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Assay Detail

CHEMBL3611591

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

Binding
Inhibition of ERK2 (unknown origin)
14
Total Activities
14
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

Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.
Bagdanoff JT, Jain R, Han W, Zhu S, Madiera AM, Lee PS, Ma X, Poon D.
Bioorg Med Chem Lett (2015) 25 : 3788 -3792
PubMed 26259804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 9.93 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3608588 1 11.00
CHEMBL3608589 1 10.72
CHEMBL3608586 1 10.59
CHEMBL3590106 ULIXERTINIB 2.0 1 10.52
CHEMBL3608462 1 10.48
CHEMBL3608464 1 10.46
CHEMBL3608463 1 10.40
CHEMBL3608587 1 10.30
CHEMBL3608591 1 9.80
CHEMBL3608458 1 9.72
CHEMBL3608461 1 9.72
CHEMBL3608459 1 9.59
CHEMBL3608460 1 8.65
CHEMBL3608590 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3608588 IC50 = 0.01 nM 11.00
CHEMBL3608589 IC50 = 0.019 nM 10.72
CHEMBL3608586 IC50 = 0.026 nM 10.59
CHEMBL3590106 ULIXERTINIB IC50 = 0.03 nM 10.52
CHEMBL3608462 IC50 = 0.033 nM 10.48
CHEMBL3608464 IC50 = 0.035 nM 10.46
CHEMBL3608463 IC50 = 0.04 nM 10.40
CHEMBL3608587 IC50 = 0.05 nM 10.30
CHEMBL3608591 IC50 = 0.16 nM 9.80
CHEMBL3608458 IC50 = 0.19 nM 9.72
CHEMBL3608461 IC50 = 0.19 nM 9.72
CHEMBL3608459 IC50 = 0.26 nM 9.59
CHEMBL3608460 IC50 = 2.26 nM 8.65
CHEMBL3608590 IC50 = 76.0 nM 7.12