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Assay Detail

CHEMBL1002018

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of CDK4 by radioactive glutathione plate-binding assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 4 (CHEMBL331)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.
Stevens KL, Reno MJ, Alberti JB, Price DJ, Kane-Carson LS, Knick VB, Shewchuk LM, Hassell AM, Veal JM, Davis ST, Griffin RJ, Peel MR.
Bioorg Med Chem Lett (2008) 18 : 5758 -5758
PubMed 18835709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.96 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526110 1 9.52
CHEMBL495696 GW778894X 1 8.40
CHEMBL468963 GW779439X 1 8.22
CHEMBL495751 1 8.10
CHEMBL188938 1 8.10
CHEMBL495545 1 7.92
CHEMBL513354 1 7.92
CHEMBL359554 1 7.92
CHEMBL497564 1 7.80
CHEMBL496360 1 7.60
CHEMBL359794 1 7.60
CHEMBL522718 1 7.58
CHEMBL521871 1 7.42
CHEMBL496162 1 7.35
CHEMBL524086 1 7.30
CHEMBL525194 1 7.10
CHEMBL523735 1 6.80
CHEMBL496778 1 6.80
CHEMBL496779 1 6.70
CHEMBL495570 1 6.60
CHEMBL503212 1 6.60
CHEMBL495771 GW708336X 1 6.40
CHEMBL497196 1 6.30
CHEMBL524059 1 6.10
CHEMBL498625 1 6.10
CHEMBL496575 1 6.10
CHEMBL513330 GW781673X 1 6.00
CHEMBL446024 GW683003X 1 6.00
CHEMBL497398 1 5.89
CHEMBL445757 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526110 IC50 = 0.3 nM 9.52
CHEMBL495696 GW778894X IC50 = 4.0 nM 8.40
CHEMBL468963 GW779439X IC50 = 6.0 nM 8.22
CHEMBL495751 IC50 = 8.0 nM 8.10
CHEMBL188938 IC50 = 8.0 nM 8.10
CHEMBL495545 IC50 = 12.0 nM 7.92
CHEMBL513354 IC50 = 12.0 nM 7.92
CHEMBL359554 IC50 = 12.0 nM 7.92
CHEMBL497564 IC50 = 16.0 nM 7.80
CHEMBL496360 IC50 = 25.0 nM 7.60
CHEMBL359794 IC50 = 25.0 nM 7.60
CHEMBL522718 IC50 = 26.0 nM 7.58
CHEMBL521871 IC50 = 38.0 nM 7.42
CHEMBL496162 IC50 = 45.0 nM 7.35
CHEMBL524086 IC50 = 50.0 nM 7.30
CHEMBL525194 IC50 = 80.0 nM 7.10
CHEMBL496778 IC50 = 160.0 nM 6.80
CHEMBL523735 IC50 = 160.0 nM 6.80
CHEMBL496779 IC50 = 200.0 nM 6.70
CHEMBL495570 IC50 = 250.0 nM 6.60
CHEMBL503212 IC50 = 250.0 nM 6.60
CHEMBL495771 GW708336X IC50 = 400.0 nM 6.40
CHEMBL497196 IC50 = 500.0 nM 6.30
CHEMBL524059 IC50 = 790.0 nM 6.10
CHEMBL498625 IC50 = 800.0 nM 6.10
CHEMBL496575 IC50 = 800.0 nM 6.10
CHEMBL513330 GW781673X IC50 = 1000.0 nM 6.00
CHEMBL446024 GW683003X IC50 = 1000.0 nM 6.00
CHEMBL497398 IC50 = 1300.0 nM 5.89
CHEMBL445757 IC50 = 1600.0 nM 5.80
CHEMBL359963 GW805758X IC50 = 2000.0 nM 5.70
CHEMBL523747 IC50 = 2000.0 nM 5.70
CHEMBL524057 GW683768X IC50 = 2000.0 nM 5.70
CHEMBL524901 GW683109X IC50 = 3200.0 nM 5.50
CHEMBL495544 IC50 > 40000.0 nM -