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Assay Detail

CHEMBL1002021

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

Binding
Inhibition of human CDK2 by HTRF assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2 (CHEMBL301)
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 19 7.59 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526110 1 9.52
CHEMBL359794 1 8.70
CHEMBL495696 GW778894X 1 8.70
CHEMBL188938 1 8.52
CHEMBL497564 1 8.52
CHEMBL468963 GW779439X 1 8.40
CHEMBL359554 1 8.10
CHEMBL523735 1 7.80
CHEMBL359963 GW805758X 1 7.40
CHEMBL524059 1 7.40
CHEMBL495751 1 7.40
CHEMBL513354 1 7.30
CHEMBL495545 1 7.00
CHEMBL525194 1 6.92
CHEMBL496162 1 6.64
CHEMBL521871 1 6.35
CHEMBL513330 GW781673X 1 6.00
CHEMBL446024 GW683003X 1 6.00
CHEMBL522718 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526110 IC50 = 0.3 nM 9.52
CHEMBL359794 IC50 = 2.0 nM 8.70
CHEMBL495696 GW778894X IC50 = 2.0 nM 8.70
CHEMBL188938 IC50 = 3.0 nM 8.52
CHEMBL497564 IC50 = 3.0 nM 8.52
CHEMBL468963 GW779439X IC50 = 4.0 nM 8.40
CHEMBL359554 IC50 = 8.0 nM 8.10
CHEMBL523735 IC50 = 16.0 nM 7.80
CHEMBL359963 GW805758X IC50 = 40.0 nM 7.40
CHEMBL524059 IC50 = 40.0 nM 7.40
CHEMBL495751 IC50 = 40.0 nM 7.40
CHEMBL513354 IC50 = 50.0 nM 7.30
CHEMBL495545 IC50 = 100.0 nM 7.00
CHEMBL525194 IC50 = 120.0 nM 6.92
CHEMBL496162 IC50 = 230.0 nM 6.64
CHEMBL521871 IC50 = 450.0 nM 6.35
CHEMBL513330 GW781673X IC50 = 1000.0 nM 6.00
CHEMBL446024 GW683003X IC50 = 1000.0 nM 6.00
CHEMBL522718 IC50 > 25000.0 nM -