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Assay Detail

CHEMBL3364483

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

Binding
Inhibition of Cdk2 (unknown origin)
15
Total Activities
15
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

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.
Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB.
Bioorg Med Chem Lett (2014) 24 : 2635 -2639
PubMed 24813737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.76 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298985 1 8.70
CHEMBL3298199 1 8.70
CHEMBL3357950 1 8.40
CHEMBL3298418 1 8.05
CHEMBL3298678 1 8.00
CHEMBL3298982 1 7.96
CHEMBL3298310 1 7.92
CHEMBL3298984 1 7.89
CHEMBL3298309 1 7.89
CHEMBL3298414 1 7.80
CHEMBL3357951 1 7.64
CHEMBL3298983 1 7.16
CHEMBL3298312 1 7.15
CHEMBL3298308 1 6.98
CHEMBL3298311 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298985 IC50 = 2.0 nM 8.70
CHEMBL3298199 IC50 = 2.0 nM 8.70
CHEMBL3357950 IC50 = 4.0 nM 8.40
CHEMBL3298418 IC50 = 9.0 nM 8.05
CHEMBL3298678 IC50 = 10.0 nM 8.00
CHEMBL3298982 IC50 = 11.0 nM 7.96
CHEMBL3298310 IC50 = 12.0 nM 7.92
CHEMBL3298984 IC50 = 13.0 nM 7.89
CHEMBL3298309 IC50 = 13.0 nM 7.89
CHEMBL3298414 IC50 = 16.0 nM 7.80
CHEMBL3357951 IC50 = 23.0 nM 7.64
CHEMBL3298983 IC50 = 69.0 nM 7.16
CHEMBL3298312 IC50 = 71.0 nM 7.15
CHEMBL3298308 IC50 = 104.0 nM 6.98
CHEMBL3298311 IC50 = 821.0 nM 6.09