1-cyclin B
27
Total Activities
27
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 1/cyclin B (CHEMBL2094127)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.
Markwalder JA, Arnone MR, Benfield PA, Boisclair M, Burton CR, Chang CH, Cox SS, Czerniak PM, Dean CL, Doleniak D, Grafstrom R, Harrison BA, Kaltenbach RF, Nugiel DA, Rossi KA, Sherk SR, Sisk LM, Stouten P, Trainor GL, Worland P, Seitz SP.
J Med Chem (2004) 47 : 5894 -5911
PubMed 15537345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.62 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188587 1 7.52
CHEMBL388978 STAUROSPORINE 1 7.52
CHEMBL536272 1 7.16
CHEMBL1790020 1 7.00
CHEMBL188650 1 7.00
CHEMBL363679 1 6.82
CHEMBL186157 1 6.82
CHEMBL433590 1 6.75
CHEMBL187522 1 6.72
CHEMBL187984 1 6.70
CHEMBL365713 1 6.66
CHEMBL425181 1 6.62
CHEMBL362075 1 6.58
CHEMBL187433 1 6.57
CHEMBL433959 1 6.39
CHEMBL188863 1 6.31
CHEMBL187816 1 6.28
CHEMBL418203 1 6.28
CHEMBL362121 1 6.07
CHEMBL364226 1 6.06
CHEMBL370283 1 5.21
CHEMBL187666 1 -
CHEMBL191312 1 -
CHEMBL190789 1 -
CHEMBL188151 1 -
CHEMBL436284 1 -
CHEMBL190636 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188587 IC50 = 30.0 nM 7.52
CHEMBL388978 STAUROSPORINE IC50 = 30.0 nM 7.52
CHEMBL536272 IC50 = 70.0 nM 7.16
CHEMBL1790020 IC50 = 100.0 nM 7.00
CHEMBL188650 IC50 = 100.0 nM 7.00
CHEMBL363679 IC50 = 150.0 nM 6.82
CHEMBL186157 IC50 = 150.0 nM 6.82
CHEMBL433590 IC50 = 180.0 nM 6.75
CHEMBL187522 IC50 = 190.0 nM 6.72
CHEMBL187984 IC50 = 200.0 nM 6.70
CHEMBL365713 IC50 = 220.0 nM 6.66
CHEMBL425181 IC50 = 240.0 nM 6.62
CHEMBL362075 IC50 = 260.0 nM 6.58
CHEMBL187433 IC50 = 270.0 nM 6.57
CHEMBL433959 IC50 = 410.0 nM 6.39
CHEMBL188863 IC50 = 490.0 nM 6.31
CHEMBL187816 IC50 = 520.0 nM 6.28
CHEMBL418203 IC50 = 520.0 nM 6.28
CHEMBL362121 IC50 = 860.0 nM 6.07
CHEMBL364226 IC50 = 870.0 nM 6.06
CHEMBL370283 IC50 = 6200.0 nM 5.21
CHEMBL187666 IC50 > 270.0 nM -
CHEMBL191312 IC50 > 510.0 nM -
CHEMBL190789 IC50 > 260.0 nM -
CHEMBL188151 IC50 > 560.0 nM -
CHEMBL436284 IC50 > 270.0 nM -
CHEMBL190636 IC50 > 270.0 nM -