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Assay Detail

CHEMBL5369258

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

Binding
Binding affinity to ERK2 (unknown origin) using Ulight-MBP as substrate assessed as inhibition constant preincubated for 30 mins followed by substrate addition measured after 90 mins in presence of ATP by TR-FRET assay
4
Total Activities
4
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

Mitogen-activated protein kinase 1 (CHEMBL4040)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
Zeng M, Grandner JM, Bryan MC, Verma V, Larouche-Gauthier R, Leclerc JP, Zhao L, Haghshenas P, Aubert-Nicol S, Yadav A, Ashley M, Chen JZ, Durk M, Samy KE, Nespi M, Levy E, Merrick K, Moffat JG, Murray J, Oh A, Orr C, Segal E, Sims J, Sneeringer C, Prangley M, Vartanian S, Magnuson S, Parr BT.
ACS Med Chem Lett (2023) 14 : 1179 -1187
PubMed 37736184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.67 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298678 1 9.82
CHEMBL5428299 1 9.77
CHEMBL5399703 1 9.66
CHEMBL4112022 1 9.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298678 Ki = 0.15 nM 9.82
CHEMBL5428299 Ki = 0.17 nM 9.77
CHEMBL5399703 Ki = 0.22 nM 9.66
CHEMBL4112022 Ki = 0.36 nM 9.44