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Assay Detail

CHEMBL660791

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Binding
Inhibitory activity against cyclin-dependent kinase 1 (CDK1) was determined
ChEMBL ↗
46
Total Activities
43
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 1 (CHEMBL308) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,6,9-trisubstituted purines: optimization towards highly potent and selective CDK1 inhibitors.
Imbach P, Capraro HG, Furet P, Mett H, Meyer T, Zimmermann J.
Bioorg Med Chem Lett (1999) 9 : 91 -96
PubMed 9990463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.80 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367625 — — 3 7.60
CHEMBL172140 — — 1 7.55
CHEMBL368215 — — 1 7.55
CHEMBL177138 — — 1 7.52
CHEMBL171891 — — 1 7.51
CHEMBL174773 — — 1 7.50
CHEMBL367691 — — 1 7.41
CHEMBL173459 — — 2 7.41
CHEMBL176559 — — 1 7.41
CHEMBL174977 — — 1 7.40
CHEMBL368351 — — 1 7.39
CHEMBL173647 — — 1 7.10
CHEMBL366734 — — 1 7.10
CHEMBL435330 — — 1 7.07
CHEMBL368202 — — 1 7.05
CHEMBL173619 — — 1 7.00
CHEMBL368278 — — 1 6.92
CHEMBL173608 — — 1 6.85
CHEMBL172848 — — 1 6.82
CHEMBL366642 — — 1 6.82
CHEMBL176834 — — 1 6.80
CHEMBL175143 — — 1 6.64
CHEMBL173737 — — 1 6.60
CHEMBL174162 — — 1 6.54
CHEMBL176576 — — 1 6.51
CHEMBL367245 — — 1 6.48
CHEMBL172811 — — 1 6.47
CHEMBL176908 — — 1 6.46
CHEMBL366620 — — 1 6.46
CHEMBL173353 — — 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367625 — IC50 = 25.0 nM 7.60
CHEMBL172140 — IC50 = 28.0 nM 7.55
CHEMBL368215 — IC50 = 28.0 nM 7.55
CHEMBL177138 — IC50 = 30.0 nM 7.52
CHEMBL171891 — IC50 = 31.0 nM 7.51
CHEMBL367625 — IC50 = 31.0 nM 7.51
CHEMBL174773 — IC50 = 32.0 nM 7.50
CHEMBL173459 — IC50 = 39.0 nM 7.41
CHEMBL176559 — IC50 = 39.0 nM 7.41
CHEMBL367691 — IC50 = 39.0 nM 7.41
CHEMBL174977 — IC50 = 40.0 nM 7.40
CHEMBL368351 — IC50 = 41.0 nM 7.39
CHEMBL366734 — IC50 = 80.0 nM 7.10
CHEMBL173647 — IC50 = 80.0 nM 7.10
CHEMBL435330 — IC50 = 85.0 nM 7.07
CHEMBL368202 — IC50 = 90.0 nM 7.05
CHEMBL173619 — IC50 = 100.0 nM 7.00
CHEMBL367625 — IC50 = 110.0 nM 6.96
CHEMBL368278 — IC50 = 120.0 nM 6.92
CHEMBL173459 — IC50 = 140.0 nM 6.85
CHEMBL173608 — IC50 = 140.0 nM 6.85
CHEMBL366642 — IC50 = 150.0 nM 6.82
CHEMBL172848 — IC50 = 150.0 nM 6.82
CHEMBL176834 — IC50 = 160.0 nM 6.80
CHEMBL175143 — IC50 = 230.0 nM 6.64
CHEMBL173737 — IC50 = 250.0 nM 6.60
CHEMBL174162 — IC50 = 290.0 nM 6.54
CHEMBL176576 — IC50 = 310.0 nM 6.51
CHEMBL367245 — IC50 = 330.0 nM 6.48
CHEMBL172811 — IC50 = 340.0 nM 6.47
CHEMBL173353 — IC50 = 350.0 nM 6.46
CHEMBL366620 — IC50 = 350.0 nM 6.46
CHEMBL176908 — IC50 = 350.0 nM 6.46
CHEMBL367614 — IC50 = 380.0 nM 6.42
CHEMBL171975 — IC50 = 440.0 nM 6.36
CHEMBL540874 — IC50 = 450.0 nM 6.35
CHEMBL176488 — IC50 = 450.0 nM 6.35
CHEMBL366698 — IC50 = 550.0 nM 6.26
CHEMBL368743 — IC50 = 550.0 nM 6.26
CHEMBL175158 — IC50 = 560.0 nM 6.25
CHEMBL557975 — IC50 = 560.0 nM 6.25
CHEMBL537838 — IC50 = 600.0 nM 6.22
CHEMBL439841 — IC50 = 600.0 nM 6.22
CHEMBL173237 — IC50 = 700.0 nM 6.16
CHEMBL534909 — IC50 = 700.0 nM 6.16
CHEMBL414651 — IC50 = 1000.0 nM 6.00